Inflammatory diseases

INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7) (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">The present invention provides novel compounds described herein, such as of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="11.35mm" wi="54.78mm" file="US20170174692A1-20170622-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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COMPOUNDS FOR THE TREATMENT OF CANCER AND INFLAMMATORY DISEASE (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">Provided herein are compounds that inhibit the phosphorylation of MAPK and thus are useful in compositions and methods for treating cancer and inflammatory disease.</p>
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2-phenylbenzofuran derivatives, method for preparing the same and use of the same for treating inflammatory disease (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">The present invention relates to a novel 2-phenylbenzofuran derivative or a pharmaceutically acceptable salt thereof, a production method for the same, and a pharmaceutical composition for preventing or treating an inflammatory disease comprising the same as an active ingredient, and the novel 2-phenylbenzofuran derivative or the pharmaceutically acceptable salt thereof according to the present invention is outstandingly effective in suppressing NO, IL-6, and TNF-alpha induced by macrophages, and therefore can advantageously be used in a pharmaceutical composition for preventing or treating an inflammatory disease.</p>
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APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">The present invention relates to compounds of Formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.19mm" wi="73.58mm" file="US20170173031A1-20170622-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">Wherein variables are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases.</p>
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HETEROARYL AMIDE SULTAM DERIVATIVES AS RORc MODULATORS (Fri, 23 Jun 2017)
Compounds of the formula I: (I) or a pharmaceutical salt thereof, wherein m, n, p, q, Het, A, W, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
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SMALL MOLECULES AGAINST CANCER (Fri, 23 Jun 2017)
Compounds capable of, or usable in, killing cancer cells, and/or modulating a biological activity of a chemokine, and/or inhibiting a kinase, and/or treating diseases and disorders associated with a biological activity of a chemokine and/or cell migration, and/or treating disease and disorders such as cancer and inflammatory diseases and disorders, are provided herein. The compounds are listed in Tables 2, 4 and 5, and/or are represented by Formulae I, IV, V and VI, as defined in the specification. Methods utilizing these compounds are also provided.
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SMALL MOLECULES FOR INHIBITING CHEMOKINE ACTIVITY, A KINASE ACTIVITY AND/OR CANCER CELLS GROWTH (Fri, 23 Jun 2017)
Compounds capable of, or usable in, inducing death of cancer cells and/or modulating a biological activity of a chemokine e.g., cell migration, and/or treating diseases and disorders associated with a biological activity of a chemokine and/or cell migration, and/or inhibiting a kinase and/or in treating a disease or disorder associated with an activity of a kinase, such as cancer and inflammatory diseases and disorders, are provided herein. The compounds are collectively represented by Formulae (Ia) or (Ib): wherein A, B D, E, G and R1-R5 are as defined in the specification.
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METHODS FOR IDENTIFYING INHIBITORS OF "STIMULATOR OF INTERFERON GENE"-DEPENDENT INTERFERON PRODUCTION (Fri, 23 Jun 2017)
The present invention relates to the use cyclic-di-nucleotide and related scaffold molecules that measurably inhibit STING signaling, and methods for their use in identifying more potent inhibitors of STING signaling. In particular, the methods provided can be used to identify potent inhibitors of STING signaling, which are useful in the treatment of autoimmune and inflammatory diseases. Also provided are compounds having STING inhibitory activity useful in the treatment of autoimmune and inflammatory diseases.
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IL-17A/F HETERODIMERIC POLYPEPTIDES AND THERAPEUTIC THEREOF (Thu, 22 Jun 2017)
The present invention is directed to a novel naturally occurring human cytokine that is comprised of a heterodimer of interleukin-17 and interleukin-17F designated herein as interleukin 17A/F (IL-17 A/F). Also provided herein are vectors and host cells comprising those nucleic acid sequences, chimeric polypeptide molecules comprising the polypeptides of the present invention fused to heterologous polypeptide sequences, specific antibodies which bind to the polypeptides of the present invention and to methods for producing the polypeptides of the present invention. Further provided herein are methods for treating degenerative cartilaginous disorders and other inflammatory diseases.
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GADD45BETA TARGETING AGENTS (Thu, 15 Jun 2017)
Compounds based around tetrapeptide, tripeptide and dipeptide moeties and corresponding peptiod moeties. Related methods and pharmaceutical compositions for use in treatment of cancer, inflammatory diseases, and other disorders.
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LIPID COMPOUNDS AND COMPOSITIONS AND THEIR OPTHALMIC USE (Fri, 09 Jun 2017)
The invention relates to lipid compounds of formula (I) and their pharmaceutically acceptable salts for the prevention and/or treatment of ophthalmic disorders such as retinal degenerative disorders and ocular inflammatory diseases: (I) (wherein R1 is either a C9 to C22 alkyl group, or a C9 to C22 alkenyl group having from 1 to 6 double bonds; R2 is selected from the group consisting of a halogen atom, a hydroxy group, an alkyl group, an alkoxy group, an alkylthio group, a carboxy group, an acyl group, an amino group, and an alkylamino group; R3 is a hydrogen atom, or a group R2; R4 is a carboxylic acid or a derivative thereof; and X is methylene (-CH2-), or an oxygen or sulfur atom).
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HOMOBISPIPERIDINYL DERIVATIVES AS LIVER X RECEPTOR BETA AGONISTS, COMPOSITIONS, AND THEIR USE (Fri, 09 Jun 2017)
In its many embodiments, the present invention provides certain substituted bispiperidinyl compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein ring A, ring B, R1, R2, R3, L, R4, X, Z, Li, Q and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver Χ-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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ANTIBODIES AND METHODS OF USE THEREOF (Fri, 09 Jun 2017)
The present disclosure provides multispecific (e.g., bispecific) antibodies that specifically bind to human GITR and/or human OX40 as well as compositions comprising such antibodies. In a specific aspect, the multispecific antibodies specifically bind to human GITR and OX40 and modulate GITR and/or OX40 activity, e.g., enhance, activate, or induce GITR and/or OX40 activity, or reduce, deactivate, or inhibit GITR and/or OX40 activity. The present disclosure also provides methods for treating disorders, such as cancer, by administering a multispecific antibody that specifically binds to human GITR and/or OX40 and modulates GITR and/or OX40 activity, e.g., enhances, activates, or induces GITR and/or OX40 activity. Also provided are methods for treating autoimmune or inflammatory diseases or disorders, by administering a multispecific antibody that specifically binds to human GITR and/or OX40 and modulates GITR and/or OX40 activity, e.g., reduces, deactivates, or inhibits GITR and/or OX40 activity.
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ANTI-OX40 ANTIBODIES AND METHODS OF USE THEREOF (Fri, 09 Jun 2017)
The present disclosure provides antibodies that specifically bind to human OX40 receptor (OX40) and compositions comprising such antibodies. In a specific aspect, the antibodies specifically bind to human OX40 and modulate OX40 activity, e.g., enhance, activate, or induce OX40 activity, or diminish, deactivate, or suppress OX40 activity. The present disclosure also provides methods for treating disorders, such as cancer, by administering an antibody that specifically binds to human OX40 and modulates OX40 activity, e.g., enhances, activates, or induces OX40 activity. Also provided are methods for treating autoimmune or inflammatory diseases or disorders, by administering an antibody that specifically binds to human OX40 and modulates OX40 activity, e.g., diminishes, deactivates, or suppresses OX40 activity.
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ANTI-GITR ANTIBODIES AND METHODS OF USE THEREOF (Fri, 09 Jun 2017)
The present disclosure provides antibodies that specifically bind to human GITR, as well as compositions comprising such antibodies. In a specific aspect, the antibodies specifically bind to human GITR and deactivate, reduce, or inhibit GITR activity. The present disclosure also provides methods for treating autoimmune or inflammatory diseases disorders, by administering an antibody that specifically binds to human GITR and deactivates, reduces, or inhibits GITR activity.
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ANTI-GITR ANTIBODIES AND METHODS OF USE THEREOF (Fri, 09 Jun 2017)
The present disclosure provides antagonist antibodies that specifically bind to human glucocorticoid-induced TNFR family related receptor (GITR) and compositions comprising such antibodies. In a specific aspect, the antibodies specifically bind to human GITR and modulate GITR activity, e.g., reduce, deactivate, or inhibit GITR activity. The present disclosure also provides methods for treating autoimmune or inflammatory diseases or disorders, by administering an antibody that specifically binds to human GITR and modulates GITR activity, e.g., reduces, deactivates, or inhibits GITR activity.
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ANTI-OX40 ANTIBODIES AND METHODS OF USE THEREOF (Fri, 09 Jun 2017)
The present disclosure provides antibodies that specifically bind to human OX40 receptor (OX40) and compositions comprising such antibodies. In a specific aspect, the antibodies specifically bind to human OX40 and modulate OX40 activity, e.g., reduce, deactivate, or inhibit OX40 activity. The present disclosure also provides methods for autoimmune or inflammatory diseases or disorders, by administering an antibody that specifically binds to human OX40 and modulates OX40 activity, e.g., reduces, deactivates, or inhibits OX40 activity.
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PHARMACEUTICAL FORMULATIONS (Fri, 02 Jun 2017)
Disclosed herein is glutathione in conjunction with an isoselenazol or isothiazol derivative, e.g., ebselen or ebsulfur derivative, to treat diabetes, lupus, or other chronic inflammatory disease. The glutathione is preferably provided in a rapid release oral formulation that presents the glutathione for absorption in the first part of the ileum. The isoselenazol or isothiazol derivative is preferably provided in a delayed release formulation to avoid overlapping high enteric concentration. These may be provided within the same unit dosage form.
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Methods of Treating Cancers, Immune and Autoimmune Diseases, and Inflammatory Diseases Based on BTK Occupancy and BTK Resynthesis Rate (Fri, 26 May 2017)
<p id="p-0001" num="0000">In an embodiment, therapeutic methods and uses of Bruton's Tyrosine Kinase (BTK) inhibitors for treatment of cancer, inflammation, immune disorders, and autoimmune disorders, including dermatoses, and for transplantation prophylaxis, based on BTK occupancies and/or BTK resynthesis rates for B cells in various diseases, tissue compartments, including bone marrow and lymph nodes, are described. In an embodiment, dosing regimens for a BTK inhibitor for treatment of cancer, inflammation, immune disorders, and autoimmune disorders, including dermatoses, and for transplantation prophylaxis, based on BTK occupancies and/or BTK resynthesis rates for B cells in various diseases, tissue compartments, including bone marrow and lymph nodes, are described.</p>
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BENZIMIDAZOLE DERIVATIVES AS PI3 KINASE INHIBITORS (Thu, 25 May 2017)
The invention relates to benzimidazole derivatives of formula (I) which modulate, notably inhibit the activity or function of the phosphoinositide 3'-OH kinase family (PI3 kinases), suitably PI3K±, PI3K´, PI3K² and/or PI3K³. The invention further relates to these benzimidazoles for use in the treatment of disease states selected from autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. Especially, the invention relates to PI3K² selective benzimidazoles for use in treating cancer.
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ARYL SULTAM DERIVATIVES AS RORc MODULATORS (Fri, 19 May 2017)
<p id="p-0001" num="0000">Compounds of the formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.44mm" wi="69.85mm" file="US20170137393A1-20170518-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, X<sup>1</sup>, X<sup>2</sup>, X<sup>3</sup>, X<sup>4</sup>, Y, Z, A, R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5 </sup>R<sup>6</sup>, R<sup>7</sup>, R<sup>8</sup>, R<sup>9</sup>, R<sup>10</sup>, R<sup>11</sup>, R<sup>12 </sup>and R<sup>13 </sup>are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis, muscular sclerosis and psoriasis.</p>
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THERAPEUTIC/ PREVENTIVE AGENT CONTAINING COUMARIN DERIVATIVE AS ACTIVE INGREDIENT (Fri, 19 May 2017)
<p id="p-0001" num="0000">A method for prophylactically or therapeutically treating an inflammatory disease and/or degenerative intervertebral disk disease in a subject is disclosed. The method includes administering to the subject an effective amount of a coumarin derivative represented by formula (I), or a pharmaceutically acceptable salt or hydrate thereof:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.60mm" wi="60.54mm" file="US20170135985A1-20170518-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">Each of R1 and R2 is independently (a) phenyl optionally substituted with alkoxy, alkyl, cyano, nitro, hydroxy, trifluoromethyl, amino, carboxy, alkoxycarbonyl, phenyl, or one or two halogen(s), (b) pyridyl, (c) alkyl, or (d) thienyl.</p>
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SUBSTITUTED PYRAZOLOPYRIDINAMINES (Fri, 19 May 2017)
The present invention relates to substituted pyrazolopyridinamine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative, angiogenesis disorders, inflammatory diseases or diseases associated with inflammatory pain, as a sole agent or in combination with other active ingredients.
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CYANOPYRIDINE DERIVATIVES AS LIVER X RECEPTOR BETA AGONISTS, COMPOSITIONS, AND THEIR USE (Fri, 19 May 2017)
In its many embodiments, the present invention provides substituted cyanopyridine containing compounds of the Formula (I): and acceptable salts thereof, wherein R1, R2, R3, R4, R5, X, Y, Q, and the moiety are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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BISPIPERIDINYL DERIVATIVES AS LIVER X RECEPTOR BETA AGONISTS, COMPOSITIONS, AND THEIR USE (Fri, 19 May 2017)
In its many embodiments, the present invention provides certain substituted bispiperidinyl compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L, R4, Q and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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4-ALKYNYL IMIDAZOLE DERIVATIVE AND MEDICINE COMPRISING SAME AS ACTIVE INGREDIENT (Fri, 12 May 2017)
<p id="p-0001" num="0000">There are provided 4-alkynylimidazole derivatives represented by the following general formula (I) or pharmaceutically acceptable salts thereof; the derivatives have a superior EP4 receptor antagonistic action and are useful as pharmaceuticals for the treatment of diseases associated with the EP4 receptor, for example, as anti-inflammatory and/or analgesic drugs for inflammatory diseases and diseases that involve various kinds of pains, and further as pharmaceuticals for the treatment of immune diseases that result from inflammations as evoked by tissue destruction due to the activation of Th1 cells and/or Th17 cells:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="53.42mm" wi="69.85mm" file="US20170128431A1-20170511-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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UREA DERIVATIVES AND USES THEREOF (Fri, 12 May 2017)
<p id="p-0001" num="0000">The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="111.17mm" wi="64.01mm" file="US20170129876A1-20170511-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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4,5,6,7-TETRAHYDRO-1H-IMIDAZO[4,5-C]PYRIDINE AND 1,4,5,6,7,8-HEXAHYDROIMIDAZO[4,5-D]AZEPINE DERIVATIVES AS JANUS KINASE INHIBITORS (Fri, 12 May 2017)
There are provided compounds of formula (I), wherein X, Ak, s, L, Q, R1 and R2 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of the JAK family) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
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4,5,6,7-TETRAHYDRO-1H-IMIDAZO[4,5-C]PYRIDINE AND 1,4,5,6,7,8-HEXAHYDROIMIDAZO[4,5-D]AZEPINE DERIVATIVES AS JANUS KINASE INHIBITORS (Fri, 12 May 2017)
There are provided compounds of formula I, wherein X, Ak, s, A, R1 and R2 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of the JAK family) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
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BIOLOGICALLY ACTIVE OLIGONUCLEOTIDES CAPABLE OF MODULATING THE IMMUNE SYSTEM (Thu, 11 May 2017)
The present invention relates to methods of identifying oligonucleotides capable of modulating the immune system in a mammalian subject, comprising analysis of which tertiary structural type said oligonucleotide adopts, in phosphate-buffered saline solution. Further, the invention provides oligonucleotides identifiable by the methods of the invention and to their use in methods of treating diseases, such as inflammatory diseases, autoimmune diseases, infectious diseases, neurodegenerative diseases and cancer.
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METHOD FOR PRODUCING INDOLE COMPOUND (Thu, 11 May 2017)
The present invention aims to provide a new method for producing an indole compound or a salt thereof, which has an ITK inhibitory action, and is useful for the prophylaxis or treatment of inflammatory disease. The present invention is a method for producing N-[2-(6,6-dimethyl-4,5,6,7-tetrahydro-1H-indazol-3-yl)-1H-indol-6-yl]-N-methyl-(2S)-2-(morpholin-4-yl)propanamide, which comprises a step of reacting with
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BET-PROTEIN INHIBITING 3,4-DIHYDROPYRIDO[2,3-B]PYRAZINONES WITH META-SUBSTITUTED AROMATIC AMINO- OR ETHER GROUPS (Fri, 05 May 2017)
<p id="p-0001" num="0000">The present invention relates to BET protein-inhibitory, especially BRD4-inhibitory 3,4-dihydropyrido[2,3-b]pyrazinones with a meta-substituted aromatic amino or ether group of the general formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="39.03mm" wi="62.57mm" file="US20170121322A1-20170504-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">in which A, X, Y, R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6 </sup>and n are each as defined in the description, to pharmaceutical compositions comprising the compounds according to the invention, and to the prophylactic and therapeutic use thereof in the case of hyperproliferative disorders, especially in the case of tumour disorders.</p> <p id="p-0004" num="0000">Furthermore, this invention relates to the use of BET protein inhibitors in viral infections, in neurodegenerative disorders, in inflammatory diseases, in atherosclerotic disorders and in male fertility control.</p>
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COMPOUNDS HAVING MUSCARINIC RECEPTOR ANTAGONIST AND BETA2 ADRENERGIC RECEPTOR AGONIST ACTIVITY (Fri, 05 May 2017)
<p id="p-0001" num="0000">Compounds of formula I, defined herein, act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for treating broncho-obstructive and inflammatory diseases.</p>
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DENDRIMER COMPOSITIONS AND USE IN TREATMENT OF NECROTIZING ENTEROCOLITIS AND OTHER GASTROINTESTINAL DISORDERS (Fri, 05 May 2017)
<p id="p-0001" num="0000">A dendrimer formulation, such as a PAMAM dendrimer or a multiarm PEG polymeric formulation has been developed for oral administration to the gastrointestinal tract for treatment of inflammatory diseases associated with infection or cancer. In the preferred embodiment, the dendrimers are in the form of dendrimer nanoparticles comprising poly(amidoamine) (PAMAM) hydroxyl-terminated dendrimers covalently linked to at least one therapeutic, prophylactic or diagnostic agent for treatment of one or more symptoms of necrotizing enterocolitis.</p>
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LANTHIONINE SYNTHETASE C-LIKE 2-BASED THERAPEUTICS (Fri, 05 May 2017)
<p id="p-0001" num="0000">Provided are compounds that target the lanthionine synthetase C-like protein 2 pathway. The compounds can be used to treat a number of conditions, including infectious disease, autoimmune disease, diabetes, and a chronic inflammatory disease.</p>
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COMBINATION THERAPIES FOR HEMATOLOGIC MALIGNANCIES (Fri, 05 May 2017)
<p id="p-0001" num="0000">The invention provides methods that relate to a novel therapeutic strategy for the treatment of hematological malignancies and inflammatory diseases. In particular, the method comprises administration of a compound of formula A,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="46.23mm" wi="62.06mm" file="US20170119771A1-20170504-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">wherein R is H, halo, or C1-C6 alkyl; R′ is C1-C6 alkyl; or</li> <li id="ul0002-0002" num="0000">a pharmaceutically acceptable salt thereof; and</li> <li id="ul0002-0003" num="0000">optionally a pharmaceutically acceptable excipient; and</li> <li id="ul0002-0004" num="0000">one or more additional therapeutic agents optionally selected from the group consisting of bendamustine, rituximah, and ofatumumab.</li> </ul> </li> </ul> </p>
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DENDERIMER COMPOSITIONS AND USE IN TREATMENT OF NECROTIZING ENTEROCOLITIS AND OTHER GASTROINTESTINAL DISORDERS (Fri, 05 May 2017)
A dendrimer formulation, such as a PAMAM dendrimer or a multiarm PEG polymeric formulation has been developed for oral administration to the gastrointestinal tract for treatment of inflammatory diseases associated with infection or cancer. In the preferred embodiment, the dendrimers are in the form of dendrimer nanoparticles comprising poly(amidoamine) (PAMAM) hydroxyl-terminated dendrimers covalently linked to at least one therapeutic, prophylactic or diagnostic agent for treatment of one or more symptoms of necrotizing enterocolitis.
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4-(4-(4-phenylureido-naphthalen-1-yl)oxy-pyridin-2-yl)amino-benzoic acid derivative as p38 kinase inhibitor (Fri, 05 May 2017)
There is provided a compound of formula I, which compound has antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and has use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
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Diaryl urea derivatives as p38 kinase inhibitors (Fri, 05 May 2017)
There are provided compounds of formula I, wherein R<sp>1A</sp> to R<sp>1E</sp>, R<sp>2</sp> to R<sp>4</sp>, R<sp>5a</sp>, L and X1 to X3 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
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6-[5-AMINO-6-(2-ETHOXYETHOXY)-IMIDAZO[4,5-B]PYRIDIN-3-YL]-NICOTINONITRILE DERIVATIVES AND THEIR USE AS IRAK INHIBITORS (Fri, 28 Apr 2017)
The present invention discloses compounds according to Formula (I): wherein R1, R2, and Cy are as defined herein. The present invention relates to compounds inhibiting IRAK family kinases, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory diseases, autoimmune diseases and/or proliferative diseases by administering the compound of the invention.
