CYCLOALKYNE DERIVATIZED SACCHARIDES (Fri, 25 Jul 2014)
The invention provides novel saccharide derivatives, conjugates, and methods for making the derivatives and conjugates.
>> read more

MEGLUMINE SALT FORMS OF 2-((1 R,4R)-4-(4-(5-(BENZOXAZOL-2-YLAMINO)PYRIDIN-2-YL)PHENYL)CYCLOHEXYL) ACETIC ACID AND THEIR USE AS DGAT1 INHIBITORS (Fri, 18 Jul 2014)
The present invention relates to novel crystalline forms of meglumine salts of 2-((1 R,4R)-4-(4-(5-(benzo[d]oxazol-2-ylamino)pyridin-2-yl) phenyl)cyclohexyl)acetic acid :Formule(I) and their use in the treatment or prevention of a condition or a disorder associated with DGATl activity in animals, particularly humans.
>> read more

SOLID FORM OF DIHYDRO-PYRIDO-OXAZINE DERIVATIVE (Fri, 04 Jul 2014)
The invention relates to an anhydrous crystalline form of (1,1-dioxo-hexahydro-1lambda*6*- thiopyran-4-yl)-{(S)-3-[1-(6-methoxy-5-methyl-pyridin-3-yl)-2,3-dihydro-1H-pyrido[3,4- b][1,4]oxazin-7-yloxy]-pyrrolidin-1-yl}-methanone; pharmaceutical compositions and combinations including these forms as well as to methods of using these forms, including their pharmaceutical compositions and combinations for the treatment of diseases.
>> read more

METHOD FOR MAKING IMPROVED UV-ABSORBING OPHTHALMIC LENSES (Fri, 27 Jun 2014)
Described herein is a cost-effective and time-efficient method for making UV-absorbing contact lenses. In contrast to the conventional method for making UV-absorbing contact lenses which involves copolymerizing a lens forming composition including a UV-absorbing vinylic monomer, a method of the invention involves dipping a contact lens in a solution of UV-absorbing polymer comprising carboxyl-containing monomeric units, UV-absorbing monomeric units and covalently bound radical-initiating moieties to form a UV-absorbing coating on the contact lens.
>> read more

ARYL-SUBSTITUTED FUSED BICYCLIC PYRIDAZINE COMPOUNDS (Fri, 27 Jun 2014)
The present invention provides a compound of formula (I) as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula (I), and pharmaceutical compositions comprising such compounds.
>> read more

AUTOTAXIN INHIBITORS (Fri, 27 Jun 2014)
The present invention relates to novel compounds of formula (I) (I) that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in the treatment of an ATX-dependent or ATX-mediated disease or condition.
>> read more

TRICYCLIC COMPOUNDS FOR INHIBITING THE CFTR CHANNEL (Fri, 27 Jun 2014)
The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
>> read more

TRICYCLIC COMPOUNDS AS CFTR INHIBITORS (Fri, 27 Jun 2014)
The present invention provides a CFTR inhibitor of formula (I) or a pharmaceutically acceptable salt thereof; and its therapeutic uses, e.g. in the treatment of diarrhea. The present invention further provides a combination of pharmacological active agents and a pharmaceutical composition.
>> read more

BICYCLIC ACETYL-COA CARBOXYLASE INHIBITORS AND USES THEREOF (Fri, 20 Jun 2014)
<p id="p-0001" num="0000">The present invention provides compounds of formula (I);</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="17.70mm" wi="57.40mm" file="US20140171363A1-20140619-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing the compounds of formula (I), their therapeutic uses, combinations with other of pharmacologically active agents, and a pharmaceutical compositions.</p>
>> read more

Autotaxin inhibitors (Fri, 20 Jun 2014)
<p id="p-0001" num="0000">The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in the treatment of an ATX-dependent or ATX-mediated disease or condition.</p>
>> read more

Autotaxin inhibitors (Fri, 20 Jun 2014)
<p id="p-0001" num="0000">The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin.</p>
>> read more

TREATING DISEASES MEDIATED BY BLOCKADE OF THE EPITHELIAL SODIUM CHANNEL WITH PYRAZINE-2-CARBOXAMIDE DERIVATIVES (Fri, 20 Jun 2014)
<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="29.13mm" wi="69.85mm" file="US20140171421A1-20140619-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">in free or salt or solvate form, where R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6</sup>, R<sup>7</sup>, R<sup>8</sup>, R<sup>9</sup>, R<sup>10 </sup>and R<sup>11 </sup>have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.</p>
>> read more

TRICYCLIC COMPOUNDS (Fri, 20 Jun 2014)
<p id="p-0001" num="0000">The present invention provides a compound of formula I 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="42.08mm" wi="53.26mm" file="US20140171417A1-20140619-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.</p>
>> read more

TRICYCLIC COMPOUNDS (Fri, 20 Jun 2014)
<p id="p-0001" num="0000">The present invention provides a compound of formula I 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="41.57mm" wi="53.00mm" file="US20140171412A1-20140619-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.</p>
>> read more

PYRIMIDO [4,5-B]QUINOLINE-4,5 (3H,10H)-DIONES AS NONSENSE MUTATION SUPPRESSORS (Fri, 20 Jun 2014)
The invention relates to compound of the formula (I); or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
>> read more

PYRIDONE DERIVATIVES AND USES THEREOF IN THE TREATMENT OF TUBERCULOSIS (Fri, 20 Jun 2014)
A compound of Formula (I) is provided that has been shown to be useful for treating a disease, disorder or syndrome that is mediated by the inhibition of mycolic acid biosynthesis through inhibition of M. tuberculosis EnoyI Acyl Carrier Protein Reductase enzyme (InhA): wherein R1, R2, R3, R4 and R5 are as defined herein.
>> read more

TRIS(TRIMETHYL SILOXY)SILANE VINYLIC MONOMERS AND USES THEREOF (Fri, 20 Jun 2014)
The invention provides a TRIS-containing vinylic monomer which comprises one sole (meth)acryloyloxy group and a tris(trimethylsiloxy)silyl group covalently linked to the ethylenically-unsaturated group through a polyoxyethylene linker. The present invention is also related to a polymer, an actinically-crosslinkable silicone-containing prepolymer, a silicone hydrogel polymeric material, or a silicone hydrogel contact lens, which comprises monomeric units derived from a TRIS-containing vinylic monomer of the invention. In addition, the invention provides a method for making a TRIS-containing vinylic monomer of the invention.
>> read more

COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES (Fri, 06 Jun 2014)
<p id="p-0001" num="0000">The present invention provides compounds 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="66.89mm" file="US20140155367A1-20140605-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a <i>Plasmodium </i>parasite, such as malaria.</p>
>> read more

BI-HETEROARYL COMPOUNDS AS VPS34 INHIBITORS (Fri, 06 Jun 2014)
<p id="p-0001" num="0000">The present invention includes novel methods of treating a disease or disorder characterized by hyperactivity of Vps34, and compound as Vps34 inhibitors; particularly compounds of Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.36mm" wi="58.17mm" file="US20140155402A1-20140605-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, as well as methods of treating a disease, disorder, or syndrome associated with Vps34 inhibition, particularly hyperproliferative diseases. The present invention also includes pharmaceutical compositions including compounds of formula I and pharmaceutically acceptable salts thereof.</p>
>> read more

CYCLIC NUCLEOSIDE DERIVATIVES AND USES THEREOF (Fri, 06 Jun 2014)
A compound of Formula (I) is provided that has been shown to be useful for treating a disease caused by a viral infection wherein R1, R2 and R3 are as defined herein.
>> read more

METHODS FOR MAKING CONJUGATES FROM DISULFIDE-CONTAINING PROTEINS (Fri, 06 Jun 2014)
The invention provides methods to prepare protein conjugates from proteins having at least two cysteines. In one embodiment, a protein with a disulfide linkage is reduced to provide two free cysteines for reaction with a 1,3-dihaloacetone or similar reactant, linking the sulfur atoms of the two cysteines together. The ketone inserted between the sulfur atoms is then used to form a Schiff base to an aminated payload molecule, thus conjugating the protein to a payload. In another embodiment, two cysteine residues are tied together by reaction with a 1,3-dihaloacetone or similar reactant. The linkage between the sulfur atoms in each case holds the protein or peptide in a constrained conformation, while also providing a convenient place for attaching a payload with good specificity and efficiency.
>> read more

Substituted carbamoylmethylamino acetic acid derivatives as novel NEP inhibitors (Thu, 29 May 2014)
The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 , R 6 , A 1 , A 2 , X 1 , sand m are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
>> read more

TYROSINE LIGATION PROCESS (Fri, 23 May 2014)
<p id="p-0001" num="0000">A process is provided for preparing a conjugate of Formula (I-A) or (I) comprising a polypeptide containing n number of tyrosine units, where n is an integer greater than or equal to 1, dispersed within the amino acid chain</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="2.71mm" wi="18.20mm" file="US20140141034A1-20140522-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">having and amino terminus end (A<sup>1</sup>) and an acid terminus end (A<sup>2</sup>) of the protein or polypeptide and having a weight average molecular weight equal to or greater than 10,000 Daltons (10 kDa), wherein the conjugate comprises a number m of tyrosine conjugates (modified tyrosine residues) as depicted in Formula (I-A) or (I), where m is at least one and is less than or equal to n:</p> <p id="p-0004" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="106.26mm" wi="69.85mm" file="US20140141034A1-20140522-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0005" num="0000">where X, Lg, L and R are as defined herein.</p>
>> read more

