Cancer

BROMODOMAIN-INHIBITING COMPOUNDS AND PHARMACEUTICAL COMPOSITION COMPRISING SAME FOR PREVENTING OR TREATING A CANCER (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">Provided is a novel compound having bromodomain and extra terminal domain (BET) protein inhibiting activities, and a pharmaceutical composition comprising the same which can be useful for prevention or treatment of precancerous transformation or cancer.</p>
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QUINOLINE DERIVATIVES AS SMO INHIBITORS (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">Disclosed are quinoline derivatives as hedgehog pathway inhibitors, especially as SMO inhibitors. Compounds of the present invention can be used in treating diseases relating to hedgehog pathway including cancer.</p>
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QUINOXALINE COMPOUNDS AND USES THEREOF (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">This invention provides compounds of formula I and subsets thereof: wherein T, J, R, R<sup>4</sup>, R<sup>q</sup>, o, R<sup>A</sup>, and R<sup>B </sup>and subsets thereof are as described in the specification. The compounds are inhibitors of NAMPT and are thus useful for treating cancer, inflammatory conditions, or T-cell mediated autoimmune disease.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="23.96mm" wi="65.53mm" file="US20170174704A1-20170622-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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MODIFICATION OF CUPREDOXIN DERIVED PEPTIDES AND METHODS OF USE THEREOF (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">The present invention provides modified cupredoxin derived peptides with pharmacologic activity that have improved pharmacokinetic properties, and methods to use them to treat mammals suffering from various conditions related to the pharmacologic activities. Modifications of the cupredoxin derived peptides include amino acid sequence variants and structural derivations that increase the plasma half-life of the peptide, increase the specific activity of the pharmacologic activity, decrease immunogenicity, and decrease the biotransformation of the peptides. The modified cupredoxin derived peptides can be used in methods to treat mammals for cancer, conditions related to inappropriate angiogenesis, viral and bacterial infections, and specifically HIV and malaria, conditions related to ephrin signaling, and to deliver cargo compounds, including diagnostic compounds, to cancer cell</p>
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Protein-Based Molecular Temperature Switch (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">A region of the TRPM8 protein that functions as a temperature switch (FIG. <b>1</b>) has been identified, and can be expressed, purified and applied in combination with other proteins. The function of the switch is maintained even when the region or domain is isolated from the entire protein. As the protein domain is a temperature switch, it can be used to control other proteins and signaling pathways in vitro and in vivo; and 2) TRPM8 is a therapeutic target that is being pursued primarily for intervention in pain (neuropathic and inflammatory) and cancer.</p>
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BENZIMIDAZOLE DERIVATIVES AS ERBB TYROSINE KINASE INHIBITORS FOR THE TREATMENT OF CANCER (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">Provided herein are benzimidazole derivatives, for example, of Formula (I), and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.79mm" wi="56.98mm" file="US20170174697A1-20170622-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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VITAMIN D RECEPTOR-COREGULATOR INHIBITORS (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">Described herein are compounds, pharmaceutical compositions and methods for inhibiting the expression of a vitamin D receptor target gene, inhibiting interactions between the vitamin D receptor and at least one vitamin D receptor coactivator, for treating cancer in a subject, and for inhibiting angiogenesis in a subject.</p>
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HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.06mm" wi="61.30mm" file="US20170174679A1-20170622-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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HETEROCYCLIC COMPOUND (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">Provided is a compound or a salt thereof, which has an excellent JAK inhibitory action, and is useful as a prophylactic or therapeutic agent for autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren's syndrome, Behcet's syndrome, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like. 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="40.81mm" wi="53.42mm" file="US20170174682A1-20170622-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 present specification, or a salt thereof.</p>
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SUBSTITUTED INDOLE MCL-1 INHIBITORS (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.</p>
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METHODS (AMACR) (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">A method of measuring α-methylacyl-CoA racemase (AMACR) activity in a sample is described comprising the steps of: (i) providing a sample; (ii) contacting said sample with a substrate compound that undergoes elimination of hydrogen and a leaving group catalysed by said AMACR to produce a product compound having an additional carbon-carbon double bond; and (iii) measuring the amount of said leaving group and/or of said product compound and/or of unreacted substrate compound. Also provided are methods of diagnosis and medical imaging, in particular for use in diagnosing prostate cancer. Also provided are substrate compounds of Formula 1 for use in the methods described herein.</p>
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NANOPARTICLE FORMULATIONS AND USES THEREOF (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">The present invention provides compositions comprising nanoparticles comprising: 1) a drug, such as a hydrophobic drug derivative; and 2) a carrier protein. Also provided are methods of treating diseases (such as cancer) using the compositions, as well as kits and unit dosages.</p>
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ANTIMITOTIC AMIDES FOR THE TREATMENT OF CANCER AND PROLIFERATIVE DISORDERS (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">Novel, antimitotic heteroaryl amides and pharmaceutically acceptable salts of Formula I where Ar, R<sup>5</sup>, R<sup>6</sup>, R<sup>8</sup>, R<sup>9</sup>, R<sup>11</sup>, X<sup>1</sup>, and X<sup>2 </sup>are as defined herein, as compounds for treatment and prevention of cancer and proliferative diseases and disorders.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.65mm" wi="62.99mm" file="US20170172984A1-20170622-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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TREATMENT OF CANCERS HAVING RESISTANCE TO CHEMOTHERAPEUTIC AGENTS (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">The present invention provides compositions and methods for treating cancer with DAST, 4{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide of the formula I, including all polymorphs, hydrates, pharmaceutically acceptable salts, metabolites, prodrugs, solvates or combinations thereof.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.67mm" wi="75.35mm" file="US20170172989A1-20170622-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">Any cancer can be treated, including cancers that have acquired resistance to another therapeutic agent, such as kinase inhibitors. DAST can also be used to treat cancers which have become refractory to other chemotherapeutic agents</p>
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IMAGE GUIDED THERAPY FOR CANCER (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">The invention provides a method to treat cancer in an animal comprising administering a tetra-arylethylene cation to the animal.</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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Antibody to Mucin 4 (MUC4) Glycopeptide and Uses Thereof (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">The present invention provides: an antibody that has specificity for MUC 4 having a sugar chain structure that is expressed at a high level in cancer cells; a glycopeptide that constitutes an antigen that is suitable for producing this antibody; and a new means and method for the diagnosis, prevention, and/or treatment of cancer by means of the aforementioned antibody. The present invention relates to a monoclonal antibody against a glycopeptide. The glycopeptide comprises a human MUC 4 tandem unit peptide having an amino acid sequence represented by SEQ ID NO: 1, and an O-linked sugar chain. The O-linked sugar chain is N-acetylgalactosamine (GalNAc) and binds to threonine, which is the 8th amino acid of the tandem unit peptide. The present invention further includes: a glycopeptide for use in the production of a monoclonal antibody against human MUC 4; a method for detecting MUC 4 in a human body fluid sample; a kit that includes the abovementioned monoclonal antibody; and a pharmaceutical composition for the prevention and/or treatment of malignant tumors that contains the abovementioned monoclonal antibody as an active component.</p>
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COMPOUND ISOLATED FROM ISODON FORRESTII VAR. FORRESTII AND PREPARATION METHOD AND APPLICATIONS THEREOF (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">A compound of Formula I or pharmaceutically acceptable salt thereof and its preparation method and applications, the new structure of the compound of formula I has not been reported in literature. It is isolated from <i>Isodon forrestii </i>var. <i>forrestii </i>and can be a compound served as Trx1 selective inhibitor. The present invention further discloses a pharmaceutical composition, preparation of the compound of</p> <p id="p-0002" num="0000">Formula I and its applications in preparing medicines for preventing or treating cancer. Iso A of the present invention has the advantages of low toxicity, high safety and strong pharmacological effect, which suggests a potential prospect in pharmaceutical applications.</p>
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HDAC INHIBITOR COMPOUNDS AND METHODS OF TREATMENT (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">The instant invention describes hydrazide-containing compounds having therapeutic activity, and methods of treating disorders such as cancer, tumors and cell proliferation related disorders, or affect cell differentiation, dedifferentiation or transdifferentiation.</p>
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NAT10 MODULATORS FOR TREATING OR PREVENTING LAMINOPATHIES, AGING AND CANCER (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">The invention relates to compounds in the treatment or prevention of disorders associated with Lamin A and/or Lamin C depletion or LMNA mutations, such as laminopathy, premature ageing disorders, normal ageing and cancer (such as a cancer characterised by low levels of LMNA expression).</p>
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3-SUBSTITUTED CARBONYL-NAPHTHO[2,3-B]FURANE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">The present invention provides a compound of the following Formula (1) or a pharmaceutically acceptable salt thereof:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.06mm" wi="41.91mm" file="US20170174646A1-20170622-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein X is an oxygen atom and the like; Y is —CO—, —SO<sub>2</sub>— and the like; R<sup>1 </sup>is an optionally-substituted C<sub>1-6 </sub>alkyl group, an optionally-substituted C<sub>1-6 </sub>alkylcarbonyl group and the like; R<sup>2 </sup>is an optionally-substituted C<sub>1-6 </sub>alkyl group, an optionally-substituted C<sub>1-6 </sub>alkoxy group, an optionally-substituted amino group, an optionally-substituted 5- to 12-membered monocyclic or polycyclic saturated heterocyclic group and the like; R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, and R<sup>6 </sup>are independently a hydrogen atom and the like which exhibits excellent effects in suppressing the proliferation and sphere-forming ability of cancer cells, and can be useful as an antitumor drug or cell growth inhibitor.</p>
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HISTONE DEMETHYLASE INHIBITORS (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted 3-aminopyridine derivative compounds, substituted 3-aminopyridazine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.</p>
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HEAT SHOCK PROTEIN 70 (HSP-70) RECEPTOR LIGANDS (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">Inducible HSP70 is overexpressed in a wide spectrum of human tumors and its expression correlates with metastasis and poor outcomes to radiation and chemotherapy in patients. Identification of small molecule inhibitors of HSP70 pose a new therapy to cancer treatment. HS72, a benzimidazole piperidinyl carboxamide has been identified as an allosteric inhibitor for HSP70 and has demonstrated good tumor growth inhibition in vivo.</p>
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PYRROLOPYRIMIDINE COMPOUNDS, USE AS INHIBITORS OF THE KINASE LRRK2, AND METHODS FOR PREPARATION THEREOF (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">The present disclosure is concerned with certain pyrrolopyrimidine compounds that are capable of inhibiting certain protein kinases, and especially the leucine-rich repeat kinase 2 (LRRK2) protein. Compounds of the present disclosure can be used to treat a number of disorders caused by or associated with abnormal LRRK2 kinase activity. Compounds of the present disclosure can be used to treat disorders including neurodegenerative diseases such as Parkinson's disease; precancerous conditions and cancer; autoimmune disorders such as Crohn's disease, rheumatoid arthritis and psoriasis; and leprosy (Hansen's disease). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.</p>
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COMBINATION THERAPY FOR CANCER (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">The present invention provides preparation of medicaments for use in treating and methods of treating non-small cell lung cancer in a patient comprising: [5-(4-ethyl-piperazin-1-ylmethyl)-pyridin-2-yl]-[5-fluoro-4-(7-fluoro-3-isopropyl-2-methyl-3H-benzoimidazol-5-yl)-pyrimidin-2-yl]-amine, or a pharmaceutically acceptable salt thereof, in combination, as further described herein, with an anti-VEGFR2 antibody, preferably, ramucirumab.</p>
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PHARMACEUTICAL FORMULATIONS OF A PAN-RAF KINASE INHIBITOR, PROCESSES FOR THEIR PREPARATION, AND METHODS OF USE (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">The invention relates to a pharmaceutical composition comprising Compound 1 or a pharmaceutically acceptable salt thereof for the treatment of cancer and a process for its preparation. The invention also relates to administering the pharmaceutical composition to a patient according to an intermittent dosing regimen.</p>
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METHOD FOR USE OF HOMOPIPERAZINIUM COMPOUNDS IN THE TREATMENT OF CANCER (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">A method for treating cancer comprising administering to a patient in need thereof an effective amount of a compound having the formula:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.95mm" wi="26.67mm" file="US20170173040A1-20170622-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R<sub>1 </sub>and R<sub>2 </sub>are independently alkyl of 1 to 6 carbon atoms or cycloalkyl of 3 to 6 carbon atoms, Xa is CH or N, Ya is hydrogen or a substituent, each of which is independently selected; n is an integer from 1 to 5, J is a counter ion.</p>
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WITHACNISTIN COMPOUNDS FOR TREATMENT OF CANCER (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">The subject invention pertains to the treatment of tumors and cancerous tissues and the prevention of tumorigenesis and malignant transformation through the modulation of STAT3 intracellular signaling. The subject invention concerns pharmaceutical compositions containing one or more withacnistin compounds, or a pharmaceutically acceptable salt or derivative thereof. In one embodiment, the subject invention concerns a composition comprising a mixture of withacnistin, 3-methoxy-2,3-dihydrowithacnistin, and 3-ethoxy-2,3-dihydrowithacnistin, or a salt or derivative of any of the foregoing. Another aspect of the invention concerns methods of inhibiting the growth of a tumor by administering one or more withacnistin compounds, or a pharmaceutically acceptable salt or derivative thereof, to a patient, wherein the tumor is characterized by the constitutive activation of the STAT3 intracellular signaling pathway. The present invention further pertains to methods of moderating the STAT3 signaling pathway in vitro or in vivo using one or more withacnistin compounds, or a pharmaceutically acceptable salt or derivative thereof.</p>
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EXOGENOUS TAP INHIBITOR ARMED ONCOLYTIC VIRUSES AND THERAPEUTIC USES THEREOF (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">The present invention relates to exogenous TAP inhibitor armed oncolytic viruses that replicate selectively in cancer cells, evade CD8+ cytolytic T-cells, and induce the immune system to recognize tumor cells. Preferred viruses of the invention have a heterologous gene that encodes a function that affects antigen presentation by inhibiting TAP. The viruses of the invention also comprise one or more heterologous genes encoding immunomodulatory polypeptides, prodrug converting enzymes, or matrix degrading enzymes. Compositions and therapeutic methods using the oncolytic viruses are also provided, including compositions and therapeutic methods for treating cancers, such as melanoma, head and neck cancer, ovarian cancer, breast cancer, glioblastoma, bladder cancer, prostate cancer, lung cancer, liver cancer, colorectal cancer, pancreatic cancer, and renal cancer.</p>
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1H-IMIDAZO[4,5-B]PYRIDINYL AND 2-OXO-2,3-DIHYDRO-1H-IMIDAZO[4,5-B]PYRIDINYL HETEROCYCLIC BET BROMODOMAIN INHIBITORS (Fri, 23 Jun 2017)
Substituted 1H-imidazo[4,5-b]pyridinyl and 2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridinyl heterocyclic compounds, which are useful as inhibitors of BET protein function by binding to bromodomains, compositions comprising said compounds, and their use in therapy are disclosed herein. These compounds are useful in the treatment of diseases and conditions, such as, cancer, autoimmune diseases, inflammation and cardiovascular diseases.
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COMPOUNDS USEFUL AS KINASE INHIBITORS (Fri, 23 Jun 2017)
This invention relates to novel compounds. The compounds of the invention are tyrosine kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Bruton's tyrosine kinase (BTK).The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of Bruton's tyrosine kinase, for example cancer, lymphoma, leukemia and immunological diseases.
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Novel Compounds (Fri, 23 Jun 2017)
The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C- terminal hydrolase 30 or Ubiquitin Specific Peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and cancer. Compounds of the invention include compounds having the formula (I): (I) or a pharmaceutically acceptable salt thereof, wherein R1a, R1b, R1c, R1d, R1e, R1f, R1g, R2, X, L and A are as defined herein.
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DIPHENYLPROPANE COMPOUNDS AND THEIR CYTOTOXIC ACTIVITY (Fri, 23 Jun 2017)
The invention relates to new derivatives of 1,3-diphenylpropane described by general formula (I), demonstrating cytotoxic activity against cancer cells, to be used as drugs in anticancer therapy, and characterized by reduced undesired side effects in comparison to related derivatives of chalcones.
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INHIBITION OF CYTOKINE-INDUCED SH2 PROTEIN IN NK CELLS (Fri, 23 Jun 2017)
The present invention relates to therapeutic and prophylactic methods based on inhibition of CIS in NK cells. In particular, the present invention relates to treating or preventing a NK-responsive condition by administering to a subject a CIS inhibitor, or administering CIS-inhibited NK cells. The invention further relates to methods for identifying a CIS inhibitor, and for determining a likelihood of cancer response to treatment with CIS inhibition.
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METAL COMPLEXED THERAPEUTIC AGENTS AND LIPID-BASED NANOPARTICULATE FORMULATIONS THEREOF (Fri, 23 Jun 2017)
Provided herein is a pharmaceutical formulation for delivery of a therapeutic agent having a metal complexation moiety and a solubility in water or a metal ion solution of less than 1 mg/ml. Said formulation comprises the therapeutic agent and a metal ion complexed inside a lipid-based nanoparticle formulation.
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HETEROCYCLES USEFUL AS ANTI-CANCER AGENTS (Fri, 23 Jun 2017)
Compounds of Formula (I) are shown below, and their pharmaceutically acceptable salts, hydrates, or solvates thereof. It involves pharmaceutical compositions of these compounds, their preparation, and their utilities in treating diseases and disorders, including cancers.