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DERIVATIVES OF NONSTEROIDAL ANTI-INFLAMMATORY DRUGS (Fri, 28 Apr 2017)
The present invention relates to novel compounds, e.g. for use as a medicament. In particular, the present invention relates to novel derivatives of certain nonsteroidal anti-inflammatory drugs, suitable as a medicament, preferably in the treatment and/or prevention of systemic diseases, autoimmune diseases, and/or inflammatory diseases, for example osteoarthritis, rheumatoid arthritis, multiple sclerosis and psoriasis. Further, the invention relates to a pharmaceutical composition comprising the novel compounds.
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NEW DERIVATIVES OF LICOFELONE (Fri, 28 Apr 2017)
The present invention relates to novel derivatives, preferably prodrugs, of licofelone suitable as a medicament, preferably in the treatment and/or prevention of systemic diseases, autoimmune diseases or inflammatory diseases. Further, the invention relates to a pharmaceutical composition comprising the novel compounds. The compounds are of formula (I) where L is a linear organic residue comprising 2 to 30 carbon atoms, and R is -OH or -OOCR', wherein -OOCR' is a carboxylate group which is hydrolyzable during small intestinal transit. Formula (I)
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Small Molecule Transcription Modulators of Bromodomains (Fri, 21 Apr 2017)
<p id="p-0001" num="0000">This disclosure relates generally to compounds and compositions comprising one or more indole analogs. These compounds are useful for treating diseases associated with NF-kB and p53 activity, such as cancer and inflammatory diseases.</p>
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CONFORMATIONALLY CONSTRAINED MACROCYCLIC COMPOUNDS AS PIN1 MODULATORS (Fri, 21 Apr 2017)
Conformationally constrained macrocyclic compounds of formula (I), including substituents E, G, and Q, as defined in the description and the claims, and salts thereof, have the property to modulate the activity of the peptidyl-prolyl cis/trans isomerases Pin1. Thus, these compounds and pharmaceutical compositions containing said compounds may be useful in the treatment and/or prevention of diseases or conditions in the area of proliferative disorders and diseases, such as e.g. cancer, inflammatory diseases, transplant rejection, viral infections, osteolytic bone diseases, cardiac diseases, cardiovascular diseases, respiratory diseases, acute neurological diseases, neurodegenerative diseases, immune disorders, and lymphoproliferative theileriosis.
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CONFORMATIONALLY CONSTRAINED MACROCYCLIC COMPOUNDS (Fri, 21 Apr 2017)
Formula (I); Conformationally constrained macrocyclic compounds of formula (I), including substituents E with at least one ester moiety, G and Q, as defined in the description and the claims, and salts thereof, can be metabolized to compounds that have the property to modulate the activity of the peptidyl-prolyl cis/trans isomerase Pin1. In addition, they show antiproliferative activity on various cancer cell lines. Thus, these compounds and pharmaceutical compositions containing said compounds may be useful in the treatment and/or prevention of diseases or conditions in the area of proliferative disorders and diseases, such as e.g. cancer, inflammatory diseases, transplant rejection, viral infections, osteolytic bone diseases, cardiac diseases, cardiovascular diseases, respiratory diseases, acute neurological diseases, neurodegenerative diseases, immune disorders, and lymphoproliferative theileriosis.
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CONFORMATIONALLY CONSTRAINED MACROCYCLIC COMPOUNDS AS PIN1 MODULATORS (Fri, 21 Apr 2017)
Conformationally constrained macrocyclic compounds of formula (I), including substituents E, G, and Q, as defined in the description and the claims, and salts thereof, have the property to modulate the activity of the peptidyl-prolyl cis/trans isomerases Pin1. Thus, these compounds and pharmaceutical compositions containing said compounds may be useful in the treatment and/or prevention of diseases or conditions in the area of proliferative disorders and diseases, such as e.g. cancer, inflammatory diseases, transplant rejection, viral infections, osteolytic bone diseases, cardiac diseases, cardiovascular diseases, respiratory diseases, acute neurological diseases, neurodegenerative diseases, immune disorders, and lymphoproliferative theileriosis.
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CONFORMATIONALLY CONSTRAINED MACROCYCLIC COMPOUNDS (Fri, 21 Apr 2017)
Conformationally constrained macrocyclic compounds of formula (I), including substituents E with at least one ester moiety, G and Q, as defined in the description and the claims, and salts thereof, can be metabolized to compounds that have the property to modulate the activity of the peptidyl-prolyl cis/trans isomerase Pin1. In addition, they show antiproliferative activity on various cancer cell lines. Thus, these compounds and pharmaceutical compositions containing said compounds may be useful in the treatment and/or prevention of diseases or conditions in the area of proliferative disorders and diseases, such as e.g. cancer, inflammatory diseases, transplant rejection, viral infections, osteolytic bone diseases, cardiac diseases, cardiovascular diseases, respiratory diseases, acute neurological diseases, neurodegenerative diseases, immune disorders, and lymphoproliferative theileriosis.
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BINDING INHIBITOR BETWEEN TCTP DIMER TYPE IGE-DEPENDENT HISTAMINE RELEASING FACTOR AND RECEPTOR THEREOF, AND USE THEREOF (Thu, 20 Apr 2017)
The present invention relates to a receptor-binding domain of an IgE-dependent histamine releasing factor (HRF), and a use thereof and, more specifically, ascertains, as an HRF framework region, an FL domain and an H2 domain which bind to a receptor of an HRF existing in a cell membrane, ascertains the C-terminus of the HRF, and ascertains that a material binding thereto inhibits IL-8 secretion, thereby determining that the FL and H2 domains and the C-terminus can be utilized in: the development of a therapeutic agent for and prevention of HRF-related diseases including malaria and inflammatory diseases such as asthma, bronchitis, chronic obstructive pulmonary disease, bronchiectasis, rhinitis, atopic dermatitis, hives, hay fever, conjunctivitis, anaphylactic allergic diseases, pneumonia, arthritis, nephritis, psoriasis, dermatitis, Crohn's disease, enteritis, gingivitis, arteriosclerosis, coronary arteritis, hepatitis, Behcet's disease, bladder cancer, prostatitis, pyelonephritis, glomerulonephritis, osteomyelitis, thyroiditis, uveitis, abdominal cavity inflammation, meningitis, pulmonary fibrosis and rheumatoid arthritis; and a method for screening for the HRF-related diseases.
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COMPOSITION COMPRISING CYCLODEXTRIN AND BUDESONIDE DERIVATIVES FOR THE TREATMENT AND PROPHYLAXIS OF PULMONARY INFLAMMATIONS (Thu, 13 Apr 2017)
The present invention relates to novel and useful pharmaceutical compositions formulated with a cyclodextrin compound and a budesonide derivative for the treatment and/or prevention of pulmonary inflammatory disease. The present invention also relates to a novel and useful analytical technique for the detection and the quantification of ΗΡ-β-CD in solution. More specifically, the present invention relates to the use of a validated 1H NMR analysis for the detection and quantification of cyclodextrins directly in pharmaceutical formulations without any extraction or separation steps for liquid formulations.
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BIOMARKERS AND METHODS FOR ASSESSING RESPONSE TO INFLAMMATORY DISEASE THERAPY WITHDRAWAL (Fri, 07 Apr 2017)
Provided herein are methods for assessing response to inflammatory disease therapy. The methods include placing a subject on a therapeutic regimen and subsequently performing an immunoassay to generate a score based on quantitative data for expression of biomarkers relating to inflammatory biomarkers. The methods further include recommending that the subject either remains on the therapeutic regimen, or is removed from the therapeutic regimen, based on the score.
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SUBSTITUTED PYRIDINE-2-CARBOXAMIDE COMPOUNDS AS APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS (Thu, 06 Apr 2017)
The present invention relates to compounds of Formula (I): Wherein variables are as defined above. The compounds have apoptosis signal-regulating kinase ("ASK1") inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases.
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Amyloid beta peptides as therapy for multiple sclerosis (Wed, 05 Apr 2017)
<p id="p-0001" num="0000">The invention provides methods for treating inflammatory diseases by administering to the subject an effective amount of an amyloid beta peptide, where the dose is effective to suppress or prevent initiation, progression, or relapses of disease, including the progression of established disease.</p>
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1-((3S,4R)-4-(3-FLUOROPHENYL)-1-(2-METHOXYETHYL)PYRROLIDIN-3-YL)-3-(4-METHYL-3-(2-METHYLPYRIMIDIN-5-YL)-1-PHENYL-1H-PYRAZOL-5-YL)UREA AS A TRKA KINASE INHIBITOR (Fri, 31 Mar 2017)
<p id="p-0001" num="0000">Provided is Compound (I) or a pharmaceutically acceptable salt thereof, which is an inhibitor of TrkA kinase and is useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation and inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis, pelvic pain syndrome, diseases related to an imbalance of the regulation of bone remodeling, and diseases resulting from Connective Tissue Growth Factor aberrant signaling.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="48.43mm" wi="66.72mm" file="US20170087156A1-20170330-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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AMINE DERIVATIVES AS POTASSIUM CHANNEL BLOCKERS (Fri, 31 Mar 2017)
<p id="p-0001" num="0000">The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.</p>
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BENZIMIDAZOLES FOR USE IN THE TREATMENT OF CANCER AND INFLAMMATORY DISEASES (Fri, 31 Mar 2017)
Provided herein are methods for treating, preventing, or ameliorating one or more symptoms of a condition, disorder, or disease mediated by a lipid kinase or a protein kinase with benzimidazoles, for example, of Formula I or II, and pharmaceutical compositions thereof. Also provided herein are benzimidazoles, and pharmaceutical compositions thereof; and methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.
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METHODS FOR THE TREATMENT OF CANCER AND INFLAMMATORY DISEASES USING CEREBLON AS A PREDICTOR (Fri, 31 Mar 2017)
Uses of the protein cereblon as a predictor of clinical sensitivity to cancer, inflammatory diseases, and patient response to drug treatment.
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PURINONE COMPOUNDS AS KINASE INHIBITORS (Thu, 30 Mar 2017)
Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
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COMPOUNDS FOR THE MODULATION OF RIP2 KINASE ACTIVITY (Fri, 24 Mar 2017)
The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of diseases and conditions mediated by the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.
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CARBORANE COMPOUNDS AND METHODS OF USE THEREOF (Fri, 24 Mar 2017)
Disclosed herein are compounds comprising dicarba-closo-dodecaborane. The compounds can be, for example, estrogen receptor beta (ERβ) agonists. In some examples, the compounds can be selective ERβ agonists. Also provided herein are methods of treating, preventing, or ameliorating cancer in a subject, suppressing tumor growth in a subject, treating an inflammatory disease in a subject, treating a neurodegenerative disease in a subject, treating a psychotropic disorder in a subject, or a combination thereof, by administering to a subject a therapeutically effective amount of one or more of the compounds or compositions described herein, or a pharmaceutically acceptable salt thereof.
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TRICYCLIC COMPOUND AND JAK INHIBITOR (Thu, 23 Mar 2017)
Novel tricyclic compounds which have JAK inhibitory activities are useful for prevention, treatment or improvement of autoimmune diseases, inflammatory diseases and allergic diseases are provided. Novel tricyclic compound represented by the formula (I), the formula (II) or the formula (III) (wherein : each of A 1 , A 2 and A 3 is a cyclohexane-1,4-diyl group or the like; each of L 1 , L 2 and L 3 is a methylene group or the like; each of X 1 and X 3 is O or NH; each of R 1 and R 3 is a cyano C 1-6 haloalkyl group or the like; and R 2 is an aromatic heterocyclic group), a tautomer or pharmaceutically acceptable salt of the compound or a solvate thereof.
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Biomarkers and Methods for Measuring and Monitoring Inflammatory Disease Activity (Fri, 17 Mar 2017)
<p id="p-0001" num="0000">Biomarkers useful for diagnosing and assessing inflammatory disease are provided, along with kits for measuring their expression. The invention also provides predictive models, based on the biomarkers, as well as computer systems, and software embodiments of the models for scoring and optionally classifying samples. The biomarkers include at least two biomarkers selected from the DAIMRK group and the score is a disease activity index (DAI).</p>
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IL-17A/F HETEROLOGOUS POLYPEPTIDES AND THERAPEUTIC USES THEREOF (Fri, 17 Mar 2017)
<p id="p-0001" num="0000">The present invention is directed to a novel naturally occurring human cytokine that is comprised of a heterodimer of interleukin-17 and interleukin-17F designated herein as interleukin 17A/F (IL-17A/F). Also provided herein are vectors and host cells comprising those nucleic acid sequences, chimeric polypeptide molecules comprising the polypeptides of the present invention fused to heterologous polypeptide sequences, specific antibodies which bind to the polypeptides of the present invention and to methods for producing the polypeptides of the present invention. Further provided herein are methods for treating degenerative cartilaginous disorders and other inflammatory diseases.</p>
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SUPRAMETALLOGELS AND USES THEREOF (Fri, 17 Mar 2017)
<p id="p-0001" num="0000">The disclosure provides nanostructures (e.g., nanospheres and nano-paddlewheels) formed through transition metal-ligand (e.g., Pd(II)-, Ni(II)-, or Fe(II)-ligand of Formula (A)) coordination and junction self-assembly. The disclosure also provides supramolecular complexes that include the nanostructures connected by divalent linkers Y. The provided supramolecular complexes are able to form gels (e.g., hydrogels). The gels are suprametallogels and exhibited excellent mechanical properties without sacrificing self-healing and showed high robustness and storage modulus. The present disclosure further provides compositions (e.g., gels) that include the nanostructures or supramolecular complexes and optionally an agent (e.g., small molecule), where the nanostructures and the nanostructure moieties of the supramolecular complexes may encapsulate and slowly release the agent. The nanostructures, supramolecular complex, and compositions may be useful in delivering an agent to a subject, tissue, or cell, as super-absorbent materials, and in treating a disease (e.g., a genetic diseases, proliferative disease (e.g., cancer or benign neoplasm), hematological disease, neurological disease, gastrointestinal disease (e.g., liver disease), spleen disease, respiratory disease (e.g., lung disease), painful condition, genitourinary disease, musculoskeletal condition, infectious disease, inflammatory disease, autoimmune disease, psychiatric disorder, or metabolic disorder).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="57.07mm" wi="51.05mm" file="US20170073311A1-20170316-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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INHIBITORS OF CYCLIN-DEPENDENT KINASES (Fri, 17 Mar 2017)
The present invention provides novel compounds of Formulae (I'), (I), (II'), and (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., CDK7, CDK12, or CDK13), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
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SALTS AND SOLID FORM OF A BTK INHIBITOR (Fri, 10 Mar 2017)
<p id="p-0001" num="0000">Disclosed herein are processes for preparing 2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile free base (compound (I)), salts of compound (I) and solid state form of said salts. Also disclosed herein are pharmaceutical compositions comprising such salts and solid state form thereof and methods of treating cancer, autoimmune, and inflammatory diseases using compound (I) or a pharmaceutically acceptable salt thereof.</p>
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WITHAFERIN A ANALOGS AND USES THEREOF (Fri, 10 Mar 2017)
<p id="p-0001" num="0000">The present invention provides a novel class of withanolides that have been isolated from <i>W. somnifera </i>under aeroponic conditions or produced semi-synthetically from withanolide natural products. The invention also provides pharmaceutical compositions thereof and methods for using the same in proliferative diseases, neurodegenerative diseases, autoimmune, and inflammatory diseases.</p>
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SUBSTITUTED AMINO TRIAZOLES USEFUL AS HUMAN CHITINASE INHIBITORS (Fri, 10 Mar 2017)
<p id="p-0001" num="0000">Disclosed are amino triazole compounds substituted with a piperidinyl ring that is itself substituted with a heterocyclic ring. These compounds are inhibitors of acidic mammalian chitinase and chitotriosidase. Also disclosed are methods of using the compounds to treat asthma reactions caused by allergens, as well as acute and chronic inflammatory diseases, autoimmune diseases, dental diseases, neurologic diseases, metabolic diseases, liver diseases, polycystic ovary syndrome, endometriosis, and cancer.</p>
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AGENTS FOR USE IN THE TREATMENT OF CARDIOVASCULAR AND INFLAMMATORY DISEASES STRUCTURALLY BASED ON 4(1 H)-QUINOLONE (Fri, 10 Mar 2017)
<p id="p-0001" num="0000">The present invention provides a compound of formula I, a tautomer thereof, or a pharmaceutically acceptable salt or N-oxide thereof for use in the treatment or prevention of cardiovascular disease or of an inflammatory disease or condition:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.86mm" wi="53.17mm" file="US20170066722A1-20170309-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">wherein:</li> <li id="ul0002-0002" num="0000">V is N or CR<sub>3</sub>;</li> <li id="ul0002-0003" num="0000">X is N or CR<sub>4</sub>;</li> <li id="ul0002-0004" num="0000">Y is N or CR<sub>5</sub>;</li> <li id="ul0002-0005" num="0000">Z is N or CR<sub>6</sub>;</li> <li id="ul0002-0006" num="0000">B is —(C═O)R<sub>1</sub>, a 5- to 10-membered heteroaryl group, or a group</li> <li id="ul0002-0007" num="0000">-L′″-NRR′, wherein R and R′ are the same or different and each represents a hydrogen atom, a C<sub>1</sub>-C<sub>6 </sub>alkyl group or a C<sub>1</sub>-C<sub>6 </sub>haloalkyl group;</li> <li id="ul0002-0008" num="0000">R<sub>1 </sub>is a 5- to 10-membered heterocyclyl group, or —OR′, wherein R′ is a hydrogen atom, a C<sub>1</sub>-C<sub>6 </sub>alkyl group or a C<sub>1</sub>-C<sub>6 </sub>haloalkyl group, or R<sub>1 </sub>is a proteinogenic α amino acid, which is linked to the carbonyl moiety in the compound of formula (I) via the α amino group, which amino acid is optionally esterified at the α carboxylic acid group with a C<sub>1</sub>-C<sub>6 </sub>alkyl group or a C<sub>6</sub>-C<sub>10 </sub>aryl group, or R<sub>1 </sub>is —NR″R′″, —NR<sup>IV</sup>-L′″-CONR″R′″, or —NR<sup>IV</sup>-L′″-COOR, wherein R, R″, R′″ and R<sup>IV </sup>are the same or different and each represents a hydrogen atom, a C<sub>1</sub>-C<sub>6 </sub>alkyl group or a C<sub>1</sub>-C<sub>6 </sub>haloalkyl group;</li> <li id="ul0002-0009" num="0000">either (a) W is N and R<sub>9 </sub>and R<sub>2 </sub>together form a bond, or (b) W is CR<sub>8</sub>, R<sub>8 </sub>and R<sub>9 </sub>together form a bond and R<sub>2 </sub>is a hydrogen atom, or a C<sub>1</sub>-C<sub>6 </sub>alkyl, C<sub>1</sub>-C<sub>6 </sub>haloalkyl, C<sub>6</sub>-C<sub>10 </sub>aryl, 5- to 10-membered heteroaryl, 5- to 10-membered heterocyclyl, -L′-A<sub>2</sub>, C<sub>3</sub>-C<sub>10 </sub>cycloalkyl, or —COOR′ group, wherein R′ is a hydrogen atom or C<sub>1</sub>-C<sub>6 </sub>alkyl group, or, when Z is a moiety CR<sub>6</sub>, R<sub>2 </sub>may form, together with R<sub>6 </sub>and the carbon and nitrogen atoms which connect R<sub>2 </sub>and R<sub>6 </sub>in the formula (I), a 5- to 6-membered heterocyclic ring;</li> <li id="ul0002-0010" num="0000">R<sub>3 </sub>is a hydrogen atom, a halogen atom, or a hydroxy, C<sub>1</sub>-C<sub>6 </sub>alkyl, C<sub>1</sub>-C<sub>6 </sub>alkoxy, C<sub>1</sub>-C<sub>6 </sub>haloalkyl, C<sub>1</sub>-C<sub>6 </sub>haloalkoxy, nitro, or —NR′R″ group, wherein R′ and R″ are the same or different and each represent a hydrogen atom or C<sub>1</sub>-C<sub>6 </sub>alkyl group;</li> <li id="ul0002-0011" num="0000">R<sub>4 </sub>and R<sub>5 </sub>are the same or different and each represent a hydrogen atom, a halogen atom, or a hydroxyl, C<sub>1</sub>-C<sub>8 </sub>alkyl, C<sub>1</sub>-C<sub>8 </sub>haloalkyl, C<sub>1</sub>-C<sub>6 </sub>alkoxy, C<sub>1</sub>-C<sub>6 </sub>haloalkoxy, nitro, —NR′R″, —CO<sub>2</sub>R′″, C<sub>6</sub>-C<sub>10 </sub>aryl, 5- to 10-membered heteroaryl, 5 to 10-membered heterocyclyl, or —CO—(C<sub>1</sub>-C<sub>6 </sub>alkyl) group, wherein R′, R″ and R′″ are the same or different and each represent a hydrogen atom or C<sub>1</sub>-C<sub>6 </sub>alkyl group, or R<sub>4 </sub>and R<sub>5 </sub>and the carbon atoms bonded to R<sub>4 </sub>and R<sub>5 </sub>together form a 5- to 6-membered heterocyclic ring;</li> <li id="ul0002-0012" num="0000">R<sub>6 </sub>is a hydrogen atom, a halogen atom, or a C<sub>1</sub>-C<sub>6 </sub>alkyl, C<sub>1</sub>-C<sub>6 </sub>haloalkyl, C<sub>1</sub>-C<sub>6 </sub>alkoxy, C<sub>1</sub>-C<sub>6 </sub>haloalkoxy or —CO<sub>2</sub>R′ group, wherein R′ is hydrogen or C<sub>1</sub>-C<sub>6 </sub>alkyl, or, when W is a moiety CR<sub>8</sub>, R<sub>6 </sub>may form, together with R<sub>2 </sub>and the carbon and nitrogen atoms which connect R<sub>6 </sub>and R<sub>2 </sub>in the formula (I), a 5- to 6-membered heterocyclic ring;</li> <li id="ul0002-0013" num="0000">R<sub>7 </sub>is a hydrogen atom, a halogen atom, or a C<sub>1</sub>-C<sub>6 </sub>alkyl, or C<sub>1</sub>-C<sub>6 </sub>haloalkyl group,</li> <li id="ul0002-0014" num="0000">A<sub>2 </sub>represents a C<sub>6</sub>-C<sub>10 </sub>aryl or 5- to 10-membered heteroaryl group;</li> <li id="ul0002-0015" num="0000">L′, and L′″ are the same or different and each represent a C<sub>1</sub>-C<sub>6 </sub>alkylene, C<sub>2</sub>-C<sub>6 </sub>alkenylene, or C<sub>2</sub>-C<sub>6 </sub>alkynylene group;</li> <li id="ul0002-0016" num="0000">said aryl, heteroaryl, cycloalkyl and heterocyclyl groups being unsubstituted or substituted with one or more substituents selected from halogen, hydroxy, C<sub>1</sub>-C<sub>4 </sub>alkyl, C<sub>1</sub>-C<sub>4 </sub>hydroxyalkyl, C<sub>1</sub>-C<sub>4 </sub>alkoxy, C<sub>1</sub>-C<sub>4 </sub>haloalkyl, C<sub>1</sub>-C<sub>4 </sub>haloalkoxy, —SOR, —SO<sub>2</sub>R, —NR′R″, —NR′(C═O)R″, —COOR, nitro and cyano substituents, wherein R, R′ and R″ are the same or different and each represents a hydrogen atom or C<sub>1</sub>-C<sub>4 </sub>alkyl group.</li> </ul> </li> </ul> </p>
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POLYFLUORINATED COMPOUNDS ACTING AS BRUTON TYROSINE KINASE INHIBITORS (Fri, 10 Mar 2017)
<p id="p-0001" num="0000">Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton's tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.</p>
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Fumarate Analogs and Uses Thereof (Fri, 10 Mar 2017)
<p id="p-0001" num="0000">Aspects of the present disclosure include compounds that find use for the treatment of a variety of autoimmune and inflammatory diseases and disorders. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.</p>
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CYCLIC COMPOUNDS (Fri, 10 Mar 2017)
<p id="p-0001" num="0000">The present invention provides compounds having a Toll-like receptor 4 (TLR4) signaling inhibitory action useful as preventive and therapeutic drugs of inflammatory disease and/or central nervous system disease or diseases such as chemotherapy-induced peripheral neuropathy (CIPN), chemotherapy-induced neuropathic pain (CINP), liver injury, ischemia-reperfusion injury (IRI) and the like. The present invention relates to a compound represented by formula (I) and a salt thereof:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.14mm" wi="60.03mm" file="US20170066737A1-20170309-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein, each symbol is explained in greater detail in the specification.</p>
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HETEROCYCLIC COMPOUNDS (Fri, 10 Mar 2017)
The present invention provides a heterocyclic compound a TLR7 and/or TLR9 and/or TLR-7/8/9 and/or TLR-7/8 and/or TLR-7/9 inhibitory action, which is useful as an agent for the prophylaxis or treatment of autoimmune diseases and/or inflammatory diseases and the like, in particular, acute decompensated heart failure, non-alcoholic steatohepatitis (NASH), IgA nephropathy, Duchenne muscular dystrophy (DMD), systemic lupus erythematosus, Sjogren's syndrome, rheumatoid arthritis, psoriasis, inflammatory bowel disease, asthma, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, B-cell malignancies, transplant rejection and graft-versus-host disease, hepatocellular carcinoma (HCC) and the like. The present invention is a compound represented by the formula (1) : wherein each symbol is as described in the specification, or a salt thereof.