NOVEL TRIFLUOROMETHYL-OXADIAZOLE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE (Fri, 23 May 2014)
<p id="p-0001" num="0000">The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, (I) in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or metabolic syndrome via inhibition of HDAC4.</p>
>> read more

COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES (Fri, 23 May 2014)
The present invention provides compounds of formula I: [INSERT FORMULA HERE] or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease, such as malaria, caused by a Plasmodium parasite.
>> read more

COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES (Fri, 23 May 2014)
The present invention provides compounds of formula I: [INSERT FORMULA HERE] or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.
>> read more

SUBSTITUTED INDOLE DERIVATIVES (Fri, 16 May 2014)
The present invention relates to substituted indole derivatives, to processes for their production, to new stable forms, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
>> read more

OXAZOLIDIN-2-ONE-PYRIMIDINE DERIVATIVES (Fri, 16 May 2014)
The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.
>> read more

Tetrahydro-Pyrido-Pyrimidine Derivatives (Fri, 09 May 2014)
<p id="p-0001" num="0000">The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I),</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="31.16mm" wi="69.85mm" file="US20140128370A1-20140508-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein Y, R<sup>1</sup>, R<sup>2 </sup>and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.</p>
>> read more

BACE-2 INHIBITORS FOR THE TREATMENT OF METABOLIC DISORDERS (Fri, 09 May 2014)
<p id="p-0001" num="0000">The present invention relates to the use of BACE-2 inhibitors and pharmaceutical compositions comprising BACE-2 inhibitors for treating metabolic disorders related to decreased β cell mass and/or function.</p>
>> read more

<i>Staphylococcus aureus </i>proteins and nucleic acids (Fri, 09 May 2014)
<p id="p-0001" num="0000">The invention provides proteins from <i>Staphylococcus aureus </i>including amino acid sequences and the corresponding nucleotide sequences. The proteins are useful for vaccines, immunogenic compositions, diagnostics, enzymatic studies and also as targets for antibiotics.</p>
>> read more

Compounds and Compositions as Protein Kinase Inhibitors (Thu, 08 May 2014)
The invention provides a novel class of compounds of formula 1, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.
>> read more

OXAZINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS (Fri, 25 Apr 2014)
<p id="p-0001" num="0000">The invention relates to novel heterocyclic compounds of the formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.65mm" wi="64.52mm" file="US20140113894A1-20140424-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.</p>
>> read more

[(1H-INDOL-5-YL) - HETEROARYLOXY] - (1-AZA-BICYCLO [3.3.1] NONANES AS CHOLINERGIC LIGANDS OF THE N-ACHR FOR THE TREATMENT OF PSYCHOTIC AND NEURODEGENRATIVE DISORDERS (Fri, 25 Apr 2014)
<p id="p-0001" num="0000">The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production to pharmaceutical compositions comprising them and to their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and nemodegenerative disorders.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.65mm" wi="66.04mm" file="US20140113908A1-20140424-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> read more

PYRAZINE DERIVATIVES AS ENAC BLOCKERS (Fri, 25 Apr 2014)
<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="34.29mm" wi="69.85mm" file="US20140113914A1-20140424-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and pharmaceutically acceptable salts and solvates thereof, wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6</sup>, R<sup>7</sup>, R<sup>8</sup>, R<sup>9</sup>, and R<sup>10 </sup>have the meanings as indicated in the specification, are useful for treating diseases mediated by blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.</p>
>> read more

HIGH REFRACTIVE INDEX OPHTHALMIC DEVICE MATERIALS WITH REDUCED TACK (Fri, 25 Apr 2014)
High refractive index copolymers with reduced tack are disclosed. The copolymers, which are particularly suitable for use as ophthalmic device materials, comprise a benzhydryl methacrylate or benzydryl methacrylate derivative monomer.
>> read more

Spiro-indole derivatives for the treatment of parasitic diseases. (Thu, 24 Apr 2014)
The invention relates to organic compounds which have interesting pharmaceutical properties. In particular, the compounds are useful in the treatment and/or prevention of infections such as those caused by Plasmodium falciparum, Plasmodium vivax, Plasmodium malariae, Plasmodium ovale, Trypanosoma cruzi and parasites of the Leishmania genus such as, for example, Leishmania donovani. The invention also relates to pharmaceutical compositions containing the compounds, as well as processes for their preparation.
>> read more

Novel Heterocyclic Derivatives and Their Use in the Treatment of Neurological Disorders (Fri, 18 Apr 2014)
<p id="p-0001" num="0000">The invention relates to novel heterocyclic compounds of the formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.98mm" wi="64.43mm" file="US20140107118A1-20140417-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.</p>
>> read more

ALDEHYDE ACETAL BASED PROCESSES FOR THE MANUFACTURE OF MACROCYCLIC DEPSIPEPTIDES AND NEW INTERMEDIATES (Fri, 18 Apr 2014)
The invention relates to a method or process for the chemical manufacture of depsipeptides of the formula I employing an aldehyde acetal intermediate Formula (I), wherein the symbols have the meaning defined in the description, to new intermediates and their manufacture, as well as related invention embodiments.
>> read more

SOLUTION PHASE PROCESSES FOR THE MANUFACTURE OF MACROCYCLIC DEPSIPEPTIDES AND NEW INTERMEDIATES (Fri, 18 Apr 2014)
The invention relates to a method or process for solution phase chemical manufacture of depsipeptides of the formula (I), wherein the symbols have the meaning defined in the description, to new intermediates and their manufacture, as well as related invention embodiments.
>> read more

IMMUNOGENIC COMPOSITION (Fri, 11 Apr 2014)
The invention provides an immunogenic composition comprising: a) a conjugate that is a capsular saccharide from GBS serotype Ia conjugated to a carrier protein; b) a conjugate that is a capsular saccharide from GBS serotype Ib conjugated to a carrier protein; c) a conjugate that is a capsular saccharide from GBS serotype III conjugated to a carrier protein; d) a conjugate that is a capsular saccharide from GBS serotype II conjugated to a carrier protein; and e) a conjugate that is a capsular saccharide from GBS serotype V conjugated to a carrier protein.
>> read more

NONLINEAR SACCHARIDE CONJUGATES (Fri, 11 Apr 2014)
This specification is directed to nonlinear saccharide conjugates that comprise polysaccharides that are linked to at least two peptides that comprise T-cell epitopes and have no conformational B-cell epitopes where one of the peptides is linked to an internal saccharide so that the conjugates have a branched (i.e., nonlinear) structure. The specification also provides methods of manufacturing these conjugates, methods of formulating these conjugates in compositions for use as vaccines and methods of using the compositions to induce an immune response to the capsular saccharide. The specification also provides a new polyepitope carrier peptidecomprising the PV1 epitope from polio virus. The new polyepitope carrier peptidecan be used in both linear saccharide conjugates as well as the nonlinear saccharide conjugates.
>> read more

Pyrrolopyrimidine compounds and their uses (Thu, 10 Apr 2014)
The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.
>> read more

Process (Fri, 04 Apr 2014)
<p id="p-0001" num="0000">The present invention relates to improved processes for the production of 2-amino-2-[2-(4-C<sub>2-20 </sub>alkyl-phenyl)ethyl]propane-1,3-diols, and to compounds for use therein.</p>
>> read more

Solid Oral Formulations and Crystalline Forms of an Inhibitor of Apoptosis Protein (Fri, 04 Apr 2014)
<p id="p-0001" num="0000">The present disclosure relates to crystalline form of (S)—N—((S)-1-cyclohexyl-2-{(S)-2-[4-(4-fluorobenzoyl)-thiazol-2-yl]-pyrrolidin-1-yl}-2-oxo-ethyl)-2-methylamino-propionamide, salts and hydrates thereof. This disclosure also relates to solid oral formulation of (S)—N—((S)-1-cyclohexyl-2-{(S)-2-[4-(4-fluoro-benzoyl)-thiazol-2-yl]-pyrrolidin-1-yl}-2-oxo-ethyl)-2-methylamino-propionamide, pharmaceutically acceptable salts, solvates (including hydrates) thereof, as well as methods of treatment using the same.</p>
>> read more

CYCLIC PEPTIDES AND USE AS MEDICINES (Fri, 04 Apr 2014)
The present invention provides a compound of formula (I); or a pharmaceutically acceptable salt thereof, wherein the variables R1, R2, R3, R4, R5, and A- B are defined herein, which are non-immunosuppresive, cyclophilin-binding, mPTP blockers and are therefore useful for the prevention or treatment of diseases or disorders such as HCV infection, stroke, multiple sclerosis, HBV infection, HPV infection, asthma, cancer, muscular dystrophy, sepsis, ischemia/reperfusion injury, and heart failure.
>> read more