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QUINOLIZINONE DERIVATIVES AS PI3K INHIBITORS (Fri, 23 Jun 2017)
Disclosed are compounds of formula (I), their tautomeric forms, stereoisomers, and pharmaceutically acceptable salts thereof (I), wherein R1-R5, and n are as defined in the specification, pharmaceutical compositions including a compound, tautomer, stereoisomer, or salt thereof, and methods of treating or preventing diseases or disorders, for example, cancer, that are amenable to treatment or prevention by inhibiting the PI3K enzyme of a subject.
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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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COMPOSITIONS FOR THERAPEUTICS, TARGETED PET IMAGING AND METHODS OF THEIR USE (Fri, 23 Jun 2017)
Described herein is a chelator for radiolabels (e.g., 89Zr) for targeted PET imaging that is an alternative to DFO. In certain embodiments, the chelator for 89Zr is the ligand, 3,4,3-(LI-1,2- HOPO) ("HOPO"), which exhibits equal or superior stability compared to DFO in chemical and biological assays across a period of several days in vivo. As shown in FIG. 1, the HOPO is an octadentate chelator that stabilizes chelation of radiolabels (e.g., 89Zr). A bifunctional ligand comprising p-SCN-Bn-HOPO is shown in FIG. 4 and FIG. 5. Such a bifunctional ligand can eliminate (e.g., 89Zr) loss from the chelate in vivo and reduce uptake in bone and non-target tissue. Therefore, the bifunctional HOPO ligand can facilitate safer and improved PET imaging with radiolabeled antibodies.
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COMPOUNDS, COMPOSITIONS AND METHODS OF TREATING CANCER (Fri, 23 Jun 2017)
Disclosed are compounds of formulas I and II, in which R, R0, R1-R4, R7-R10, n, X, Y, Y', and E are as described herein, pharmaceutical compositions containing such compounds. The compounds and pharmaceutical compositions are for use in treating or preventing diseases, for example, cancer.
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NAPTHOQUINONES, PRO-DRUGS, AND METHODS OF USE THEREOF (Fri, 23 Jun 2017)
Provided herein are naphthoquinones compounds such as those with a hydrogen bond donating group of the formula (I): wherein: R1, R2, R3, R4, R5, and n are as defined herein. Also provided herein are pharmaceutical composition of the present compounds and methods of treatment using the compounds including their use in the treatment of cancer.
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PROCESS FOR THE PREPARATION OF TRICYCLIC PI3K INHIBITOR COMPOUNDS AND METHODS FOR USING THE SAME FOR THE TREATMENT OF CANCER (Fri, 23 Jun 2017)
The present disclosure provides for methods for preparing tricyclic PI3K inhibitor compounds in high yield and purity in aqueous solvent systems.
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NUCLEOTIDE AND NUCLEOSIDE THERAPEUTIC COMPOSITIONS AND USES RELATED THERETO (Fri, 23 Jun 2017)
This disclosure relates to nucleotide and nucleoside therapeutic compositions and uses in treating infectious diseases, viral infections, and cancer, where the base of the nucleotide or nucleoside contains at least one thiol, thione or thioether.
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PYRROLOPYRIMIDINE COMPOUNDS, USE AS INHIBITORS OF THE KINASE LRRK2, AND METHODS FOR PREPARATION THEREOF (Fri, 23 Jun 2017)
The present disclosure is concerned with certain pyrrolopyrimidine compounds that are capable of inhibiting certain protein kinases, and especially the leucine-rich repeat kinase 2 (LRRK2) protein. Compounds of the present disclosure can be used to treat a number of disorders caused by or associated with abnormal LRRK2 kinase activity. Compounds of the present disclosure can be used to treat disorders including neurodegenerative diseases such as Parkinson's disease; precancerous conditions and cancer; autoimmune disorders such as Crohn's disease, rheumatoid arthritis and psoriasis; and leprosy (Hansen's disease). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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TRITERPENE SAPONIN VARIANTS, METHODS OF SYNTHESIS AND USE THEREOF (Fri, 23 Jun 2017)
A number of triterpene saponin variants with different modifications on their central glycosyl ester linkage are described. Also described are methods of making and method of using such triterpene saponin variants.
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QUINAZOLINE DERIVATIVE (Thu, 22 Jun 2017)
Provided are a quinazoline derivative, a pharmaceutical composition containing the same, a method for preparation of said derivative, and an application of same as an anti-cancer drug.
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AMINOPYRIMIDINE COMPOUNDS AS INHIBITORS OF T790M CONTAINING EGFR MUTANTS (Thu, 22 Jun 2017)
This invention relates to novel compounds of formula (I) which are inhibitors of T790M containing EGFR mutants, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of cancer.
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PYRIDINE AMIDOPYRIMIDINE DERIVATIVE, PREPARATION METHOD AND USE THEREOF (Thu, 22 Jun 2017)
The present invention relates to pyridinylaminopyrimidine derivatives represented by the following formula (I), and pharmaceutically acceptable salts, preparation process and use thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , m and A are defined as in the description. Pyridinylaminopyrimidine derivatives of the present invention can selectively inhibit the activity of mutant-type epidermal growth factor receptor (EGFR), have a good inhibition for the cancer cell proliferation, and therefore can be used as a therapeutic agent for treating tumors and relevant diseases.
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CHEMICAL INHIBITOR OF P53-SNAIL BINDING AND PHARMACEUTICAL COMPOSITION FOR TREATING CANCER DISEASE CONTAINING SAME AS ITS ACTIVE INGREDIENT (Thu, 22 Jun 2017)
Provided are compounds for inhibiting Snail-p53 binding and therapeutic agents for cancer including the compounds as an effective component. The Snail-p53 binding inhibitors induce expression of p53 in K-Ras mutant cell lines, thereby enabling effective treatment or prevention of K-Ras mutant cancer, such as, pancreatic cancer, lung cancer, cholangioma, and colon cancer, of which diagnosis or treatment is not easy.
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HYDROXAMIC ACID-BASED COMPOUNDS (Fri, 16 Jun 2017)
The present invention relates to hydroxamic acid-based compounds, their intermediates, preparation and uses. The compounds are useful in imaging, particularly for the imaging of tumours and cancer, and especially for the imaging of prostate cancer. The present invention also relates to compositions including the compounds, and to methods of imaging cells, in vitro biopsy samples and/or patients using the compounds.
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GOLD PORPHYRIN-PEG CONJUGATES AND METHODS OF USE (Fri, 16 Jun 2017)
Disclosed are conjugates, compositions, and methods that include or use one or more gold (III) porphyrin complexes. Preferred conjugates are gold (III) porphyrin-poly (ethylene glycol) (PEG) conjugates. Preferred compositions and methods include or use such gold (III) porphyrin-PEG conjugates. Disclosed is a method for treatment of cancer comprising administering to a human in need of such treatment a composition containing a therapeutically effective amount of gold (III) porphyrin-poly (ethylene glycol) (PEG) conjugates. The gold (III) porphyrin-PEG conjugates can be in the form of nanostructures formed by self-assembly of the gold (III) porphyrin-PEG conjugates; or nanocomposites formed by encapsulation of other therapeutic agents by the nanostructures of gold (III) porphyrin-PEG conjugates.
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CPAP-TUBULIN MODULE (Fri, 16 Jun 2017)
The invention relates to CPAP-tubulin inhibitors having the general formula (1) or a physiologically acceptable salt thereof; and their use as cancer therapeutics.
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MONOMALEIMIDE-FUNCTIONALIZED PLATINUM COMPOUNDS FOR CANCER THERAPY (Fri, 16 Jun 2017)
The present invention relates to novel monomaleimide-functionalized platinum compounds of formula (I), including in particular novel monomaleimide-functionalized oxaliplatin and carboplatin derivatives, as well as their use as medicaments, particularly for the treatment or prevention of cancer.
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COMBINED PREPARATIONS OF PKM2 MODULATORS AND HMGB1 (Fri, 16 Jun 2017)
The present invention relates to a combined preparation comprising (i) a modulator of pyruvate kinase M2 (PKM2) activity, and (ii) an agent providing high mobility group box 1 (HMGB1) polypeptide or a derivative thereof. The present invention also relates to the aforesaid combined preparation for use as a medicament and for use in the treatment of inappropriate cellular proliferation, preferably in the treatment of cancer. Moreover, the present invention relates to a method for determining whether a subject suffering from inappropriate cellular proliferation is amenable to a treatment comprising administration of a modulator of PKM2 activity as the only PKM2 inhibitor and to treatment methods related thereto.
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BENZOTHIADIAZINE COMPOUNDS (Fri, 16 Jun 2017)
The invention is directed to substituted benzothiadiazine derivatives. Specifically, the invention is directed to compounds according to Formula (I):wherein R, R1, R2, R3, R4 and R5 are as defined herein. The compounds of the invention are inhibitors of CD73 and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases associated with CD73 inhibition, such as AIDS, autoimmune diseases, infections, atherosclerosis, and ischemia-reperfusion injury. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CD73 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
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THERAPEUTIC COMPOUNDS (Fri, 16 Jun 2017)
The invention provides compounds of formula (I): and salts thereof, wherein R1, R2, R3, B, X, Y, and Z have any of the values defined herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, processes for preparing compounds of formula (I) and salts thereof, intermediates useful for preparing compounds of formula (I) and salts thereof, and therapeutic methods for treating cancer using a compound of formula (I) or a pharmaceutically acceptable salt thereof.
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INHIBITORS FOR PROLIFERATING CELL NUCLEAR ANTIGEN AND USES (Fri, 16 Jun 2017)
The present invention relates to series of compounds as an inhibitor targeting Proliferating Cell Nuclear Antigen (PCNA). Pharmaceutical compositions of those compounds and methods of using them in the treatment of cancer are within the scope of this disclosure.
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CHEMICAL COMPOUND FOR INHIBITION OF SHP2 FUNCTION AND FOR USE AS AN ANTI-CANCER AGENT (Fri, 16 Jun 2017)
This invention provides a compound that is 4,4'-(4'-Carboxy)-4-nonyloxy-[1,1'-biphenyl]-3,5-diyl)dibutanoic acid (CNBDA), derivative compounds of CNBDA, and pharmaceutical compositions thereof. The derivative compounds of CNBDA have one or more of the following substitutions (a) replacement of one or both of the carboxylic acid groups of the CNBDA compound with an organic acid group having 1-3, or 5-30, or more carbon atoms in chain length, wherein the carbon atom chains are either saturated, partially saturated, or unsaturated with respect to the carbon to carbon bonding, (b) replacement of the carboxylic groups of (a) with a phosphate, a sulphate, an amide, a hydroxyl, an aldehyde, or a halide group, and (c) replacement of the nonane group with an alkane having a carbon chain length of 1-8 or 10-30, or more carbon atoms. A method of treating a patient having cancer is provided.
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COMPOSITION OF ANTIBODY CONSTRUCT-AGONIST CONJUGATES AND METHODS OF USE THEREOF (Fri, 16 Jun 2017)
Various antibody construct compositions are disclosed. The compositions of antibody construct-immune stimulatory compound conjugates are also provided. Additionally provided are themethods of preparation and used of the antibody construct-immune stimulatory compoundconjugates. This includes methods for treating disorders, such as cancer. A genus of STING agonist compounds and method of synthesis is also disclosed.
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VESICLE CONTAINING METALLIC NANOPARTICLE AND METHOD FOR PRODUCTION THEREOF (Fri, 16 Jun 2017)
Disclosed is a method of producing a vesicle containing a metallic nanoparticle that is covalently bound to at least one hydrophilic polymer and at least one hydrophobic polymer, wherein the method involves dispersing the polymer-bound metallic nanoparticle in an organic solvent, adding an aqueous solution containing a dispersing aid to form a mixed solution, sonicating the mixed solution to form an emulsion; and removing the organic solvent from the emulsion until the vesicle forms. Using this method, the formed vesicle has a diameter of 20-150 nm, which is useful for a method of conducting photothermal therapy (PTT) for killing cells, such as cancer cells.
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LIPOPHILIC ANALOGS OF CJ-16264, METHODS OF USE, AND SYNTHESIS THEREOF (Fri, 16 Jun 2017)
In one aspect, the present disclosure provides compounds and derivatives of CJ-16,264 of the formula (I) wherein the variables are as defined herein. The application also provides compositions, methods of treatment, and methods of synthesis thereof. In some embodiments, these compounds are used in the treatment of bacterial infections or in the treatment of cancer.
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SUBSTITUTED BENZIMIDAZOLIUM, PYRIDO-IMIDAZOLIUM, OR PYRAZINO-IMIDAZOLIUM COMPOUNDS AS CHEMOTHERAPEUTICS (Fri, 16 Jun 2017)
Provided herein are compounds of the formula:(I) wherein: R1, R2, R3, R4, R5, X, A1, A2, A3, and A4 are as defined herein. In some aspects, these compounds may be used to treat cancer and other hyperproliferative disease. In some aspects, compositions, methods of treatment, and methods of synthesis are also provided herein.
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POLYMERIC DRUG DELIVERY SYSTEMS FOR TREATMENT OF DISEASE (Fri, 16 Jun 2017)
Provided are compositions and nanoparticle formulations that may be used, e.g., to deliver a therapeutic compound to a subject. In some embodiments, the nanoparticles may be used to deliver one or more chemotherapeutic agents to treat a cancer such, e.g., as a pancreatic ductal adenocarcinoma.
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FUMAGILLOL DERIVATIVES AND POLYMORPHS THEREOF (Fri, 16 Jun 2017)
The present disclosure relates to salts and polymorphs of aminoalkylfumagillol carbamates (e.g., fumagill-6-yl N-(trans-4-aminocyclohexyl)carbamate benzenesulfonic acid salt and fumagill-6-yl N-(trans-4-aminocyclohexyl)carbamate hydroxynaphthoic acid salt). The polymorphs are characterized by X-ray powder diffraction, differential scanning calorimetry, and thermogravimetric analysis, among other methods. The polymorphs and salts can be used as intermediates in the production of fumagillol derivatives (e.g., polymer-conjugated fumagillol derivatives) as well as therapeutic agents for the treatment of various diseases and conditions such as cancer.
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MODULATION OF GLOBOSERIES GLYCOSPHINGOLIPID SYNTHESIS AND CANCER BIOMARKERS (Fri, 16 Jun 2017)
The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta- 4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for disgnostic and therapeutic uses.
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Androgen receptor modulator for the treatment of prostate cancer and androgen receptor-associated diseases (Fri, 16 Jun 2017)
A hydantoin compound useful for the prevention or treatment of hyperproliferative diseases or disorders
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TREATMENT OF HOT FLUSHES, VASOMOTOR SYMPTOMS, AND NIGHT SWEATS WITH SEX STEROID PRECURSORS IN COMBINATION WITH SELECTIVE ESTROGEN RECEPTOR MODULATORS (Thu, 15 Jun 2017)
Novel methods for reduction or elimination of the incidence of hot flushes, vasomotor symptoms, and night sweats while decreasing the risk of acquiring breast, uterine or endometrial cancer and furthermore having beneficial effect by inhibiting the development of osteoporosis, hypercholesterolemia, hyperlipidemia, atherosclerosis, hypertension, insulin resistance, diabetes type 2, loss of muscle mass, adiposity, Alzheimer's disease, loss of cognition, loss of memory, or vaginal dryness in susceptible warm-blooded animals including humans involving administration of an amount of a sex steroid precursor, particularly dehydroepiandrosterone (DHEA) and an antiestrogen or a selective estrogen receptor modulator, particularly benzopyran compounds. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.
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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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PYRAZOLYL QUINOXALINE KINASE INHIBITORS (Thu, 15 Jun 2017)
The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
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1,3,4-THIADIAZOLE COMPOUNDS AND THEIR USE IN TREATING CANCER (Fri, 09 Jun 2017)
A compound of Formula (I) or a pharmaceutically acceptable salt thereof, where: Q can be 1,2,4-triazin-3-yl, pyridazin-3-yl, 6-methylpyridazin-3-yl, or 6-fluoropyridazin-3-yl; R1 can be hydrogen, methoxy, trifluoromethoxy, oxetan-3-yl, 3-fluoroazetidin-1-yl, 3-methoxyazetidin-1-yl, or 3,3- difluoroazetidin-1-yl; R2 can be hydrogen or fluoro; R3 can be hydrogen or methoxy; and R4 can be methoxy, ethoxy, or methoxymethyl; provided that when R1 is hydrogen, methoxy or trifluoromethoxy, then R3 is not hydrogen, and/or R4 is methoxymethyl. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.
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1,3,4-THIADIAZOLE COMPOUNDS AND THEIR USE IN TREATING CANCER (Fri, 09 Jun 2017)
A compound of Formula (I) or a pharmaceutically acceptable salt thereof, where: Q can be 5-methylpyridazin-3-yl, 5-chloropyridazin-3-yl, 6-methylpyridazin-3-yl, or 6-fluoropyridazin-3-yl; R can be hydrogen, fluoro, or methoxy; R1 can be hydrogen, methoxy, difluoromethoxy, or trifluoromethoxy; and R2 can be methyl or ethyl. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.
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1,3,4-THIADIAZOLE COMPOUNDS AND THEIR USE IN TREATING CANCER (Fri, 09 Jun 2017)
A compound of Formula (I) or a pharmaceutically acceptable salt thereof, is described. Q can be pyridazin-3-yl, 6- fluoropyridazin-3-yl; R1 can be H; R2 and R3 can each independently be C1-C6 alkyl, or R2 and R3 taken together are -(CH2)3; or R1 and R2 taken together can be -(CH2)2- and R3 can be -CH3; R4 halo, -CH3, -OCH3, -OCHF2, -OCF3, or -CN; and n can be 0, 1, or 2. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.