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SUBSTITUTED AMINO TRIAZOLES USEFUL AS HUMAN CHITINASE INHIBITORS (Fri, 10 Mar 2017)
Disclosed are amino triazole compounds substituted with a piperidinyl ring that is itself substituted with a heterocyclic ring. These compounds are inhibitors of acidic mammalian chitinase and chitotriosidase. Also disclosed are methods of using the compounds to treat asthma reactions caused by allergens, as well as acute and chronic inflammatory diseases, autoimmune diseases, dental diseases, neurologic diseases, metabolic diseases, liver diseases, polycystic ovary syndrome, endometriosis, and cancer.
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MALT1 INHIBITORS AND USES THEREOF (Fri, 10 Mar 2017)
Provided herein are compounds of Formula (I) and pharmaceutical compositions thereof, which may be useful as MALT1 inhibitors. Also provided are for the treatment of proliferative disorders (e.g., cancer (e.g., non-Hodgkin' s lymphoma, diffuse large B-cell lymphoma, MALT lymphoma), benign neoplasm, a disease associated with angiogenesis,an autoimmune disease, an inflammatory disease, an autoinflammatory disease) by administering a compound of Formula (I).
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Site directed mutagenesis of trem-1 antibodies for decreasing viscosity (Fri, 10 Mar 2017)
Antibodies that are capable of specifically binding and preventing the activation of TREM-1, a protein expressed on monocytes, macrophages and neutrophils with both good affinity and low viscosity at clinically relevant concentrations are described. Such antibodies find utility in the treatment of individuals with an inflammatory disease, such as rheumatoid arthritis and inflammatory bowel disease.
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POLYFLUORINATED COMPOUNDS ACTING AS BRUTON'S TYROSINE KINASE INHIBITORS (Thu, 09 Mar 2017)
Provided herein are novel multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof, methods for preparing the same, and therapeutic methods by administering the compounds and formulation thereof to treat and inhibit autoimmune diseases or disorders, heteroimmune diseases or disorders, inflammatory diseases and cancers or disorders.
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TRICYCLIC INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (Fri, 03 Mar 2017)
<p id="p-0001" num="0000">The invention provides for compositions comprising phosphorous containing tricyclic compounds, including phthalazin-1(2H)-one derivatives. The compounds are potent inhibitors of the enzyme poly(ADP-ribose)polymerase (PARP), particularly PARP-1 and potentially PARP-2. The also show good cellular activity in inhibiting poly(ADP-ribose) oligomer formation. The compounds may be useful as mono-therapy or in combination with other therapeutic agents in the treatment conditions where PARP is implicated, such as cancer, inflammatory diseases and ischemic conditions. Thus, also provided are methods for the treatment of a condition where PARP is implicated comprising administering to an effective amount of a compound of the invention to an individual in need thereof.</p>
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NOVEL COMPOUNDS (Fri, 03 Mar 2017)
<p id="p-0001" num="0000">There are provided compounds of formula (I) as defined in the specification which are p38 MAP kinase inhibitors for use as medicaments for the treatment inter alia of inflammatory diseases.</p>
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NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS (Fri, 03 Mar 2017)
<p id="p-0001" num="0000">The present invention discloses compounds according to Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="34.54mm" wi="69.85mm" file="US20170057928A1-20170302-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein Cy, R<sup>1</sup>, L<sub>1</sub>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, L<sub>a</sub>, and R<sup>a </sup>are as defined herein.</p> <p id="p-0004" num="0000">Novel benzimidazoles according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic diseases, inflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons.</p>
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SIALYLTRANSFERASE INHIBITORS AND USES THEREOF (Fri, 03 Mar 2017)
Disclosed herein are novel sialyltransferase inhibitors, and compositions and methods for treating diseases and/or conditions associated with the activation of sialyltransferase, such as a cancer, an immune disease or an inflammatory disease.
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METHOD OF PROVIDING MONOCLONAL AUTO-ANTIBODIES WITH DESIRED SPECIFICITY (Fri, 24 Feb 2017)
<p id="p-0001" num="0000">Provided are novel binding molecules of human origin, particularly human antibodies as well as fragments, derivatives and variants thereof that recognize antigens such as native endogenous proteins associated with, e.g., immune response, autoimmune disorders, inflammatory diseases, metabolic disorders, vascular function, neurodegenerative diseases or tumors. More particularly, a human Auto-Immunosome and corresponding monoclonal antibody reservoir are provided. In addition, pharmaceutical compositions, kits and methods for use in diagnosis and therapy of are described.</p>
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INHIBITORS OF BRUTON'S TYROSINE KINASE (Fri, 24 Feb 2017)
<p id="p-0001" num="0000">Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.</p>
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INHIBITING THE TRANSIENT RECEPTOR POTENTIAL A1 ION CHANNEL (Fri, 24 Feb 2017)
<p id="p-0001" num="0000">The present invention relates to compounds of the Formula (I), or a pharmaceutically acceptable salt, pharmaceutical preparation, or pharmaceutical composition thereof, and their use for the treatment of pain, inflammatory disease, neuropathy, dermatological disorders, pulmonary conditions, and cough, as well as inhibiting the Transient Receptor Potential A1 ion channel (TRPA1).</p>
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TETRAHYDROOXEPINOPYRIDINE COMPOUND (Fri, 24 Feb 2017)
<p id="p-0001" num="0000">[Problem] Provided is a compound having a positive allosteric modulating activity (PAM activity) on an α7 nicotinic acetylcholine receptor (α7 nACh receptor).</p> <p id="p-0002" num="0000">[Means for Solution] The present inventors have studied on a PAM activity on an α7 nACh receptor, and they have found that a tetrahydrooxepinopyridine compound has a PAM activity on an α7 nACh receptor, thereby completing the present invention. The tetrahydrooxepinopyridine compound of the present invention has a PAM activity on an α7 nACh receptor and can be expected as an agent for preventing or treating dementia, cognitive impairment, schizophrenia, Alzheimer's disease, CIAS, negative symptoms of schizophrenia, inflammatory diseases, or pain.</p>
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3-(PYRIDIN-3-YL)-ACRYLAMIDE AND N-(PYRIDIN-3-YL)-ACRYLAMIDE DERIVATIVES AND THEIR USE AS PAK OR NAMPT MODULATORS (Fri, 24 Feb 2017)
The invention generally relates to cyclic compounds and, more particularly, to a compound represented by Structural Formula I: or a pharmaceutically acceptable salt thereof and pharmaceutical compositions comprising the multicyclic compounds. The invention also relates to a method for treating a disease or disorder selected from cancer (e.g., lymphoma, such as mantle cell lymphoma), a neurodegenerative disease, an inflammatory diseases or an immune system disease (e.g., a T- Cell mediated autoimmune diseases) in a subject in need thereof. The method comprises administering to a subject in need thereof a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof, or a composition comprising a compound of the invention, or a pharmaceutically acceptable salt thereof.
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(S,E)-3-(6-AMINOPYRIDIN-3-YL)-N-((5-(4-(3-FLUORO-3-METHYLPYRROLIDINE-1-CARBONYL)PHENYL)-7-(4-FLUOROPHENYL)BENZOFURAN-2-YL)METHYL)ACRYLAMIDE FOR THE TREATMENT OF CANCER (Fri, 24 Feb 2017)
The invention generally relates to substituted benzofuranyl compounds and, more particularly, to a compound represented by Structural Formula la: (I) or a pharmaceutically acceptable salt thereof. The invention also includes the synthesis and use of the compound of Structural Formula la, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of diseases or disorder selected from cancer (e.g., lymphoma, such as mantle cell lymphoma), a neurodegenerative disease, an inflammatory diseases or an immune system disease (e.g., a T-Cell mediated autoimmune disesase) in a subject in need thereof. The method comprises administering to a subject in need thereof a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof, or a composition comprising a compound of the invention, or a pharmaceutically acceptable salt thereof.
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CYCLOPROPYLDERIVATIVES AND THEIR USE AS KINASE INHIBITORS (Fri, 24 Feb 2017)
The invention generally relates to cyclic compounds and, more particularly, to a compound represented by Structural Formula I: or a pharmaceutically acceptable salt thereof and pharmaceutical comopositions comprising the multicyclic compounds. The invention also relates to a method for treating a disease or disorder selected from cancer (e.g., lymphoma, such as mantle cell lymphoma), a neurodegenerative disease, an inflammatory diseases or an immune system disease (e.g., a T-Cell mediated autoimmune disesase) in a subject in need thereof. The method comprises administering to a subject in need thereof a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof, or a composition comprising a compound of the invention, or a pharmaceutically acceptable salt thereof.
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NEW COMPOUNDS I (Fri, 17 Feb 2017)
<p id="p-0001" num="0000">The present invention relates to compounds of formula (I),</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.21mm" wi="60.28mm" file="US20170044157A1-20170216-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and their pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers or N-oxides, which are inhibitors of SSAO activity. The invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the treatment of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases and immune disorders.</p>
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TRICYCLIC COMPOUND AND JAK INHIBITOR (Fri, 17 Feb 2017)
<p id="p-0001" num="0000">Novel tricyclic compounds which have JAK inhibitory activities are useful for prevention, treatment or improvement of autoimmune diseases, inflammatory diseases and allergic diseases are provided.</p> <p id="p-0002" num="0000">Novel tricyclic compound represented by the formula (I), the formula (II) or the formula (III) (wherein each of A<sup>1</sup>, A<sup>2 </sup>and A<sup>3 </sup>is a cyclohexane-<b>1,4</b>-diyl group or the like; each of L<sup>1</sup>, L<sup>2 </sup>and L<sup>3 </sup>is a methylene group or the like: each of X<sup>1 </sup>and X<sup>3 </sup>is O or NH; each of R<sup>1 </sup>and R<sup>3 </sup>is a cyano C<sub>1-6 </sub>haloalkyl group or the like; and R<sup>2 </sup>is an aromatic heterocyclic group), a tautomer or pharmaceutically acceptable salt of the compound or a solvate thereof.</p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="111.34mm" wi="69.85mm" file="US20170044161A1-20170216-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Prostaglandin Receptor EP2 Antagonists, Derivatives, Compositions, and Uses Related Thereto (Fri, 17 Feb 2017)
<p id="p-0001" num="0000">The disclosure relates to Prostaglandin receptor EP2 antagonists, derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing conditions and diseases in which EP2 receptor activation has a physiological role, such as but not limited to, brain injury, inflammatory diseases, neuroinflamation after a seizure, pain, endometriosis, cancer, rheumatoid arthritis, skin inflammation, vascular inflammation, colitis, and neurological disorders by administering a pharmaceutical composition comprising a compound disclosed herein to a subject in need thereof.</p>
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TETRA-O-SUBSTITUTED BUTANE-BRIDGE MODIFIED NDGA DERIVATIVES, THEIR SYNTHESIS AND PHARMAECUTICAL USE (Fri, 17 Feb 2017)
<p id="p-0001" num="0000">The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers.</p>
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METHODS OF TREATING CANCERS, IMMUNE AND AUTOIMMUNE DISEASES, AND INFLAMMATORY DISEASES BASED ON BTK OCCUPANCY AND BTK RESYNTHESIS RATE (Fri, 17 Feb 2017)
In an embodiment, therapeutic methods and uses of Bruton's Tyrosine Kinase (BTK) inhibitors for treatment of cancer, inflammation, immune disorders, and autoimmune disorders, including dermatoses, and for transplantation prophylaxis, based on BTK occupancies and/or BTK resynthesis rates for B cells in various diseases, tissue compartments, including bone marrow and lymph nodes, are described. In an embodiment, dosing regimens for a BTK inhibitor for treatment of cancer, inflammation, immune disorders, and autoimmune disorders, including dermatoses, and for transplantation prophylaxis, based on BTK occupancies and/or BTK resynthesis rates for B cells in various diseases, tissue compartments, including bone marrow and lymph nodes, are described.
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PHENYLSULFONAMIDO-BENZOFURAN DERIVATIVES AND USES THEREOF IN THE TREATMENT OF PROLIFERATIVE DISEASES (Fri, 17 Feb 2017)
Described herein are phenylsulfonamido-benzofuran derivatives, and pharmaceutically acceptable salts thereof. Also provided are pharmaceutical compositions, methods, uses, and kits involving compounds of Formulae (I), (II), (III), (IV), (V), or (VI) for treating and/or preventing proliferative diseases (e.g. cancers, inflammatory diseases, and autoimmune diseases) in a subject. The compounds and pharmaceutical compositions as described herein inhibit at least one protein of the BCL-2 family in a biological sample or subject to treat and/or prevent a proliferative disease. In certain embodiments, compounds described herein are selective inhibitors of MCL-1, a BCL-2 family member protein.
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PHENYLSULFONAMIDO-BENZOFURAN DERIVATIVES AND USES THEREOF IN THE TREATMENT OF PROLIFERATIVE DISEASES (Fri, 17 Feb 2017)
Described herein are phenylsulfonamido-benzofuran derivatives, and pharmaceutically acceptable salts thereof. Also provided are pharmaceutical compositions, methods, uses, and kits involving compounds of Formulae (I), (II), (III), (IV), (V), or (VI) for treating and/or preventing proliferative diseases (e.g. cancers, inflammatory diseases, and autoimmune diseases) in a subject. The compounds and pharmaceutical compositions as described herein inhibit at least one protein of the BCL-2 family in a biological sample or subject to treat and/or prevent a proliferative disease. In certain embodiments, compounds described herein are selective inhibitors of MCL-1, a BCL-2 family member protein.
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NOVEL COMPOUND HAVING IMMUNE DISEASE TREATMENT EFFECT AND USE THEREOF (Thu, 16 Feb 2017)
The present invention relates to a novel compound capable of effectively preventing and treating immune diseases and a use thereof. The novel compound of the present invention has effects of inhibiting the formation of proinflammatory cytokines, increasing the activity of regulatory T cells having immunoregulatory functions, inhibiting the production of autoantibodies to regulate excessive immune responses, and inhibiting the differentiation to osteoclasts, and thus can be used for treating immune diseases, such as autoimmune diseases, inflammatory diseases, and transplant rejection diseases, which are caused by abnormal regulation of various kinds of immune responses.
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NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES (Fri, 10 Feb 2017)
<p id="p-0001" num="0000">[1,2,4]triazolo[1,5-a]pyridine compounds are disclosed that have a formula represented by the following:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.26mm" wi="69.85mm" file="US20170035738A1-20170209-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn's disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.g. diseases involving the anabolic stimulation of chondrocytes), congenital cartilage malformations, diseases associated with hypersecretion of IL6 and transplantation rejection (e.g. organ transplant rejection) and proliferative diseases.</p>
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DRUG DELIVERY CONJUGATES FOR TREATING RESISTANT CANCER AND FOR USE IN COMBINATION THERAPY (Fri, 10 Feb 2017)
<p id="p-0001" num="0000">Described herein are drug delivery conjugates for targeted therapy. In particular, described herein are drug delivery conjugates that include polyvalent linkers comprising one or more unnatural amino acids that are useful for treating cancers and inflammatory diseases. In some embodiments, the cancer is selected from the group consisting of a carcinoma, a sarcoma, a lymphoma, Hodgekin's disease, a melanoma, a mesothelioma, Burkitts lymphoma, a nasopharyngeal carcinoma, a leukemia, and a myeloma.</p>
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COMPOSITIONS AND METHODS FOR DELIVERY OF KINASE INHIBITING PEPTIDES (Fri, 10 Feb 2017)
<p id="p-0001" num="0000">The invention relates to compositions and methods for the treatment of inflammatory disease states. In particular, the invention relates to the use of a nanoparticle incorporated kinase inhibiting peptide to treat inflammatory disease states.</p>
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MANNOSE DERIVATIVES USEFUL FOR TREATING PATHOLOGIES ASSOCIATED WITH ADHERENT E. COLI (Fri, 10 Feb 2017)
The present invention relates to mannose derivatives of formula (I): wherein R1 represents H, CO-(C1-C6)-alkyl or CO-alkylaryl, Y represents a single bond, CH2, O, NR3, S, A represents O, NH or S, X represents H and X' represents OH or X and X' taken together with the carbon atom bearing them form a CO group, R2 represents H, a linear or branched (C1-C6 )-alkyl or CF3, R3 represents H, a C1-C6 alkyl, a CO-(C1-C6 )-alkyl, CF3 or COCF3, and R is as described in claim 1. The mannose derivatives of formulae (I) are useful for treating pathologies associated with the presence of adherent Escherichia coli (AEC), in particular inflammatory bowel diseases (IBD), such as Crohn's disease and ulcerative colitis; a urinary tract infection, in particular painful bladder syndrome and cystitis, more particularly interstitial cystitis; irritable bowel syndrome; metabolic diseases such as metabolic obesity, diabetes, hypercholesterolemia; autoimmune inflammatory diseases; and colorectal cancer, in particular colon cancer.