COMPOUNDS FOR USE IN GASTRIC COMPLICATION (Fri, 04 Apr 2014)
The present invention relates to the use of low molecular weight (lmw) compounds, especially lmw compounds with GPR4-affinity, in the treatment of diseases and disorders which includes gastroesophageal reflux disease (GERD), and / or non-erosive reflux disease (NERD) and the like.
>> read more

Cyclohexyl Amide Derivatives and Their Use as CRF-1 Receptor Antagonists (Fri, 28 Mar 2014)
<p id="p-0001" num="0000">There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF<sub>1</sub>) receptor antagonists.</p>
>> read more

Substituted carbamoylmethylamino acetic acid derivatives as novel NEP inhibitors (Fri, 28 Mar 2014)
<p id="p-0001" num="0000">The present invention provides a compound 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="68.66mm" file="US20140088165A1-20140327-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, wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>6</sup>, A<sup>1</sup>, A<sup>2</sup>, X<sup>1</sup>, s and m are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.</p>
>> read more

DIHYDROPYRROLIDINO-PYRIMIDINES AS KINASE INHIBITORS (Fri, 28 Mar 2014)
The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof; as further described herein. The present invention further provides pharmaceutical compositions comprising these compounds, and combinations comprising these compounds combined with or used with a therapeutic co-agent, as well as therapeutic uses of these compounds and compositions. These are useful in the treatment of diseases such as cancer that are associated with activation of ERKl and/or ERK2, and especially for MAPK pathway dependent cancers showing resistance to Raf and/or MEK inhibitory cancer therapeutics
>> read more

CLOSTRIDIUM DIFFICILE POLYPEPTIDES AS VACCINE (Fri, 28 Mar 2014)
The invention provides methods, proteins, nucleic acids and antibodies for preventing or treating a C. difficile infection in a mammal.
>> read more

KINASE INHIBITORS AND METHODS OF THEIR USE (Fri, 21 Mar 2014)
<p id="p-0001" num="0000">New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.</p>
>> read more

Processes for the Manufacture of Macrocyclic Depsipeptides and New Intermediates (Fri, 21 Mar 2014)
<p id="p-0001" num="0000">The invention relates to a method or process for the chemical manufacture of depsipeptides of the formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="45.80mm" wi="68.41mm" file="US20140080995A1-20140320-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein the symbols have the meaning defined in the description, to new intermediates and their manufacture, as well as related invention embodiments.</p>
>> read more

IL-18 BINDING MOLECULES (Fri, 14 Mar 2014)
IL-18 participates in both innate and acquired immunity. The bioactivity of IL-18 is negatively regulated by the IL-18 binding protein (IL18BP), a naturally occurring and highly specific inhibitor. This soluble protein forms a complex with free IL-18 preventing its interaction with the IL-18 receptor, thus neutralizing and inhibiting its biological activity. The present invention discloses binding molecules, in particular antibodies or fragments thereof, which bind IL-18 and do not bind IL-18 bound to IL-18BP (IL-18/IL-18BP complex). Apart from its physiological role, IL-18 has been shown to mediate a variety of autoimmune and inflammatory diseases. The binding molecules of the inventions may be used as therapeutic molecules for treating IL-18- related autoimmune and inflammatory diseases or as diagnostic tools for characterizing, detecting and/or measuring IL-18 not bound to IL-18BP as component of the total IL-18 pool.
>> read more

INDOLE CARBOXAMIDE DERIVATIVES AND USES THEREOF (Fri, 14 Mar 2014)
A compound of Formula (I) is provided that has been shown to be useful for treating a disease, disorder or syndrome that is mediated by the transportation of essential molecules in the mmpL3 pathway: (I) wherein R1, R2, R3, R4, R5 and R6 are as defined herein.
>> read more

COMBINATION VACCINES WITH SEROGROUP B MENINGOCOCCUS AND D/T/P (Fri, 14 Mar 2014)
Serogroup B meningococcus antigens can successfully be combined with diphtheria, tetanus and pertussis toxoids ("DTP") to provide effective combination vaccines for protecting against multiple pathogens. These combinations are effective with a range of different adjuvants, and with both pediatric-type and booster-type DTP ratios. The adjuvant can improve the immune response which the composition elicits; alternatively, by including an adjuvant it is possible for the compositions to have a relatively lower amount of antigen while nevertheless having immunogenicity which is comparable to unadjuvanted combination vaccines.
>> read more

Silicone hydrogel lenses with water-rich surfaces (Thu, 13 Mar 2014)
Hydrated silicone hydrogel contact lens having a layered structural configuration: a low water content silicone hydrogel core (or bulk material) completely covered with a layer of a water-rich (e.g., a water content greater than 80%), hydrogel totally or substantially free of silicone. The hydrated silicone hydrogel contact lens possesses high oxygen permeability for maintaining the corneal health and a soft, water-rich, lubricious surface for wearing comfort.
>> read more

2'-Branched Nucleosides for Treatment of Viral Infections (Fri, 07 Mar 2014)
<p id="p-0001" num="0000">The present invention provides a compound 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="69.85mm" file="US20140065101A1-20140306-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, wherein R<sup>1 </sup>is defined herein, which is a 2′-branched nucleoside useful for the treatment or prevention of viral infections, particularly dengue virus, yellow fever virus, West Nile virus, Japanese encephalitis virus, tick-borne encephalitis virus, Kunjin virus, Murray Valley encephalitis, St Louis encephalitis, Omsk hemorrhagic fever virus, bovine viral diarrhea virus, Zika virus and Hepatitis C virus.</p>
>> read more

Beta2-Adrenoreceptor Agonists (Fri, 07 Mar 2014)
<p id="p-0001" num="0000">Compounds of formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.86mm" wi="69.85mm" file="US20140066478A1-20140306-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">in free or salt or solvate form, where <br/> Ar is a group of formula </p> <p id="p-0004" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="22.27mm" wi="69.85mm" file="US20140066478A1-20140306-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0005" num="0000">Y is carbon or nitrogen and R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6</sup>, R<sup>7</sup>, R<sup>8</sup>, R<sup>9</sup>, R<sup>10</sup>, X, n, p, q and r are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of obstructive or inflammatory airways disease.</p>
>> read more

NEW PROCESS (Fri, 07 Mar 2014)
Provided is a new enantioselective process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ -amino- δ -biphenyl- a -methylalkanoic acid, or acid ester, backbone.
>> read more

NOVEL AMINOTHIAZOLE CARBOXAMIDES AS KINASE INHIBITORS (Fri, 07 Mar 2014)
The present invention provides a compound of formula (I), as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
>> read more

N-(3-PYRIDYL) BIARYLAMIDES AS KINASE INHIBITORS (Fri, 07 Mar 2014)
The present invention provides a compound of formula (I): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula (I), and pharmaceutical compositions comprising such compounds.
>> read more

SALTS OF BENZOTHIAZOLONE COMPOUND AS BETA-2-ADRENOCEPTOR AGONIST (Fri, 07 Mar 2014)
The present invention provides a compound of formula (I) in acetate salt form (I) a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.
>> read more

2'-ETHYNYL NUCLEOSIDE DERIVATIVES FOR TREATMENT OF VIRAL INFECTIONS (Fri, 07 Mar 2014)
The present invention provides a compound of formula A or a pharmaceutically acceptable salt thereof, wherein B, Q, R1, R5, R6, R7, R8 and Z are defined herein, which is a 2'-branched nucleoside useful for the treatment or prevention of viral infections, particularly dengue virus, yellow fever virus, West Nile virus, Japanese encephalitis virus, tick-borne encephalitis virus, Kunjin virus, Murray Valley encephalitis, St Louis encephalitis, Omsk hemorrhagic fever virus, bovine viral diarrhea virus, Zika virus and Hepatitis C virus.
>> read more

DIAZEPINONE DERIVATIVES USEFUL FOR THE TREATMENT OF FRAGILE X SYNDROME, PARKINSONS OR REFLUX DISEASE (Fri, 28 Feb 2014)
The invention relates to compound of the formula (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
>> read more

CHEMOKINE RECEPTOR BINDING POLYPEPTIDES (Fri, 21 Feb 2014)
<p id="p-0001" num="0000">The present invention relates to polypeptides directed against or specifically binding to chemokine receptor CXCR2 and in particular to polypeptides capable of modulating signal transduction from CXCR2. The invention also relates to nucleic acids, vectors and host cells capable of expressing the polypeptides of the invention, pharmaceutical compositions comprising the polypeptides and uses of said polypeptides and compositions for treatment of diseases involving aberrant functioning of CXCR2.</p>
>> read more

LOW DENSITY LIPOPROTEIN - RELATED PROTEIN 6 (LRP6) - HALF LIFE EXTENDER CONSTRUCTS (Fri, 21 Feb 2014)
<p id="p-0001" num="0000">The present invention relates to LRP6 constructs that bind to LRP6 receptor. The LRP6 constructs comprise at least one LRP6 binding moiety and a half-life extender molecule such that the LRP6 construct inhibit the Wnt signaling pathway without potentiation of the Wnt signal. The LRP6 constructs also have an increased half-life to provide more time for the therapeutic benefit.</p>
>> read more