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3-PYRIMIDINYL PYRROLO [2,3-B] PYRIDINE AS NEW ANTICANCER AGENTS AND THE PROCESS FOR THE PREPARATION THEREOF (Fri, 09 Jun 2017)
The present invention relates to novel 3-pyrimidinyl pyrrolo [2,3-b] pyridine. Particularly, the present invention relates to the preparation of compounds and their anti-cancer activities. More particularly, the present invention relates to new compounds useful as modulators of cyclin-dependent kinase.
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1-CYANO-PYRROLIDINE DERIVATIVES AS INHIBITORS OF USP30. (Fri, 09 Jun 2017)
The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylatingenzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C- terminal hydrolase 30 or Ubiquitin Specific Peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and cancer. Compounds of the invention include compounds having the formula (I) (I) or a pharmaceutically acceptable salt thereof, wherein R1, R 2, R 3, m, L and X are as defined herein.
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CYCLIC PURINE DINUCLEOTIDES AS MODULATORS OF STING (Fri, 09 Jun 2017)
A compound of Formula (I) wherein Y 1, Y2, X 1, X 2, R 1, R 2, R3, R4, R5, R6, R8, and R9 are as defined herein; and pharmaceutically acceptable salts and tautomers thereof, 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, in the treatment of diseases in which modulation of STING (Stimulator of Interferon Genes) is beneficial, for example inflammation, allergic and autoimmune diseases, infectious diseases, cancer, pre-cancerous syndromes and as vaccine adjuvants.
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SALTS OF CONJUGATES FOR CANCER THERAPY (Fri, 09 Jun 2017)
The present invention relates to pharmaceutically acceptable salts of conjugates comprising a chemotherapeutic drug and an amino acid or a derivative thereof, which are readily taken up by a target cell and reduce side effects induced by the chemotherapeutic drug. In particular, the present invention relates to pharmaceutically acceptable salts of conjugates comprising cytidine analog drugs and aspartic or glutamic acid and analogs thereof, pharmaceutical compositions comprising these conjugates and use thereof for the treatment of cancer or a pre-cancer condition or disorder.
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ARYL ACYLSULFONAMIDES AS BLT1 ANTAGONISTS (Fri, 09 Jun 2017)
Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatohepatitis, metabolic syndrome, atherosclerosis, and cancer.
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ARYL ACYLSULFONAMIDES AS BLT1 ANTAGONISTS (Fri, 09 Jun 2017)
Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatohepatitis, metabolic syndrome, atherosclerosis, and cancer.
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ARYL SULFONAMIDES AS BLT1 ANTAGONISTS (Fri, 09 Jun 2017)
Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatohepatitis, metabolic syndrome, atherosclerosis, and cancer.
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ARYL SULFONAMIDES AS BLT1 ANTAGONISTS (Fri, 09 Jun 2017)
Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatohepatitis, metabolic syndrome, atherosclerosis, and cancer.
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COMPOSITIONS AND METHODS FOR MODULATING CANCER CELL METABOLISM (Fri, 09 Jun 2017)
Compositions typically including a modulator of cancer cell metabolism and a cancer cell- or a glucose-depleted and/or lactate-rich disease environment targeting moiety, wherein the targeting moiety is associated with, linked, conjugated, or otherwise attached directly or indirectly to the modulator, or to a nanoparticle or other delivery vehicle thereof, and methods of use for treating cancer are provided. Pharmaceutical compositions including the modulator and a pharmaceutically acceptable carrier are also provided. The pharmaceutical compositions can be administered to a subject in need thereof in an effective amount to reduce one or symptoms of the cancer. Such pharmaceutical compositions can be administered prior to or in conjunction with an immune therapy such as adoptive T cell therapy. In an embodiment, PLGA-PEG nanoparticles, which are targeted to the mitochondria by a lipophilic triphenylphosphonium (TPP) cation and which contain a modulator of cancer cell metabolism, are used.
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COMPOUNDS FOR TREATING PROLIFERATIVE DISEASES (Fri, 09 Jun 2017)
The present disclosure provides compounds of Formula (I). The compounds described herein may be useful in treating and/or preventing proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.
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CYCLING THERAPY USING 3-(5-AMINO-2-METHYL-4-OXO-4H-QUINAZOLIN-3-YL)-PIPERIDINE-2,6-DIONE (Fri, 09 Jun 2017)
Provided herein are methods of treating, preventing and/or managing cancer, including lymphoma, which comprise administering to a patient 3-(5-amino-2-methyl-4- oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione, or an enantiomer or a mixture of enantiomers thereof, or a pharmaceutically acceptable salt, solvate, hydrate, co-crystal, clathrate, or polymorph thereof in a cyclic therapy regimen.
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MULTIVALENT RAS BINDING COMPOUNDS (Fri, 09 Jun 2017)
Described herein are compounds that modulate Ras signaling, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with altered Ras signaling. Further described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds and methods of using such compounds in the treatment of cell proliferative disorders, including cancer.
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MICELLES AND METHODS (Fri, 09 Jun 2017)
The present invention relates to micelle drug carriers and methods of using the micelles to deliver drugs to target cells. The micelles are useful, for example, for carrying and targeting drugs for the treatment of cancer to cancer cells. As one example, the disclosure provides pegylated octadecyl lithocholate micelles that are labeled with a peptide ligand for colorectal neoplasia and that carry the small molecule mTOR inhibitor rapamycin to colorectal cancer cells.
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THIENO-PYRIMIDINE DERIVATIVES AND USES THEREOF (Fri, 09 Jun 2017)
Compounds having the general formula I or III,and pharmaceutical compositions comprising the same. The compounds of the present invention are useful as selective mutant epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitor, and for the treatment of EGFR related diseases and disorders such as cancer.
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HETEROCYCLE COMPOUNDS AND USES THEREOF (Fri, 09 Jun 2017)
Compounds having the general formula (I) and pharmaceutical compositions that can be used as Bruton's Tyrosine Kinase (BTK), ITK, JAK3, and selective mutant epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitor and their uses in the treatment of related diseases and disorders such as cancer.
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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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SLC45A2 PEPTIDES FOR IMMUNOTHERAPY (Fri, 09 Jun 2017)
Provided are SLC45A2 peptides that bind to MHC I (HLA-A2) on melanoma cells or other antigen-presenting cells and are recognized by T-cell receptors on T cells. The SLC45 A2 peptides may be therapeutically used to treat a cancer, such as a cutaneous melanoma, uveal melanoma, a mucosal melanoma, or a metastatic melanoma. Methods for expanding a population of T cells that target SLC45A2 are also provided.
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CONJUGATES OF QUATERNIZED TUBULYSIN COMPOUNDS (Fri, 09 Jun 2017)
Compounds and compositions are disclosed in which a quaternized drug unit is linked to a targeting ligand unit from which a tertiary amine-containing drug is released at the targeted site of action. Methods for treating diseases characterized by the targeted abnormal cells, such as cancer or an autoimmune disease using the compounds and compositions of the invention are also disclosed.
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METHODS FOR TREATING CANCER USING RSPO3 ANTAGONISTS (Fri, 09 Jun 2017)
The present invention provides compositions for identifying tumors likely to respond to treatment with an RSPO3 antagonist (e.g., anti-RSPO3 antibody). Also provided are methods for identifying tumors and/or patients that are likely to be responsive or non-responsive to treatment with an RSPO3 antagonist (e.g., anti-RSPO3 antibody). Methods for treating a patient with cancer are provided, wherein the cancer is predicted to respond to an RSPO3 antagonist (e.g., anti-RSPO3 antibody).
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USE OF SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINES (Fri, 09 Jun 2017)
The present invention relates to: - use of a 2,3-dihydroimidazo[1,2-c]quinazoline compound, or of a pharmaceutical composition containing same, as a sole active agent, or of a combination of a) said compound or a pharmaceutical composition containing said compound and b) one or more further active agents, for the preparation of a medicament for the treatment or prophylaxis of cancer
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18F-saccharide-folates (Fri, 09 Jun 2017)
The present invention is directed towards new 18F-folate radiopharmaceuticals, wherein the 18F isotope is linked via a prosthetic group, more specifically via a prosthetic group having a saccharide group, such as acyclic mono-or oligosaccharide, preferably based on a pyranoside or furanoside, which is covalently linked to the glutamate portion of a folate or derivative thereof. The invention is also directed towards the method of preparation of said radiopharmaceuticals, as well as their use in diagnosis and monitoring of cancer and inflammatory and autoimmune diseases and therapy.
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STABILIZED ALPHA HELICAL PEPTIDES AND USES THEREOF (Fri, 09 Jun 2017)
Novel polypeptides and methods of making and using the same are described herein. The polypeptides include cross-linking ("hydrocarbon stapling") moieties to provide a tether between two amino acid moieties, which constrains the secondary structure of the polypeptide. The polypeptides described herein can be used to treat diseases characterized by excessive or inadequate cellular death.
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Crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo(1,5-a)pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate (Fri, 09 Jun 2017)
A novel crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.
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Fused 1,3-azole derivatives useful for the treatment of proliferative diseases (Fri, 09 Jun 2017)
The present disclosure provides compounds of Formula (I-a), Formula (I), and Formula (II),. The compounds described herein may be Myc modulators (<i>e.g</i>., Myc inhibitors) and may be useful in treating in a subject in need thereof diseases associated with Myc and proliferative diseases (<i>e.g</i>., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including a compound described herein. (Formulae (I-a), (I), (II))
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Combination therapy for treatment of cancer (Fri, 09 Jun 2017)
Described herein are combination therapies for the treatment of cancer and other diseases. In one aspect, the methods described herein for the treatment of cancer and other diseases comprise administering a RSPO-LGR pathway inhibitor in combination with a mitotic inhibitor. The present invention relates to methods of treating cancer comprising administering to a subject a therapeutically effective amount of an RSPO-LGR pathway inhibitor, such as an antiRSP03 antibody or anti-LGR5 antibody. In certain embodiments, the methods further comprise administration of a mitotic inhibitor to the patient. In certain embodiments the RSPO-LGR pathway inhibitor is administered about 1 day, about 2 days, or about 3 days prior to the mitotic inhibitor.
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SUBSTITUTED TRICYCLIC COMPOUNDS AS FGFR INHIBITORS (Thu, 08 Jun 2017)
The present invention relates to tricyclic compounds of formula (I), and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.
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GLYCOLIPIDS AS TREATMENT FOR DISEASE (Thu, 08 Jun 2017)
This invention provides compounds, compositions, and methods for treating a disorder selected from cancer, hyperinsulinemia, hypoglycemia, hyperinsulinemia with hypoglycemia, atypical Parkinson's disease, Huntington's disease, mutliple systems atrophy, GM3 synthase deficiency, GM2 synthase deficiency or tauopathy.
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INDOLIZINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM (Fri, 02 Jun 2017)
<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="51.90mm" wi="68.50mm" file="US20170151251A1-20170601-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R<sub>a</sub>, R<sub>b</sub>, R<sub>c</sub>, R<sub>d</sub>, R<sub>1</sub>, R<sub>2</sub>, R<sub>3</sub>, R<sub>4</sub>, R<sub>5</sub>, X, Y and Het are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.</p>
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METHOD OF TREATING NON-SMALL CELL LUNG CANCER AND/OR SMALL CELL LUNG CANCER USING THIENOTRIAZOLODIAZEPINE COMPOUNDS (Fri, 02 Jun 2017)
<p id="p-0001" num="0000">A method of treating non-small cell lung cancer and/or small cell lung cancer in a mammal comprises the step of administering to a patient a pharmaceutical acceptable amount of a compound being a thienotriazolodiazepine compound of the Formula (1).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="48.94mm" wi="57.07mm" file="US20170151255A1-20170601-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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FUNCTIONALISED AND SUBSTITUTED INDOLES AS ANTI-CANCER AGENTS (Fri, 02 Jun 2017)
<p id="p-0001" num="0000">The present invention relates to anti-tropomyosin compounds, processes for their preparation, and methods for treating or preventing a disease or disorder, such as a proliferative disease (preferably cancer), using compounds of the invention.</p>
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NITROGEN-CONTAINING AROMATIC HETEROCYCLIC COMPOUND (Fri, 02 Jun 2017)
<p id="p-0001" num="0000">As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen-containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.</p>
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COMPOUND OF GLYCOSAMINOGLYCAN AND ITS FABRICATION METHOD AS WELL AS APPLICATION (Fri, 02 Jun 2017)
<p id="p-0001" num="0000">The present invention is related to a compound conjugating a drug with a glycosaminoglycan, such as hyaluronic acid (HA), where the drug is useful for the treatment of diseases such as inflammation, auto-immune disease, allergy, infection and preferably cancer. The conjugated compound of the present invention can increase the concentration of drug at the specific site of disease by an interaction of the glycosaminoglycan used as target drug delivery carrier and the CD44 cell surface receptor, then enhancing the therapeutic efficacy and reducing the systemic side effect of the site-delivered drug.</p>
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TARGETED CONJUGATES AND PARTICLES AND FORMULATIONS THEREOF (Fri, 02 Jun 2017)
<p id="p-0001" num="0000">Particles, including nanoparticles and microparticles, and pharmaceutical formulations thereof, comprising conjugates of an active agent such as a therapeutic, prophylactic, or diagnostic agent attached to a targeting moiety via a linker have been designed which can provide improved temporospatial delivery of the active agent and/or improved biodistribution. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or infectious diseases.</p>
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COT MODULATORS AND METHODS OF USE THEREOF (Fri, 02 Jun 2017)
<p id="p-0001" num="0000">The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.</p>
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bis-Pyridazine Compounds and Their Use in Treating Cancer (Fri, 02 Jun 2017)
<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="23.71mm" wi="72.81mm" file="US20170152244A1-20170601-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or a pharmaceutically acceptable salt thereof, where R<sup>1 </sup>can be hydro, methoxy, difluoromethoxy or trifluoromethoxy; R<sup>2 </sup>can be hydro, methoxy, trifluoromethoxy or trifluoromethyl; and R<sup>3 </sup>can be hydro or methoxy. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.</p>
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Methods for the Treatment of HER2 Amplified Cancer (Fri, 02 Jun 2017)
<p id="p-0001" num="0000">Described herein are methods and compositions for treating HER2-amplified cancer. The methods include administering to an individual in need thereof ibrutinib.</p>
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HSP90 INHIBITORS (Fri, 02 Jun 2017)
<p id="p-0001" num="0000">The disclosure relates to Compounds of Formula (1):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.40mm" wi="67.65mm" file="US20170151247A1-20170601-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and pharmaceutically acceptable salts thereof wherein Z<sub>1</sub>, Z<sub>2</sub>, Z<sub>3</sub>, Xa, Xb, Xc, Y, X<sub>2</sub>, and X<sub>4 </sub>are as defined herein, compositions comprising an effective amount of a Compound of Formula (1) or a pharmaceutically acceptable salt thereof, and methods to treat or prevent a condition, such as cancer which overexpresses Her-kinases, comprising administering to an patient in need thereof a therapeutically effective amount of a Compound of Formula (1) or a pharmaceutically acceptable salt thereof.</p>
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TARGETED RADIOLABELED COMPOUNDS AND THEIR USE FOR THE TREATMENT AND DIAGNOSIS OF CANCER (Fri, 02 Jun 2017)
<p id="p-0001" num="0000">Method of using androgen receptor and/or butyrylcholinesterase targeted radiolabeled compounds, e.g., cycloSalingenyl pyrimidine nucleoside monophosphates, for the treatment and diagnosis of cancer.</p>
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METHOD FOR CULTURE OF HUMAN BLADDER CELL LINES AND ORGANOIDS AND USES THEREOF (Fri, 02 Jun 2017)
<p id="p-0001" num="0000">The invention discloses a methodology for the culture of bladder cell lines and organoids from human bladder, both non-cancerous as well as cancer tissue.</p>
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1,3,4-Thiadiazole Compounds and Their Use in Treating Cancer (Fri, 02 Jun 2017)
<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="40.64mm" wi="68.41mm" file="US20170152254A1-20170601-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">or a pharmaceutically acceptable salt thereof, where: Q can be 5-methylpyridazin-3-yl, 5-chloropyridazin-3-yl, 6-methylpyridazin-3-yl, or 6-fluoropyridazin-3-yl; R can be hydrogen, fluoro, or methoxy; R<sup>1 </sup>can be hydrogen, methoxy, difluoromethoxy, or trifluoromethoxy; and R<sup>2 </sup>can be methyl or ethyl. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.</li> </ul> </li> </ul> </p>
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1,3,4-Thiadiazole Compounds and Their Use in Treating Cancer (Fri, 02 Jun 2017)
<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="41.15mm" wi="68.41mm" file="US20170152255A1-20170601-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or a pharmaceutically acceptable salt thereof, where: Q can be 1,2,4-triazin-3-yl, pyridazin-3-yl, 6-methylpyridazin-3-yl, or 6-fluoropyridazin-3-yl; R<sup>1 </sup>can be hydrogen, methoxy, trifluoromethoxy, oxetan-3-yl, 3-fluoroazetidin-1-yl, 3-methoxyazetidin-1-yl, or 3,3-difluoroazetidin-1-yl; R<sup>2 </sup>can be hydrogen or fluoro; R<sup>3 </sup>can be hydrogen or methoxy; and R<sup>4 </sup>can be methoxy, ethoxy, or methoxymethyl; provided that when R<sup>1 </sup>is hydrogen, methoxy or trifluoromethoxy, then R<sup>3 </sup>is not hydrogen, and/or R<sup>4 </sup>is methoxymethyl. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.</p>
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PHENANTHROINDOLIZIDINE AND PHENANTHROQUINOLIZIDINE ALKALOID HAVING A HYDROXYL GROUP ON THE PHENANTHRENE RING THEREOF, PREPARATION METHOD AND USE THEREOF (Fri, 02 Jun 2017)
<p id="p-0001" num="0000">A phenanthroindolizidine and phenanthroquinolizidine alkaloid having a hydroxyl group on the phenanthrene ring thereof was synthesized, which exhibits potent activity as an anticancer agent against, such as breast cancer, lung cancer, and prostate cancer.</p>
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STAT3 INHIBITOR (Fri, 02 Jun 2017)
<p id="p-0001" num="0000">Provided are STAT3 inhibitors and methods of treating inflammation or a hyperproliferative disease such as, e.g., cancer. In some aspects, compounds may be used to treat breast cancer, a head/neck cancer, a lung cancer, a prostate cancer, or pancreatic cancer.</p>
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MICROBUBBLE-CHEMOTHERAPEUTIC AGENT COMPLEX FOR SONODYNAMIC THERAPY (Fri, 02 Jun 2017)
The invention relates to methods of sonodynamic therapy comprising the co-administration of a microbubble-chemotherapeutic agent complex together with a microbubble-sonosensitiser complex. It further relates to pharmaceutical compositions comprising these complexes and their use in methods of sonodynamic therapy and/or sonodynamic diagnosis. Such methods find particular use in the treatment of cancer, e.g. pancreatic cancer.