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ANTAGONISTS OF THE GOLGI REASSEMBLY-STACKING PROTEIN OF 55 KDA (GRASP55) AND USES THEREOF (Fri, 10 Feb 2017)
The present invention relates to new compounds useful as antagonists of the Golgi reassembly-stacking protein of 55 k Da (Grasp55), and in particular to their use as a non-hormonal male contraceptive. The present invention also relates to these compounds for use as a medicament, in particular for the treatment or the prevention of a disease selected from the group consisting of cancer, metastases and an inflammatory disease.
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PYRAZOLE PYRIMIDINE DERIVATIVE AND USES THEREOF (Fri, 10 Feb 2017)
The present invention provides pyrazole pyrimidine derivatives which inhibit Casein kinase I (CKI) and/or lnterleukin-1 receptor-associated kinase 1 (IRAKI) and methods of their manufacture, compositions comprising them and uses thereof in methods of treating malignant disease and disorders and methods for treating inflammatory diseases and disorders.
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MOTILE SPERM DOMAIN CONTAINING PROTEIN 2 AND INFLAMMATION (Fri, 10 Feb 2017)
Disclosed herein are methods of treating, preventing, or reducing the incidence of an inflammatory disease or disorder and methods of inhibiting, preventing, or reducing the incidence of one or more activities in a cell with an inhibitor of a Motile Sperm Domain containing Protein 2 (MOSPD2). Also disclosed are inhibitors of MOSPD2 and pharmaceutical compositions containing MOSPD2 inhibitors.
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Compositions and Methods for Treating Neoplasia, Inflammatory Disease and Other Disorders (Fri, 03 Feb 2017)
<p id="p-0001" num="0000">The invention features compositions and methods for treating or preventing a neoplasia. More specifically, the invention provides compositions and methods for disrupting the interaction of a BET family polypeptide comprising a bromodomain with chromatin (e.g., disrupting a bromodomain interaction with an acetyl-lysine modification present on a histone N-terminal tail).</p>
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HETEROCYCLIC COMPOUNDS AND USES THEREOF (Fri, 03 Feb 2017)
<p id="p-0001" num="0000">The present invention relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder, a cancer, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, dry eye or an immunologically related disease, and in some embodiments diseases or disorders related to the dysregulation of kinase such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, FLT3(D835Y), ITK, TEC, TXK, BTK, or JAK, and the respective pathways.</p>
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KINASE INHIBITOR (Fri, 03 Feb 2017)
<p id="p-0001" num="0000">There is provided a compound of formula VIIa,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.69mm" wi="75.52mm" file="US20170029378A1-20170202-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein Q<sup>x </sup>represents —C(O)O—C<sub>1-4 </sub>alkyl, or a salt or protected derivative thereof, and other compounds that are useful in the preparation of compounds that have antiinflammatory activity (e.g., through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and has use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.</p>
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MMF-DERIVATIVES OF ETHYLENEGLYCOLS (Fri, 03 Feb 2017)
<p id="p-0001" num="0000">The present invention relates to novel compounds, e.g. for use as a medicament. In particular, the present invention relates to novel prodrugs of monomethyl fumarate (MMF) suitable as a medicament, preferably in the treatment and/or prevention of systemic diseases, autoimmune diseases, inflammatory diseases, for example multiple sclerosis, rheumatoid arthritis and psoriasis.</p>
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NOVEL SULPHUR CONTAINING LIPIDS FOR USE AS FOOD SUPPLEMENT OR AS MEDICAMENT (Fri, 03 Feb 2017)
<p id="p-0001" num="0000">The present disclosure relates to lipid compounds of the general formula (I): (I) wherein R<sub>1 </sub>is selected from a C<sub>10</sub>-C<sub>22 </sub>alkyl, a C<sub>10</sub>-C<sub>22 </sub>alkenyl having 1-6 double bonds, and a C<sub>10</sub>-C<sub>22 </sub>alkynyl having 1-6 triple bonds; R<sub>2 </sub>and R<sub>3 </sub>are the same or different substituents; Y is selected from sulphur, sulfoxide, and sulfone; and X represents a carboxylic acid or a derivative thereof, a carboxylic ester, a carboxylic anhydride or a carboxamide; or a pharmaceutically acceptable salt, complex or solvate thereof. The disclosure also relates to pharmaceutical compositions and lipid compositions comprising such compounds, and to such compounds for use as medicaments or for use in therapy, in particular for the treatment of diseases related to the cardiovascular, metabolic and inflammatory disease area.</p>
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2-amino-benzimidazole derivatives and their use as 5-lipoxygenase and/or prostaglandin e synthase inhibitors (Fri, 03 Feb 2017)
The present invention relates to benzimidazole derivatives having the general formula I, wherein n is 0 or 1; X<sp>1</sp> and X<sp>2</sp> are independently, at each occurrence, CR<sp>5</sp> or N; Y is C<sb>1</sb>-C<sb>6</sb> alkylene, wherein alkylene is optionally substituted with one to two C<sb>1</sb>-C<sb>3</sb> alkyl groups; R<sp>1</sp> is selected from the group consisting of hydrogen, halogen, C<sb>1</sb>-C<sb>6</sb> alkoxy, -NH<sb>2</sb>, -NHR<sp>6</sp>, -NR<sp>7</sp>R<sp>8</sp> and -NH-(R<sp>9</sp>)<sb>n</sb>-R<sp>10</sp>, n being 0 or 1; R<sp>2</sp> is selected from the group consisting of hydrogen, halogen, C<sb>1</sb>-C<sb>6</sb> alkyl, -NH<sb>2</sb>, -NHR<sp>6</sp>, - NR<sp>7</sp>R<sp>8</sp> and -NH-(R<sp>9</sp>)<sb>n</sb>-R<sp>10</sp>; R<sp>3</sp> is selected from the group consisting of hydrogen, hydroxyl, OR<sp>11</sp>, -NR<sp>7</sp>R<sp>8</sp>, C<sb>1</sb>-C<sb>6</sb> alkoxy, C<sb>1</sb>-C<sb>6</sb> alkyl, C<sb>3</sb>-C<sb>10</sb> cycloalkyl, C<sb>1</sb>-C<sb>3</sb> haloalkyl, -C(O)NHR<sp>11</sp>, aryl, heteroaryl and heterocyclyl, wherein each of said cycloalkyl, aryl, heteroaryl and heterocyclyl is optionally and independently substituted with one to four R<sp>a</sp> groups; and R<sp>4</sp> is selected from the group consisting of -NH<sb>2</sb>, -N(R<sp>12</sp>)(V)<sb>p</sb>R<sp>13</sp>, - NH(V)<sb>p</sb>-OR<sp>14</sp>, -NHC(O)R<sp>15</sp>, and groups of formula la shown below, and their use in the treatment of diseases, in particular inflammatory diseases, cancer, stroke and/or Alzheimer's disease.
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Novel formulations of a Bruton's tyrosine kinase inhibitor (Fri, 03 Feb 2017)
Described herein is the Brutons tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including novel pharmaceutical formulations thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
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Quinoline derivatives for the treatment of inflammatory diseases (Fri, 03 Feb 2017)
The present invention relates to a compound of formula (I) wherein: Formula (II) means an aromatic ring wherein V is C or N and when V is N; Q is N or O, provided that R" does not exist when Q is O; R' independently represent a hydrogen atom or a group chosen among a (C<sb>1</sb>-C<sb>3</sb>)alkyl group, a halogen atom, a hydroxy! group, a - COOR<sb>1</sb> group, a -NO2 group, a -NR<sb>1</sb>R<sb>2</sb> group, a morpholinyl or a morpholino group, a N- methylpiperazinyl group, a (Ci-C3)fluoroalkyl group, a -O-P(=O)-(OR<sb>3</sb>XOR<sb>4</sb>) group, a (C<sb>1</sb>-C<sb>4</sb>)alkoxy group and a -CN group, and can further be a group chosen among:(IIa), (IIIa) or anyone of its pharmaceutically acceptable salt, for use in the treatment and/or prevention of an inflammatory disease.
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HETEROCYCLIC COMPOUND (Thu, 02 Feb 2017)
Provided is a compound having a superior PKC inhibitory action, and useful as a prophylactic or therapeutic agent for immune diseases, inflammatory diseases and the like, or a salt thereof. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a superior PKC inhibitory action, and is useful as a prophylactic or therapeutic agent for immune diseases, inflammatory diseases and the like.
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NATURAL AND SYNTHETIC COMPOUNDS FOR TREATING CANCER AND OTHER DISEASES (Fri, 27 Jan 2017)
<p id="p-0001" num="0000">This invention provides a method of synthesizing new active compounds for pharmaceutical uses including cancer treatment, wherein the cancers comprise breast, leukocytic, liver, ovarian, bladder, prostatic, skin, bone, brain, leukemia, lung, colon, CNS, melanoma, renal, cervical, esophageal, testicular, spleenic, kidney, lymphatic, pancreatic, stomach and thyroid cancers. This invention is an anti-adhesion therapy which uses the compound as a mediator or inhibitor of adhesion proteins and angiopoietins. It inhibits excess adhesion and inhibits cell attachment. It modulates angiogenesis. The compounds also use as mediator of cell adhesion receptor, cell circulating, cell moving and inflammatory diseases. The compounds are attached with angeloyl, acetyl, tigloyl, senecioyl, Crotonoyl, 3,3-Dimethylartyloyl, Cinnamoyl, Pentenoyl, Hexanoyl, benzoyl, Ethylbutyryl, benzoyl, dibenzoyl, alkanoyl, alkenoyl, benzoyl alkyl substituted alkanoyl, ethanoyl, propanoyl, propenoyl, butanoyl, butenoyl, pentanoyl, hexenoyl, heptanoyl, heptenoyl, octanoyl, octenoyl, nonanoyl, nonenoyl, decanoyl, decenoyl, propionyl, 2-propenoyl, 2-butenoyl, Isobutyryl, 2-methylpropanoyl, 2-ethylbutyryl, ethylbutanoyl, 2-ethylbutanoyl, butyryl, (E)-2,3-Dimethylacryloyl, (E)-2-Methylcrotonoyl, 3-cis-Methyl-methacryloyl, 3-Methyl-2-butenoyl, 3-Methylcrotonoyl, 4-Pentenoyl, (2E)-2-pentenoyl, Caproyl, 5-Hexenoyl, Capryloyl, Lauroyl, Dodecanoyl, Myristoyl, Tetradecanoyl, Oleoyl, O—C(2-18) Acyl.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="54.53mm" wi="72.14mm" file="US20170022246A1-20170126-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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LICOFELONE DERIVATIVES AND METHODS OF USE (Fri, 27 Jan 2017)
Derivatives of licofelone for the treatment of chronic inflammatory diseases and epithelial cancers associated with chronic inflammation are disclosed. The agents target mPGES-1 and 5-LOX.
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OXADIAZOLE DERIVATIVES USEFUL AS HDAC INHIBITORS (Fri, 27 Jan 2017)
The present invention provide a heterocyclic compound having a HDAC inhibitory action, and useful for the treatment of autoimmune diseases and/or inflammatory diseases, graft versus host disease, cancers, central nervous diseases including neurodegenerative diseases, Charcot-Marie-Tooth disease and the like, and a pharmaceutical composition comprising the compound. The present invention relates to a compound represented by the formula (I) : wherein each symbol is as defined in the specification, or a salt thereof.
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THERAPEUTIC/PREVENTIVE AGENT CONTAINING COUMARIN DERIVATIVE AS ACTIVE INGREDIENT (Thu, 26 Jan 2017)
An object of the present invention is to provide a preventive or therapeutic agent for inflammatory diseases or degenerative intervertebral disk diseases. A coumarin derivative or a pharmaceutically acceptable salt or hydrate thereof which is an active ingredient of the preventive or therapeutic agent of the present invention exhibits an excellent suppressive action in a pharmacological test where production of inflammation-related factor such as inflammatory cytokine or fibrosis-related factor as an index. Moreover, said compound also exhibits an excellent suppressive action to pulmonary fibrosis model animals and degenerative intervertebral disk disease model animals. Accordingly, the present invention is very useful as a preventive or therapeutic agent for inflammatory diseases and degenerative intervertebral disk diseases.
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BIOMARKERS AND METHODS FOR MEASURING AND MONITORING JUVENILE IDIOPATHIC ARTHRITIS ACTIVITY (Fri, 20 Jan 2017)
<p id="p-0001" num="0000">Biomarkers useful for assessing inflammatory disease or flare activity, in particular in juvenile idiopathic arthritis, are provided, along with kits for measuring expression of the biomarkers. The invention also provides predictive models, based on the biomarkers, as well as computer systems, and software embodiments of the models for scoring and optionally classifying samples.</p>
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HETEROCYCLIC COMPOUND (Fri, 20 Jan 2017)
<p id="p-0001" num="0000">The present invention provide a heterocyclic compound having a HDAC inhibitory action, and useful for the treatment of autoimmune diseases and/or inflammatory diseases, graft versus host disease, cancers, central nervous diseases including neurodegenerative diseases, Charcot-Marie-Tooth disease and the like, and a pharmaceutical composition comprising the compound.</p> <p id="p-0002" num="0000">The present invention relates to a compound represented by the formula (I):</p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="23.28mm" wi="69.85mm" file="US20170015655A1-20170119-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0004" num="0000">wherein each symbol is as defined in the specification, or a salt thereof.</p>
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BROMODOMAIN INHIBITORS (Fri, 20 Jan 2017)
<p id="p-0001" num="0000">The present invention provides for compounds of formula (I) wherein R<sup>x</sup>, X, Y, Y<sup>1</sup>, L<sup>1</sup>, A<sup>1</sup>, A<sup>2</sup>, A<sup>3</sup>, A<sup>4</sup>, A<sup>5</sup>, A<sup>6</sup>, A<sup>7</sup>, and A<sup>8</sup>, have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.52mm" wi="58.08mm" file="US20170015673A1-20170119-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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INHIBITORS OF BRUTON'S TYROSINE KINASE (Fri, 20 Jan 2017)
<p id="p-0001" num="0000">Disclosed herein are amido compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.</p>
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PECTIN COMPOSITIONS FOR PREVENTING AND TREATING INFLAMMATORY DISEASES (Fri, 20 Jan 2017)
This invention relates generally to compositions and methods for combating inflammatory disease and particularly to the use of feed or food compositions for preventing, reducing and/or treating inflammatory disorders, diseases, or discomforts, wherein the compositions comprising at least one specific pectin.
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INHIBITORS OF BRUTON'S TYROSINE KINASE (Fri, 13 Jan 2017)
<p id="p-0001" num="0000">Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.</p>
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1-PYRAZOLYL-3-(4-((2-ANILINOPYRIMIDIN-4 -YL) OXY) NAPTHTHALEN-1 - YL) UREAS AS P38 MAP KNASE INHIBITORS (Fri, 13 Jan 2017)
<p id="p-0001" num="0000">There are provided compounds of formula (I) which are inhibitors of the family of p38 mitogen-activated protein kinase enzymes, and to their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as asthma and COPD.</p>
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Pyrrolo[3,2-c]pyridine derivatives as TLR inhibitors (Fri, 13 Jan 2017)
<p id="p-0001" num="0000">The present invention provides a heterocyclic compound having a TLR7, TLR9, TLR7/8, TLR7/9 or TLR7/8/9 inhibitory action, which is useful as an agent for the prophylaxis or treatment of autoimmune diseases, inflammatory diseases and the like, in particular, systemic lupus erythematosus, Sjogren's syndrome, rheumatoid arthritis, psoriasis, inflammatory bowel disease and the like. The present invention is a compound represented by the formula (1): wherein each symbol is as described in the specification, or a salt thereof.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.87mm" wi="59.77mm" file="US09643967-20170509-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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ARYL SULTAM DERIVATIVES AS RORc MODULATORS (Fri, 13 Jan 2017)
Compounds of the formula I: or a pharmaceutical salt thereof, wherein p, s, A, R3 and Re are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
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HETEROBICYCLIC N-AMINOPHENYL-AMIDES AS INHIBITORS OF HISTONE DEACETYLASE (Fri, 13 Jan 2017)
This invention provides compounds that are inhibitors of HDAC2. The compounds (e.g., compounds according to Formula (I) or any one of Compounds 100-175) accordingly are useful for treating, alleviating, or preventing a condition in a subject such as a neurological disorder, memory or cognitive function disorder or impairment, extinction learning disorder, fungal disease or infection, inflammatory disease, hematological disease, or neoplastic disease, or for improving memory or treating, alleviating, or preventing memory loss or impairment.
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HETERO-HALO INHIBITORS OF HISTONE DEACETYLASE (Fri, 13 Jan 2017)
This invention provides compounds that are inhibitors of HDAC2. The compounds (e.g., compounds according to Formula I, II or any of Compounds 100-128 or any of those in Tables 2 or 3) accordingly are useful for treating, alleviating, or preventing a condition in a subject such as a neurological disorder, memory or cognitive function disorder or impairment, extinction learning disorder, fungal disease or infection, inflammatory disease, hematological disease, or neoplastic disease, or for improving memory or treating, alleviating, or preventing memory loss or impairment.
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ARYL SULTAM DERIVATIVES AS RORc MODULATORS (Fri, 13 Jan 2017)
Compounds of the formula I, or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, X1, X2, X3, X4, Y, Z, A, Het, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined herein.. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis, muscular sclerosis and psoriasis.
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1-((3S,4R)-4-(3-fluorophenyl)-1-(2-methoxyethyl)pyrrolidin-3-yl)-3-(4-methyl-3-(2-methylpyrimidin-5-yl)-1-phenyl-1h-pyrazol-5-yl)urea as a TrkA kinase inhibitor (Fri, 13 Jan 2017)
Provided is Compound (I) or a pharmaceutically acceptable salt thereof, which is an inhibitor of TrkA kinase and is useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation and inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis, pelvic pain syndrome, diseases related to an imbalance of the regulation of bone remodeling, and diseases resulting from Connective Tissue Growth Factor aberrant signaling.
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A novel compound isolated from Pseudolysimachion rotundum var. subintegrum containing abundant amount of active ingredient, the composition comprising the same for preventing or treating allergy disease, inflammatory disease, asthma or chronic obstructive pulmonary disease and the use thereof (Fri, 13 Jan 2017)
The present invention relates to a novel methanocyclopenta[e][1,3]dioxepin-7-yl 3,4-dihydroxybenzoate derivative (KS534) represented below as the Chemical Formula 1, the pharmaceutically acceptable salt or solvates thereof, a composition comprising the same as an active ingredient for preventing or treating allergic disease, inflammatory disease, asthma or chronic obstructive pulmonary disease (COPD) and the use thereof. Formula (1)
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Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity (Fri, 13 Jan 2017)
This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.
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A novel compound (KS 513) isolated from pseudolysimachion rotundum var. subintegrum, the composition comprising the same as an active ingredient for preventing or treating allergy disease, inflammatory disease, asthma or chronic obstructive pulmonary disease and the use thereof (Fri, 13 Jan 2017)
The present invention relates to a novel (1aS,1bS,2S,4S,5aR,6S,6aS)-1a-(hydroxymethyl)-4-methoxy-2-(((2S,3R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)octahydrooxireno[2',3':4,5]cyclopenta[1,2-c]pyran-6-yl 4-hydroxybenzoate} (KS-513), the isomer thereof, the pharmaceutically acceptable salt or solvates thereof, a composition comprising the same as an active ingredient for preventing or treating allergic disease, inflammatory disease, asthma or chronic obstructive pulmonary disease (COPD) and the use thereof.