Triazine-oxadiazoles (Fri, 21 Feb 2014)
<p id="p-0001" num="0000">The invention relates to new derivatives of formula (I),</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="44.20mm" wi="69.85mm" file="US20140051676A1-20140220-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of chronic pain.</p>
>> read more

BICYCLIC HETEROARYL CYCLOALKYLDIAMINE DERIVATIVES AS INHIBITORS OF SPLEEN TYROSINE KINASES (SYK) (Fri, 21 Feb 2014)
The present invention relates to bicyclic heteroaryl cycloalkyldiamine derivatives, to processes for their production, to their use as SYK inhibitors and to pharmaceutical compositions comprising them. Formula (I)
>> read more

1,4-DISUBSTITUTED PYRIDAZINE ANALOGS AND METHODS FOR TREATING SMN-DEFICIENCY-RELATED CONDITIONS (Fri, 21 Feb 2014)
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
>> read more

17a-HYDROXYLASE/C17,20-LYASE INHIBITORS (Fri, 14 Feb 2014)
<p id="p-0001" num="0000">The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R<sub>1</sub>, R<sub>2</sub>, R<sub>3</sub>, R<sub>4</sub>, R<sub>5</sub>, R<sub>6</sub>, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.50mm" wi="70.10mm" file="US20140045872A1-20140213-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> read more

Salts of 4-Methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide (Fri, 07 Feb 2014)
<p id="p-0001" num="0000">Salts of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide are prepared by various processes.</p>
>> read more

METHODS TO IDENTIFY AMINO ACID RESIDUES INVOLVED IN MACROMOLECULAR BINDING AND USES THEREFOR (Fri, 07 Feb 2014)
The present disclosure relates to methods and computational tools based, at least in part, on computer simulations that identify hot-spot amino acid residues and binding- region amino acid residues of a protein.
>> read more

SELECTIVE HYDROXAMIC ACID BASED MMP-12 AND MMP-13 INHIBITORS (Fri, 31 Jan 2014)
<p id="p-0001" num="0000">The present invention provides a compound of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="23.88mm" wi="67.39mm" file="US20140031399A1-20140130-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).</p>
>> read more

COMBINATION THERAPY (Fri, 24 Jan 2014)
<p id="p-0001" num="0000">The present invention relates to a pharmaceutical combination comprising an alpha-isoform specific phosphatidylinositol 3-kinase inhibitor compound, such as (S)-Pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl}-amide), or pharmaceutically acceptable salt thereof, and an IGF1R inhibitor (e.g., the IGF1R inhibitor ANTIBODY A, or a variant or derivative thereof), a pharmaceutical composition comprising such combination, methods for treating cancer comprising administration of therapeutically effective amounts of such inhibitors to a subject in need thereof, and uses of such combination for the treatment of cancer.</p>
>> read more

ORGANIC COMPOUNDS (Fri, 24 Jan 2014)
<p id="p-0001" num="0000">The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.</p>
>> read more

Ophthalmic And Otorhinolaryngological Device Materials Containing An Alkylphenol Ethoxylate (Fri, 24 Jan 2014)
<p id="p-0001" num="0000">Disclosed are soft, high refractive index, acrylic device materials. The materials contain a functionalized alkylphenol ethoxylate to reduce glistenings.</p>
>> read more

CARBAMATE/UREA DERIVATIVES (Fri, 24 Jan 2014)
The invention relates to compound of the formula (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
>> read more

COMBINATION THERAPY OF INHIBITORS FOR IGF1 R AND PI3K (Fri, 24 Jan 2014)
The present invention relates to a pharmaceutical combination comprising an alpha- isoform specific phosphatidylinositol 3-kinase inhibitor compound, such as (S)-Pyrrolidine- 1,2-dicarboxylic acid 2-amide l-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin- 4-yl]-thiazol-2-yl}-amide), or pharmaceutically acceptable salt thereof, and an IGF1R inhibitor (e.g., the IGF1R inhibitor ANTIBODY A, or a variant or derivative thereof), a pharmaceutical composition comprising such combination, methods for treating cancer comprising administration of therapeutically effective amounts of such inhibitors to a subject in need thereof, and uses of such combination for the treatment of cancer.
>> read more

COMPLEMENT PATHWAY MODULATORS AND USES THEREOF (Fri, 17 Jan 2014)
The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
>> read more

IMIDAZOPYRROLIDINONE COMPOUNDS (Fri, 10 Jan 2014)
<p id="p-0001" num="0000">The invention relates to compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.26mm" wi="37.42mm" file="US20140011798A1-20140109-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.</p>
>> read more

Compounds and Compositions as Protein Kinase Inhibitors (Fri, 10 Jan 2014)
<p id="p-0001" num="0000">The present invention provides compounds of Formula I or II:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="79.84mm" wi="68.50mm" file="US20140011825A1-20140109-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R<sup>1</sup>, R<sup>1b</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6 </sup>and R<sup>7 </sup>are defined herein. The compounds of Formula (I) or (II) and pharmaceutical compositions thereof are useful for the treatment of B-Raf-associated diseases.</p>
>> read more

CRYSTALLINE FORMS OF L-(2-((LR,3S,5R)-3-( (2 -FLUORO-3 - (TRIFLUOROMETHOXY) PHENYL) CARBAMOYL) - 2 -AZABICYCL O [3.1.0] HEXAN- 2 -YL) - 2 -OXOETHYL) - 5 -METHYL - 1H - PYRAZOLO [3, 4 -C] PYRIDINE - 3 - CARBOXAMI DE AND SALTS THEREOF (Sat, 04 Jan 2014)
Crystalline forms and pharmaceutically acceptable salts of l-(2- ((1 R,3S,5R)-3-((2-fluoro- 3-(trifluoromethoxy)phenyl)carbamoyl)-2- azabicyclo[3.1.0]hexan-2-yl)-2-oxoethyl)-5- methyl-1 H-pyrazolo[3,4- c]pyridine-3-carboxamide. l-(2-((l R,3S,5R)3-((2-fluoro-3- (trifluoromethoxy)phenyl)carbamoyl)-2-azabicyclo[3.1.0]hexan-2-yl) -2-oxoethyl)-5- methyl-1 H-pyrazolo[3,4-c]pyridine-3-carboxamide is useful in treating Age-related Macular Degeneration (AMD).
>> read more

PYRROLIDINE DERIVATIVES AND THEIR USE AS COMPLEMENT PATHWAY MODULATORS (Sat, 04 Jan 2014)
The present invention provides a compound of formula (I) a method for manufacturing the compounds of the invention, and its therapeutic uses as a factor D inhibitor for the treatment of ophthalmic diseases. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
>> read more

PYRROLIDINE DERIVATIVES AND THEIR USE AS COMPLEMENT PATHWAY MODULATORS (Sat, 04 Jan 2014)
The present invention provides a compound of formula (I) a method for manufacturing the compounds of the invention and its therapeutic uses as complement pathway modulators for the treatment of ocular diseases. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
>> read more

PYRROLIDINE DERIVATIVES AND THEIR USE AS COMPLEMENT PATHWAY MODULATORS (Sat, 04 Jan 2014)
The present invention provides a compound of formula (I) a method for manufacturing the compounds of the invention, and its therapeutic uses as complement pathway modulators for the treatment of ocular diseases. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
>> read more

PYRROLIDINE DERIVATIVES AND THEIR USE AS COMPLEMENT PATHWAY MODULATORS (Sat, 04 Jan 2014)
The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses as complement alternative inhibitors for the treatment of ocular diseases. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
>> read more

COMPLEMENT PATHWAY MODULATORS AND USES THEREOF (Sat, 04 Jan 2014)
The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
>> read more

COMPLEMENT PATHWAY MODULATORS AND USES THEREOF (Sat, 04 Jan 2014)
The present invention provides a compound of formula (I) : a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
>> read more

Pyrrolidine-1,2-dicarboxamide derivatives (Fri, 03 Jan 2014)
<p id="p-0001" num="0000">The present invention relates 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="33.27mm" wi="61.64mm" file="US08710085-20140429-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a salt thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase. </p>
>> read more

COMPLEMENT PATHWAY MODULATORS AND USES THEREOF (Sat, 28 Dec 2013)
The present invention provides a compound of formula I a method for manufacturing the compounds of the invention, and its therapeutic uses as inhibitor of the complement alternative pathway and particularly as inhibitor of Factor B for the treatment of e.g. age-related macular degeneration and diabetic retinopathy. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
>> read more

Bi-heteroaryl compounds as Vps34 inhibitors (Fri, 20 Dec 2013)
<p id="p-0001" num="0000">The present invention includes novel methods of treating a disease or disorder characterized by hyperactivity of Vps34, and compound as Vps34 inhibitors; particularly compounds of Formula I or a pharmaceutically acceptable salt thereof, as well as methods of treating a disease, disorder, or syndrome associated with Vps34 inhibition, particularly hyperproliferative diseases. The present invention also includes pharmaceutical compositions including compounds of formula I and pharmaceutically acceptable salts thereof.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.36mm" wi="58.50mm" file="US08685993-20140401-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> read more