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CD39 VASCULAR ISOFORM TARGETING AGENTS (Fri, 02 Jun 2017)
The present disclosure relates to antigen-binding compounds that inhibit CD39. The disclosure also relates to cells producing such compounds; methods of making such compounds, and antibodies, fragments, variants, and derivatives thereof; pharmaceutical compositions comprising the same; methods of using the compounds to diagnose, treat or prevent diseases, e.g. cancer.
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BIS-PYRIDAZINE COMPOUNDS AND THEIR USE IN TREATING CANCER (Fri, 02 Jun 2017)
A compound of Formula (I) or a pharmaceutically acceptable salt thereof, where R1 can be hydro, methoxy, difluoromethoxy or trifluoromethoxy; R2 can be hydro, methoxy, trifluoromethoxy or trifluoromethyl; and R3 can be hydro or methoxy. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.
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INHIBITORS OF PI3 KINASES (Fri, 02 Jun 2017)
The present invention is directed to the compounds of Formula (I) or isomers, stereoisomers, tautomers, pharmaceutically acceptable salts, isotopes, solvates, metabolites, polymorphs or prodrugs thereof, wherein R1, R2, R3, R4, /A, B, L1, L2, Z, n and X are herein defined as inhibitors of PI3K. These compounds are used for the preventive and/or therapeutic treatment of diseases or disorders associated with abnormal activities of PI3K's such as Inflammation, Cancer, Restenosis, Atherosclerosis, Psoriasis, Thrombosis, immmuno-oncology, renal carcinoma, hepatitis C, haematological malignancies, and multiple myeloma.
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ENHANCED CANCER IMMUNOTHERAPY USING ANTIBODY-INTERFERON FUSION MOLECULES (Fri, 02 Jun 2017)
The present invention relates to fusion molecules designed to improve the efficacy of cancer immunotherapy, comprising one or more IFN molecules attached to an antibody which specifically binds to an immune-checkpoint protein antigen. The fusion molecules of the present invention may be administered alone, or in combination with other non- fused immune-checkpoint protein antigen inhibitors or targeted immunotherapies to treat patients that initially failed to respond to previous anti-cancer therapy.
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PLATINUM ANTICANCER AGENTS (Fri, 02 Jun 2017)
Disclosed herein, inter alia, are platinum-based compounds useful for treating cancer.
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BIVALENT BROMODOMAIN INHIBTORS AND USES THEREOF (Fri, 02 Jun 2017)
The present invention provides bivalent inhibitors of BET bromodomains, such as compounds of Formulae (I), (II), (III), (IV), (V) and (VI). Some bromdomain-containing proteins (e.g., BRD4) have a tandem bromodomain primary structure comprising more than one bromodomain binding site (e.g., BRD4 comprises BDl and BD2). Bivalent inhibitors of BET bromodomains provided herein can target bromodomains through advantageous multivalent interactions, and can therefore can be to treat diseases or conditions associated with bromodomain-containing proteins. The present also provides pharmaceutical compositions and kits comprising the inventive compounds, as well as methods of using the inventive compounds.
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DRUG FORMULATIONS FOR CANCER TREATMENT (Fri, 02 Jun 2017)
Compounds and pharmaceutical formulations containing these compounds are described. Also described are methods of making and using the compounds. The compounds include nucleobases, nucleobase analogues, or combinations thereof. In one embodiment, a nucleobase analogue is combined with doxorubicin and encapsulated within a liposome for use in inhibiting or preventing the growth of cancer cells. Further described are pharmaceutical compositions containing two or more therapeutically active agents encapsulated within a vesicle, such as a liposome, wherein the molar ratio of the agents provides a synergistic therapeutic effect.
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Novel Methods for Targeting Cancer Stem Cells (Fri, 02 Jun 2017)
The invention provides naphthofuran compounds, polymorphs of naphthofuran compounds, naphthofuran compounds in particle form, purified compositions that contain one or more naphthofuran compounds, purified compositions that contain one or more naphthofuran compounds in particle form, methods of producing these naphthofuran compounds, polymorphs, purified compositions and/or particle forms, and methods of using these naphthofuran compounds, polymorphs, purified compositions and/or particle forms to treat subjects in need thereof.
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PHARMACEUTICAL COMPOSITIONS COMPRISING POH DERIVATIVES (Thu, 01 Jun 2017)
The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene (or sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.
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HETEROCYCLIC COMPOUNDS AND USES AS ANTICANCER AGENTS (Thu, 01 Jun 2017)
Novel compounds having a fused bicyclic heteroaromatic ring system substituted with a heteroaryl five-membered ring are disclosed. The compounds inhibit growth of a variety of types of cancer cells, and are thus useful for treating cancer. Efficacy of these compounds is demonstrated with a system for monitoring cell growth/migration, which shows they are potent inhibitors of growth and/or migration of cancer cells. In addition, compounds of the invention were shown to stop growth of tumors in vivo, and to reduce the size of tumors in vivo. Compositions comprising these compounds, and methods to use these compounds and compositions for treatment of cancers, are disclosed.
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ACTIVATORS OF HUMAN PYRUVATE KINASE (Thu, 01 Jun 2017)
Disclosed are pyruvate kinase M2 activators, which are, bis sulfonamide piperazinyl compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and R 1 to R 16 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia,
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NEW MOLECULES FROM SEAWEEDS WITH ANTI-CANCER ACTIVITY (Sat, 27 May 2017)
The present invention provides purified compounds extracted from seaweeds having the formula (I): wherein R1 and R2 is each independently H or a fatty acid and their use for inhibiting the growth of cancer cells.
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QUINOLONE CHALCONE COMPOUNDS AND USES THEREOF (Sat, 27 May 2017)
The present disclosure relates to novel compounds, compositions comprising these compounds, and their use, for example for the treatment of cancer. In particular, the present disclosure includes compounds of Formula (I), and compositions and uses thereof.
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NOVEL COMPOUNDS AS INHIBITORS OF DNA METHYLTRANSFERASES (Sat, 27 May 2017)
It relates to the compounds of formula (I), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures thereof, wherein A, R1, R2, and R3 are as defined herein, which are inhibitors of one or more DNMTs selected from the group consisting of DNMT1, DNMT3A and DNMT3B. It also relates to pharmaceutical or veterinary compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of cancer, fibrosis and/or immunomodulation.
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(R)- AND (S)-1-(3-(3-N,N-DIMETHYLAMINOCARBONYL)PHENOXYL-4-NITROPHENYL)-1-ETHYL-N,N'-BIS (ETHYLENE)PHOSPHORAMIDATE, COMPOSITIONS AND METHODS FOR THEIR USE AND PREPARATION (Sat, 27 May 2017)
Provided herein are optically active compounds of the formulae (ii); and (III) and pharmaceutical compositions thereof. Also provided herein are processes of making these compounds and resolving the racemic mixture or the enrichment of same with in one of its enantiomers to provide (R)- and (S)-1-(3-(3-N,N-dimethylaminocarbonyl)phenoxyl-4-nitrophenyl)-1-ethyl-N,N'-bis(ethylene)phosphoramidate, and methods of treating cancer comprising administering such compounds.
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2-SUBSTITUTED QUINAZOLINE COMPOUNDS COMPRISING A SUBSTITUTED HETEROCYCLIC GROUP AND METHODS OF USE THEREOF (Sat, 27 May 2017)
Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): (I) or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R1, R2a, R2b, R2c, R3a, R3b, R4a, R4b, R5a, R5b, R6, A, G1, G2, L1, L2, m1, m2, n, X and E are as defined herein, and wherein at least one of R3a, R3b, R4a or R4b is not H. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
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PD-L1-BINDING AGENTS AND USES THEREOF (Sat, 27 May 2017)
Agents that specifically bind PD-L1 are disclosed. The PD-L1-binding agents may include polypeptides, antibodies, bispecific agents, homodimeric molecules, and/or heterodimeric molecules. Also disclosed are methods of using the agents for enhancing the immune response and/or treatment of diseases such as cancer.
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A SOLID STATE FORM OF PLADIENOLIDE PYRIDINE COMPOUNDS AND METHODS OF USE (Sat, 27 May 2017)
The present disclosure provides a novel solid state form of pladienolide pyridine compounds, compositions comprising at least one such solid state form, and methods of preparation and use and the same. The novel solid state form of pladienolide pyridine compounds may be useful in the treatment of cancer, such as, for example, cancers in which agents that target the spliceosome and mutations therein are known to be useful.
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ANTIBODIES AGAINST GLUCOCORTICOID-INDUCED TUMOR NECROSIS FACTOR RECEPTOR (GITR) AND USES THEREOF (Sat, 27 May 2017)
Provided herein are antibodies, or antigen binding portions thereof, that bind to glucocorticoid-inducible TNF receptor (GITR). Also provided are uses of these proteins in therapeutic applications, such as in the treatment of cancer. Further provided are cells that produce the antibodies, polynucleotides encoding the heavy and/or light chain variable region of the antibodies, and vectors comprising the polynucleotides encoding the heavy and/or light chain variable region of the antibodies.
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DUAL SRC/P38 KINASE INHIBITOR COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS (Sat, 27 May 2017)
Dual Src/p38 kinase inhibitor compounds and compositions comprising the same are disclosed. Methods of using the compounds in the treatment of hyperproliferative disease such as cancer are also disclosed.
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BIOCOMPATIBLE PARTICLES AND METHODS OF MAKING AND USE THEREOF (Sat, 27 May 2017)
Biocompatible particles comprising a metallic core and a plurality of drug-loading ligands coordinated to the metallic core are described. The metallic core can, for example, have a melting point of 100°C or less. The biocompatible particles can, in some examples, further comprise a therapeutically effective amount of a drug coordinated to the plurality of drug-loading ligands. In some examples, the biocompatible particles can further comprise a plurality of targeting ligands coordinated to the metallic core. Also disclosed herein are methods of making the biocompatible particles described herein, for example using sonication. Also disclosed herein are methods of treating cancer in a subject comprising administering to the subject a therapeutically effective amount of the biocompatible particles or compositions disclosed herein.
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ANTIBODIES AGAINST GLUCOCORTICOID-INDUCED TUMOR NECROSIS FACTOR RECEPTOR (GITR) AND USES THEREOF (Fri, 26 May 2017)
<p id="p-0001" num="0000">Provided herein are antibodies, or antigen binding portions thereof, that bind to glucocorticoid-inducible TNF receptor (GITR). Also provided are uses of these proteins in therapeutic applications, such as in the treatment of cancer. Further provided are cells that produce antibodies, polynucleotides encoding the heavy and/or light chain variable region of the antibodies, and vectors comprising the polynucleotides encoding the heavy and/or light chain variable region of the antibodies.</p>
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DIAGNOSTIC TEST FOR EARLY STAGE CANCER (Fri, 26 May 2017)
<p id="p-0001" num="0000">Disclosed are methods of identifying tumor-derived exosomes as an early cancer diagnostic, as well as for staging, assessing progression and assessing therapy of cancer.</p>
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CRYSTALLINE FORMS AND PROCESSES FOR THE PREPARATION OF CANNABINOID RECEPTOR MODULATORS (Fri, 26 May 2017)
<p id="p-0001" num="0000">The present invention relates to crystalline forms of (1aS,5aS)-2-(4-oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid ((S)-1-hydroxymethyl-2,2-dimethyl-propyl)-amide (Compound 1) and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB<sub>2 </sub>receptor and are therefore useful in the treatment of CB<sub>2 </sub>receptor-mediated disorders, for example, osteoarthritis; pain; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation for example; atherosclerosis; undesired immune cell activity, and inflammation associated with a disorder selected from: osteoarthritis, anaphylaxis, Behcet's disease, graft rejection, vasculitis, gout, spondylitis, viral disease, bacterial disease, lupus, inflammatory bowel disease, autoimmune hepatitis, and type 1 diabetes mellitus; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis; and Parkinson's disease.</p>
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PYRIMIDINE-2,4-DIAMINE DERIVATIVE AND ANTICANCER PHARMACEUTICAL COMPOSITION COMPRISING SAME AS EFFECTIVE INGREDIENT (Fri, 26 May 2017)
<p id="p-0001" num="0000">The present invention relates to a pyrimidine-2,4-diamine derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition for prevention or treatment of cancer comprising the same as an effective ingredient. A compound according to the present invention has the good effect of inhibiting anaplastic lymphoma kinase (ALK) activity, whereby a therapeutic effect on cancer cells having an anaplastic lymphoma kinase (ALK) fusion protein such as EML4-ALK, NPM-ALK, etc. can be enhanced and it is expected that a recurrence of cancer will be effectively inhibited. As such, the compound can be effectively used in a pharmaceutical composition for prevention or treatment of cancer.</p>
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DIHYDROPTERIDINONE DERIVATIVES AND USES THEREOF (Fri, 26 May 2017)
<p id="p-0001" num="0000">The present disclosure provides compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) have been found to bind bromodomains and/or bromodomain-containing proteins (e.g., bromo and extra terminal (BET) proteins). Also provided are methods, uses, and kits of the compounds and pharmaceutical compositions for inhibiting the activity (e.g., increased activity) of bromodomains and/or bromodomain-containing proteins and for treating and/or preventing in a subject diseases associated with bromodomains or bromodomain-containing proteins (e.g., proliferative diseases, cardiovascular diseases, viral infections, fibrotic diseases, neurological diseases, metabolic diseases, endocrine diseases, and radiation poisoning). The compounds, pharmaceutical compositions, and kits are also useful for male contraception.</p>
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KINASE INHIBITOR (Fri, 26 May 2017)
<p id="p-0001" num="0000">[Problem]</p> <p id="p-0002" num="0000">To provide a novel PIM-3 inhibitor and a novel cancer therapeutic drug, in particular, a therapeutic drug for pancreatic cancer.</p> <p id="p-0003" num="0000">[Solution]</p> <p id="p-0004" num="0000">A PIM-3 kinase inhibitor comprising a compound represented by general formula (I) or a pharmacologically acceptable salt, hydrate or solvate thereof.</p> <p id="p-0005" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="37.34mm" wi="69.85mm" file="US20170145005A1-20170525-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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METHODS AND COMPOSITIONS OF MOLECULAR PROFILING FOR DISEASE DIAGNOSTICS (Fri, 26 May 2017)
<p id="p-0001" num="0000">The present invention relates to compositions, kits, and methods for molecular profiling and cancer diagnostics, including but not limited to gene expression product markers, alternative exon usage markers, and DNA polymorphisms associated with cancer. In particular, the present invention provides molecular profiles associated with thyroid cancer, methods of determining molecular profiles, and methods of analyzing results to provide a diagnosis.</p>
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MARMELIN ANALOGS AND METHODS OF USE IN CANCER TREATMENT (Fri, 26 May 2017)
<p id="p-0001" num="0000">A pharmaceutical composition can include: a marmelin analog compound, and a pharmaceutically acceptable carrier having the compound. The compound can be present in a therapeutically effective amount to treat or inhibit a disease state. The disease state can be cancer. The cancer can be selected from brain cancers, head and neck cancers, thyroid cancers, gastrointestinal cancers, esophageal cancers, stomach cancers, pancreatic cancers, liver cancers, colo-rectal cancers, lung cancers, kidney cancers, prostate cancers, bladder cancers, testicular cancers, breast cancers, ovarian cancers, cervical cancers, and melanomas. The carrier includes a cyclodextrin, which may form a complex with the compound. The compounds and compositions can be used to treat or inhibit progression of cancers. Colorectal, bladder, and prostate cancers are examples of some of the cancers that can be treated with the marmelin analog compounds.</p>
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HETEROCYCLIC INHIBITORS OF THE SODIUM CHANNEL (Fri, 26 May 2017)
<p id="p-0001" num="0000">The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns heterocyclic compounds (e.g., compounds according to any of Formulas (1)-(11 1) or Compounds (1)-(65) of Table 1) that are that are useful in treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's Disease, mood disorders, schizophrenia, psychosis, tinnitus, amyotropic lateral sclerosis, glaucoma, ischaemia, spasticity disorders, obsessive compulsive disorder, restless leg syndrome and Tourette syndrome.</p>
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LIN28/LET-7 CRYSTAL STRUCTURES, PURIFICATION PROTOCOLS, AND MOLECULAR PROBES SUITABLE FOR SCREENING ASSAYS AND THERAPEUTICS (Fri, 26 May 2017)
<p id="p-0001" num="0000">The invention provides compositions and methods for regulating microRNA (miRNA) biogenesis. The invention also relates to compositions and methods for treating or preventing cancer in a subject in need thereof.</p>
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Algorithms for Disease Diagnostics (Fri, 26 May 2017)
<p id="p-0001" num="0000">The present invention relates to compositions and methods for molecular profiling and diagnostics for genetic disorders and cancer, including but not limited to gene expression product markers associated with cancer or genetic disorders. In particular, the present invention provides algorithms and methods of classifying cancer, for example, thyroid cancer, methods of determining molecular profiles, and methods of analyzing results to provide a diagnosis.</p>
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IMMUNOREGULATORY AGENTS (Fri, 26 May 2017)
<p id="p-0001" num="0000">Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.</p>
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PHOSPHATE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM (Fri, 26 May 2017)
<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="52.07mm" wi="69.85mm" file="US20170143746A1-20170525-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein X, Y, A<sub>1</sub>, A<sub>2</sub>, R<sub>a</sub>, R<sub>b</sub>, R<sub>c</sub>, R<sub>d</sub>, R<sub>3</sub>, R<sub>4</sub>, T and R<sub>5 </sub>are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.</p>
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ANTI-TUMOR PHARMACEUTICAL APPLICATION OF PENTACYCLIC TRITERPENE SAPONIN COMPOUNDS OF SZECHUAN MELANDIUM ROOT (Fri, 26 May 2017)
<p id="p-0001" num="0000">The invention provides compounds of structural formula I or a salt thereof, and total saponins comprising such compounds in the preparation of anti-tumor agents. The present study of this invention showed that the compounds of formula I and the related total saponins had strong inhibitory effects on the proliferation of several human tumor cell lines, such as hepatocarcinoma, gastric cancer, colon cancer, breast cancer and melanoma cell lines, also the combination of structural formula I and the chemical agents could fairly well reduce toxicity and increase treatment effects.</p>
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IMMUNE REGULATORY OLIGONUCLEOTIDE (IRO) COMPOUNDS TO MODULATE TOLL-LIKE RECEPTOR BASED IMMUNE RESPONSE (Fri, 26 May 2017)
<p id="p-0001" num="0000">The invention provides novel immune regulatory oligonucleotides (IRO) as antagonist of TLRs and methods of use thereof. These IROs have unique sequences that inhibit or suppress TLR-mediated signaling in response to a TLR ligand or TLR agonist. The methods may have use in the prevention and treatment of cancer, an autoimmune disorder, airway inflammation, inflammatory disorders, infectious disease, skin disorders, allergy, asthma or a disease caused by a pathogen.</p>
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COMPOUNDS, COMPOSITIONS AND METHODS OF AGELASTATIN ALKALOIDS (Fri, 26 May 2017)
<p id="p-0001" num="0000">The present invention, among other things, provides compounds, compositions and methods for treatment of cancer. In some embodiments, the present invention provides methods for treating blood cancer using agelastatin alkaloids.</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, 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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Piperidinone Derivatives as MDM2 Inhibitors for the Treatment of Cancer (Fri, 26 May 2017)
<p id="p-0001" num="0000">The present invention provides MDM2 inhibitor compounds of Formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="39.88mm" wi="32.43mm" file="US20170144971A1-20170525-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 the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.</li> </ul> </li> </ul> </p>
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TRIPHENYLETHYLENE COMPOUNDS AND USES THEREOF (Fri, 26 May 2017)
<p id="p-0001" num="0000">Triphenylethylene compounds as dual aromatase inhibitors and selective estrogen receptors modulators are described. Also described are methods for treating patients of breast cancers, and patients of breast cancer comorbid with osteoporosis, using the described triphenylethylence compounds or pharmaceutical formulations thereof.</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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6-([1,2,4]TRIAZOLO[4,3-A]PYRIDIN-3-YLMETHYL)-1,6-NAPHTHYRIDIN-5(6H)-ONE DERIVATIVES AS C-MET INHIBITORS (Thu, 25 May 2017)
Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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TOFACITINIB MONO-MALATE SALT (Thu, 25 May 2017)
The present invention is directed to Tofacitinib mono-malate salt. The Tofacitinib mono-malate salt can be in amorphous form. The invention is also directed towards a pharmaceutical composition comprising Tofacitinib mono-malate and a process for preparing the composition. The Tofacitinib mono-malate salt can be used to prepare Tofacitinib mono-citrate salt. Another aspect of the invention is a process for preparing Tofacitinib mono-citrate. The Tofacitinib mono-malate salt is also useful as a medicament for the treatment of cancer.