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TARGETING AGENT ANTIBODY CONJUGATES AND USES THEREOF (Fri, 06 Jan 2017)
<p id="p-0001" num="0000">Methods, compositions and uses are provided for bispecific antibodies comprising one or more unnatural amino acids. The bispecific antibodies may bind to two or more different receptors, co-receptors, antigens, or cell markers on one or more cells. The bispecific antibodies may be used to treat a disease or condition (e.g., cancer, autoimmune disease, pathogenic infection, inflammatory disease). The bispecific antibodies may be used to modulate (e.g., stimulate or suppress) an immune response.</p>
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DERIVATIVES OF POLYHYDROXY COMPOUNDS (Fri, 06 Jan 2017)
<p id="p-0001" num="0000">The present invention relates to novel compounds, e.g. for use as a medicament. In particular, the present invention relates to novel prodrugs of monomethyl fumarate (MMF) suitable as a medicament, preferably in the treatment and/or prevention of systemic diseases, autoimmune diseases, inflammatory diseases, for example multiple sclerosis and psoriasis.</p>
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USE OF CELL-FREE NUCLEOSOMES AS BIOMARKERS IN FECAL SAMPLES (Fri, 06 Jan 2017)
The invention relates to the use of a cell-free nucleosome as a biomarker in a fecal sample for the diagnosis or detection of cancer, adenoma, autoimmune disease or inflammatory disease. The invention also relates to methods of detecting said cell free nucleosomes in fecal samples, in particular in methods of diagnosis.
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USE OF CELL-FREE NUCLEOSOMES AS BIOMARKERS IN SPUTUM SAMPLES (Fri, 06 Jan 2017)
The invention relates to the use of a cell-free nucleosome as a biomarker in a sputum sample for the diagnosis or detection of cancer, adenoma, autoimmune disease or inflammatory disease. The invention also relates to methods of detecting said cell free nucleosomes in sputum samples, in particular in methods of diagnosis.
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PYRROLOPYRIMIDINE COMPOUNDS AS KINASE INHIBITORS (Fri, 30 Dec 2016)
<p id="p-0001" num="0000">Disclosed herein are methods of using pyrrolo[2,3-d]pyrimidine Btk inhibitors, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, and inflammatory diseases or conditions.</p>
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COMPOSITION FOR TREATING OR PREVENTING INFLAMMATORY SKIN DISEASE, COMPRISING, AS ACTIVE INGREDIENT, IMMATURE CITRUS FRUIT EXTRACT, OR SYNEPHRINE OR SALT THEREOF (Fri, 30 Dec 2016)
<p id="p-0001" num="0000">The present invention relates to a composition for treating or preventing an inflammatory skin disease, comprising, as an active ingredient, an unripe <i>Citrus unshiu </i>fruit extract and/or Synephrine or salt thereof. The composition of the present invention prevents an inflammatory reaction by inhibiting activity of STAT6, expression of eotaxin-1 and an agglomeration function of eosinophil, and thus, shows effects of preventing and treating an allergic inflammatory disease, atopic dermatitis, eczema, psoriasis, etc. Also, the composition of the present invention does not have cytotoxicity and a skin side effect, and thus, can be safely applied to pharmaceutical products and cosmetics.</p>
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Bioactivity proanthocyanidin compound isolated from Lasia spinosa (L.) Thwait (Fri, 30 Dec 2016)
<p id="p-0001" num="0000">The present invention disclosed a compound, proanthocyanidin A1 (PA1), which is isolated from <i>Lasia spinosa </i>(L.) Thwait, for its effects in shortening of clolon length, reducing colonic tissue damage, suppressing colonic myeloperoxidase activity with colitis. The said compound can be used in treating inflammatory diseases and anti-cancer leading compound.</p>
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IL-18 binding molecules (Fri, 30 Dec 2016)
<p id="p-0001" num="0000">IL-18 participates in both innate and acquired immunity. The bioactivity of IL-18 is negatively regulated by the IL-18 binding protein (IL18BP), a naturally occurring and highly specific inhibitor. This soluble protein forms a complex with free IL-18 preventing its interaction with the IL-18 receptor, thus neutralizing and inhibiting its biological activity. The present invention discloses binding molecules, in particular antibodies or fragments thereof, which bind IL-18 and do not bind IL-18 bound to IL-18BP (IL-18/IL-18BP complex). Apart from its physiological role, IL-18 has been shown to mediate a variety of autoimmune and inflammatory diseases. The binding molecules of the inventions may be used as therapeutic molecules for treating IL-18-related autoimmune and inflammatory diseases or as diagnostic tools for characterizing, detecting and/or measuring IL-18 not bound to IL-18BP as component of the total IL-18 pool.</p>
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KINASE INHIBITORS (Fri, 30 Dec 2016)
<p id="p-0001" num="0000">There are provided compounds of formula IIb,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.68mm" wi="69.85mm" file="US20160376232A1-20161229-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein LG<sup>1 </sup>represents imidazolyl, chloro or aryloxy, which compounds are useful in the preparation of compounds that have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.</p>
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4,6-PYRIMIDINYLENE DERIVATIVES AND USES THEREOF (Fri, 30 Dec 2016)
The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., lung cancer, breast cancer, leukemia, lymphoma, melanoma, multiple myeloma, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase (e.g. a protein kinase (e.g. a cyclin-dependent kinase (CDK) (e.g. CDK7, CDK12, or CDK13) or a lipid kinase such as a phosphatidylinositol- 5 -phosphate 4- kinase (PIP4K) (e.g., ΡΙ5Ρ4Κα, ΡΙ5Ρ4Κβ, or ΡΙ5Ρ4Κγ)) in the subject.
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FUSED BICYCLIC PYRIMIDINE DERIVATIVES AND USES THEREOF (Fri, 30 Dec 2016)
The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., lung cancer, breast cancer, leukemia, lymphoma, melanoma, multiple myeloma, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase (e.g. a protein kinase (e.g. a cyclin-dependent kinase (CDK) (e.g. CDK7, CDK12, or CDK13) or a lipid kinase such as a phosphatidylinositol- 5 -phosphate 4- kinase (PIP4K) (e.g., ΡΙ5Ρ4Κα, ΡΙ5Ρ4Κβ, or ΡΙ5Ρ4Κγ)) in the subject.
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NOVEL 5-HT2 ANTAGONISTS (Fri, 30 Dec 2016)
The present invention relates to 1-amidino-3-aryl-2-pyrazoline derivatives of the general formula I The invention specifically relates to such derivatives which exhibit antagonizing activity towards serotonin 5-HT2B receptors. The present invention also relates to use of said compounds as a medicament and for the treatment of fibrosis, cardiovascular diseases, pain, IBD, and other inflammatory diseases, as well as pharmaceutical compositions comprising one or more of said compounds and methods of treatment.
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CRYSTALLINE L-ARGININE SALT OF (R)-2-(7-(4-CYCLOPENTYL-3-(TRIFLUOROMETHYL)BENZYLOXY)-1,2,3,4-TETRAHYDROCYCLO-PENTA[B]INDOL-3-YL)ACETIC ACID(COMPOUND1) FOR USE IN SIPI RECEPTOR-ASSOCIATED DISORDERS (Fri, 30 Dec 2016)
The present invention relates to, inter alia, a novel crystalline free- plate habit or morphology, processes for preparing the crystalline free-plate habit, and uses of the crystalline free-plate habit of the L- arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy) -l,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid(Compound1) in the treatment of SIPjreceptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditionscharacterized byan underlying defect in the vascular integrity or that are associated with angiogenesis such as may be pathologic(e.g.,as may occur in inflammation, tumor development, and atherosclerosis).
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NOVEL 5-HT2 ANTAGONISTS (Thu, 29 Dec 2016)
The present invention relates to 1-amidino-3-aryl-2-pyrazoline derivatives of the general formula I The invention specifically relates to such derivatives which exhibit antagonizing activity towards serotonin 5-HT 2B receptors. The present invention also relates to use of said compounds as a medicament and for the treatment of fibrosis, cardiovascular diseases, pain, IBD, and other inflammatory diseases, as well as pharmaceutical compositions comprising one or more of said compounds and methods of treatment.
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N-CONTAINING HETEROCYCLIC COMPOUNDS (Thu, 29 Dec 2016)
The present invention relates to N-containing heterocyclic compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2, JAK3 or TYK2 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.
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PROMOTION OF LYMPHATIC FUNCTION (Fri, 23 Dec 2016)
<p id="p-0001" num="0000">The present invention refers to lipophilic extracts of members of the Iridaceae family, such as <i>Iris germanica </i>and/or <i>Iris pallida</i>, that have been found to promote lymphatic function. These extracts are suitable for the treatment of skin inflammation, rheumatoid arthritis, impaired wound healing, chronic inflammatory diseases, chronic airway inflammation, inflammatory bowel disease, rosacea, primary and/or secondary lymphedemas. The most active components were found to be the iridals.</p>
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Histidyl-tRNA synthetases for treating autoimmune and inflammatory diseases (Fri, 23 Dec 2016)
<p id="p-0001" num="0000">The present invention relates generally to compositions and methods comprising histidyl-tRNA synthetase polypeptides or other specific blocking agents for the treatment autoimmune diseases and other inflammatory diseases, including those related to Jo-1 antibodies.</p>
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PURINONE COMPOUNDS AS KINASE INHIBITORS (Fri, 23 Dec 2016)
<p id="p-0001" num="0000">Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.</p>
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INHIBITORS OF C-JUN-N-TERMINAL KINASE (JNK) (Fri, 23 Dec 2016)
<p id="p-0001" num="0000">The present invention provides novel compounds according to Formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.98mm" wi="70.36mm" file="US20160368910A1-20161222-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">where Ring A, Ring B, X, L<sub>1</sub>, L<sub>2</sub>, R<sup>A</sup>, R<sup>C</sup>, R<sup>D</sup>, R<sup>E</sup>, m, n, and p are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of human diseases associated with kinase activity, for example, proliferative diseases, neurodegenerative diseases, metabolic disorders, inflammatory diseases, and cardiovascular diseases.</p>
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Inhibitor of p38 MAP kinase (Fri, 23 Dec 2016)
<p id="p-0001" num="0000">A compound of formula (XV):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="37.00mm" wi="68.07mm" file="US09624196-20170418-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R<sub>1 </sub>represents an amino group, a protected amino group or nitro group; or a salt thereof. The compound is a p38 MAP kinase inhibitor. The compound and its pharmaceutically acceptable salts can be used for treatment of conditions, such as inflammatory diseases.</p>
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TGR5 MODULATORS AND METHODS OF USE THEREOF (Fri, 23 Dec 2016)
The application relates to compounds of formula (A): or a salt, solvate, ester, tautomer, amino acide conjugate, or metabolite thereof. The compounds of formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.
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IBRUTINIB PRODRUGS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USE (Fri, 23 Dec 2016)
Prodrugs of ibrutinib, pharmaceutical compositions comprising the prodrugs, and methods of using the prodrugs and pharmaceutical compositions for treating autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions are disclosed.
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A NOVEL COMPOUND (KS 513) ISOLATED FROM PSEUDOLYSIMACHION ROTUNDUM VAR. SUBINTEGRUM, THE COMPOSITION COMPRISING THE SAME AS AN ACTIVE INGREDIENT FOR PREVENTING OR TREATING ALLERGY DISEASE, INFLAMMATORY DISEASE, ASTHMA OR CHRONIC OBSTRUCTIVE PULMONARY DISEASE AND THE USE THEREOF (Fri, 23 Dec 2016)
The present invention relates to a novel (1aS,1bS,2S,4S,5aR,6S,6aS)-1a-(hydroxymethyl)-4-methoxy-2-(((2S,3R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)octahydrooxireno[2',3':4,5]cyclopenta[1,2-c]pyran-6-yl 4-hydroxybenzoate} (KS-513), the isomer thereof, the pharmaceutically acceptable salt or solvates thereof, a composition comprising the same as an active ingredient for preventing or treating allergic disease, inflammatory disease, asthma or chronic obstructive pulmonary disease (COPD) and the use thereof.
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APPLICATIONS OF PARTIALLY AND FULLY SULFATED HYALURONAN (Fri, 16 Dec 2016)
<p id="p-0001" num="0000">Described herein is the use of partially and fully sulfated hyaluronan or the pharmaceutically acceptable salt or ester thereof for therapeutic and cosmetic applications as well as the treatment of a number of systemic, dermatological, periodontal, ophthalmic, and urological inflammatory diseases.</p>
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MCT4 INHIBITORS FOR TREATING DISEASE (Fri, 16 Dec 2016)
<p id="p-0001" num="0000">Disclosed herein are compounds and compositions useful in the treatment of MCT4 mediated diseases, such as proliferative and inflammatory diseases, having the structure of Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.67mm" wi="47.92mm" file="US20160362378A1-20161215-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">Methods of inhibition MCT4 activity in a human or animal subject are also provided.</p>
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IBRUTINIB PRODRUGS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USE (Fri, 16 Dec 2016)
<p id="p-0001" num="0000">Prodrugs of ibrutinib, pharmaceutical compositions comprising the prodrugs, and methods of using the prodrugs and pharmaceutical compositions for treating autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions are disclosed.</p>
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MCT4 INHIBITORS FOR TREATING DISEASE (Fri, 16 Dec 2016)
Disclosed herein are compounds and compositions useful in the treatment of MCT4 mediated diseases, such as proliferative and inflammatory diseases, having the structure of Formula I: Methods of inhibition MCT4 activity in a human or animal subject are also provided.
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SULFANIDE ADENOSINE DERIVATIVES AND USES THEREOF (Fri, 16 Dec 2016)
Described herein are sulfamide adenosine derivatives of Formula (I) or (II), and pharmaceutically acceptable salts, and pharmaceutical compositions thereof. Also provided are methods, uses, and kits involving the inventive compounds or pharmaceutical compositions for treating and/or preventing proliferative diseases (e.g., cancers, inflammatory diseases, and autoimmune diseases) or infectious diseases (e.g., bacterial infections, viral infections, fungal infections, and parasitic diseases) in a subject. The compounds and pharmaceutical compositions as described herein are thought to inhibit aminoacyl tRNA synthetase activity in a biological sample or subject to achieving the treatment of proliferative diseases or infectious diseases.
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HETEROCYCLIC COMPOUNDS (Fri, 16 Dec 2016)
The present invention provides a compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof has an BET family protein inhibitory action, and is useful as an agent for the prophylaxis or treatment of autoimmune diseases and/or inflammatory diseases (e.g., rheumatoid arthritis, multiple sclerosis, idiopathic pulmonary fibrosis, psoriasis, atopic dermatitis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, systemic lupus erythematosus etc.), cancer and the like.
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4-CARBOXYBENZYLAMINO DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS (Thu, 15 Dec 2016)
The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the 4-carboxybenzylamino derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the 4-carboxybenzylamino derivatives in vivo.
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BICYCLIC UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS USEFUL FOR THE TREATMENT OF PAIN (Fri, 09 Dec 2016)
<p id="p-0001" num="0000">Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="31.92mm" wi="49.28mm" file="US20160355521A1-20161208-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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NOVEL CHOLESTEROL METABOLITE, 5-CHOLESTEN, 3BETA-25-DIOL, DISULFATE (25HCDS) FOR THERAPY OF METABOLIC DISORDERS, HYPERLIPIDEMIA, DIABETES, FATTY LIVERS DISEASES AND ATHEROSCLEROSIS (Fri, 09 Dec 2016)
<p id="p-0001" num="0000">5-cholesten, 3β, 25-diol, disulfate (25HCDS) has been found to be an authentic PPAR<sub>γ</sub> agonist and LXR antagonist, and is used for the therapy of lipid disorders and inflammatory diseases, including without limitation fatty liver, inflammatory bowel, and atherosclerotic diseases.</p>
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BICYCLIC HETEROARYL UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS (Fri, 09 Dec 2016)
<p id="p-0001" num="0000">Compounds of Formula I or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="36.15mm" wi="51.73mm" file="US20160355517A1-20161208-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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NOVEL COMPOUNDS (Fri, 09 Dec 2016)
<p id="p-0001" num="0000">A compound of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="41.49mm" wi="59.69mm" file="US20160355505A1-20161208-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000">or a salt thereof;</li> <li id="ul0001-0002" num="0000">which is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory diseases and/or allergic conditions, in cancer therapy, specifically heme malignancies, and autoimmune conditions.</li> </ul> </p>
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Inhibitors of Bruton's tyrosine kinase (Fri, 09 Dec 2016)
<p id="p-0001" num="0000">Disclosed herein are reversible and irreversible inhibitors of Bruton's tyrosine kinase (Btk). Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are described, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.</p>
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INHIBITORS OF BRUTON'S TYROSINE KINASE (Fri, 09 Dec 2016)
Disclosed herein are reversible and irreversible inhibitors of Bruton's tyrosine kinase (Btk). Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are describeded, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
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COMPOUNDS FOR THE MODULATION OF MYC ACTIVITY (Fri, 09 Dec 2016)
The present invention provides novel compounds of Formula (I) and Formula (II) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases, e.g., cancers (e.g., breast cancer, prostate cancer, lymphoma, lung cancer, pancreatic cancer, ovarian cancer, neuroblastoma, or colorectal cancer), benign neoplasms, angio genesis, inflammatory diseases, fibrosis (e.g., polycystic kidney disease), autoinflammatory diseases, and autoimmune diseases in a subject.
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COMPOUNDS FOR THE MODULATION OF MYC ACTIVITY (Fri, 09 Dec 2016)
The present invention provides novel compounds of Formulas (I) and (II) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases, e.g., cancers (e.g., breast cancer, prostate cancer, lymphoma, lung cancer, pancreatic cancer, ovarian cancer, neuroblastoma, or colorectal cancer), benign neoplasms, angio genesis, inflammatory diseases, fibrosis (e.g., polycystic kidney disease), autoinflammatory diseases, and autoimmune diseases in a subject.
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NOVEL 2-PHENYLBENZOFURAN DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PRODUCTION METHOD FOR SAME AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING INFLAMMATORY DISEASE COMPRISING SAME AS ACTIVE INGREDIENT (Thu, 08 Dec 2016)
The present invention relates to a novel 2-phenylbenzofuran derivative or a pharmaceutically acceptable salt thereof, to a production method for same and to a pharmaceutical composition for preventing or treating an inflammatory disease comprising same as an active ingredient, and the novel 2-phenylbenzofuran derivative or the pharmaceutically acceptable salt thereof according to the present invention is outstandingly effective in suppressing NO, IL-6 and TNF-alpha due to macrophages, and therefore can advantageously be used in a pharmaceutical composition for preventing or treating an inflammatory disease.
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UREA DERIVATIVE OR PHARMACOLOGICALLY ACCEPTABLE SALT THEREOF (Fri, 02 Dec 2016)
The present invention provides a urea derivative or a pharmacologically acceptable salt thereof that has a formyl peptide receptor like 1 (hereinafter may be abbreviated as FPRL1) agonist effect, a pharmaceutical composition containing the urea derivative or the pharmacologically acceptable salt thereof, and a pharmaceutical use thereof. It has been found that a urea derivative represented by the general formula (I) below or a pharmacologically acceptable salt thereof has a superior FPRL1 agonist effect. Compound (I) or a pharmacologically acceptable salt thereof is highly useful for treatment, prevention, or suppression of inflammatory diseases, chronic airway diseases, cancers, septicemia, allergic symptoms, HIV retrovirus infection, circulatory disorders, neuroinflammation, nervous disorders, pains, prion diseases, amyloidosis, immune disorders and the like.
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UREA DERIVATIVE OR PHARMACOLOGICALLY ACCEPTABLE SALT THEREOF (Fri, 02 Dec 2016)
The present invention provides a urea compound or a pharmacologically acceptable salt thereof that has a formyl peptide receptor like 1 (hereinafter may be abbreviated as FPRL1) agonist effect, a pharmaceutical composition containing the urea compound or the pharmacologically acceptable salt thereof, and a pharmaceutical use thereof. It has been found that a urea derivative represented by the general formula (I) below or a pharmacologically acceptable salt thereof has a superior FPRL1 agonist effect. Compound (I) or a pharmacologically acceptable salt thereof is highly useful for treatment, prevention, or suppression of inflammatory diseases, chronic airway diseases, cancers, septicemia, allergic symptoms, HIV retrovirus infection, circulatory disorders, neuroinflammation, nervous disorders, pains, prion diseases, amyloidosis, immune disorders and the like.
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HETEROCYCLICALKYL DERIVATIVE COMPOUNDS AS SELECTIVE HISTONE DEACETYLASE INHIBITORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME (Fri, 02 Dec 2016)
The present invention relates to novel heterocyclicalkyl derivatives having histone deacetylase (HDAC) inhibitory activity, optical isomers thereof or pharmaceutically acceptable salts thereof, the use thereof for the preparation of medicaments, pharmaceutical compositions containing the same, a method for treating diseases using the composition, and methods for preparing the novel heterocyclicalkyl derivatives. The novel heterocyclicalkyl derivatives according to the present invention are selective histone deacetylase (HDAC) inhibitors, and may be effectively used for the treatment of histone deacetylase-mediated diseases, such as cell proliferative diseases, inflammatory diseases, autosomal dominant diseases, genetic metabolic diseases, autoimmune diseases, acute/chronic neurological disease, hypertrophy, heart failure, ocular diseases, or neurodegenerative diseases.