AZETIDINIUM-CONTAINING COPOLYMERS AND USES THEREOF (Fri, 20 Dec 2013)
The invention is related to azetidinium-containing copolymers and vinylic monomers and their uses in formation of non-silicone hydrogel coatings on silicone hydrogel contact lenses.
>> read more

VACCINES FOR SEROGROUP X MENINGOCOCCUS (Fri, 20 Dec 2013)
A method for immunising a subject against serogroup X meningococcus by administering a vaccine comprising one, two or all three of: (i) a meningococcal fHbp antigen; (ii) a meningococcal NHBA antigen; and/or (iii) a meningococcal NadA antigen.The vaccine may also include meningococcal outer membrane vesicles.
>> read more

ANTIBODIES FOR EPIDERMAL GROWTH FACTOR RECEPTOR 3 (HER3) (Fri, 13 Dec 2013)
<p id="p-0001" num="0000">This invention relates to antibodies or fragments thereof which interact with HER family of receptors, e.g., HER3 receptor. In particular, it relates to antibodies or fragments thereof that recognize a conformational epitope of HER3 receptor comprising residues from both domains 2 and 4 resulting in inhibition of both ligand-dependent and ligand-independent signal transduction; and allow ligand binding (e.g., neuregulin), whilst preventing ligand-induced activation of signal transduction. These antibodies or fragments can be used to treat a number of diseases or disorders characterized by increased levels of HER3 expression (e.g., esophageal cancer). These antibodies or fragments can be used to treat a number of diseases or disorders characterized by the antibodys or fragments ability to decrease tissue weight (e.g., prostate or uterine weights) or to induce atrophy of tissue (e.g., atrophy of male breast).</p>
>> read more

3-Spirocyclic Piperidine Derivatives as Ghrelin Receptor Agonists (Fri, 13 Dec 2013)
<p id="p-0001" num="0000">The invention relates to derivatives of formula (I),</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="23.96mm" wi="67.39mm" file="US20130331369A1-20131212-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor.</p>
>> read more

ACETYLENE DERIVATIVES HAVING MGLUR 5 ANTAGONISTIC ACTIVITY (Fri, 13 Dec 2013)
<p id="p-0001" num="0000">The invention provides compounds of formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.99mm" wi="63.50mm" file="US20130331568A1-20131212-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein n, A, R, R′, R″, R<sub>0</sub>, X and Y are as defined in the description, and their preparation. The compounds of formula I are useful as pharmaceuticals.</p>
>> read more

QUINOXALINE CARBOXAMIDE DERIVATIVES AS PROTEIN TYROSINE KINASE INHIBITORS (Fri, 06 Dec 2013)
<p id="p-0001" num="0000">The invention relates to compounds of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.51mm" wi="74.59mm" file="US20130324519A1-20131205-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein the substituents are as defined in the specification, in free form or in the form of a pharmaceutically acceptable salt, solvate, ester, N-oxide thereof; processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases.</p>
>> read more

PYRROLOPYRROLIDINONE COMPOUNDS (Fri, 29 Nov 2013)
The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
>> read more

NOVEL RING-SUBSTITUTED N-PYRIDINYL AMIDES AS KINASE INHIBITORS (Fri, 29 Nov 2013)
The present invention provides a compound of formula (A): I as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
>> read more

MENINGOCOCCUS SEROGROUP X CONJUGATE (Fri, 29 Nov 2013)
The invention provides a conjugate of a Neisseria meningitidis serogroup X capsular polysaccharide and a carrier molecule. The conjugate is typically made by (a) oxidising a primary hydroxyl group in the capsular polysaccharide, to give an oxidised polysaccharide with an aldehyde group; and (b) coupling the oxidised polysaccharide to a carrier molecule via the aldehyde group, thereby giving the conjugate. The conjugate may be part of an immunogenic composition. This composition may comprise one or more further antigens, particularly capsular polysaccharides from serogroups A, W135, C and Y and conjugated forms thereof. The composition may be in an aqueous formulation. The composition is useful as a vaccine, e.g. for raising an immune response in a mammal. The invention also provides processes for making the conjugate.
>> read more

MONOCYCLIC HETEROARYL CYCLOALKYLDIAMINE DERIVATIVES (Fri, 22 Nov 2013)
The present invention relates to monocyclic heteroaryl cycloalkyldiamine derivatives of formula (I), to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.
>> read more

BENZAMIDE DERIVATIVES FOR INHIBITING THE ACTIVITY OF ABL1, ABL2 AND BCR-ABL1 (Fri, 22 Nov 2013)
The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
>> read more

BENZAMIDE DERIVATIVES FOR INHIBITING THE ACTIVITY OF ABL1, ABL2 AND BCR-ABL1 (Fri, 22 Nov 2013)
The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson- related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
>> read more

COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF ABL1, ABL2 AND BCR-ABL1 (Fri, 22 Nov 2013)
The present invention relates to compounds of formula I: in which Y, Y1, Y 4, Y5, Y 6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
>> read more

BENZAMIDE DERIVATIVES FOR INHIBITING THE ACTIVITY OF ABL1, ABL2 AND BCR-ABL1 (Fri, 22 Nov 2013)
The present invention relates to compounds of formula (I): in which Y, Y1, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
>> read more

SUBSTITUTED HETERO-BIARYL COMPOUNDS AND THEIR USES (Fri, 15 Nov 2013)
<p id="p-0001" num="0000">The present invention provides a compound of formula (II):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="41.83mm" wi="33.19mm" file="US20130303507A1-20131114-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">where R<sup>1 </sup>is a substituted alkyl, heterocyclic, or cycloalkyl, group, and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof, and pharmaceutical compositions comprising these compounds. Also provided are methods of using these compounds to treat a disease or condition mediated by CDK9, such as cancers and other conditions described herein.</li> </ul> </li> </ul> </p>
>> read more

PROCESS FOR THE MANUFACTURE OF CYCLIC UNDECAPEPTIDES (Fri, 15 Nov 2013)
The present invention relates to processes and intermediates useful for the manufacture of cyclic undecapeptides, such as Alisporivir, a non-immunosuppressive cyclosporine A derivative. The cyclosporin is acylated on the butenyl-methyl-threonine side chain and then subjected to a ring-opening reaction (the ring opens between the sarcosine and the N-methyl-leucine residues). This linear peptide intermediate is subjected to Edman degradation (removal of the N-terminal residue) as to give the second linear decapeptide intermediate, e.g. of sequence Val-N(Me)Leu-Ala-Ala-N(Me)Leu-N(Me) Leu-N(Me)Val-N(Me)Bmt-Abu-Sar when starting from CsA.
>> read more

BIPARATOPIC BINDING POLYPEPTIDES FOR CXCR2 AND USES THEREOF (Fri, 15 Nov 2013)
The present invention relates to polypeptides directed against or specifically binding to chemokine receptor CXCR2 and in particular to polypeptides capable of modulating signal transduction from CXCR2. The invention also relates to nucleic acids, vectors and host cells capable of expressing the polypeptides of the invention, pharmaceutical compositions comprising the polypeptides and uses of said polypeptides and compositions for treatment of diseases involving aberrant functioning of CXCR2.
>> read more

1H-QUINAZOLINE-2,4-DIONES (Fri, 08 Nov 2013)
<p id="p-0001" num="0000">The present invention relates to 1H-Quinazoline-2,4-diones of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="23.45mm" wi="69.85mm" file="US20130296332A1-20131107-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R<sup>1 </sup>and R<sup>2 </sup>are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.</p>
>> read more

L-MALATE SALT OF 2, 7 - DIAZA - SPIRO [4.5 ] DEC- 7 - YLE DERIVATIVES AND CRYSTALLINE FORMS THEREOF AS GHRELIN RECEPTOR AGONISTS (Fri, 08 Nov 2013)
The invention relates to: 2-Amino-N-[(R)-l-benzyloxymethyl-2-((4S,5R)-2-methyl-l- oxo-4- phenyl-2,7-diaza-spiro[4.5]dec-7-yl)-2-oxo-ethyl]-2-methyl- propionamide L- malate salt, 2-amino-N-((2R)-3-(benzyloxy)-l-(2-methyl-l-oxo-4-p-tolyl- 2,7- diazaspiro[4.5]decan-7-yi)-l-oxopropan-2-yi)-2-methyipropanamide L- malate salt and 2-Amino-N-((R)-l-benzyloxymethyl-2-[(45,5R)-4-fluoro- phenyl) -2-methyl-l-oxo-2,7-diaza-spiro[4,5]dec-7-yl]-2-oxoethyl}2- methylpropionamide L-malate salt and to the crystalline forms thereof; pharmaceutical compositions comprising such compounds and such compounds for the treatment of a disorder or a disease mediated by the ghrelin receptor.
>> read more

COMPLEMENT PATHWAY MODULATORS AND USES THEREOF (Fri, 08 Nov 2013)
The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
>> read more

CYCLIC BRIDGEHEAD ETHER DGAT1 INHIBITORS (Fri, 01 Nov 2013)
The invention relates to compounds of formula (I): (I) useful for treating disorders mediated by acyl coA-diacylglycerol acyl transferase 1 (DGAT1), e.g. metabolic disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment.
>> read more