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TOFACITINIB MONO-OXALATE SALT (Thu, 25 May 2017)
The present invention is directed to Tofacitinib mono-oxalate salt. The Tofacitinib mono-oxalate salt can be in amorphous form. The invention is also directed towards apharmaceutical composition comprising Tofacitinib mono-oxalate salt, and a process for preparing the composition. The Tofacitinib mono-oxalate salt can be used to prepare Tofacitinib mono-citrate salt. Another aspect of the invention is a process for preparing Tofacitinib mono-citrate. The Tofacitinib mono-oxalate salt is also useful as a medicament for the treatment of cancer.
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Method of treating cancer and gold(III) complexes as anti-cancer agents (Wed, 24 May 2017)
<p id="p-0001" num="0000">A method for treating cancer and gold(III) complexes with diaminocyclohexane ligand as anticancer agents. Also described are a pharmaceutical composition incorporating the gold(III) complexes and a method of synthesizing the gold(III) complexes.</p>
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THERAPEUTIC USES OF SELECTED PYRROLOPYRIMIDINE COMPOUNDS WITH ANTI-MER TYROSINE KINASE ACTIVITY (Fri, 19 May 2017)
<p id="p-0001" num="0000">Uses of pyrrolopyrimidines with anti-Mer tyrosine kinase activity as anti-infective agents, immunostimulatory and immunomodulatory agents, anti-cancer agents (including against MerTK−/− tumors and ITD and TKD mutant forms of Acute Myeloid Leukemia (AML)), and as adjunctive agents in combination with chemotherapeutic, radiation or other standard of care for neoplasms.</p>
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INHIBITORS OF LYSINE SPECIFIC DEMETHYLASE-1 (Fri, 19 May 2017)
<p id="p-0001" num="0000">The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.</p>
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PLATINUM COMPLEXES AS ANTICANCER AGENTS (Fri, 19 May 2017)
<p id="p-0001" num="0000">Novel compounds comprising a Pt(II) metal center and S-containing ligands as anticancer agents including tetrakis(1,3-diazinane-2-thione)platinum(II) chloride monohydrate complex [Pt(Diaz)<sub>4</sub>]Cl<sub>2</sub>.H<sub>2</sub>O, wherein Diaz=1,3-diazinane-2-thione. Cytotoxic evaluations reveal that the compound possesses better cytotoxic activities against MCF7 than cisplatin. Methods of treating cancer comprising administering the compound are also provided.</p>
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TARGETED THERAPEUTICS (Fri, 19 May 2017)
<p id="p-0001" num="0000">The present invention provides pharmacological compounds including a peptide epoxy ketone protease inhibitor conjugated to a binding moiety that directs the peptide epoxy ketone protease inhibitor to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and a peptide epoxy ketone protease inhibitor. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the peptide epoxy ketone protease inhibitor.</p>
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CAR BASED IMMUNOTHERAPY (Fri, 19 May 2017)
<p id="p-0001" num="0000">The disclosure provides chimeric antigen receptors (CARs), T cells comprising such CARs, nucleic acids that encode such CARS, and methods of use thereof, e.g., to treat cancer such as B cell malignancies.</p>
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DIARYLALKYLAMINE REV-ERB ANTAGONISTS AND THEIR USE AS MEDICAMENTS (Fri, 19 May 2017)
<p id="p-0001" num="0000">The present invention relates to compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.97mm" wi="54.86mm" file="US20170136009A1-20170518-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">It further discloses a pharmaceutical composition comprising the compounds of Formula (I) and their uses as anti-proliferative and proapoptotic agents for cancer therapy.</p>
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Therapeutic Combinations of a BTK Inhibitor, a PI3K Inhibitor and/or a JAK-2 Inhibitor (Fri, 19 May 2017)
<p id="p-0001" num="0000">Therapeutic combinations of a Janus kinase-2 (JAK-2) inhibitor, a Bruton's tyrosine kinase (BTK) inhibitor, and/or a phosphoinositide 3-kinase (PI3K) inhibitor, including PI3K inhibitors selective for the γ- and δ-isoforms and selective for both γ- and δ-isoforms, are described. In some embodiments, the invention provides pharmaceutical compositions comprising combinations of (1) a PI3K-δ inhibitor and a BTK inhibitor, (2) a JAK-2 inhibitor and a BTK inhibitor, or (3) a JAK-2 inhibitor, PI3K-δ inhibitor, and BTK inhibitor, and methods of using the pharmaceutical compositions for treating a disease, in particular a cancer.</p>
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COMPOSITIONS AND METHODS FOR THE PRODUCTION OF PYRIMIDINE AND PYRIDINE COMPOUNDS WITH BTK INHIBITORY ACTIVITY (Fri, 19 May 2017)
<p id="p-0001" num="0000">The present invention provides novel pyrimidine and pyridine compounds according to Formula (I), Formula (II), Formula (III), Formula (IV) and Formula (V) their manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren's disease and rheumatoid arthritis. In preferred embodiments, the present invention describes irreversible kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase.</p>
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SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF (Fri, 19 May 2017)
<p id="p-0001" num="0000">This invention provides novel 3-amino propanamide selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.</p>
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Chemokine CXCR4 and CCR5 Receptor Modulators and Uses Related Thereto (Fri, 19 May 2017)
<p id="p-0001" num="0000">The disclosure relates to chemokine receptor modulators and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising compounds disclosed herein or pharmaceutically acceptable salts or prodrugs thereof. In certain embodiments, the compositions disclosed herein are used for managing chemokine related conditions, typically prevention or treatment of viral infections such as HIV or for managing cancer.</p>
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SUBSTITUTED TRICYCLIC COMPOUNDS AS FGFR INHIBITORS (Fri, 19 May 2017)
<p id="p-0001" num="0000">The present invention relates to tricyclic compounds, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.</p>
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PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) TARGETED NANOPARTICLES FOR THERAPY OF PROSTATE CANCER (Fri, 19 May 2017)
<p id="p-0001" num="0000">The invention provides a nanoparticle composition that is decorated with a urea-based small-molecule peptidomimetic inhibitor of prostate specific membrane antigen (PSMA), which is expressed by almost all solid tumors. This strategy takes advantage of both the avidity of the functionalized nanoparticle for binding to PSMA and the ability of the nanoparticle to be retained for longer periods of time in the tumor due to enhanced leakage via EPR into the tumor interstitium and poor clearance due to underdeveloped or non-existent lymphatics within the tumor.</p>
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RIBONUCLEOTIDE REDUCTASE INHIBITORS AND METHODS OF USE (Fri, 19 May 2017)
<p id="p-0001" num="0000">Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme, as well as methods of synthesizing these novel compounds. The compounds may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases.</p>
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REGIOSELECTIVE N-2 ARYLATION OF INDAZOLES (Fri, 19 May 2017)
<p id="p-0001" num="0000">A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="41.49mm" wi="65.19mm" file="US20170137403A1-20170518-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">comprising a copper-catalyzed, carbon-nitrogen cross-coupling step. The process described as part of the present invention can be used to manufacture poly (ADP-ribose) polymerase (PARP) inhibitors, which may be useful for the treatment of cancer. In particular, the present invention describes a process for the manufacture of the PARP inhibitor, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide.</p>
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FUSED CYCLOALKYL-PYRIMIDINE COMPOUNDS AND USES THEREOF (Fri, 19 May 2017)
<p id="p-0001" num="0000">Fused cycloalkyl-pyrimidine compounds that are kinase inhibitors, such as multi-kinase inhibitors, are provided. The compounds may be used in a method of treating cancer. Pharmaceutical compositions containing a fused cycloalkyl-pyrimidine compound and a pharmaceutically acceptable carrier are also provided, as are kits containing a fused cycloalkyl-pyrimidine compound or salt thereof and instructions for use, e.g., in a method of treating cancer.</p>
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CATIONIC LIPID CORDIARIMIDE HYBRID COMPOUNDS AND A PROCESS FOR PREPARATION THEREOF (Fri, 19 May 2017)
<p id="p-0001" num="0000">The present invention relates to the cationic lipid cordiaroimide hybrid compounds of formula I. The present invention provides a process for preparation of these compounds is also being elaborated. The compounds described provides anticancerous activity against cell lines including PC-3 (prostate cancer), HepG2 (liver cancer), MCF-7 (breast cancer) and NIH-1/3T3 (non cancer cells. The compound was also capable of inducing caspase-3 mediated apoptosis in HepG2 cells by arresting the cell cycle in the G1 phase. Furthermore, the compound exhibited DNA ligase I inhibition. The present class of cationic lipid cordiarimide hybrids is likely to find specific use in developing novel targeted therapies for liver and prostate cancers.</p>
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COMPOUNDS AND THEIR METHODS OF USE (Fri, 19 May 2017)
<p id="p-0001" num="0000">Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.</p>
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SYNTHESIS OF HALICHONDRIN ANALOGS AND USES THEREOF (Fri, 19 May 2017)
<p id="p-0001" num="0000">The present invention provides halichondrin analogs, such as compounds of Formula (I). The compounds may bind to microtubule sites, thereby inhibiting microtubule dynamics. Also provided are methods of synthesis, pharmaceutical compositions, kits, methods of treatment, and uses that involve the compounds for treatment of a proliferative disease (e.g., cancer). Compounds of the present invention are particularly useful for the treatment of metastatic breast cancer, non-small cell lung cancer, prostate cancer, and sarcoma. The included methods of synthesis are useful for the preparation of compounds of Formula (I)-(III) along with naturally occurring halicondrins (e.g., halichondrin B & C, norhalichondrin A, B, & C, and homohalichondrin A, B, & C). Also included are methods for interconverting between the halichondrins, norhalichondrins, and homohalichondrins and their unnatural epimers at the C38 ketal stereocenter through the use of an acid-mediated equilibration.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="71.29mm" wi="76.20mm" file="US20170137437A1-20170518-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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FLAVAGLINE DERIVATIVES (Fri, 19 May 2017)
<p id="p-0001" num="0000">The invention relates to compounds of the following general formula (I) in the form of one of the enantiomers thereof or a mixture of the enantiomers thereof, and the pharmaceutically acceptable salts and/or solvates thereof, especially for the use thereof as a medicament, more specifically in cancer treatment. The invention also relates to pharmaceutical compositions containing same and to the methods for the production thereof.</p>
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QUINOLIZINONE DERIVATIVES AS PI3K INHIBITORS (Fri, 19 May 2017)
<p id="p-0001" num="0000">Disclosed are compounds of formula (I), their tautomeric forms, stereoisomers, and pharmaceutically acceptable salts thereof, wherein R<sup>1</sup>-R<sup>4</sup>, and n are as defined in the specification, pharmaceutical compositions including a compound, tautomer, stereoisomer, or salt thereof, and methods of treating or preventing diseases or disorders, for example, cancer, that are amenable to treatment or prevention by inhibiting the PI3K enzyme of a subject.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.26mm" wi="59.01mm" file="US20170137421A1-20170518-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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TREATMENT OF CANCERS RELATED TO CHRONICALLY ACTIVE RAS (Fri, 19 May 2017)
The present invention discloses that naphthofuranquinones and dihydroxynaphthofurans, and derivatives thereof, such as a compound of formula (I) or (II), are effective in deactivating chronically active Ras. The present invention also discloses a method of treating or preventing cancer comprising steps of: 1) identifying a patient suffering from or susceptible to a cancer related to chronically active Ras; and 2) administering a therapeutically effective amount of a compound of formula (I) or (II), or a pharmaceutically acceptable salt thereof. The present invention further discloses a method of treating or preventing cancer comprising steps of: 1) identifying a patient suffering from or susceptible to a cancer related to a K-Ras mutation; and 2) administering a therapeutically effective amount of a compound of formula (I) or (II), or a pharmaceutically acceptable salt thereof.
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TETRAHYDROPALMATINE DERIVATIVE, ITS PREPARATION METHOD AND USE (Fri, 19 May 2017)
Provided a compound of formula (I): or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and the compound is tetrahydropalmatine derivative. The compound has a use in preparation of a medicament, and the medicament is used for inhibiting proliferation of a cancer cell of a eukaryote and/or treating or preventing cancer.
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DIHYDROIMIDAZOPYRAZINONE DERIVATIVES USEFUL IN THE TREATMENT OF CANCER (Fri, 19 May 2017)
The present disclosure concerns compounds of Formula (I) or pharmaceutically-acceptable salts thereof, wherein R1, R2 and R3 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of cancer.