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PHARMACEUTICALLY ACTIVE COMPOUNDS AS DAG-LIPASE INHIBITORS (Fri, 02 Dec 2016)
The present invention relates to novel compounds which are selective inhibitors of diacylglycerol lipase alpha and beta. These compounds are suitable for the treatment or prevention of disorders associated with, accompanied by or caused by increased 2-arachidonoylglycerol levels. Diacylglycerol lipase-a (alternative name: Snl-specific diacylglycerol hydrolase a; DAGL-a) and -β are enzymes responsible for the biosynthesis of the endocannabinoid 2-arachidonoylglycerol. Selective and reversible inhibitors are required to study the function of DAGLs in neuronal cells in an acute and temporal fashion. The inventive compounds are in particular suitable for the treatment of neurodegenerative diseases, inflammatory diseases, drug abuse and impaired energy balance, such as obesity, wherein X1 is -CH-, -CF- or -N-.
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PYRANOCHROMENYL PHENOL DERIVATIVE, AND PHARMACEUTICAL COMPOSITION FOR TREATING METABOLIC SYNDROME OR INFLAMMATORY DISEASE (Thu, 01 Dec 2016)
Provided are a pyranochromenyl phenol derivative, a pharmaceutically acceptable salt thereof, or a solvate thereof. Also provided is a pharmaceutical composition for preventing or treating metabolic syndrome or inflammatory disease comprising same. The present invention is efficacious in preventing or treating metabolic syndrome or inflammatory disease and is chemically stable.
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SUBSTITUTED BICYCLIC DIHYDROPYRIMIDINONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY (Fri, 25 Nov 2016)
<p id="p-0001" num="0000">This invention relates to substituted bicyclic dihydropyrimidinones of formula 1</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.77mm" wi="69.85mm" file="US20160340319A1-20161124-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.</p>
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A METHOD FOR TREATING PERIPHERAL INFLAMMATORY DISEASE (Fri, 25 Nov 2016)
An active for use in the treatment or inhibition of an inflammatory disease associated with over- activation of Toll-like Receptor 4 (TLR4), Toll-like Receptor 2 (TLR2) and Myeloid differentiating protein 88 (Myd88) adaptor-like protein (Ma1) while maintaining a subject's ability to respond normally to a pathogen, in which the active is an oleamide or an immunomodulatory analogue thereof.
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A METHOD OF TREATING PERIPHERAL INFLAMMATORY DISEASE (Thu, 24 Nov 2016)

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BROMODOMAIN INHIBITORS (Fri, 18 Nov 2016)
<p id="p-0001" num="0000">The present invention provides for compounds of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.52mm" wi="50.72mm" file="US20160331749A1-20161117-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein Y<sup>1</sup>, Y<sup>2</sup>, R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, A<sup>1</sup>, A<sup>2</sup>, A<sup>3</sup>, and A<sup>4</sup>, have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents for the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).</p>
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NOVEL 2-PHENYLBENZOFURAN DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PRODUCTION METHOD FOR SAME AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING INFLAMMATORY DISEASE COMPRISING SAME AS ACTIVE INGREDIENT (Fri, 18 Nov 2016)
<p id="p-0001" num="0000">The present invention relates to a novel 2-phenylbenzofuran derivative or a pharmaceutically acceptable salt thereof, a production method for the same, and a pharmaceutical composition for preventing or treating an inflammatory disease comprising the same as an active ingredient, and the novel 2-phenylbenzofuran derivative or the pharmaceutically acceptable salt thereof according to the present invention is outstandingly effective in suppressing NO, IL-6, and TNF-alpha induced by macrophages, and therefore can advantageously be used in a pharmaceutical composition for preventing or treating an inflammatory disease.</p>
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Urea hydantoin derivatives as formyl peptide modulators (Fri, 18 Nov 2016)
<p id="p-0001" num="0000">The present invention relates to urea hydantoin compounds, processes for preparing them, pharmaceutical compositions containing them, and their use as pharmaceuticals as modulators of the FPR2 receptor, and to methods of treating inflammatory diseases or conditions in a subject in need thereof by administering the compound(s) or pharmaceutical composition to the subject.</p>
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CYCLIC COMPOUNDS (Fri, 18 Nov 2016)
The present invention provides compounds having a Toll-like receptor 4 (TLR4) signaling inhibitory action useful as preventive and therapeutic drugs of inflammatory disease and/or central nervous system disease or diseases such as chemotherapy-induced peripheral neuropathy (CIPN), chemotherapy-induced neuropathic pain (CINP), liver injury, ischemia-reperfusion injury (IRI) and the like. The present invention relates to a compound represented by formula (I) and a salt thereof: (wherein, each symbol is explained in greater detail in the specification).
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Novel compound having immune disease treatment effect and use thereof (Fri, 18 Nov 2016)
The present invention relates to a novel compound capable of effectively preventing and treating immune diseases and a use thereof. The novel compound of the present invention has effects of inhibiting the production of inflammatory cytokines, increasing the activity of regulatory T cells having immune regulatory functions, inhibiting the production of auto-antibodies to regulate excessive immune responses, and inhibiting the differentiation of osteoclasts, and thus can be used for treating immune diseases, such as autoimmune disease, inflammatory disease, and transplant rejection diseases, which are caused by abnormal regulation of various kinds of immune responses.
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Derivatives of tartaric acid (Fri, 11 Nov 2016)
<p id="p-0001" num="0000">The present invention relates to novel compounds, e.g. for use as a medicament. In particular, the present invention relates to novel medicaments, preferably in the treatment and/or prevention of systemic diseases, autoimmune diseases, and/or inflammatory diseases, for example multiple sclerosis and psoriasis.</p>
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Cyclic compounds (Fri, 11 Nov 2016)
<p id="p-0001" num="0000">The present invention provides compounds having a Toll-like receptor 4 (TLR4) signaling inhibitory action useful as preventive and therapeutic drugs of inflammatory disease and/or central nervous system disease or diseases such as chemotherapy-induced peripheral neuropathy (CIPN), chemotherapy-induced neuropathic pain (CINP), liver injury, ischemia-reperfusion injury (IRI) and the like. The present invention relates to a compound represented by formula (I) and a salt thereof:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="36.15mm" wi="60.03mm" file="US09533966-20170103-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> (wherein, each symbol is explained in greater detail in the specification). </p>
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Cyclic compounds (Fri, 11 Nov 2016)
<p id="p-0001" num="0000">The present invention provides compounds having a Toll-like receptor 4 (TLR4) signaling inhibitory action useful as preventive and therapeutic drugs of inflammatory disease and/or central nervous system disease or diseases such as chemotherapy-induced peripheral neuropathy (CIPN), chemotherapy-induced neuropathic pain (CINP), liver injury, ischemia-reperfusion injury (IRI) and the like.</p> <p id="p-0002" num="0000">The present invention relates to a compound represented by formula (I) and a salt thereof:</p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.56mm" wi="59.94mm" file="US09611244-20170404-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> (wherein, each symbol is explained in greater detail in the specification). </p>
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PYRIDAZINE COMPOUNDS, COMPOSITIONS AND METHODS (Fri, 11 Nov 2016)
<p id="p-0001" num="0000">The invention relates to novel chemical compounds, compositions and methods of making and using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of making and using pyridazine compounds and/or related heterocyclic derivatives and compositions comprising the same, for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications.</p>
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PYRIDAZINE DERIVATIVES AS RORc MODULATORS (Fri, 11 Nov 2016)
Compounds of formula (I): or pharmaceutical salts thereof, wherein m, n, A, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
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PYRIDAZINE DERIVATIVES AS RORc MODULATORS (Fri, 11 Nov 2016)
Compounds of formula I, or pharmaceutical salts thereof, wherein R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
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ANTI-OX40 ANTIBODIES AND METHODS OF USE THEREOF (Fri, 11 Nov 2016)
The present disclosure provides antibodies that specifically bind to human OX40 receptor (OX40) and compositions comprising such antibodies. In a specific aspect, the antibodies specifically bind to human OX40 and modulate OX40 activity, e.g., enhance, activate, or induce OX40 activity, or reduce, deactivate, or inhibit OX40 activity. The present disclosure also provides methods for treating disorders, such as cancer, by administering an antibody that specifically binds to human OX40 and modulates OX40 activity, e.g., enhances, activates, or induces OX40 activity. Also provided are methods for treating autoimmune or inflammatory diseases or disorders, by administering an antibody that specifically binds to human OX40 and modulates OX40 activity, e.g., reduces, deactivates, or inhibits OX40 activity.
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COMPOSITION AND METHODS OF INHIBITING AMYLASE-MEDIATED HYDROLYSIS OF ALPHA (1 to 4)-LINKED GLUCOSE POLYMERS (Fri, 11 Nov 2016)
PAZ320, a mixture of two galactomannans (GMa and GN/ΙΡβ), is being developed to treat diabetes and inflammatory diseases. Both GMα and GMβ have a β(1->4) mannan backbone, with a high density of α( 1->6) linked galactose units. When ingested by diabetic patients, PAZ320 reduces the magnitude of postprandial glucose excursions. PAZ320 functions by binding to enzymes that hydrolyze starch in the gastrointestinal track and thereby reduces steady-state concentrations of low molecular weight sugars like glucose. PAZ320 binds to the α-amylase enzyme from human and porcine sources and thereby attenuates the rate of amylase-mediated hydrolysis of α(1->4)-linked glucose polymers (starch and maltohexaose).
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PYRIDAZINE DERIVATIVES AS RORc MODULATORS (Fri, 11 Nov 2016)
Compounds of formula I: or pharmaceutical salts thereof, wherein m, A, X, Y, Z, R1, R2, R3, R4 and R5are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
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ANTI-INFLAMMATORY COMPOUNDS (Fri, 04 Nov 2016)
<p id="p-0001" num="0000">Compositions comprising isolated ido-BR1 are described for use in therapy or prophylaxis, including the treatment of inflammatory diseases (for example as anti-inflammatory drugs) and to reduce inflammation. Also described are methods for monitoring the quality of a Cucurbitaceae extract, to processes for producing a Cucurbitaceae extract as well as to Cucurbitaceae extracts obtainable by such processes.</p>
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UREA DERIVATIVES USEFUL AS KINASE INHIBITORS (Fri, 04 Nov 2016)
<p id="p-0001" num="0000">There are provided compounds of formula I, wherein R<sup>1</sup>, R<sup>1A</sup>, R<sup>1C </sup>to R<sup>1E</sup>, R<sup>a</sup>, R<sup>b</sup>, X<sup>1</sup>, E and G have meanings given in the description, which compounds have antiinflammatory activity (e.g., through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.</p>
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KINASE INHIBITORS (Fri, 04 Nov 2016)
<p id="p-0001" num="0000">There are provided compounds of formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="39.62mm" wi="75.78mm" file="US20160318909A1-20161103-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein: <br/> Y represents NR<sup>2</sup>R<sup>3</sup>; <br/> one of R<sup>2 </sup>and R<sup>3 </sup>represents —[C<sub>2-4 </sub>alkylene-O]<sub>1-12</sub>—[C<sub>2-4 </sub>alkylene]-R<sup>2a </sup>and the other of R<sup>2 </sup>and <br/> R<sup>3 </sup>has a meaning given in the description; and <br/> R, R<sup>1</sup>, R<sup>2a</sup>, R<sup>a</sup>, R<sup>b</sup>, Q, X and Y have meanings given in the description, <br/> which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines. </p>
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METHODS FOR THE TREATMENT OF CANCER AND INFLAMMATORY DISEASES USING CEREBLON AS A PREDICTOR (Fri, 04 Nov 2016)
<p id="p-0001" num="0000">Uses of the protein cereblon as a predictor of clinical sensitivity to cancer, inflammatory diseases, and patient response to drug treatment.</p>
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Inhibitors of bruton's tyrosine kinase (Fri, 04 Nov 2016)
<p id="p-0001" num="0000">This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.36mm" wi="75.44mm" file="US09624201-20170418-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Substituted pyridine-2-carboxamide compounds as apoptosis signal-regulating kinase inhibitors (Fri, 04 Nov 2016)
The present invention relates to compounds of Formula (I) wherein variables are as defined above. The compounds have apoptosis signal-regulating kinase ("ASKl") inhibitory activity, and are thus useful in the treatment of ASK1 -mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases.
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Polyfluorinated compounds acting as Bruton's tyrosine kinase inhibitors (Fri, 04 Nov 2016)
Provided are new polyfluoro-substituted pyrazolopyrimidine compounds or salts represented by formulae (I) to (IX), a preparation method therefor, and a method for using said compounds and a preparation thereof to treat and inhibit autoimmune diseases or disorders, heteroimmune diseases or disorders, inflammatory diseases and cancers or disorders.
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HETEROARYL SULTAM DERIVATIVES AS RORc MODULATORS (Fri, 28 Oct 2016)
<p id="p-0001" num="0000">Compounds of the formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.45mm" wi="68.83mm" file="US20160311817A1-20161027-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or a pharmaceutical salt thereof, wherein m, n, q, r, A, W, X<sup>1</sup>, X<sup>2</sup>, X<sup>3</sup>, X<sup>4</sup>, Y, Z, R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6</sup>, R<sup>7</sup>, R<sup>8</sup>, R<sup>9</sup>, R<sup>10 </sup>and R<sup>11 </sup>are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.</p>
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HETEROCYCLIC COMPOUND (Fri, 28 Oct 2016)
<p id="p-0001" num="0000">The present invention provides a heterocyclic compound having an IRAK-4 inhibitory action, which is useful for the prophylaxis or treatment of inflammatory disease, autoimmune disease, osteoarticular degenerative disease, neoplastic disease and the like, and a medicament containing thereof. The present invention relates to a compound represented by the formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="37.76mm" wi="55.12mm" file="US20160311811A1-20161027-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein each symbol is as defined in the specification, or a salt thereof.</p>
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MOLECULAR DIAGNOSTIC PANEL OF EOSINOPHILIC GASTROINTESTINAL DISORDERS (Fri, 28 Oct 2016)
<p id="p-0001" num="0000">The disclosure provides compositions and methods related to the diagnosis, prognosis, and treatment of inflammatory diseases and disorders, especially allergic inflammatory diseases and disorders.</p>
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Inhibitors of bruton's tyrosine kinase (Fri, 28 Oct 2016)
<p id="p-0001" num="0000">This application discloses compounds according to generic Formula (I) wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.35mm" wi="69.85mm" file="US09556150-20170131-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Drug delivery conjugates for treating resistant cancer and for use in combination therapy (Fri, 28 Oct 2016)
Described herein are drug delivery conjugates for targeted therapy. In particular, described herein are drug delivery conjugates that include polyvalent linkers comprising one or more unnatural amino acids that are useful for treating cancers and inflammatory diseases. In some embodiments, the cancer is selected from the group consisting of a carcinoma, a sarcoma, a lymphoma, Hodgekin's disease, a melanoma, a mesothelioma, Burkitfs lymphoma, a nasopharyngeal carcinoma, a leukemia, and a myeloma.
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SERINE/THREONINE KINASE INHIBITORS (Fri, 21 Oct 2016)
<p id="p-0001" num="0000">Compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.79mm" wi="61.04mm" file="US20160303126A1-20161020-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS FOR USE IN TREATING INFLAMMATORY DISEASES (Fri, 21 Oct 2016)
<p id="p-0001" num="0000">Compounds of formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.60mm" wi="57.83mm" file="US20160303075A1-20161020-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">are useful in treating and/or preventing inflammatory diseases.</p>
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INHIBITORS OF BRUTON'S TYROSINE KINASE (Fri, 21 Oct 2016)
<p id="p-0001" num="0000">This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="39.45mm" wi="69.85mm" file="US20160304497A1-20161020-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Oxidized Lipids and Methods of Use Thereof (Fri, 21 Oct 2016)
<p id="p-0001" num="0000">The present invention is directed to oxidized lipids and pharmaceutical compositions comprising the same. The present invention is also directed to methods of making an oxidized lipid of the invention and to methods of treating or preventing fibrosis or inflammatory diseases or disorders comprising an oxidized lipid of the invention.</p>
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Composition comprising cyclodextrin and budesonide derivatives for the treatment and prophylaxis of pulmonary inflammations (Fri, 21 Oct 2016)
The present invention relates to novel and useful pharmaceutical compositions formulated with a cyclodextrin compound and a budesonide derivative for the treatment and/or prevention of pulmonary inflammatory disease. The present invention also relates to a novel and useful analytical technique for the detection and the quantification of ΗΡ-β-CD in solution. More specifically, the present invention relates to the use of a validated 1H NMR analysis for the detection and quantification of cyclodextrins directly in pharmaceutical formulations without any extraction or separation steps for liquid formulations.
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Inhibitors of cyclin-dependent kinase 7 (CDK7) (Fri, 21 Oct 2016)
The present invention provides novel compounds described herein, such as of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
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Inhibitors of cyclin-dependent kinase 7 (CDK7) (Fri, 21 Oct 2016)
The present invention provides novel compounds of Formula (I) and Formula (II) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
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TERT-BUTYL N-[2-ETHYL]-L-ALANINATE OR A SALT,HYDRATE OR SOLVATE THEREOF (Fri, 14 Oct 2016)
<p id="p-0001" num="0000">The present invention provides a compound which is: tert-butyl N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alaninate or a salt, hydrate or solvate thereof. The present invention also provides a pharmaceutical composition comprising the compound together with one or more pharmaceutically acceptable carriers and/or excipients. The compound and composition are useful for inhibiting the activity of a p38 MAP kinase enzyme. As such they may be used in the treatment of a autoimmune or inflammatory disease, or a cell proliferative disease. In addition, the invention provides an acid produced by hydrolysis of the ester group of the compound of the invention. The acid is N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alanine.</p>
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PYRROLIDINYL UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS (Fri, 14 Oct 2016)
<p id="p-0001" num="0000">Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R<sup>1</sup>, R<sup>2</sup>, R<sup>a</sup>, R<sup>b</sup>, R<sup>c</sup>, R<sup>d</sup>, X, Ring B, and Ring C are as defined herein, and wherein Ring B moiety and the NH—C(═X)—NH moiety are in the trans configuration, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="43.10mm" wi="51.39mm" file="US20160297758A1-20161013-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES (Fri, 14 Oct 2016)
<p id="p-0001" num="0000">A novel compound able to inhibit JAK is disclosed, this compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.</p>
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COMPOSITION FOR PREVENTION AND TREATMENT OF ALLERGIC AND/OR INFLAMMATORY DISEASES (Fri, 14 Oct 2016)
<p id="p-0001" num="0000">A prophylactic antiallergenic composition includes at least one arabinogalactan or arabinogalactan protein. The arabinogalactan or arabinogalactan protein is isolated from a grass or corresponds in its structural arrangement to an arabinogalactan that can be isolated from a grass.</p>
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PYRROLIDINYL UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS (Fri, 14 Oct 2016)
<p id="p-0001" num="0000">Compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R<sup>1</sup>, R<sup>2</sup>, R<sup>a</sup>, R<sup>b</sup>, R<sup>c</sup>, R<sup>d</sup>, X, Ring B, and Ring C are as defined herein, and wherein Ring B moiety and the NH—C(═X)—NH moiety are in the trans configuration, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="45.38mm" wi="53.17mm" file="US20160297796A1-20161013-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Compounds for the treatment of cancer and inflammatory diseases (Fri, 14 Oct 2016)
<p id="p-0001" num="0000">The present invention relates to novel compounds and pharmaceutical compositions thereof which may be useful in the treatment and/or prevention of various conditions. The present invention also provides methods of preparing such compounds and compositions, and methods of using the same.</p>
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Inhibiting the Transient Receptor Potential A1 ion channel (Fri, 14 Oct 2016)
The present invention relates to compounds of the Formula (I), or a pharmaceutically acceptable salt, pharmaceutical preparation, or pharmaceutical composition thereof, and their use for the treatment of pain, inflammatory disease, neuropathy, dermatological disorders, pulmonary conditions, and cough, as well as inhibiting the Transient Receptor Potential Al ion channel (TRPA1).