TETRAHYDROPYRAN DGAT1 INHIBITORS (Fri, 01 Nov 2013)
The invention relates to compounds of formula (I): useful for treating disorders mediated by acyl coA-diacylglycerol acyl transferase 1 (DGAT1), e.g. metabolic disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment.
>> read more

Oxazine Derivatives and their Use in the Treatment of Neurological Disorders (Fri, 25 Oct 2013)
<p id="p-0001" num="0000">The invention relates to novel heterocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, in free form or in pharmaceutically acceptable salt form, to their preparation, to their medical use and to medicaments comprising them.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.65mm" wi="64.18mm" file="US20130281449A1-20131024-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> read more

SUBSTITUTED ISOQUINOLINONES AND QUINAZOLINONES (Fri, 25 Oct 2013)
<p id="p-0001" num="0000">The invention relates to substituted nitrogen containing bicyclic heterocycles of the formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="39.03mm" wi="69.85mm" file="US20130281473A1-20131024-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein Z is CH<sub>2 </sub>or N—R<sup>4 </sup>and X, R<sup>1</sup>, R<sup>2</sup>, R<sup>4</sup>, R<sup>6</sup>, R<sup>7 </sup>and n are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.</p>
>> read more

Use of (R)-Penciclovir Triphosphate for the Manufacture of a Medicament for the Treatment of Viral Diseases (Fri, 25 Oct 2013)
<p id="p-0001" num="0000">A method of treatment of: i) HIV-1 infections in mammals, including humans; or ii) HBV infections in mammals, including humans; which method comprises the administration to the human in need of such treatment, an effective amount of the (R)-enantiomer of the triphosphate of a compound of formula (A) or a pharmaceutically acceptable salt thereof; and compounds for use in the method.</p>
>> read more

DIAZA-SPIRO[5.5]UNDECANES USEFUL AS OREXIN RECEPTOR ANTAGONISTS (Fri, 25 Oct 2013)
<p id="p-0001" num="0000">The invention relates to compound of the formula (I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="23.37mm" wi="69.85mm" file="US20130281463A1-20131024-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> read more

ANTIBODIES FOR EPIDERMAL GROWTH FACTOR RECEPTOR 3 (HER3) DIRECTED TO DOMAIN II OF HER3 (Fri, 18 Oct 2013)
<p id="p-0001" num="0000">The present invention relates to antibodies or fragments thereof that target an epitope of a HER3 receptor residing in domain 2 of the HER3 receptor to block both ligand-dependent and ligand-independent signal transduction and tumor growth; and compositions and methods of use thereof.</p>
>> read more

ADSORPTION OF IMMUNOPOTENTIATORS TO INSOLUBLE METAL SALTS (Fri, 18 Oct 2013)
<p id="p-0001" num="0000">Immunopotentiators can be adsorbed to insoluble metal salts, such as aluminium salts, to modify their pharmacokinetics, pharmacodynamics, intramuscular retention time, and/or immunostimulatory effect. Immunopotentiators are modified to introduce a moiety, such as a phosphonate group, which can mediate adsorption. These modified compounds can retain or improve their in vivo immunological activity even when delivered in an adsorbed form.</p>
>> read more

DIMERIC IAP INHIBITORS (Fri, 11 Oct 2013)
<p id="p-0001" num="0000">The present invention provides compounds of formula M-L-M′ (where M and M′ are each independently a monomeric moiety of Formula (I), (II), (III) or (IV) and L is a linker). The dimeric compounds have been found to be effective in promoting apoptosis in rapidly dividing cells.</p>
>> read more

PYRROLOPYRIDINE DERIVATIVES AND THEIR USE AS CRTH2 ANTAGONISTS (Fri, 11 Oct 2013)
<p id="p-0001" num="0000">There are provided according to the invention compounds of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="36.24mm" wi="69.85mm" file="US20130267518A1-20131010-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">in free or salt form, wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6</sup>, Q, W, X, m, n and p are as described in the specification, process for preparing them, and their use as pharmaceuticals.</p>
>> read more

Thiopeptide precursor protein, gene encoding it and uses thereof (Thu, 10 Oct 2013)
The present invention relates to the precursor proteins for thiopeptide biosynthesis, and the corresponding structural genes and uses thereof. The present invention also relates to methods for genetically manipulating the thiopeptide precursor protein or host cells expressing a gene encoding said thiopeptide precursor protein to produce thiopeptide compounds or their derivatives. The present invention further relates to the cloning and characterization of genes involved in thiopeptide biosynthesis and their use in thiopeptide compounds production
>> read more

PYRIDAZINYL DERIVATIVES AS SMO INHIBITORS (Fri, 04 Oct 2013)
<p id="p-0001" num="0000">The present invention relates to compounds of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="51.22mm" wi="27.18mm" file="US20130261299A1-20131003-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">in which L, W, X, Y, Z, m, p, R1, R2, R3, R4 and R7 are defined in the Summary of the Invention; capable of inhibiting the Hedgehog and Smo signaling pathway. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the diagnosis and treatment of pathologies relating to the Hedgehog and Smo signaling pathway, for example, tumor formation, cancer, neoplasia and non-malignant hyperproliferative disorders.</li> </ul> </li> </ul> </p>
>> read more

SILICONE HYDROGEL LENSES WITH WATER-RICH SURFACES (Fri, 27 Sep 2013)
<p id="p-0001" num="0000">The invention is related to a hydrated silicone hydrogel contact lens having a layered structural configuration: a lower water content silicone hydrogel core (or bulk material) completely covered with a layer of a higher water content hydrogel totally or substantially free of silicone. A hydrated silicone hydrogel contact lens of the invention possesses high oxygen permeability for maintaining the corneal health and a soft, water-rich, lubricious surface for wearing comfort.</p>
>> read more

ANTIBODIES FOR EPIDERMAL GROWTH FACTOR RECEPTOR 3 (HER3) DIRECTED TO DOMAIN III AND DOMAIN IV OF HER3 (Fri, 27 Sep 2013)
<p id="p-0001" num="0000">The present invention relates to antibodies or fragments thereof that bind to a non-linear epitope within domain 3 of the HER3 receptor and inhibit both ligand-dependent and ligand-independent signal transduction. The invention also relates antibodies or fragments thereof that bind to amino acid residues within domains 3-4 of HER3 and inhibit both ligand-dependent and ligand-independent signal transduction; and compositions and methods of use of such antibodies or fragments thereof.</p>
>> read more

Macrocycles and their uses (Fri, 27 Sep 2013)
<p id="p-0001" num="0000">The present application describes a method of treating a bacterial infection comprising administering to a subject in need thereof a pharmaceutically acceptable amount of a defined macrocycle compound.</p>
>> read more

CRYSTALLINE FORM OF A SUCCINATE SALT (Fri, 27 Sep 2013)
This invention relates to a new crystalline form of the succinate salt of the epithelial sodium channel (ENaC) blocker 3-(3-{2-[(E)-3,5-Diamino-6-chloro-pyrazine-2-carbonylimino]-1,3,8- triaza-spiro[4.5]decane-8-carbonyl}-benzenesulfonylamino)-propionic acid dipropylcarbamoylmethyl ester, pharmaceutical compositions comprising said crystalline form, uses of said crystalline form and pharmaceutical compositions, and methods for preparing said crystalline form.
>> read more

CHEMICAL PROCESS FOR PREPARING SPIROINDOLONES AND INTERMEDIATES THEREOF (Fri, 27 Sep 2013)
The present invention relates to processes and intermediates useful for the manufacture of spiroindolone compounds such as (1'R,3'S)-5,7'-dichloro-6'-fluoro-3'-methyl-2',3',4',9'-tetrahydrospiro[indoline-3,1'-pyrido[3, 4-b]indol]-2-one and salts and hydrates and solvates thereof.
>> read more

Triazolopyridine Compounds (Fri, 20 Sep 2013)
<p id="p-0001" num="0000">The invention relates to compounds of formula (I) and salts thereof:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.61mm" wi="66.46mm" file="US20130245002A1-20130919-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).</p>
>> read more

CRYSTALLINE FORM OF AN INHIBITOR OF MDM2/4 AND P53 INTERACTION (Fri, 20 Sep 2013)
<p id="p-0001" num="0000">A crystalline form of (S)-1-(4-Chloro-phenyl)-7-isopropoxy-6-methoxy-2-(4-{methyl-[4-(4-methyl-3-oxo-piperazin-1-yl)-trans-cyclohexylmethyl]-amino}-phenyl)-1,4-dihydro-2H-isoquinolin-3-one, which is useful in the treatment of a disease or disorder associated with the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively.</p>
>> read more

BENZOTHIAZOLONE COMPOUND (Fri, 20 Sep 2013)
<p id="p-0001" num="0000">The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="44.79mm" wi="72.47mm" file="US20130245080A1-20130919-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.</p>
>> read more

Silicone hydrogel lenses with water-rich surfaces (Thu, 19 Sep 2013)
Hydrated silicone hydrogel contact lens having a layered structural configuration: a low water content silicone hydrogel core (or bulk material) completely covered with a layer of a water-rich (e.g., a water content greater than 80%), hydrogel totally or substantially free of silicone. A hydrated silicone hydrogel contact lens of the invention possesses high oxygen permeability for maintaining the corneal health and a soft, water-rich, lubricious surface for wearing comfort.
>> read more