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DIHYDROPYRROLOPYRAZINONE DERIVATIVES USEFUL IN THE TREATMENT OF CANCER (Fri, 19 May 2017)
The invention concerns compounds of Formula (I) or pharmaceutically-acceptable salts thereof, wherein R1 has any of the meanings hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of cancer.
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GLYPICAN 2 AS A CANCER MARKER AND THERAPEUTIC TARGET (Fri, 19 May 2017)
The present disclosure is directed to antibodies binding to Glypican 2 and methods of using such antibodies to treat cancers that express or overexpress the Glypican 2 antigen.
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BIARYL COMPOUNDS AS ANTIMICROBIAL AND CHEMOTHERAPEUTIC AGENTS (Fri, 19 May 2017)
In one aspect, the present disclosure provides diaryl compounds of the formula presented herein. The application also provides compositions and methods of treatment thereof. In some embodiments, these compounds are used in the treatment of bacterial infections or in the treatment of cancer.
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Methods for Increasing Efficacy of FOLR1 Cancer Therapy (Fri, 19 May 2017)
Methods to improve the success of cancer therapies that target the human folate receptor 1 are provided. Kits comprising reagent useful in the methods are further provided.
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SUBSTITUTED 2-THIOXO-IMIDAZOLIDIN-4-ONES AND SPIRO ANALOGUES THEREOF, ACTIVE ANTI-CANCER INGREDIENT, PHARMACEUTICAL COMPOSITION, MEDICINAL PREPARATION, METHOD FOR TREATING PROSTATE CANCER (Thu, 18 May 2017)
The invention relates to novel ( R )-stereoisomers of substituted 2-thioxo-imidazolidin-4-ones of formula 1 , or spiro analogues thereof, which exhibit androgen receptor antagonist properties, variants of a method for producing the same, and intermediate compounds for producing compounds of formula 1 . Compounds of formula 1 can be used to produce a medicinal agent suitable for treating cancers, such as prostate cancer and breast cancer. The invention also relates to a pharmaceutical composition in the form of tablets, capsules, injections. In formula 1 wherein R1 is OH, NH 2 , or an OR4 group; R2 and R3 are methyl, or R2 and R3 are a CH 2 -CH 2 group; R4 is C 1 -C 4 alkyl or cyclopropyl.
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Salicylic acid derivatives, pharmaceutically acceptable salt thereof, composition thereof and method of use thereof (Wed, 17 May 2017)
<p id="p-0001" num="0000">The present invention relates to novel compounds, compositions containing same and methods for inhibiting STAT3 and/or STAT5 activity or for the treatment of a STAT3 or STAT5-dependent cancer using said compounds; or a pharmaceutically acceptable salt, solvate or prodrug thereof.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="19.30mm" wi="36.58mm" file="US09650399-20170516-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Method for treating prostate cancer and/or gastrointestinal cancer (Wed, 17 May 2017)
<p id="p-0001" num="0000">Gold(III) complexes having mixed ligands as anticancer agents. The gold(III) complexes are coordinated to bidentate ligands having diamino functional groups: a diaminocyclohexane ligand and an ethylenediamine ligand. These complexes can exist in both cis- and trans-configurations. Also described are pharmaceutical compositions incorporating the gold(I) complexes, methods of synthesis, methods of treating cancer and methods of inhibiting cancer cell proliferation and inducing cancer cell apoptosis.</p>
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Heterocycle-substituted pyridyl benzothiophenes as kinase inhibitors (Wed, 17 May 2017)
<p id="p-0001" num="0000">This invention is directed to a compound of Formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.96mm" wi="66.38mm" file="US09650366-20170516-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt thereof, wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4 </sup>and X are as defined herein. The compounds of Formula I are useful as receptor tyrosine kinase (RTK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders and metabolic diseases. </p>
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METHODS OF TREATING ANDROGEN RECEPTOR-MEDIATED DISORDERS WITH IMIDAZOLINE DERIVATIVES (Fri, 12 May 2017)
<p id="p-0001" num="0000">Methods for treating androgen receptor-mediated diseases, such as breast cancer, with imidazoline derivatives of formula (I) are provided:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.79mm" wi="67.90mm" file="US20170128422A1-20170511-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Cyclic Amine Azaheterocyclic Carboxamides (Fri, 12 May 2017)
<p id="p-0001" num="0000">The invention provides novel cyclic amine azaheterocyclic carboxamide according to Formula (I), Formula (II) and Formula (III) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.</p>
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INHIBITORS OF LYSINE SPECIFIC DEMETHYLASE-1 (Fri, 12 May 2017)
<p id="p-0001" num="0000">The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.</p>
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HETEROCYCLIC COMPOUNDS AS PI3K-y INHIBITORS (Fri, 12 May 2017)
<p id="p-0001" num="0000">This application 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="54.95mm" wi="58.59mm" file="US20170129899A1-20170511-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or pharmaceutically acceptable salts or stereoisomers thereof, which are inhibitors of PI3K-γ which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.</p>
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NEW COMPOUND FOR INHIBITING BINDING BETWEEN DX2 PROTEIN AND P14/ARF PROTEIN, AND PHARMACEUTICAL COMPOSITION FOR TREATING OR PREVENTING CANCER DISEASE CONTAINING SAME AS EFFECTIVE INGREDIENT (Fri, 12 May 2017)
<p id="p-0001" num="0000">Disclosed is a new compound that inhibits binding between a DX2 protein and a p14/ARF protein, a pharmaceutical composition including the new compound as an effective component for treating or preventing a cancer disease, an anticancer adjuvant for improving an anticancer effect of a drug-resistant anticancer drug, and a composition including an AIMP2-DX2 protein or a fragment thereof for diagnosing lung cancer.</p>
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Humanized Anti-Epiregulin Antibody, and Cancer Therapeutic Agent Comprising Said Antibody as Active Ingredient (Fri, 12 May 2017)
<p id="p-0001" num="0000">The inventors successfully produced anti-Epiregulin antibodies showing cross-species reactivity between cynomolgus monkey (non-human animals) and human, anti-Epiregulin antibodies with suppressed chemical degradation, anti-Epiregulin antibodies with lowered isoelectric point, anti-Epiregulin antibodies with increased thermal denaturation midpoint temperature, and anti-Epiregulin antibodies with reduced amount of aggregate by performing appropriate amino acid residue substitutions in the variable-region sequences of the humanized EP27 antibody which inhibits growth of cancer cells by exhibiting cytotoxic activity and neutralizing activity against human Epiregulin-expressing cells.</p>
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TUMOR SUPPRESSOR AND ONCOGENE BIOMARKERS PREDICTIVE OF ANTI-IMMUNE CHECKPOINT INHIBITOR RESPONSE (Fri, 12 May 2017)
<p id="p-0001" num="0000">The present invention is based on the identification of novel biomarkers predictive of responsiveness to anti-immune checkpoint inhibitor therapies.</p>
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Pharmaceutical Compositions and Methods (Fri, 12 May 2017)
<p id="p-0001" num="0000">This invention relates the use of cortisol blockers (e.g., glucocorticoid receptor [GR] antagonists) for the treating or preventing viral infections, treating or preventing treatment resistant prostate cancer, treating or preventing neoplasia, and treating or preventing infection related to acute or chronic injury or disease.</p>
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METHOD FOR TREATING CANCER USING CHEMOKINE ANTAGONISTS (Fri, 12 May 2017)
<p id="p-0001" num="0000">What is described is a method for treating cancer in a patient in need of such treatment through the use of an antagonist to CXCR1 and/or CXCR2 receptors by administering a therapeutically effective amount of an antagonist of CXCR1 and/or CXCR2, or pharmaceutical compositions thereof, either alone as monotherapy, or in combination with at least one other anticancer therapy.</p>
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FAP-Activated Therapeutic Agents, and Uses Related Thereto (Fri, 12 May 2017)
<p id="p-0001" num="0000">Disclosed are prodrugs of anthracyclines (such as doxorubicin) and derivatives thereof that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of “warhead” anthracycline or anthracycline derivative to FAP-expressing tissues, including cancer (e.g., solid tumors). Also provided are pharmaceutical compositions comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation, e.g., cancer, undesirable fibrosis, and undesirable inflammation.</p>
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PHARMACEUTICAL COMPOSITIONS COMPRISING POH DERIVATIVES (Fri, 12 May 2017)
<p id="p-0001" num="0000">The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene (or sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.</p>
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TARGETED THERAPEUTICS (Fri, 12 May 2017)
<p id="p-0001" num="0000">The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.</p>
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TARGETED POLYMERIC NANO-COMPLEXES AS DRUG DELIVERY SYSTEM (Fri, 12 May 2017)
<p id="p-0001" num="0000">The present invention provides targeted polymeric nano-complexes for delivery of drugs such as anti-mitotic agents or anti-cancer agents. The present invention also provides a process for the preparation of such targeted nano-complexes.</p>
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LSD1 Inhibitors (Fri, 12 May 2017)
<p id="p-0001" num="0000">The present invention relates to compounds that inhibit LSD1 activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.</p>
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Pyrazolopyrimidine Derivatives Useful as Inhibitors of Bruton's Tyrosine Kinase (Fri, 12 May 2017)
<p id="p-0001" num="0000">This invention relates to compounds of formula (I). The compounds of the invention are tyrosine kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Bruton's tyrosine kinase (BTK). The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of Bruton's tyrosine kinase, for example cancer, lymphoma, leukemia and immunological diseases.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.09mm" wi="69.68mm" file="US20170129897A1-20170511-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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NANOPARTICLES CONTAINING AZOLIUM AND N-HETEROCYCLIC CARBENE COMPOUNDS AND USE THEREOF (Fri, 12 May 2017)
<p id="p-0001" num="0000">The present application provides a composition comprising a core formed by gold nanoparticle, a compound of Formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.40mm" wi="62.82mm" file="US20170129907A1-20170511-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein dashed lines in Formula (I) represent (i) with or without an attachment of benzol group, (ii) a delocalized bond where shown within a ring; R<sub>1 </sub>is hydrogen or a halogen; R<sub>2 </sub>is a linker selected from C<sub>6-20 </sub>alkyl or polyethylene glycol; R<sub>3 </sub>is C<sub>1-20 </sub>alkyl, C<sub>1-20 </sub>substituted alkyl, hexadecanyl amido, pyridinyl, benzyl or pyrimidinyl; and a compound of Formula (II):</p> <p id="p-0004" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="66.72mm" wi="63.25mm" file="US20170129907A1-20170511-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0005" num="0000">wherein dashed lines, R<sub>1</sub>, R<sub>2 </sub>and R<sub>3 </sub>are defined as in Formula (II), and M is a metal. The composition has an inhibition ability against a cancer.</p>
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H. Pylori Lipopolysaccharide Outer Core Epitope (Fri, 12 May 2017)
<p id="p-0001" num="0000"><i>Helicobacter pylori</i>, one of the most common human pathogens, is associated with the development of human chronic gastritis, peptic ulcers and gastric cancer. The invention relates to a α1,6-glucan-containing <i>Helicobacter pylori </i>compound comprising the structure of Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.23mm" wi="76.20mm" file="US20170129941A1-20170511-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R is a α-DDHep-3-α-L-Fuc-3-β-GlcNAc trisaccharide substituted with an α1,6-glucan linked to an α1,3-DD-heptan, and wherein the last DD-Hep residue of α1,3-DD-heptan is capped with β-GlcNAc residue. Compositions comprising the compound, uses of the compound, and antibodies raised against the compound are also described.</p>
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ROR GAMMA AGONISTS AS ENHANCERS OF PROTECTIVE IMMUNITY (Fri, 12 May 2017)
The T cell specific RORgamma isoform RORgammat has been shown to be the key lineage-defining transcription factor to initiate the differentiation program of TH17 and TC17 cells, cells that have demonstrated anti-tumor efficacy, RORgammat controls gene networks that enhance immunity including increased IL17 production and decreased immune suppression. Agonists of RORgammat have been shown to increase the basal activity of RORgammat enhancing TH17 cell proliferation. Here we show that activation of RORgammat using synthetic agonists drives proliferation of TH17 cells while decreasing levels of the immune checkpoint protein PD-1, a mechanism that should enhance anti-tumor immunity while blunting tumor associated adaptive immune resistance. Interestingly, putative endogenous agonists drive proliferation of TH17 cells but do not repress PD-1. These findings suggest that synthetic agonists of RORgammat should activate Tc17/TH17 cells, decrease the population of Tregs, repress PD-1, and produce IL17 in situ, an immune factor associated with good prognosis in cancer.
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HETERO-SUBSTITUTED CYCLIC LACTONE ANALOGUES AND USES THEREOF (Fri, 12 May 2017)
The present disclosure provides SL and SL derivatives comprising a polar substituent adjacent to the lactone ring. Additionally, the present disclosure provides methods of using the SL and SL derivatives to inhibit the growth of leukemic cancer cells.
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LSD1 INHIBITORS (Fri, 12 May 2017)
The present invention relates to compounds that inhibit LSD1 activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.
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HETEROCYCLIC COMPOUNDS AS PI3K-GAMMA INHIBITORS (Fri, 12 May 2017)
This application relates to compounds of Formula (I): or pharmaceutically acceptable salts or stereoisomers thereof, which are inhibitors of PI3K-γ which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.
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1,4-DICARBONYL-PIPERIDYL DERIVATIVES (Fri, 12 May 2017)
Compounds of the formula I in which Z, W, Q, R and Y have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
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IMIDAZO[4,5-C]QUINOLIN-2-ONE COMPOUNDS AND THEIR USE IN TREATING CANCER (Fri, 12 May 2017)
The specification generally relates to compounds of Formula (I) and pharmaceutically acceptable salts thereof, where x, R1, R2, R3, R4 and R5 have any of the meanings defined herein. The specification also relates to the use of compounds of Formula (I) and salts thereof to treat or prevent ATM mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising substituted imidazo[4,5-c]quinolin-2-one compounds and pharmaceutically acceptable salts thereof; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; and intermediates useful in such manufacture.
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IMIDAZO[4,5-C]QUINOLIN-2-ONE COMPOUNDS AND THEIR USE IN TREATING CANCER (Fri, 12 May 2017)
The specification generally relates to compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, where R1, R2, R3 and R4 have any of the meanings defined herein. The specification also relates to the use of compounds of Formula (I) and salts thereof to treat or prevent ATM mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising substituted imidazo[4,5-c]quinolin-2-one compounds and pharmaceutically acceptable salts thereof; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; and intermediates useful in such manufacture.
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SELECTIVE HDAC8 INHIBITORS AND THEIR USES (Fri, 12 May 2017)
The present invention relates to small molecule compounds based on benzopyrimido- or benzoimidazo-thiazin-imine as well as their (synthesis) intermediates and their use as HDAC inhibitors, in particular HDAC8 inhibitors. The present invention also relates to the use of said compounds in the treatment of cancer and as therapeutic agents for eukaryotic parasites and respective methods of treatment.
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TETRAHYDROINDAZOLES AND MEDICAL USES THEREOF (Fri, 12 May 2017)
There is herein provided a compound of formula I (I) or a pharmaceutically acceptable salt thereof, for use in the treatment of cancer and/or the treatment or prevention of a viral infection, wherein A1, A2, L1, R1, R2 and n have meanings as provided in the description.
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THERAPY AND PHARMACEUTICAL COMPOSITION (Fri, 12 May 2017)
A novel class of compounds called perenosins, and their use in the treatment and/or prevention of cancer or a neoplastic condition.
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TARGETED THERAPEUTICS (Fri, 12 May 2017)
The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
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Nitrogen-containing aromatic heterocyclic compound (Fri, 12 May 2017)
Provided is a compound useful as a prophylactic and/or therapeutic agent for bladder cancer. As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.
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METHODS FOR THE DIAGNOSIS OF COLORECTAL CANCER AND OVARIAN CANCER HEALTH STATES (Thu, 11 May 2017)
The present invention relates to the diagnosis of colorectal and ovarian cancers (CRC and OC, respectively). The present invention describes the relationship between endogenous small molecules and CRC or OC. Specifically, the present invention relates to the diagnosis of CRC and OC through the measurement of vitamin E isoforms and related metabolites. The present invention also relates to diagnostic markers identified in said method. The present invention relates to the underlying case and pre-symptomatic phases of CRC, the diagnosis of various stages and severity of CRC, the early detection of CRC, monitoring and diagnosing the effect of therapy on CRC and OC health states.
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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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CHLOROTOXIN VARIANTS, CONJUGATES AND METHODS FOR THEIR USE (Thu, 11 May 2017)
Chlorotoxin variants, chlorotoxin variant conjugates, compositions that include the chlorotoxin variants or conjugates, and methods for using the chlorotoxin variants, conjugates, and compositions. In particular, conjugates comprising a chlorotoxin variant where lysine K15 and/or lysine K23 are substituted by other amino acids, coupled to a fluorescent label.