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Substituted triazole boronic acid compounds (Wed, 12 Oct 2016)
<p id="p-0001" num="0000">The invention is concerned with the compounds of formula (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are LMP7 inhibitors and may be useful in treating associated inflammatory diseases and disorders such as, for example, rheumatoid arthritis, lupus and irritable bowel disease.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="45.72mm" wi="69.85mm" file="US09464098-20161011-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Azaindole derivatives as selective histone deacetylase (HDAC) inhibitors and pharmaceutical compositions comprising the same (Fri, 07 Oct 2016)
<p id="p-0001" num="0000">The present invention relates to novel azaindole derivatives, and more particularly, to novel azaindole derivatives having histone deacetylase (HDAC) inhibitory activity, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof or solvates thereof, the use thereof for the preparation of pharmaceutical compositions, pharmaceutical compositions containing the same, a method of treating disease using the pharmaceutical compositions, and methods for preparing the novel azaindole derivatives. The novel azaindole derivatives according to the present invention are selective histone deacetylase (HDAC) inhibitors, and may be used as agents for treating malignant tumor diseases, inflammatory diseases, rheumatoid arthritis, and neurodegenerative diseases.</p>
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7-(MORPHOLIN-4-YL)PYRAZOLE[1,5-A]PYRIMIDINE DERIVATIVES WHICH ARE USEFUL FOR THE TREATMENT OF IMMUNE OR INFLAMMATORY DISEASES OR CANCER (Fri, 07 Oct 2016)
A compound of the general formula (I) wherein Y represents -CH2- or >C=0; R1 is selected from the group consisting of A1, A2 and A3; R2 represents dioxothiomorpholino moiety B1, piperazinyl moiety B2, azetidinyl moiety B3, or piperidinyl moiety B4; R3 is selected from the group consisting of H, halogen, and C1 -C4 alkyl; R4 is selected from the group consisting of C1 -C4 alkyl, C3-C4- cycloalkyl, C1 -C4 alkyl substituted with C1 -C4 alkoxy, and CHF2, and their pharmaceutically acceptable salts. Pharmaceutical compositions comprising said compounds and their use in the treatment of diseases of immune system, inflammatory diseases and cancer.
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INHIBITORS OF CYCLIN-DEPENDENT KINASES (Fri, 07 Oct 2016)
The present invention provides novel compounds of Formula (I), (II), or (III), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., CDK7, CDK12, or CDK13), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
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Tricyclic compound and JAK inhibitor (Fri, 07 Oct 2016)
Provided is a novel tricyclic compound which has JAK inhibitory activity and is especially useful for prophylaxis, treatment or amelioration of autoimmune diseases, inflammatory diseases and allergic diseases. A novel tricyclic compound which is represented by formula (I), formula (II) or formula (III) (wherein each of A<sp>1</sp>, A<sp>2</sp> and A<sp>3</sp> represents a cyclohexane-1,4-diyl group or the like; each of L<sp>1</sp>, L<sp>2</sp> and L<sp>3</sp> represents a methylene group or the like; each of X<sp>1</sp> and X<sp>3</sp> represents O or NH; each of R<sp>1</sp> and R<sp>3</sp> represents a cyano C<sb>1-6</sb> haloalkyl group or the like; and R<sp>2</sp> represents an aromatic heterocyclic group), a tautomer or a pharmaceutically acceptable salt of the compound, or a solvate of the compound, the tautomer or the pharmaceutically acceptable salt.
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N-PYRROLIDINYL,N'-PYRAZOLYL-UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS (Fri, 30 Sep 2016)
<p id="p-0001" num="0000">Compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R<sup>1</sup>, R<sup>2</sup>, R<sup>a</sup>, R<sup>b</sup>, R<sup>c</sup>, R<sup>d</sup>, X, Ring B, and Ring C are as defined herein, and wherein Ring B and the NH—C(═X)—NH moiety are in the trans configuration, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="44.11mm" wi="52.92mm" file="US20160280682A1-20160929-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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NATURAL IGM ANTIBODIES AND INHIBITORS THEREOF (Fri, 30 Sep 2016)
<p id="p-0001" num="0000">The invention provides natural IgM antibody inhibitors that may be used to treat various inflammatory diseases or disorders.</p>
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N-(MONOCYCLIC ARYL),N'-PYRAZOLYL-UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS (Fri, 30 Sep 2016)
<p id="p-0001" num="0000">Compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="31.92mm" wi="48.34mm" file="US20160280692A1-20160929-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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PYRAZOLYL UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS (Fri, 30 Sep 2016)
<p id="p-0001" num="0000">Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.00mm" wi="48.18mm" file="US20160280690A1-20160929-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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N-bicyclic aryl,N'-pyrazolyl urea, thiourea, guanidine cyanoguanidine compounds as TrkA kinase inhibitors (Fri, 30 Sep 2016)
<p id="p-0001" num="0000">Compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.99mm" wi="48.51mm" file="US09546156-20170117-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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ISOLATED PEPTIDES AND FRAGMENTS THEREOF FROM FIBRINOGEN FOR USE AS DRUGS, PARTICULARLY IN SKIN INFLAMMATORY DISEASES (Fri, 30 Sep 2016)
A present invention relates to isolated peptides obtained from human fibrinogen for their use as drug, particularly for the prevention and/or the treatment of inflammatory skin diseases, more particularly acne. The present invention also relates to fragments of these polypeptides, nucleic acid molecules encoding them, expression vectors, host cells, a pharmaceutical composition and a combination product containing them, and their use for treating and/or preventing inflammatory skin diseases, particularly acne.
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N-(ARYLALKYL)-N'-PYRAZOLYL-UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS (Fri, 23 Sep 2016)
<p id="p-0001" num="0000">Compounds of Formula I or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C, X, Ra, Rb, Rc, Rd and n are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="47.58mm" wi="47.07mm" file="US20160272592A1-20160922-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Bromodomain Inhibitors (Fri, 23 Sep 2016)
<p id="p-0001" num="0000">Compounds of formula (I) and pharmaceutically acceptable salts thereof are provided. The compounds are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Pharmaceutical compositions comprised of one or more compounds of formula (I) are also provided.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.52mm" wi="58.25mm" file="US20160272630A1-20160922-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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PYRANOCHROMENYL PHENOL DERIVATIVE, AND PHARMACEUTICAL COMPOSITION FOR TREATING METABOLIC SYNDROME OR INFLAMMATORY DISEASE (Fri, 23 Sep 2016)
<p id="p-0001" num="0000">Provided are a pyranochromenyl phenol derivative, a pharmaceutically acceptable salt thereof, or a solvate thereof. Also provided is a pharmaceutical composition for preventing or treating metabolic syndrome or inflammatory disease comprising same.</p> <p id="p-0002" num="0000">The present invention is efficacious in preventing or treating metabolic syndrome or inflammatory disease and is chemically stable.</p>
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Keto-imidazopyridine derivatives as RORc modulators (Fri, 23 Sep 2016)
<p id="p-0001" num="0000">Compounds of the formula I or II:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="75.01mm" wi="69.85mm" file="US09550771-20170124-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or pharmaceutically acceptable salts thereof, wherein R<sup>1 </sup>is a group of formula (a), (b), (c); (d) or (e): </p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="199.90mm" wi="69.85mm" file="US09550771-20170124-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and m, n, X, Y, R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>b </sup>and R<sup>c </sup>are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis. </p>
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GRP94 DERIVED POLYPEPTIDES FOR INHIBITING PCSK9 AND METHODS OF USE (Fri, 23 Sep 2016)
The present invention relates to PCSK9 inhibitors and methods of use thereof. Specifically, the invention relates to PCSK9 cell-based assay, PCSK9 inhibiting polypeptides and derivatives thereof. The invention includes pharmaceutical compositions comprising a PCSK9 inhibitor polypeptide together with a pharmaceutically acceptable carrier and method for treating cardiovascular disorders, inflammatory diseases or inflammatory response to infection.
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DERIVATIVES OF 1-[(CYCLOPENTYL OR 2-PYRROLIDINYL)CARBONYLAMINOMETHYL]-4-(1,3-THIAZOL-5-YL) BENZENE WHICH ARE USEFUL FOR THE TREATMENT OF PROLIFERATIVE, AUTOIMMUNE OR INFLAMMATORY DISEASES (Fri, 23 Sep 2016)
There is provided novel small molecule E3 ubiquitin ligase protein binding ligand compounds, having utility in PROteolysis Targeted Chimeras (PROTACs), as well as processes for the preparation thereof, and use in medicine. There is particularly provided PROTACs which bind to a protein within the bromo- and Extra-terminal (BET) family of proteins, and especially to PROTACs including novel small molecule E3 ubiquitin ligase protein binding ligand compounds which selectively induce degradation of the BRD4 protein within the bromodomain of the BET family of proteins.
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TGR5 AGONISTS (Fri, 23 Sep 2016)
The invention relates to novel 1,4-diazepan-2-one compounds, which are TGR5 agonists and useful for the treatment of metabolic disorders, inflammatory diseases, atherosclerosis and dyslipidemias.
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BENZIMIDAZOLE DERIVATIVES AS BROMODOMAIN INHIBITORS (Fri, 23 Sep 2016)
Compounds of formula (I) and salts thereof: wherein R1, R2, R3, R4 are defined herein. Compounds of formula (I) and salts thereof have been found to inhibit the binding of the BET family of bromodomain proteins to, for example, acetylated lysine residues and thus may have use in therapy, for example in the treatment of autoimmune and inflammatory diseases, such as rheumatoid arthritis; and cancers.
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Novel compounds as histone deacetylase 6 inhibitors and pharmaceutical compositions comprising the same (Fri, 23 Sep 2016)
The present invention relates to novel compounds having histone deacetylase 6 (HDAC6) inhibitory activity, isomers thereof, or pharmaceutically acceptable salts thereof, the use thereof for the preparation of therapeutic medicaments, pharmaceutical compositions comprising the same, a method of treating disease using the composition, and methods for preparing the novel compounds. The novel compounds according to the present invention have histone deacetylase 6 (HDAC6) inhibitory activity, and are effective for the prevention or treatment of HDAC6-associated diseases, including cancer, inflammatory diseases, autoimmune diseases, neurological diseases and neurodegenerative disorders.
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BENZODIOXOLE DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS (Thu, 22 Sep 2016)
NOVEL PHOSPHODIESTERASE INHIBITORS Compounds of the general formula I wherein each of m and n is independently 0 or 1; R 1 and R 2 , together with the carbon atom to which they are attached, form a heterocyclic ring comprising one or two heteroatoms selected from oxygen, sulfur, -S(O)- and - S(O) 2 -; R 3 is -CHF 2 , -CF 3 , -OCHF 2 , -OCF 3 , -SCHF 2 or -SCF 3 ; X is a bond, -CH 2 -, or -NH-; A is aryl, cycloalkyl, cycloalkenyl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkenyl, optionally substituted with one or more, same or different substituents selected from R 4 ; and R 4 is hydrogen, amino, thioxo, alkyl, haloalkyl, hydroxyalkyl, alkoxy, haloalkoxy, halogen, oxo, thia, or hydroxy; or pharmaceutically acceptable salts, hydrates or solvates thereof, have been found to exhibit PDE4 inhibiting activity, and may therefore be useful in the treatment of inflammatory diseases and disorders.
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HETEROMAROMATIC COMPOUNDS USEFUL FOR THE TREATMENT OF PROLFERATIVE DISEASES (Fri, 16 Sep 2016)
<p id="p-0001" num="0000">The present invention provides novel compounds of Formula (I) and Formula (II), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7)), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject. (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.94mm" wi="69.85mm" file="US20160264552A1-20160915-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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POLYCYCLIC INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7) (Fri, 16 Sep 2016)
<p id="p-0001" num="0000">The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma, lung cancer), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7), cyclin-dependent kinase 12 (CDK12), or cyclin-dependent kinase 13 (CDK13)), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.46mm" wi="69.85mm" file="US20160264554A1-20160915-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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COMPOUNDS (Fri, 16 Sep 2016)
<p id="p-0001" num="0000">The present invention relates to compounds of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="64.26mm" wi="69.85mm" file="US20160264583A1-20160915-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and to compositions comprising the same and to the use of the compounds and their compositions in treatment, for example in the treatment of inflammatory diseases, in particular respiratory inflammatory disease. The invention also extends to methods of making said compounds.</p>
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HETEROAROMATIC COMPOUNDS USEFUL FOR THE TREATMENT OF PROLFERATIVE DISEASES (Fri, 16 Sep 2016)
<p id="p-0001" num="0000">The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7)), and therefore, in duce cellular apoptosis and/or inhibit transcription in the subject.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.08mm" wi="70.95mm" file="US20160264551A1-20160915-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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CT-1 INHIBITORS (Thu, 15 Sep 2016)
The present invention relates to an inhibitor of CT-1 polypeptide for reducing or eliminating autophagy of fibroblasts in an inflammatory disease. The invention also discloses a method of treating a patient by administering a CT-1 inhibitor, a method of reducing stroma supported tumor growth and an in vitro method for detecting and monitoring tumor growth.
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PYRIDINONE COMPOUND, PHARMACEUTICAL COMPOSITION CONTAINING THE SAME AND USE (Sat, 10 Sep 2016)
The present invention is directed to the compound of formula (I), which is 5-[1-(1,3-dimethoxypropan-2-yl)-5-(morpholin-4-yl)-1H-1,3-benzodiazol-2-yl]-1,3-dimethyl-1,2-dihydropyridin-2-one or a salt thereof, in particular pharmaceutically acceptable salts thereof. The compound of formula (I) has been identified as a BET inhibitor and thus has potential for use in therapy, for example in the treatment of autoimmune and inflammatory diseases, such as rheumatoid arthritis; and cancers.
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BENZOPIPERAZINE COMPOSITIONS AS BET BROMODOMAIN INHIBITORS (Fri, 09 Sep 2016)
<p id="p-0001" num="0000">The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.86mm" wi="56.30mm" file="US20160257699A1-20160908-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein X, Y, Z, R<sub>1</sub>, R<sub>2</sub>, R<sub>4 </sub>and R<sub>7 </sub>are defined herein.</p>
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TETRAHYDROQUINOLINE COMPOSITIONS AS BET BROMODOMAIN INHIBITORS (Fri, 09 Sep 2016)
<p id="p-0001" num="0000">The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="22.01mm" wi="32.43mm" file="US20160257692A1-20160908-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein W, X, Y, Z, R<sup>1</sup>, R<sup>2</sup>, R<sup>5</sup>, and R<sup>8 </sup>are as described herein.</p>
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BIFUNCTIONAL STAPLED POLYPEPTIDES AND USES THEREOF (Fri, 09 Sep 2016)
<p id="p-0001" num="0000">The invention relates to bifunctional stapled or stiched peptides comprising a targeting domain, a linker moiety, and an effector domain, that can be used to tether, or to bring into close proximity, at least two cellular entities (e.g., proteins). Certain aspects relate to bifunctional stapled or stiched peptides that bind to an effector biomolecule through the effector domain and bind to a target biomolecule through the targeting domain. Polypeptides and/or polypeptide complexes that are tethered by the bifunctional stapled or stiched peptides of the invention, where the effector polypeptide bound to the effector domain of the bifunctional stapled or stiched peptide modifies or alters the target polypeptide bound to the targeting domain of the bifunctional peptide. Usesses of the inventive bifunctional stapled or stiched peptides including methods for treatment of disease (e.g., cancer, inflammatory diseases) are also provided.</p>
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PROCESSES FOR PREPARING JAK INHIBITORS AND RELATED INTERMEDIATE COMPOUNDS (Fri, 09 Sep 2016)
<p id="p-0001" num="0000">The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="40.89mm" wi="50.55mm" file="US20160257687A1-20160908-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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COMPOSITIONS AND METHODS OF INHIBITING N-ACYLETHANOLAMINE-HYDROLYZING ACID AMIDASE (Fri, 09 Sep 2016)
<p id="p-0001" num="0000">Compounds and pharmaceutical compositions are contemplated that inhibit N-acyl-ethanolamine-hydrolyzing acid amidase (NAAA) to so increase the concentration of the substrate of NAAA, palmitoylethanolamide (PEA). NAAA inhibition is contemplated to be effective to alleviate conditions associated with a reduced concentration of PEA. Among other uses, various NAAA inhibitors are especially contemplated as therapeutic agents in the treatment of inflammatory diseases.</p>
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BENZOPIPERAZINE COMPOSITIONS AS BET BROMODOMAIN INHIBITORS (Fri, 09 Sep 2016)
<p id="p-0001" num="0000">The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.86mm" wi="55.63mm" file="US20160256458A1-20160908-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein X, Y, Z, R<sub>1</sub>, R<sub>2</sub>, R<sub>4 </sub>and R<sub>7 </sub>are defined herein.</p>
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TETRAHYDROQUINOLINE COMPOSITIONS AS BET BROMODOMAIN INHIBITORS (Fri, 09 Sep 2016)
<p id="p-0001" num="0000">The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="22.10mm" wi="32.43mm" file="US20160256448A1-20160908-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein W, X, Y, Z, R<sup>1</sup>, R<sup>2</sup>, R<sup>5</sup>, and R<sup>8 </sup>are as described herein.</p>
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Salts and solid form of a BTK inhibitor (Fri, 09 Sep 2016)
Disclosed herein are processes for preparing 2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile free base (compound (I) ), salts of compound (I) and solid state form of said salts. Also disclosed herein are pharmaceutical compositions comprising such salts and solid state form thereof and methods of treating cancer, autoimmune, and inflammatory diseases using compound (I) or a pharmaceutically acceptable salt thereof.
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NOVEL RECEPTOR TREM (TRIGGERING RECEPTOR EXPRESSED ON MYELOID CELLS) AND USES THEREOF (Fri, 02 Sep 2016)
<p id="p-0001" num="0000">Novel activating receptors of the lg super-family expressed on human myeloid cells, called TREM(s) (triggering receptor expressed on myeloid cells) are provided. Specifically, two (2) members of TREMs, TREM-1 and TREM-2 are disclosed. TREM-1 is a transmembrane glycoprotein expressed selectively on blood neutrophils and a subset of monocytes but not on lymphocytes and other cell types and is upregulated by bacterial and fungal products. Use of TREM-1 in treatment and diagnosis of various inflammatory diseases is also provided. TREM-2 is also a transmembrane glycoprotein expressed selectively on mast cells and peripheral dendritic cells (DCs) but not on granulocytes or monocytes. DC stimulation via TREM-2 leads to DC maturation and resistance to apoptosis, and induces strong upregulation of CCR7 and subsequent chemotaxis toward macrophage inflammatory protein 3-β. TREM-2 has utility in modulating host immune responses in various immune disorders, including autoimmune diseases and allergic disorders.</p>
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INHIBITORS OF HISTONE DEACETYLASE (Fri, 02 Sep 2016)
<p id="p-0001" num="0000">The present invention relates to compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.73mm" wi="61.64mm" file="US20160251351A1-20160901-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R<sup>1a</sup>, R<sup>2b</sup>, R<sup>2c</sup>, R<sup>5 </sup>and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.</p>
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CHROMENE DERIVATIVES AS INHIBITORS OF TCR-NCK INTERACTION (Fri, 02 Sep 2016)
<p id="p-0001" num="0000">The present invention relates to a group of compounds of formula (I) containing a chromene nucleus:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.52mm" wi="60.37mm" file="US20160251330A1-20160901-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and which present the ability to inhibit the lymphocytes proliferation mediated by the TCR interaction with Nck, so that the present invention also relates to the use of these compounds for the treatment of diseases or conditions wherein said interaction triggers a complication such as transplant rejection reactions, immune or autoimmune diseases, inflammatory diseases or proliferative diseases.</p>
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VITAMIN B6 DERIVATIVES OF NUCLEOTIDES, ACYCLONUCLEOTIDES AND ACYCLONUCLEOSIDE PHOSPHONATES (Fri, 02 Sep 2016)
<p id="p-0001" num="0000">Provided herein are compounds, compositions, and methods of using them to treat infections, neoplastic disease, inflammatory disease, and pain. Such compounds are nucleotides, acyclonucleotides, and ANP phosphonates conjugated with forms and/or moieties of Vitamin B6 for delivery past the cell membrane and into the cell.</p>
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8-oxoprotoberberine derivative or pharmaceutically acceptable salt thereof, preparation method therefor and pharmaceutical composition for preventing or treating diseases associated with activity of NFAT5, containing same as active ingredient (Fri, 02 Sep 2016)
<p id="p-0001" num="0000">The preset invention relates to a novel 8-oxoprotoberberine derivative or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition for preventing or treating diseases associated with the activity of NFAT5 containing the same as an active ingredient. The novel 8-oxoproteoberberine derivative or the pharmaceutically acceptable salt thereof according to the present invention can be useful in a pharmaceutical composition for preventing or treating diseases associated with the activity of NFAT5, particularly rheumatoid arthritis or inflammatory diseases, since it is ascertained that the derivative or a pharmaceutically acceptable salt thereof has remarkably increased oral absorption compared with known protoberberine due to an improvement in the properties thereof, and inhibits the activity of NFAT5 and the secretion of inflammatory cytokines and reduces the expression of NAFT5 in mice with rheumatoid arthritis by directly inhibiting the transcription of NFT5.</p>
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Tricyclic heterocyclic compounds as phosphoinositide 3-kinase inhibitors (Fri, 02 Sep 2016)
A compound of formula I: (I) or a pharmaceutically acceptable salt thereof, wherein: W is O, N-H, N-(C<sb>1</sb> -C 10 alkyl) or S; each X is independently CH or N; R<sp>1</sp> is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R<sp>2</sp> is LY; each L is a direct bond, C<sb>1</sb> -C <sb>10</sb> alkylene, C<sb>2</sb> -C<sb>10</sb> alkenylene or C<sb>2</sb> -C <sb>10</sb> alkynylene; Y is an optionally substituted fused, bridged or spirocyclic non-aromatic 5-12 membered heterocycle containing up to 4 heteroatoms selected from N or O; and each R<sp>3</sp> is independently H, C<sb>1</sb>-C <sb>10 </sb>alkyl, halogen, fluoro C<sb>1</sb> -C<sb>10</sb> alkyl, O- C<sb>1</sb> -C<sb>10</sb> alkyl, NH-C<sb>1</sb> -C<sb>10</sb> alkyl, S-C<sb>1</sb> -C<sb>10</sb> alkyl, O- fluoro C<sb>1</sb> -C<sb>10</sb> alkyl, NH-acyl, NH-C(O)-NH-C<sb>1</sb> -C<sb>10</sb> alkyl, C(O)-NH-C<sb>1</sb> -C<sb>10</sb> alkyl, aryl or heteroaryl, are useful as inhibitors of the class IA phosphoinositide 3- kinase enzyme, PI3K-p110δ, and therefore have potential utility in the therapy of cancer, immune and inflammatory diseases.