Silicone hydrogel lenses with water-rich surfaces (Thu, 19 Sep 2013)
Hydrated silicone hydrogel contact lens having a layered structural configuration: a low water content silicone hydrogel core (or bulk material) completely covered with a layer of a water-rich (e.g., a water content greater than 80%), hydrogel totally or substantially free of silicone. A hydrated silicone hydrogel contact lens of the invention possesses high oxygen permeability for maintaining the corneal health and a soft, water-rich, lubricious surface for wearing comfort.
>> read more

DEVELOPMENTS IN MENINGOCOCCAL OUTER MEMBRANE VESICLES (Fri, 13 Sep 2013)
<p id="p-0001" num="0000">A first aspect of the invention provides meningococcal outer membrane vesicles in which NHBA is over-expressed. A second aspect of the invention provides meningococcal outer membrane vesicles in which NadA is over-expressed. A third aspect of the invention provides a panel of bacterial strains, each member of which is isogenic except for a single gene which in each strain encodes a different variant of an antigen of interest.</p>
>> read more

IMMUNOLOGICALLY USEFUL ARGININE SALTS (Fri, 13 Sep 2013)
The invention is in the field of salt forms of an immunopotentiator compound and their formulation for in vivo use. In particular the invention relates to arginine salts.
>> read more

IN VITRO POTENCY ASSAY FOR PROTEIN-BASED MENINGOCOCCAL VACCINES (Fri, 13 Sep 2013)
The invention uses ELISA or similar assays for analysing a meningococcal vaccine. The assay uses antibodies which bind to meningococcal proteins within the vaccine, and in particular monoclonal antibodies which are bactericidal for meningococcus and/or which recognise conformational epitopes within the meningococcal proteins. By performing the assay on a series of dilutions of a test vaccine, and by comparing the results with those obtained using a reference vaccine of known potency, it is possible to determine the relative potency of the test vaccine. This value can be used as a parameter for determining whether a manufactured batch of a vaccine is suitable for release to the public, or whether it has experienced a production failure and so should not be used.
>> read more

ADJUVANTED FORMULATIONS OF STREPTOCOCCUS PNEUMONIAE ANTIGENS (Fri, 13 Sep 2013)
The efficacy of S. pneumoniae vaccines can be enhanced by adjuvanting S. pneumoniae saccharide and/or protein antigens with a mixture of a TLR agonist (preferably a TLR7 agonist) and an insoluble metal salt (preferably an aluminium salt). The TLR agonist is typically adsorbed to the metal salt. The S. pneumoniae antigen can also be adsorbed to the metal salt.
>> read more

SPIROHYDANTOIN COMPOUNDS AND THEIR USE AS SELECTIVE ANDROGEN RECEPTOR MODULATORS (Sat, 07 Sep 2013)
The present invention relates to a compound of formula (1-1 ) in free form or in pharmaceutically acceptable salt form in which the substituents are as defined in the specification; to its preparation, to its use as a medicament and to medicaments comprising it. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
>> read more

AMINIOTHIAZOLES AND THEIR USES (Fri, 06 Sep 2013)
<p id="p-0001" num="0000">The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases particularly bacterial infections.</p>
>> read more

BETA2-adrenoreceptor agonists (Fri, 06 Sep 2013)
<p id="p-0001" num="0000">Compounds of formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.65mm" wi="69.85mm" file="US08658673-20140225-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in free or salt or solvate form, where <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000">Ar is a group of formula</li> </ul> </p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="20.24mm" wi="69.85mm" file="US08658673-20140225-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">Y is carbon or nitrogen and R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6</sup>, R<sup>7</sup>, R<sup>8</sup>, R<sup>9</sup>, R<sup>10</sup>, X, n, p, q and r are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of obstructive or inflammatory airways diseases.</li> </ul> </p>
>> read more

Oxazole and thiazole compounds as KSP inhibitors (Fri, 30 Aug 2013)
<p id="p-0001" num="0000">Disclosed are new substituted oxazole and thiazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.09mm" wi="54.19mm" file="US08748626-20140610-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> read more

OXAZOLIDIN- 2 -ONE COMPOUNDS AND USES THEREOF AS PI3KS INHIBITORS (Fri, 30 Aug 2013)
The present invention relates to oxazolidin-2-one subsituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.
>> read more

Chimeric factor H binding proteins (fHBP) containing a heterologous B domain and methods of use (Thu, 29 Aug 2013)
Chimeric fHBPs that can elicit antibodies that are bactericidal for different fHBP variant strains of N. meningitidis, and methods of use, are provided.
>> read more

CHIMERIC, HYBRID AND TANDEM POLYPEPTIDES OF MENINGOCOCCAL NMB1870 (Fri, 23 Aug 2013)
<p id="p-0001" num="0000">NMB 1870 is a protein in <i>Neisseria meningitidis</i>. Three families of NMB 1870 are known. To increase the ability of a NMB1870 protein to elicit antibodies that are cross-reactive between the families, NMB1870 is engineered. Sequences can be substituted from one NMB1870 family into the corresponding position in another family. Proteins of NMB1870 sequences from different families can be joined to each other.</p>
>> read more

Glycoside derivatives and uses thereof (Fri, 09 Aug 2013)
<p id="p-0001" num="0000">The present invention provides a compound of formula I;</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="51.48mm" wi="67.65mm" file="US08722633-20140513-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. </p>
>> read more

PROMOTERS FOR INCREASED PROTEIN EXPRESSION IN MENINGOCOCCUS (Fri, 09 Aug 2013)
New promoters are described to drive transcription in meningococcus e.g. for over-expression of protein antigens for retention in membrane vesicles. Modified porA promoters lack the wild-type poly-G sequence which can cause phase variation. Meningococcal rRNA-coding genes (e.g. for 16S rRNA) can be used to drive transcription of a protein-coding gene. These approaches can be used in combination.
>> read more

PROCESS FOR PREPARING N-(4-CYCLOHEXYL-3-TRIFLUOROMETHYL-BENZYLOXY)-ACETIMIDIC ACID ETHYL ESTER (Fri, 09 Aug 2013)
This invention relates to novel processes for synthesizing N-(4-cyclohexyl-3-trifluoromethyl-benzyloxy)-acetimidic acid ethyl ester and to the compound of formula I and other intermediates that are used in such processes.
>> read more

BACTERICIDAL ANTIBODY ASSAYS TO ASSESS IMMUNOGENICITY AND POTENCY OF MENINGOCOCCAL CAPSULAR SACCHARIDE VACCINES (Fri, 02 Aug 2013)
<p id="p-0001" num="0000">The disclosure provides compositions, methods and kits for assessing immunogenicity, potency, or both, of meningococcal capsular saccharide vaccines. The assessment is based upon measurement of binding of a bactericidal antibody to a capsular saccharide component in the vaccine.</p>
>> read more

5-MEMBERED HETEROARYLCARBOXAMIDE DERIVATIVES AS PLASMA KALLIKREIN INHIBITORS (Fri, 02 Aug 2013)
The invention relates to a compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
>> read more

AMINOPYRIDINE DERIVATIVES AS PLASMA KALLIKREIN INHIBITORS (Fri, 02 Aug 2013)
The invention relates to compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
>> read more

IMIDAZOPYRROLIDINONE COMPOUNDS (Fri, 02 Aug 2013)
The invention relates to compounds of formula (I): (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
>> read more

CARRIER MOLECULE (Fri, 26 Jul 2013)
<p id="p-0001" num="0000">The invention provides a conjugate comprising an antigen and a carrier molecule, wherein the carrier molecule comprises a spr0096 antigen and a spr2021 antigen. spr0096 and spr2021 are <i>Streptococcus pneumoniae </i>antigens. The conjugate may be used in a method for raising an immune response in a mammal, the method comprising administering the conjugate to the mammal. Also provided are pharmaceutical compositions, particularly vaccines, comprising the conjugate.</p>
>> read more

COMBINATIONS OF MENINGOCOCCAL FACTOR H BINDING PROTEINS (Fri, 26 Jul 2013)
<p id="p-0001" num="0000">The M01573 sequence of meningococcal fHbp offers poor coverage in a vaccine. The invention addresses this poor coverage in two ways. In a first aspect, a fHbp-based vaccine includes two family I fHbp sequences, one which is more closely related to MC58 than to M01573, and vice versa. In a second aspect, a multi-family fHbp-based vaccine uses a family I fHbp sequence which is more closely related to MC58 than to M01573, in combination with a family III fHbp sequence.</p>
>> read more

TETRAHYDROPYRIDO-PYRIDINE AND TETRAHYDROPYRIDO-PYRIMIDINE COMPOUNDS AND USE THEREOF AS C5A RECEPTOR MODULATORS (Fri, 19 Jul 2013)
<p id="p-0001" num="0000">The present invention provides a compound of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.60mm" wi="47.58mm" file="US20130184253A1-20130718-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">(I) <br/> a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. </p>
>> read more