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SUBSTITUTED BENZENE COMPOUNDS (Thu, 11 May 2017)
The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and such compounds for use in treating cancer. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
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Combinational compositions and methods for treatment of cancer (Wed, 10 May 2017)
<p id="p-0001" num="0000">The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or a pyrroloquinolinyl-pyrrolidine-2,5-dione compound in combination with a therapeutically effective amount of a second anti-proliferative agent.</p>
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AMORPHOUS SOLID FORM OF A BET PROTEIN INHIBITOR (Fri, 05 May 2017)
<p id="p-0001" num="0000">The present invention relates to an amorphous solid form of (4S)-7-(3,5-dimethylisoxazol-4-yl)-4-pyridin-2-yl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2(1H)-one, and processes for its preparation, which is an inhibitor of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and is useful in the treatment of various diseases such as cancer.</p>
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Molecular Analysis of Tumor Samples (Fri, 05 May 2017)
<p id="p-0001" num="0000">This invention relates to methods for diagnosing cancer, e.g., cancer of epithelial origin, by detecting the presence of tumor cells in a sample, based (at least in some embodiments) on the quantification of levels of four biomarkers, MUC1, EGFR, EpCAM, and HER2. In some embodiments, the methods are performed using diagnostic magnetic resonance (DMR), e.g., with a portable relaxometer or MR imager.</p>
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SALTS OF A PIM KINASE INHIBITOR (Fri, 05 May 2017)
<p id="p-0001" num="0000">The present invention relates to salt forms of the Pim kinase inhibitor N-{(7R)-4-[(3R,4R,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, including methods of preparation thereof, and intermediates in the preparation thereof, where the compound is useful in the treatment of Pim kinase-related diseases such as cancer.</p>
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Selective androgen receptor modulators (Fri, 05 May 2017)
<p id="p-0001" num="0000">This invention provides compounds of Formula (II), or (IIa) and or salts thereof, pharmaceutical compositions comprising a compound of Formula (II), or (IIa) and a pharmaceutically acceptable excipient, processes for making compounds for Formula (II), or (IIa) and intermediates useful in the preparation of same; and methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type II diabetes related disorders or diseases, anemia, depression, and renal disease) using compounds of Formula (I), (II), or (IIa).</p>
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DIPEPTIDES AS INHIBITORS OF HUMAN IMMUNOPROTEASOMES (Fri, 05 May 2017)
<p id="p-0001" num="0000">The compounds of the present invention are represented by the following compounds having Formula (I) where the substituents R<sup>1</sup>-R<sup>10</sup>, X, Y, k, m, n, q, and s are as defined herein. These compounds are used in the treatment of cancer, immunologic disorders, autoimmune disorders, neurodegenerative disorders, or inflammatory disorders or for providing immunosuppression for transplanted organs or tissues.</p>
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ANTIBODY CONJUGATES COMPRISING TOLL-LIKE RECEPTOR AGONIST (Fri, 05 May 2017)
<p id="p-0001" num="0000">Provided herein are antibody conjugates comprising toll-like receptor agonists and the use of such conjugates for the treatment of cancer. In some embodiments, the conjugates comprise anti-HER2 antibodies.</p>
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COMPOSITIONS AND METHODS FOR CHARACTERIZING, REGULATING, DIAGNOSING, AND TREATING CANCER (Fri, 05 May 2017)
<p id="p-0001" num="0000">The present invention relates to compositions and methods for characterizing, regulating, diagnosing, and treating cancer. For example, the present invention provides compositions and methods for inhibiting tumorigenesis of certain classes of cancer cells, including breast cancer cells and preventing metastasis. The present invention also provides systems and methods for identifying compounds that regulate tumorigenesis.</p>
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DIGLYCIDIC ETHER DERIVATIVE THERAPEUTICS AND METHODS FOR THEIR USE (Fri, 05 May 2017)
<p id="p-0001" num="0000">This invention provides compound having a structure of Formula I or Formula II. Uses of such compounds for treatment of various indications, including prostrate cancer as well as methods of treatment involving such compounds are also provided.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="74.25mm" wi="69.93mm" file="US20170121261A1-20170504-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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USE OF A NOVEL 3-ARYL-4-CATECHOL-PYRROLE-N-PROPANOL COMPOUND AND THE DERIVATIVES THEREOF TO TREAT CANCER AND DISEASES RELATED TO EXCESSIVE ANGIOGENESIS (Fri, 05 May 2017)
<p id="p-0001" num="0000">The present invention relates to a 3-aryl-4 catechol-pyrrole-n-propanol compound and the derivatives thereof having General Formula (I), wherein:—R<sup>1 </sup>is an aryl group, particularly a phenyl, optionally substituted by one or more (C<sub>1</sub>-C<sub>2</sub>)alkyl groups one or more halogens, one or more —OH, —CN or CF<sub>3 </sub>groups, or a combination of same, and—R<sup>2 </sup>is a (C<sub>1</sub>-C<sub>2</sub>)alkyl group, a hydroxy(C<sub>1</sub>-C<sub>8</sub>)alkyl group, a (C<sub>1</sub>-C<sub>4</sub>)alocoxy(C<sub>1</sub>-C<sub>8</sub>)alkyl group, or a pharmaceutically acceptable hydrate or solvate of same. The invention also relates to the methods for preparing said compound and derivatives, to the pharmaceutical compositions containing same, and to the use of same as a drug or in the form of a prodrug converted via dimerization, particularly via oxidative coupling in the presence of a superoxide anion, in the treatment of cancer and diseases related to excessive angiogenesis.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.95mm" wi="69.85mm" file="US20170121283A1-20170504-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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COMPOSITIONS AND METHODS FOR INHIBITING ARGINASE ACTIVITY (Fri, 05 May 2017)
<p id="p-0001" num="0000">The invention relates to a novel class of compounds that exhibit activity inhibitory activity toward arginase, and pharmaceutical compositions comprising the compounds of the invention. Also provided herein are methods of treating cancer with the arginase inhibitors of the invention.</p>
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HISTONE ACETYLTRANSFERASE MODULATORS AND USES THEREOF (Fri, 05 May 2017)
<p id="p-0001" num="0000">The invention provides compounds and compositions comprising compounds that modulate histone acyl transferase (HAT). The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a compound that modulates HAT to a subject.</p>
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NOVEL COMPOUNDS COMPRISING A BOMBESIN DERIVATIVE, A PROCESS FOR THE PREPARATION THEREOF AND A NUCLEAR MOLECULAR IMAGING AGENT COMPRISING THE SAME (Fri, 05 May 2017)
<p id="p-0001" num="0000">Provided are a novel compound, in which a bombesin derivative known as having selectivity with respect to prostate cancer bonds with a ligand via aminomethyl galacturonic acid, a complex compound that covalently bonds with a radioactive isotope via the ligand of the novel compound, methods of preparing the compounds, and a nuclear-based molecular imaging agent including the complex compound.</p>
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A THERAPEUTIC PROTOCOL FOR TREATING OVARIAN CANCER (Fri, 05 May 2017)
<p id="p-0001" num="0000">The present invention is directed to a pharmaceutical combination for treating proliferative disease comprising a compound of formula (I), or a salt, solvate or prodrug thereof, carboplatin or cisplatin, and gemcitabine. The present invention is further directed to a therapeutic protocol to manage ovarian cancer treatment in a female subject involving the administration of the combination to an ovarian cancer subject with recurrent or persistent ovarian cancer following treatment with platinum-based therapy. Kits comprising the combination as well as the use of the combination in the treatment of a proliferative disease are further contemplated.</p>
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AURORA A KINASE INHIBITOR (Fri, 05 May 2017)
<p id="p-0001" num="0000">The present invention provides an aminopyridine compound, or a pharmaceutically acceptable salt thereof, that inhibits Aurora A and, therefore may be useful in treating cancer.</p>
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COMBINATIONS (Fri, 05 May 2017)
<p id="p-0001" num="0000">The invention relates to a combination of a first compound selected from N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine or a pharmaceutically acceptable salt thereof or a solvate thereof, and N-(2-fluoro-3,5-dimethoxyphenyl)-N-(1H-imidazol-2-ylmethyl)-3-(1-methyl-1H-pyrazol-4-yl)pyrido[2,3-b]pyrazin-6-amine or a pharmaceutically acceptable salt thereof or a solvate thereof; and a second compound which is a cMet inhibitor. The combination is for use in the treatment of a proliferative disorder, in particular for use in the treatment of cancer. The FGFR inhibitor (N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine or a pharmaceutically acceptable salt thereof or a solvate thereof, and N-(2-fluoro-3,5-dimethoxyphenyl)-N-(1H-imidazol-2-ylmethyl)-3-(1-methyl-1H-pyrazol-4-yl)pyrido[2,3-b]pyrazin-6-amine or a pharmaceutically acceptable salt thereof or a solvate thereof) and the cMet inhibitor can be administered simultaneously, separately or sequentially. The invention further relates to a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a combination according to the invention.</p>
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BICYCLIC HETEROCYCLES AS FGFR4 INHIBITORS (Fri, 05 May 2017)
<p id="p-0001" num="0000">The present disclosure relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR4 enzyme and are useful in the treatment of FGFR4-associated diseases such as cancer.</p>
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NOVEL GLUCOSE DERIVATIVE, AND CELL IMAGING METHOD AND IMAGING AGENT USING SAID DERIVATIVE (Fri, 05 May 2017)
<p id="p-0001" num="0000">Provided is a glucose derivative, which is taken into cells via a membrane sugar transport system and is represented by formula (1). Also provided are an imaging agent and an imaging method for a cell or intracellular molecule using said glucose derivative. Further provided are a method for detecting cancer cells with good accuracy using said glucose derivative and an imaging agent to be used in said method. More specifically provided are D-glucose derivatives and L-glucose derivatives in which glucose is bound to the 7-position of a fluorescent molecular group with a coumarin backbone or a quinolone backbone. Also provided are a cell imaging agent and imaging method using the derivative. A cancer cell imaging agent and imaging method using the L-glucose derivative is also provided. G is a group selected from formulas (G1)-(G4) below.</p>
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CYCLOPROPYLAMINES AS LSD1 INHIBITORS (Fri, 05 May 2017)
<p id="p-0001" num="0000">The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.</p>
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HETEROCYCLIC MODULATORS OF HIF ACTIVITY FOR TREATMENT OF DISEASE (Fri, 05 May 2017)
<p id="p-0001" num="0000">The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.</p>
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FUSION MOLECULE BASED ON NOVEL TAA VARIANT (Fri, 05 May 2017)
<p id="p-0001" num="0000">This invention provides novel carbonic anhydrase (CAIX) nucleic acid and peptide sequences, as well as related methods and compositions, including anti-cancer immunogenic agent(s) (e.g. vaccines and chimeric molecules) that elicit an immune response specifically directed against cancer cells expressing a CAIX antigenic marker. The novel CAIX variant and related compositions are useful in a wide variety of treatment modalities including, but not limited to protein vaccination, DNA vaccination, and adoptive immunotherapy.</p>
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AMINO SPHINGOGLYCOLIPID ANALOGUES (Fri, 05 May 2017)
<p id="p-0001" num="0000">The invention relates to amino sphingoglycolipid analogues and peptide derivatives thereof, compositions comprising these compounds and methods of treating or preventing diseases or conditions using such compounds, especially diseases or conditions relating to cancer, infection, atopic disorders, autoimmune disease or diabetes.</p>
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2- (AZAINDOL-2-YL) BENZIMIDAZOLES AS PAD4 INHIBITORS (Fri, 05 May 2017)
<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="27.86mm" wi="73.24mm" file="US20170119750A1-20170504-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein; <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">R<sub>1 </sub>is hydrogen or C<sub>1-6</sub>alkyl;</li> <li id="ul0002-0002" num="0000">R<sub>2 </sub>is hydrogen, C<sub>1-6</sub>alkyl, perhalomethylC<sub>0-5</sub>alkyl-O—, or C<sub>1-6</sub>alkoxy;</li> <li id="ul0002-0003" num="0000">R<sub>3 </sub>is hydrogen, C<sub>1-6</sub>alkyl, or C<sub>1-6</sub>alkoxyC<sub>1-6</sub>alkyl;</li> <li id="ul0002-0004" num="0000">R<sub>4 </sub>is hydrogen, C<sub>1-6</sub>alkyl, perhalomethylC<sub>1-6</sub>alkyl; or unsubstituted C<sub>3-6</sub>cycloalkylC<sub>1-6</sub>alkyl;</li> <li id="ul0002-0005" num="0000">A is C—R<sub>5 </sub>or N;</li> <li id="ul0002-0006" num="0000">B is C—R<sub>6 </sub>or N;</li> <li id="ul0002-0007" num="0000">D is C—R<sub>7 </sub>or N;</li> <li id="ul0002-0008" num="0000">with the proviso that at least one of A, B, and D, is N;</li> <li id="ul0002-0009" num="0000">R<sub>5 </sub>is hydrogen or C<sub>1-6</sub>alkyl;</li> <li id="ul0002-0010" num="0000">R<sub>6 </sub>is hydrogen or C<sub>1-6</sub>alkyl;</li> <li id="ul0002-0011" num="0000">R<sub>7 </sub>is hydrogen, C<sub>1-6</sub>alkyl, C<sub>1-6</sub>alkoxy, or hydroxy;</li> <li id="ul0002-0012" num="0000">R<sub>8 </sub>is hydrogen or C<sub>1-6</sub>alkyl, with the proviso that one of R<sub>4 </sub>and R<sub>8 </sub>is hydrogen;</li> <li id="ul0002-0013" num="0000">R<sub>9 </sub>is hydrogen or hydroxy;</li> <li id="ul0002-0014" num="0000">R<sub>10 </sub>is hydrogen or C<sub>1-6</sub>alkyl; <br/> and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis. </li> </ul> </li> </ul> </p>
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ARYL- OR HETEROARYL-SUBSTITUTED BENZENE COMPOUNDS (Fri, 05 May 2017)
<p id="p-0001" num="0000">The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.</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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HETEROCYCLIC MODULATORS OF LIPID SYNTHESIS (Fri, 05 May 2017)
<p id="p-0001" num="0000">Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).</p>
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PH-SENSITIVE AND BIOREDUCIBLE POLYMER-VIRUS COMPLEX FOR CANCER TREATMENT (Fri, 05 May 2017)
<p id="p-0001" num="0000">The present invention relates to a pH-sensitive and bioreducible polymer-virus complex which can destroy tumor cells more effectively by increasing the efficiency of virus transduction, to a pH-sensitive and bioreducible polymer, and to a pharmaceutical composition containing the polymer-virus complex.</p>
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PHARMACEUTICAL COMPOSITIONS COMPRISING POH DERIVATIVES (Fri, 05 May 2017)
<p id="p-0001" num="0000">The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene for sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.</p>
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METHODS FOR IDENTIFICATION, ASSESSMENT, PREVENTION, AND TREATMENT OF METABOLIC DISORDERS USING PM20D1 AND N-LIPIDATED AMINO ACIDS (Fri, 05 May 2017)
The present invention relates to methods for identifying, assessing, preventing, and treating metabolic disorders and modulating metabolic processes using PM20D1 and N- lipidated amino acids.
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ANTI-NRG1 (HEREGULIN) ANTIBODIES AND USES THEREOF (Fri, 05 May 2017)
The disclosure relates to human anti-NRG1 neutralizing monoclonal antibodies that do not interfere with the NRG1 binding to the HER3 receptor and uses thereof. More particularly, an isolated human monoclonal antibody comprising a heavy and light chain variable regions with specific CDRs defined by their sequences is disclosed.
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ISOTOPIC METHODS FOR MEASUREMENT OF TRYPTOPHAN AND METABOLITES THEREOF (Fri, 05 May 2017)
Tryptophan degradation is a key metabolic pathway controlling immune reactions and evidence suggests that during cancer progression generation of tryptophan metabolites may be fundamental for immune escape promoting the malignant phenotype of cancer cells in an autocrine fashion. The present invention relates to methods of measuring mass tag labelled tryptophan and metabolites thereof and methods using the labelled molecules for monitoring in a subject the effectiveness of a treatment and of disease recurrence after treatment, for stratifying patients and for diagnosing suppression of an immune response in a subject.
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ANTIBODY CONJUGATES COMPRISING TOLL-LIKE RECEPTOR AGONIST (Fri, 05 May 2017)
Provided herein are antibody conjugates comprising toll-like receptor agonists and the use of such conjugates for the treatment of cancer. In some embodiments, the conjugates comprise anti-HER2 antibodies.
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HUMANIZED ANTI-DKK2 ANTIBODY AND USES THEREOF (Fri, 05 May 2017)
The present invention relates to the discovery that inhibition of Dickkopf2 (DKK2) increases CD8+ cytotoxic T lymphocyte (CTL) activity, attenuates tumor, and hence suppresses tumor formation. Thus, in various embodiments described herein, the methods of the invention relate to methods of treating cancer by administering to a patient an effective amount of a humanized anti-DKK2 antibody, methods for providing anti-tumor immunity in a subject, methods of stimulating a T cell mediated immune response to a cell population or a tissue and suppressing tumor in a subject. Additionally, the current invention includes methods of diagnosing a cancer or a predisposition of developing a cancer or a metastasis and methods for determining the use of immunotherapy treatment or cancer vaccine for treating cancer. Furthermore, the invention encompasses a pharmaceutical composition for treating cancer as well as a kit for carrying out the aforementioned methods.
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COMPOSITIONS AND METHODS FOR TARGETING CANCER-SPECIFIC SEQUENCE VARIATIONS (Fri, 05 May 2017)
The present invention relates to compositions and methods for targeting cancer-specific DNA sequences, such as copy number amplifications and other types of cancer-specific sequence variations, such as cancer-specific polymorphisms, insertions, or deletions. The present invention provides hereto sequence-specific DNA targeting agents targeting a sequence within the amplified DNA region or a sequence otherwise specific for a cancer cell compared to a non- cancer cell. The invention further relates to methods for treating cancer, comprising administering such sequence-specific DNA targeting agents. The invention further relates to methods for preparing sequence-specific DNA targeting agent, as well as screening methods using the DNA targeting agents.