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Benzimidazole derivatives and pharmaceutical compositions thereof for the treatment of inflammatory disorders (Fri, 02 Sep 2016)
The present invention discloses compounds according to Formula (I) wherein Cy, R<sp>1</sp>, L<sb>1</sb> R<sp>3</sp>, R<sp>4</sp>, R<sp>5</sp>, L<sb>a,</sb> and R<sp>a</sp> are as defined herein. Novel benzimidazoles according to Formula (I), able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic diseases, inflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons.
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Pyrazole amide derivative (Fri, 02 Sep 2016)
The present invention relates to a novel compound having a function of inhibiting RORγ activity. The present invention also relates to pharmaceutical composition comprising the compound, a use of the compound in treating or preventing autoimmune diseases, inflammatory diseases, metabolic diseases, or cancer diseases.
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Processes for preparing JAK inhibitors and related intermediate compounds (Fri, 02 Sep 2016)
The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimi dines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d~pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.
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Bromodomain inhibitors (Wed, 31 Aug 2016)
<p id="p-0001" num="0000">The present invention provides for compounds of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.61mm" wi="50.72mm" file="US09428514-20160830-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein Y<sup>1</sup>, Y<sup>2</sup>, R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, A<sup>1</sup>, A<sup>2</sup>, A<sup>3</sup>, and A<sup>4</sup>, have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents for the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I). </p>
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Substituted 3-Haloallylamine Inhibitors of SSAO and uses thereof (Fri, 26 Aug 2016)
<p id="p-0001" num="0000">The present invention is related to the preparation and pharmaceutical use of substituted 3-haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I, as defined in the specification:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.98mm" wi="56.73mm" file="US20160244406A1-20160825-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">The invention also relates to methods of using compounds of Formula I, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases, ocular diseases, fibrotic diseases, diabetes-induced diseases and cancer.</p>
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CHROMENE DERIVATIVES SUBSTITUTED BY ALKOXIDE AS INHIBITORS OF THE TCR-NCK INTERACTION (Fri, 26 Aug 2016)
<p id="p-0001" num="0000">The present invention relates to a group of compounds of formula (I) containing a chromene nucleus:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.52mm" wi="63.25mm" file="US20160244423A1-20160825-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and that present the capacity to inhibit the proliferation of lymphocytes mediated by the Nck interaction with TCR, so that the present invention also relates to the use of these compounds for the treatment of diseases or conditions where said interaction triggers a complication such as transplant rejection reactions, immune or autoimmune diseases, inflammatory diseases or proliferative diseases.</p>
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NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS (Fri, 26 Aug 2016)
<p id="p-0001" num="0000">The present invention discloses compounds according to Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="49.28mm" wi="69.85mm" file="US20160244443A1-20160825-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">Wherein R<sup>1a</sup>, R<sup>1b</sup>, R<sup>2</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6a</sup>, R<sup>6b</sup>, R<sup>7</sup>, R<sup>8</sup>, W, X, Cy, and the subscript a are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.</p>
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PI3K/AKT/mTOR inhibitors and pharmaceutical uses thereof (Fri, 26 Aug 2016)
<p id="p-0001" num="0000">The invention relates to new PI3K/AKT/m TOR inhibitors and their use for the prevention and/or the treatment of a disease selected from the group consisting of: inflammatory diseases, autoimmune diseases, neurodegenerative diseases, cancers, transplant rejection, diseases characterized by a premature aging and tuberous sclerosis.</p>
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CHROMENE DERIVATIVES AS INHIBITORS OF TCR-NCK INTERACTION (Thu, 25 Aug 2016)
The present invention relates to a group of compounds of formula (I) containing a chromene nucleus: and which present the ability to inhibit the lymphocytes proliferation mediated by the TCR interaction with Nck, so that the present invention also relates to the use of these compounds for the treatment of diseases or conditions wherein said interaction triggers a complication such as transplant rejection reactions, immune or autoimmune diseases, inflammatory diseases or proliferative diseases.
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CHROMENE DERIVATIVES SUBSTITUTED BY ALKOXIDE AS INHIBITORS OF THE TCR-NCK INTERACTION (Thu, 25 Aug 2016)
The present invention relates to a group of compounds of formula (I) containing a chromene nucleus: and that present the capacity to inhibit the proliferation of lymphocytes mediated by the Nck interaction with TCR, so that the present invention also relates to the use of these compounds for the treatment of diseases or conditions where said interaction triggers a complication such as transplant rejection reactions, immune or autoimmune diseases, inflammatory diseases or proliferative diseases.
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Pyridopyrimidine derivatives and use thereof (Wed, 24 Aug 2016)
<p id="p-0001" num="0000">The invention provides novel substituted pyridopyrimidines represented by Formula I or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of the phosphoinositide 3′ OH kinase family (PI3K) for the treatment of inflammatory diseases, cancer, cardiovascular diseases, allergy, asthma and autoimmune disorders.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.75mm" wi="68.16mm" file="US09422298-20160823-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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3-HETEROAROYLAMINO-PROPIONIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS (Fri, 19 Aug 2016)
<p id="p-0001" num="0000">The present invention relates to compounds of the formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="17.95mm" wi="55.37mm" file="US20160237060A1-20160818-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein Ht, G, R<sup>10</sup>, R<sup>30</sup>, R<sup>40</sup>, R<sup>50 </sup>and R<sup>60 </sup>have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.</p>
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Novel Amino Pyrimidine Derivatives (Fri, 19 Aug 2016)
<p id="p-0001" num="0000">The present invention describes new amino pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel amino pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors.</p>
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Compounds having muscarinic receptor antagonist and BETA2 adrenergic receptor agonist activity (Fri, 19 Aug 2016)
<p id="p-0001" num="0000">Compounds of formula I, defined herein, act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for treating broncho-obstructive and inflammatory diseases.</p>
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DIHYDRO-PYRROLOPYRIDINONE INHIBITORS (Fri, 19 Aug 2016)
<p id="p-0001" num="0000">The present invention provides for compounds of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.26mm" wi="69.85mm" file="US20160237084A1-20160818-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, and R<sup>5 </sup>have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).</p>
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DISUBSTITUTED BETA-LACTONES AS INHIBITORS OF N-ACYLETHANOLAMINE ACID AMIDASE (NAAA) (Fri, 19 Aug 2016)
<p id="p-0001" num="0000">The present invention provides compounds and pharmaceutical compositions for inhibiting N-acylethanolamine acid amidase (NAAA). Inhibition of NAAA is contemplated as a method to sustain the levels of palmitoylethanolamide (PEA) and oleylethanolamide (OEA), two substrates of NAAA, in conditions characterized by reduced concentrations of PEA and OEA. The invention also provides methods for treating inflammatory diseases and pain, and other disorders in which decreased levels of PEA and OEA are associated with the disorder.</p>
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BIARYLTRIAZOLE INHIBITORS OF MACROPHAGE MIGRATION INHIBITORY FACTOR (Fri, 19 Aug 2016)
The present disclosure describes biaryl triazole compounds, as well as their compositions and methods of use. The compounds inhibit the activity of macrophage migration inhibitory factor and are useful for the treatment of diseases, e.g., inflammatory diseases and cancer.
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Pyrazolyl-ureas as kinase inhibitors (Fri, 19 Aug 2016)
There are provided compounds of formula (I) as defined in the specification which are p38 MAP kinase inhibitors for use as medicaments for the treatment <i>inter alia </i>of inflammatory diseases.
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Quinazolin-4 (3H)-one derivatives used as P13 kinase inhibitors (Fri, 05 Aug 2016)
<p id="p-0001" num="0000">The present invention relates to the compound of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="69.17mm" wi="61.04mm" file="US09637494-20170502-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and to compositions comprising the same and to the use of the compound and to compositions of the compound in treatment, for example in the treatment of inflammatory diseases, in particular respiratory inflammatory disease. The invention also extends to methods of making the said compound. </p>
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Purinone compounds as kinase inhibitors (Fri, 05 Aug 2016)
Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
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NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS (Fri, 29 Jul 2016)
<p id="p-0001" num="0000">The present invention discloses compounds according to Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="49.36mm" wi="69.85mm" file="US20160214986A1-20160728-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">Wherein R<sup>1a</sup>, R<sup>1b</sup>, R<sup>2</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6</sup>, R<sup>7</sup>, R<sup>8</sup>, W, X, Y, Z, Cy, and the subscript a are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.</p>
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NOVEL COMPOUND USEFUL FOR THE TREATEMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES (Fri, 29 Jul 2016)
<p id="p-0001" num="0000">A pyrazolopyridine compound according to Formula I, able to inhibit JAK is disclosed, as well as pharmaceutically acceptable salts, a solvate thereof, solvates of the pharmaceutically acceptable salts and biologically active metabolites thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment or prophylaxis of a variety of conditions in mammals including humans, and particularly, such conditions as may be associated with aberrant JAK activity, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="53.93mm" wi="69.85mm" file="US20160213666A1-20160728-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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DIPHENYLOXYALKYLAMINE DERIVATIVES AND ARYLOXYALKYLAMINE DERIVATIVES, PHARMACEUTICAL COMPOSITION, USE OF SAID PHARMACEUTICAL COMPOSITION FOR TREATING, PREVENTING OR INHIBITING CHRONIC PULMONARY INFLAMMATORY DISEASES AND METHOD FOR TREATING OR PREVENTING SUCH DISEASES (Fri, 29 Jul 2016)
<p id="p-0001" num="0000">The present invention relates to diphenyloxyalkylamine derivatives and aryloxyalkylamine derivatives that are structurally analogous to mexiletine, said derivatives having important biological activity and not causing the undesired side effects observed with the prototype, as well as with other drugs from the same therapeutic class as the prototype. The derivatives of the present invention have formulas II and III and are used for treating, preventing or inhibiting pulmonary inflammatory diseases, for example, asthma and chronic obstructive pulmonary disease (COPD).</p>
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INHIBITORS OF TRKA KINASE (Fri, 29 Jul 2016)
The present invention is directed to the compounds of Formula I which are inhibitors of tropomyosin-related kinase A (TrkA): Formula (I) or steroisomers, tautomers or a pharmaceutically acceptable salts, metabolites, isotopes, solvates or prodrugs thereof, wherein, Ra, Rb, Rc, Rd, R1, R2, L and Het-Ar are as defined herein. These compounds can be used for the preventive and/or therapeutic treatment of diseases or disorders associated with abnormal activities of nerve growth factor (NGF) receptor TrkA such as Pain, inflammation or an inflammatory diseases, Cancer, atherosclerosis, restenosis, thrombosis, Neurodegenerative diseases, Erectile Dysfunction (ED), Skin disorders, Autoimmune disease like Multiple sclerosis, Sjögren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis, Infectious diseases, diseases related to an imbalance of the regulation of bone remodeling, endometriosis, pelvic pain syndrome and diseases resulting from abnormal tissue remodelling and fibrotic disorders; or a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination.
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Substituted pyroolopyridines and pyrrolopyrazines for treating cancer or inflammatory diseases (Fri, 29 Jul 2016)
Disclosed herein are substituted pyrrolopyridine and pyrrolopyrazine compounds and compositions useful in the treatment of TAK mediated diseases, such as cancer, having the structure of Formula (I): wherein R<sp>1</sp>, R<sp>2</sp>, R<sp>3</sp>, and R<sp>4</sp> are as defined in the detailed description. Methods of modulation of TAK activity in a human or animal subject are also provided, providing therapeutic benefit to subjects with disease conditions, especially cancer.
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INHIBITORS OF KINASE ACTIVITY (Thu, 28 Jul 2016)
The present invention relates to pyridines or pyrazines that inhibit kinases. In particular the compounds of the invention inhibit members of the class III PTK receptor family such as FMS (CSF-1R), c-KIT, PDGFR², PDGFR± or FLT3 and KDR, SRC, EphA2, EphA3, EphA8, FLT1, FLT4, HCK, LCK, PTK5 (FRK), SYK, DDR1 and DDR2 and RET. The compounds of the invention are useful in the treatment of kinase associated diseases such as immunological and inflammatory diseases; hyperproliferative diseases including cancer and diseases involving neo-angiogenesis; renal and kidney diseases; bone remodeling diseases; metabolic diseases; and vascular diseases.
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MAO-B Selective Inhibitor Compounds, Pharmaceutical Compositions Thereof and Uses Thereof (Fri, 22 Jul 2016)
<p id="p-0001" num="0000">Described herein are a series of compounds having the structure of Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="37.68mm" wi="57.40mm" file="US20160207878A1-20160721-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">for use in the inhibition of MAO and uses thereof for the treatment of a barrier disease, obesity, solid epithelial cell tumor metastasis, diabetes, an auto-immune and inflammatory disease or a cardiometabolic disorder.</p>
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DI-PIDOTIMOD BENZATHINE AND SOLID FORMS THEREOF (Fri, 22 Jul 2016)
The present invention relates to di-pidotimod benzathine. In particular, it relates to di-pidotimod benzathine in solid form such as in crystalline or amorphous; specific polymorphs are also disclosed such as Form M. Form H and hydrate Form H of di-pidotimod benzathine, in an additional aspect of the invention, solvates and cocrystals of hydrate Form H di-pidotimod benzathine are provided. In a further aspect of the invention, variable isopropanol solvates: variable ethanol solvates; variable hydrates; and a particular anhydrate are provided. Particular solid forms include variable isopropanol solvates Form J and Form O of di-pidotimod benzathine; variable ethanol solvates Form S and Form W of di-pidotimod benzathine; variable hydrate Form X of di-pidotimod benzathine; and anhydrate Form T of di-pidolimod benzathine. in further aspects of the invention, processes for making such solid forms are provided. In additional aspects of the invention, methods of treating infections or inflammatory diseases using one or more of such solid forms are provided.
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INHIBITORS OF PHOSPHOGLYCERATE DEHYDROGENASE (PHGDH) AND USES THEREOF (Fri, 22 Jul 2016)
The present invention provides compounds of Formula (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, pro-drugs, and compositions thereof. Also provided are methods and kits involving the compounds of Formula (I), (II) or (III) for treating diseases associated with the over-expression of phosphoglycerate dehydrogenase (PHGDH) in a subject, such as proliferative diseases (e.g., cancers (e.g., breast cancer, ER negative breast cancer, melanoma, cervical cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases). Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the activity of PHGDH or inhibit the serine biosynthetic pathway, or both.
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DI-PIDOTIMOD BENZATHINE AND SOLID FORMS THEREOF (Fri, 22 Jul 2016)
The present invention relates to di-pidotimod benzathine. In particular, it relates to di-pidotimod benzathine in solid form such as in crystalline or amorphous; specific polymorphs are also disclosed such as Form M, Form H and hydrate Form H of di-pidotimod benzathine. In an additional aspect of the invention, solvates and cocrystals of hydrate Form H di-pidotimod benzathine are provided. In further aspects of the invention, processes for making solid di-pidotimod benzathine, crystalline di-pidotimod benzathine, amorphous di-pidotimod benzathine, Form M di-pidotimod benzathine, hydrate Form H di-pidotimod benzathine and Form H di-pidotimod benzathine are provided. In additional aspects of the invention, methods of treating infections or inflammatory diseases using one or more of di-pidotimod benzathine, solid di- pidotimod benzathine, crystalline di-pidotimod benzathine; amorphous di- pidotimod benzathine, Form M di-pidotimod benzathine, Form H di-pidotimod benzathine or solvates, cocrystals or hydrates thereof are provided.
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1,5-DIPHENYL-PENTA-1,4-DIEN-3-ONE COMPOUNDS (Thu, 21 Jul 2016)
This invention relates to compounds of Formula (I), (II), or (III) as shown in the specification, which contain a 1,5-diphenylpenta-1,4-dien-3-one backbone. These compounds can be used to treat cancer, inflammatory disease, or autoimmune disease.
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Ibrutinib prodrugs, pharmaceutical compositions thereof, and methods of use (Wed, 20 Jul 2016)
<p id="p-0001" num="0000">Prodrugs of ibrutinib, pharmaceutical compositions comprising the prodrugs, and methods of using the prodrugs and pharmaceutical compositions for treating autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions are disclosed.</p>
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Polyfluorinated compounds acting as bruton tyrosine kinase inhibitors (Fri, 15 Jul 2016)
<p id="p-0001" num="0000">Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton's tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.</p>
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Aromatic heterocyclic compounds as antiinflammatory compounds (Fri, 15 Jul 2016)
There is provided a compound of formula (I) as defined in the specification which is a p38 MAP kinase inhibitor for use as medicament for the treatment <i>inter alia</i> of inflammatory diseases.
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Inhibitors of Bruton's tyrosine kinase (Wed, 06 Jul 2016)
<p id="p-0001" num="0000">Disclosed herein are reversible and irreversible inhibitors of Bruton's tyrosine kinase (Btk). Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are described, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.</p>
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ARSENIC-BASED TREATMENT OF CANCERS AND INFLAMMATORY DISORDERS (Fri, 01 Jul 2016)
<p id="p-0001" num="0000">In one embodiment, the invention provides a method of treating a subject who suffers from a cancer (particularly a chemotherapeutic or radiotherapeutic-resistant cancer) or from an inflammatory disorder, the method comprising co-administering to the subject a pharmaceutically-effective amount of: (a) one or more elements or compounds selected from the group consisting of arsenic, an arsenite and arsenic trioxide (ATO); and optionally (b) at least one anticancer agent (preferably a DNA damaging agent); and/or (c) at least one or more Poly(ADP-ribose) polymerase (PARP) inhibitors other than arsenic, an arsenite and arsenic trioxide (ATO). In preferred embodiments, the arsenic for the treatment of cancer, arsenite and ATO serve as radio sensitizers for concomitant radiotherapy as well as PARP inhibitors. Methods for treating inflammatory disease are also disclosed. Related pharmaceutical formulations are also provided.</p>
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Bromodomain Inhibitors (Fri, 01 Jul 2016)
<p id="p-0001" num="0000">The present invention provides for compounds of formula (I). wherein R<sup>x</sup>, R<sup>y</sup>, R<sup>x1</sup>, L<sup>1</sup>, G<sup>1</sup>, A<sup>1</sup>, A<sup>2</sup>, A<sup>3</sup>, and A<sup>4 </sup>have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.52mm" wi="58.25mm" file="US20160185769A1-20160630-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7) (Fri, 01 Jul 2016)
The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7)), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
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SITE SPECIFIC DOSING OF A BTK INHIBITOR (Fri, 01 Jul 2016)
Disclosed herein are formulations and methods of site specific administration of Compound (I) or a pharmaceutically acceptable salt thereof. Compound (I) is a potent BTK inhibitor and hence can be useful for the treatment of diseases such as cancer, autoimmune, and inflammatory diseases.
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HETEROCYCLIC DERIVATIVES AS RORGAMMA MODULATORS (Fri, 01 Jul 2016)
The present invention provides novel compounds of formula (I) that are modulators of RORgamma. These compounds, and pharmaceutical compositions comprising the same, are suitable means for treating any disease wherein the modulation of RORgamma has therapeutic effects, for instance in autoimmune diseases, autoimmune-related diseases, inflammatory diseases, fibrotic diseases, or cholestatic diseases.
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3-HETEROAROYLAMINO-PROPIONIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS (Thu, 30 Jun 2016)
3-Heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals The present invention relates to compounds of the formula I, wherein Ht, G, R 10 , R 30 , R 40 , R 50 and R 60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
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