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COMPOSITIONS AND METHODS FOR INHIBITING ARGINASE ACTIVITY (Fri, 05 May 2017)
The invention relates to a novel class of compounds that exhibit activity inhibitory activity toward arginase, and pharmaceutical compositions comprising the compounds of the invention. Also provided herein are methods of treating cancer with the arginase inhibitors of the invention.
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AMORPHOUS SOLID FORM OF A BET PROTEIN INHIBITOR (Fri, 05 May 2017)
The present invention relates to an amorphous solid form of (4S)-7-(3,5-dimethylisoxazol-4-yl)-4-pyridin-2-yl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2(1H)-one, and processes for its preparation, which is an inhibitor of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and is useful in the treatment of various diseases such as cancer.
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SSTR-TARGETED CONJUGATES AND PARTICLES AND FORMULATIONS THEREOF (Fri, 05 May 2017)
Conjugates of an active agent such as DM1 attached to a targeting moiety, such as a somatostatin receptor binding moiety, via a linker, and particles comprising such conjugates have been designed. Such conjugates and particles can provide improved temporospatial delivery of the active agent, improved biodistribution and penetration in tumor, and/or decreased toxicity. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer.
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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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COMPOSITION FOR THE TREATMENT OF IGF-1R EXPRESSING CANCER (Fri, 05 May 2017)
The present invention relates to a method for the treatment of IGF-IR expressing cancers as well as to a compositions and a kit for said traitment. From one aspect, the invention reates to the combined use of a first antibody for the determination of the IGF-IR status of a cancer and a second antibody used as an ADC for the treatment of said cancer.
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NOVEL PROCESS FOR PREPARING THIENOPYRIMIDINE COMPOUND AND INTERMEDIATES USED THEREIN (Fri, 05 May 2017)
The present invention relates to a novel method for preparing thienopyrimidine compound having an activity of selectively inhibiting tyrosine kinase, specifically the mutant epidermal growth factor receptor tyrosine kinase; and a novel intermediate used therein. According to the method of the present invention, the industrial mass-production of the compound of Formula 1, which is useful as a therapeutic agent for non-small cell lung cancer induced by the mutant epidermal growth factor receptor tyrosine kinase, can be implemented more conveniently and efficiently than the conventional technology.
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PODOPHYLLOTOXIN DERIVATIVES AND THEIR USE (Fri, 05 May 2017)
Provided herein are relates to derivatives of podophyllotoxin, compositions thereof, and using them for treating various types of cancer in a subject and/or delaying or regressing various types of tumor growths in a subject.
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WEE 1 KINASE INHIBITORS AND METHODS OF MAKING AND USING THE SAME (Fri, 05 May 2017)
A compound, or a pharmaceutically acceptable salt thereof, having a chemical structure of formula (I) or formula (II), and methods of using these compounds to treat cancer in an individual.
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HDAC inhibitors and therapeutic methods using the same (Fri, 05 May 2017)
Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
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Treatment or prophylaxis of proliferative conditions (Fri, 05 May 2017)
The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are, for example, characterized by cells that express cytochrome P450 1B1 (CYPiB1) and allelic variants thereof The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example, in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are, for example, characterized by cells that express CYPiBI and allelic variants thereof The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.
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Compounds useful for treating cancer (Fri, 05 May 2017)
The present invention relates to compound (I) wherein: z means a pyridazine, a pyrimidine or a pyrazine group, R independently represent a hydrogen atom, a halogen atom or a group chosen among a -CN group, a hydroxyl group, a -COOR 1 group, a (CI-C3)fluoroalkyl group, a (CI-C3)fluoroalkoxy group, a -NO 2 group, a -NR 1 R2 group, a (CI-C4)alkoxy group, a phenoxy group and a (CI-C 3 )alkyl group, said alkyl being optionally mono-substituted by a hydroxyl group, n is 1, 2 or 3, n' is 1 or 2, R' is a hydrogen atom, a halogen atom or a group chosen among a (C1-C3)alkyl group, , a hydroxyl group, a -COOR 1 group, a -NO 2 group, a -NR1 R2 group, a morpholinyl or a morpholino group, a N-methylpiperazinyl group, a (C1-C3)fluoroalkyl group, a (C1-C4)alkoxy group and a -CN group, Z is N or C, Y is N or C, X is N or C, W is N or C, T is N or C, U is N or C, for use as an agent for preventing, inhibiting or treating cancer. Some of said compounds are new and also form part of the invention.
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PYRAZOLYL QUINOXALINE KINASE INHIBITORS (Fri, 05 May 2017)
The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
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Radiopharmaceutical conjugate of a metabolite and an EPR agent, for targeting tumour cells (Fri, 05 May 2017)
This invention relates new radiopharmaceutical conjugates for use in improved methods of diagnosis and treatment of cancer. The radiopharmaceutical conjugate comprises, in sequence: a metabolite that targets tumour cells, bound to a chelating agent capable of containing a radionuclide, bound to a linker capable of binding with an EPR agent in vitro or in vivo; or a chelating agent capable of containing a radionuclide, bound to a metabolite that targets tumour cells, bound to a linker capable of binding with an EPR agent in vitro or in vivo. The radiopharmaceutical conjugates of the present invention provide active and passive targeted radionuclide delivery systems that can help to improve the biodistribution and pharmacological toxicity of the radiopharmaceuticals used for the diagnosis and therapy of cancer.
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Thiazolyl-containing compounds for treating proliferative diseases (Fri, 05 May 2017)
The present disclosure provides thiazolyl-containing compounds of Formula (I), (II), or (III). The compounds described herein may be able to inhibit protein kinases (e.g., Src family kinases (e.g., hemopoietic cell kinase (HCK)), Bruton' s tyrosine kinase (BTK)) and may be useful in treating and/or preventing proliferative diseases (e.g., myelodysplasia, leukemia, lymphoma (e.g., Waldenstrom's macroglobulinemia)) and in inducing apoptosis in a cell (e.g., malignant blood cell). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.
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NEW COMPOUND FOR INHIBITING BINDING BETWEEN DX2 PROTEIN AND P14/ARF PROTEIN, AND PHARMACEUTICAL COMPOSITION FOR TREATING OR PREVENTING CANCER DISEASE CONTAINING SAME AS EFFECTIVE INGREDIENT (Thu, 04 May 2017)
The present invention relates to a new compound for inhibiting binding between a DX2 protein and a p14/ARF protein, and a medical use thereof. A review of the in vitro and in vivo anticancer effect of the compound shows that the compound has an excellent anticancer effect and thus is useful as a drug for treating various cancer diseases including lung cancer, and has a more improved anticancer effect particularly by inhibiting resistance to an anticancer drug of Adriamycin in a cell line which is resistant to an anticancer drug such as Adriamycin, and thus can be used as an anticancer adjuvant for improving the anticancer effect. In addition, the present invention relates to a composition for diagnosing lung cancer comprising an AIMP2-DX2 protein or a fragment thereof, and is effective in diagnosis of lung cancer because whether or not a subject has lung cancer is confirmed only by using a serum sample of the subject.
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Substituted pyrrolopyrimidines as HDM2 inhibitors (Wed, 03 May 2017)
<p id="p-0001" num="0000">The present invention provides substituted pyrrolopyrimidines of Formula I as described herein or a pharmaceutically acceptable salt or solvate thereof:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="22.10mm" wi="54.95mm" file="US09637493-20170502-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same. </p>
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CONJUGATE OF MONOMETHYL AURISTATIN F AND TRASTUZUMAB AND ITS USE FOR THE TREATMENT OF CANCER (Fri, 28 Apr 2017)
<p id="p-0001" num="0000">The present invention relates to an antibody-drug-conjugate or pharmaceutical composition comprising the same. From one aspect, the invention relates to an antibody-drug-conjugate (ADC) comprising an antibody consisting of the Trastuzumab or a biosimilar thereof, said antibody being conjugated to at least one drug consisting of a monomethyl auristatin F derivative. The invention also comprises method of treatment of cancer comprising administering to the subject an effective amount of said antibody-drug-conjugate or composition comprising the same.</p>
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COMPOSITIONS AND METHODS OF REGULATING CANCER RELATED DISORDERS AND DISEASES (Fri, 28 Apr 2017)
Provided herein are naphthylic derivative compounds, or pharmaceutically acceptable salts thereof, that are useful for inhibiting cancers. Also provided herein are methods of using effective amounts of said compounds, optionally with pharmaceutical carriers, for the treatment of cancers within human subjects.
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MODULATION OF NOVEL IMMUNE CHECKPOINT TARGETS (Fri, 28 Apr 2017)
Dysfunctional or exhausted T cells arise in chronic diseases including chronic viral infections and cancer, and express high levels of co-inhibitory receptors. Therapeutic blockade of these receptors has clinical efficacy in the treatment of cancer. While co- inhibitory receptors are co-expressed, the triggers that induce them and the transcriptional regulators that drive their co-expression have not been identified. The immunoregulatory cytokine IL-27 induces a gene module in T cells that includes several known co-inhibitory receptors (Tim-3, Lag-3, and TIGIT). The present invention provides a novel immunoregulatory network as well as novel cell surface molecules that have an inhibitory function in the tumor microenvironment. The present invention further provides the novel discovery that the transcription factors Prdm1 and c-Maf cooperatively regulate the expression of the co-inhibitory receptor module. This critical molecular circuit underlies the co-expression of co-inhibitory receptors in dysfunctional T cells and identifies novel regulators of T cell dysfunction.
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PYRIDONE DERIVATIVES AND THEIR USE AS KINASE INHIBITORS (Fri, 28 Apr 2017)
Disclosed in the present application is a compound of formula (I) as defined herein as well as a pharmaceutical composition comprising said compound. Further disclosed in the present application is the use of such pharmaceutical compositions for treating diseases, namely inter alia for use in the treatment of cancer, metabolic, inflammatory, autoimmune and viral diseases. The compounds disclosed herein are inhibitors of MNK1 and/or MNK2 kinases.
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PRODRUGS OF 2-(4-(3-((4-AMINO-7-CYANO-IMIDAZO[2,1-F][1,2,4]TRIAZIN-2-YL)AMINO)PHENYL)PIPERAZ IN-1-YL)PROPANAMIDE DERIVATIVES AS CK2 INHIBITORS FOR THE TREATMENT OF CANCER (Fri, 28 Apr 2017)
PRODRUGS OF IMIDAZOTRIAZINE COMPOUNDS AS CK2 INHIBITORS The invention provides pharmaceutically active compounds of formula (I) and prodrugs thereof. The formula (I) 2-(aminophenylamino)-4- amino-7-cyano-imidazo[2,1-f][1,2,4]triazine derivatives inhibit CK2 protein kinase activity, thereby making them useful for treating cancer, psoriasis and rheumatoid arthritis.
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COFACTOR ANALOGS AS METHYLTRANSFERASE INHIBITORS FOR TREATING CANCER (Fri, 28 Apr 2017)
Compounds having methyltransferase inhibitory activity are disclosed. The compounds have the structure (I) They are useful in the treatment of cancer and similar diseases associated with inappropriate methyltransferase activity.
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PIPERAZINYL NORBENZOMORPHAN COMPOUNDS AND METHODS FOR USING THE SAME (Fri, 28 Apr 2017)
Disclosed herein, inter alia, are piperazinyl norbenzom orphan compounds and uses thereof, including, for example, methods for treating a CNS disease, treating traumatic brain injury, improving cognition, or diagnosing and treating cancer.
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BENZOLACTAM COMPOUNDS AS PROTEIN KINASE INHIBITORS (Fri, 28 Apr 2017)
The invention provides a compound of formula (0): or a pharmaceutically acceptable salt, N-oxide or tautomer thereof. The compounds are inhibitors of ERK 1/2 kinases and will be useful in the treatment of ERKl/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.
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PHENYL INDOLE ALLOSTERIC INHIBITORS OF P97 ATPASE (Fri, 28 Apr 2017)
The present invention is directed to methods of inhibiting p97 and compounds and compositions useful in such methods. Diseases and conditions the can be treated with the compounds and compositions of the invention include, but are not limited to, cancer and neurodegenerative disorders susceptible to treatment by inhibition of p97.
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2-BETA-NAPHTHYL-ACETIC ACID ANALOGS AS AKR1C3 INHIBITORS AND METHODS OF USING SAME (Fri, 28 Apr 2017)
The invention includes 2-β-naphthyl-acetic acid derivatives, which are selective AKR1C3 inhibitors. In certain embodiments, the compounds of the invention are R-naproxen analogs. The invention further includes methods of treating cancer, such as prostate cancer and/or castration-resistant prostate cancer, using at least one compound of the invention.
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LAPACHONE DERIVATIVES CONTAINING TWO REDOX CENTERS AND METHODS OF USE THEREOF (Fri, 28 Apr 2017)
Provided herein are compounds containing two redox centers including a chalcogen redox center of the formula: wherein: R1, R2, X1, X2, Y1, and m are as defined herein. Also provided herein are pharmaceutical composition of the present compounds and methods of treatment using the compounds including their use in the treatment of cancer.
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PSMA TARGETED RADIOHALOGENATED UREAS FOR CANCER RADIOTHERAPY (Fri, 28 Apr 2017)
PPSMA binding scaffolds with radioiodinated, radiobrominated and radioastatinated labeled prosthetic groups are disclosed. Pharmaceutical compositions and methods of treating PSMA expressing cells or tumors also are disclosed.
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METHODS FOR DIAGNOSING PANCREATIC CANCER (Thu, 27 Apr 2017)
The present disclosure relates to the use of one or more biomarkers to determine the presence of pancreatic cancer precursor lesions or pancreatic cancer in a subject. This disclosure is based, at least in part, on the discovery that early to invasive stages of pancreatic cancer release or secrete biomarkers that can be detected in biological samples of a subject. Accordingly, in certain non-limiting embodiments, the present disclosure provides for methods and kits for determining the presence of one or more biomarkers in a biological sample of a subject, and methods of using such determinations in selecting a therapeutic regimen for a cancer subject and in methods of treating cancer subjects.
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SUBSTITUTED BENZOAZEPINES AS TOLL-LIKE RECEPTOR MODULATORS (Thu, 27 Apr 2017)
Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease.
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PYRIMIDINE-2,4-DIAMINE DERIVATIVE AND ANTICANCER PHARMACEUTICAL COMPOSITION COMPRISING SAME AS EFFECTIVE INGREDIENT (Thu, 27 Apr 2017)
The present invention relates to a pyrimidine-2,4-diamine derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition for prevention or treatment of cancer comprising the same as an effective ingredient. A compound according to the present invention has the good effect of inhibiting anaplastic lymphoma kinase (ALK) activity, whereby a therapeutic effect on cancer cells having an anaplastic lymphoma kinase (ALK) fusion protein such as EML4-ALK, NPM-ALK, etc. can be enhanced and it is expected that a recurrence of cancer will be effectively inhibited. As such, the compound can be effectively used in a pharmaceutical composition for prevention or treatment of cancer.
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METHODS OF TREATMENT USING ANTI-ERBB ANTIBODY MAYTANSINOID CONJUGATES (Fri, 21 Apr 2017)
<p id="p-0001" num="0000">The application concerns methods of treatment using anti-ErbB receptor antibody-maytansinoid conjugates, and articles of manufacture suitable for use in such methods. In particular, the invention concerns ErbB receptor-directed cancer therapies, using anti-ErbB receptor antibody-maytansinoid conjugates.</p>
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COMPOUNDS USEFUL AS IMMUNOMODULATORS (Fri, 21 Apr 2017)
<p id="p-0001" num="0000">The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.</p>
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GEMCITABINE PRODRUGS AND USES THEREOF (Fri, 21 Apr 2017)
<p id="p-0001" num="0000">The present invention provides compounds according to formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="40.89mm" wi="53.76mm" file="US20170107245A1-20170420-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and pharmaceutically acceptable salts thereof. For compounds of formula I, R<sup>1 </sup>and R<sup>2 </sup>are independently selected from the group consisting of H, —C(═O)—(CH<sub>2</sub>)<sub>2</sub>-aryl, and —C(═O)—(CH<sub>2</sub>)<sub>n</sub>—C(═O)—NH-aryl. The subscript n is from 2 to 6. R<sup>3 </sup>is selected from the group consisting of H and —C(═O)—O—R<sup>4</sup>; and R<sup>4 </sup>is selected from the group consisting of alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, arylalkyl, substituted arylalkyl, cycloheteroalkyl, substituted cycloheteroalkyl, heteroalkyl and substituted heteroalkyl. Compounds are provided wherein at least one of R<sup>1 </sup>and R<sup>2 </sup>is other than H. Pharmaceutical compositions, methods for inhibiting the growth of cancer cells, and methods for the treatment of cancer are also provided.</p>
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NEW COMPOUNDS (Fri, 21 Apr 2017)
<p id="p-0001" num="0000">The invention relates to new naphthyridine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.</p>
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MACROCYCLIC COMPOUNDS AS TRK KINASE INHIBITORS (Fri, 21 Apr 2017)
<p id="p-0001" num="0000">Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R<sup>2</sup>, R<sup>2a </sup>R<sup>3 </sup>and R<sup>3a </sup>are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="34.54mm" wi="56.30mm" file="US20170107232A1-20170420-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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