PYRROLOPYRIMIDINE COMPOUNDS AND THEIR USES (Fri, 19 Jul 2013)
<p id="p-0001" num="0000">The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.</p>
>> read more

IP RECEPTOR AGONIST HETEROCYCLIC COMPOUNDS (Fri, 19 Jul 2013)
<p id="p-0001" num="0000">The present invention provides heterocyclic derivatives which activate the IP receptor, processes for preparing them, pharmaceutical compositions comprising said derivatives and uses thereof. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients.</p>
>> read more

CRYSTALLINE FORMS OF THE SODIUM SALT OF (4--CYCLOHEXYL)-ACETIC ACID (Fri, 19 Jul 2013)
<p id="p-0001" num="0000">The present invention relates to novel crystalline forms of (4-{4-[5-(6-Trifluoromethyl-pyridin-3-ylamino)-pyridin-2-yl]-phenyl}-cyclohexyl)-acetic acid, sodium and their use in the treatment or prevention of a condition or a disorder associated with DGAT1 activity in animals, particularly humans. It also relates to processes for making such novel crystalline forms.</p>
>> read more

FUSED PYRROLES AS IP RECEPTOR AGONISTS FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION (PAH) AND RELATED DISORDERS (Fri, 19 Jul 2013)
The present invention provides heterocyclic derivatives which activate the IP receptor, processes for preparing them, pharmaceutical compositions comprising said derivatives and uses thereof. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Formula (1a) (1b)
>> read more

SALTS OF AN IP RECEPTOR AGONIST (Fri, 19 Jul 2013)
The invention relates to salts of (7-(2,3-di-p-tolyl-7,8-dihydropyrido[2,3-b]pyrazin-5(6H)- yl)heptanoic acid which are useful for treating diseases affected by the activation of the IP receptor, pharmaceutical compositions that contain the salts and processes for preparing the salts are also described.
>> read more

FUSED PIPERIDINES AS IP RECEPTOR AGONISTS FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION (PAH) AND RELATED DISORDERS (Fri, 19 Jul 2013)
The present invention provides heterocyclic derivatives which activate the IP receptor, processes for preparing them, pharmaceutical compositions comprising said derivatives and uses thereof. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Formula (I):
>> read more

FUSED PIPERIDINES AS IP RECEPTOR AGONISTS FOR THE TREATMENT OF PAH AND RELATED DISORDERS (Fri, 19 Jul 2013)
The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed.
>> read more

7,8- DIHYDROPYRIDO [3, 4 - B] PYRAZINES AS IP RECEPTOR AGONISTS FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION (PAH) AND RELATED DISORDERS (Fri, 19 Jul 2013)
The present invention provides heterocyclic derivatives which activate the IP receptor, processes for preparing them, pharmaceutical compositions comprising said derivatives and uses thereof. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Formula (I)
>> read more

FUSED DIHYDROPYRIDO [2,3 -B] PYRAZINES AS IP RECEPTOR AGONISTS FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION (PAH) AND RELATED DISORDERS (Fri, 19 Jul 2013)
The present invention provides heterocyclic derivatives which activate the IP receptor, processes for preparing them, pharmaceutical compositions comprising said derivatives and uses thereof. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Formula (I):
>> read more

USE OF CYCLIC DEPSIPEPTIDES TO INHIBIT KALLIKREIN 7 (Fri, 05 Jul 2013)
<p id="p-0001" num="0000">The present application relate to cyclic depsipeptides, or derivatives thereof, having the formula (I), and uses thereof, e.g. as inhibitors of kallikrein 7.</p>
>> read more

HETEROARYL COMPOUNDS AND THEIR USES (Fri, 05 Jul 2013)
<p id="p-0001" num="0000">The present invention provides a compound of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="41.83mm" wi="33.19mm" file="US20130172354A1-20130704-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">and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided is a method of treating a disease or condition mediated by CDK9.</li> </ul> </li> </ul> </p>
>> read more

INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE (Fri, 05 Jul 2013)
<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="28.45mm" wi="69.85mm" file="US20130172349A1-20130704-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">in free or salt form, wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3 </sup>and R<sup>4 </sup>have the meanings as indicated in the specification, are useful for treating conditions that are mediated by phosphatidylinositol 3-kinase.</p> <p id="p-0004" num="0000">Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.</p>
>> read more

5-membered heterocycle-based p38 kinase inhibitors (Fri, 05 Jul 2013)
<p id="p-0001" num="0000">Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38α, and p38β kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.</p>
>> read more

ADJUVANTED COMBINATIONS OF MENINGOCOCCAL FACTOR H BINDING PROTEINS (Fri, 05 Jul 2013)
The M01573 sequence of meningococcal fHbp offers poor coverage in a vaccine. The invention addresses this poor coverage in two ways. In a first aspect, a fHbp-based vaccine includes two family I fHbp sequences, one which is more closely related to MC58 than to M01573, and vice versa. In a second aspect, a multi-family fHbp-based vaccine uses a family I fHbp sequence which is more closely related to MC58 than to M01573, in combination with a family III fHbp sequence. The compositions are adjuvanted with an aluminium phosphate adjuvant.
>> read more

COMPOSITIONS AND METHODS TO TREAT BONE RELATED DISORDERS (Fri, 28 Jun 2013)
<p id="p-0001" num="0000">The present invention relates to the use of modulators of the sclerostin: sclerostin-binding-partner interaction for the treatment, amelioration, and diagnosis of sclerostin-related disorders, e.g., osteoporosis and sclerosteosis, and sclerostin-related disorders, e.g., cancers and cardiovascular disorders. The invention also relates to the use of sclerostin-binding-partner mimetics for the treatment, amelioration, and diagnosis of sclerostin-related disorders. Assays for the identification of modulators of the sclerostin: sclerostin-binding-partner interaction, as well as the resulting signaling, are also provided.</p>
>> read more

Dihydro-Benzo-Oxazine and Dihydro-Pyrido-Oxazine Derivatives (Fri, 28 Jun 2013)
<p id="p-0001" num="0000">The invention relates to dihydro-benzo-oxazine and dihydro-pyrido-oxazine compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="39.03mm" wi="69.85mm" file="US20130165436A1-20130627-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein Y, V, W, U, Q, R<sup>1</sup>, R<sup>5</sup>, R<sup>7 </sup>and R<sup>30 </sup>are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.</p>
>> read more

Crystalline Forms of 4-Methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide (Fri, 28 Jun 2013)
<p id="p-0001" num="0000">Crystalline forms of 4-methyl-N-3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide free base and salts thereof are prepared by various processes.</p>
>> read more

COMPOUNDS FOR INHIBITING THE INTERACTION OF BCL2 WITH BINDING PARTNERS (Fri, 28 Jun 2013)
The present invention relates to compounds of formula I: in which R1, R2, R3 and R4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases.
>> read more

COMPOUNDS FOR INHIBITING THE INTERACTION OF BCL2 WITH BINDING PARTNERS (Fri, 28 Jun 2013)
The present invention relates to compounds of formula (I) in which R1, R2, R3 and R4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases.
>> read more

COMPOUNDS FOR INHIBITING THE INTERACTION OF BCL2 WITH BINDING PARTNERS (Fri, 28 Jun 2013)
The present invention relates to compounds of formula I: in which R1, R2, R3 and R4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases.
>> read more

COMPOUNDS FOR INHIBITING THE INTERACTION OF BCL2 WITH BINDING PARTNERS (Fri, 28 Jun 2013)
The present invention relates to compounds of formula I: in which R1, R2, R3 and R4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases.
>> read more

COMPOUNDS FOR INHIBITING THE INTERACTION OF BCL2 WITH BINDING PARTNERS (Fri, 28 Jun 2013)
The present invention relates to compounds of formula I: in which R1, R2, R3 and R4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases.
>> read more

DIHYDRO-BENZO-OXAZINE AND DIHYDRO-PYRIDO-OXAZINE DERIVATIVES (Fri, 28 Jun 2013)
The invention relates to dihydro-benzo-oxazine and dihydro-pyrido-oxazine compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein Y, V, W, U, Q, R1, R5, R7 and R30 are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
>> read more

QUINOLINE DERIVATIVES (Fri, 28 Jun 2013)
The invention relates to quinoline compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein Y, W, U, Q, R1, R5 R7 and R30 are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
>> read more

Amorphous form of beta- L-2'-deoxythymidine (Thu, 27 Jun 2013)
Amorphous forms of beta-L-2'-deoxythymidine are disclosed that can be characterized by physical appearance, purity levels, Infra-Red and Raman spectroscopy, X-ray powder diffraction patterns, thermal properties, and methods of manufacture. These forms of beta-L-2'-deoxythymidine can be used in the manufacture of other forms of beta-L-2'-deoxythymidine, or in pharmaceutical compositions. Particularly preferred use is the treatment of hepatitis B.
>> read more

PROCESS FOR THE PREPARATION OF INTERMEDIATES FOR THE MANUFACTURE OF NEP INHIBITORS (Fri, 21 Jun 2013)
<p id="p-0001" num="0000">The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, or acid ester, backbone, such as N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.</p>
>> read more

NEW PROCESS FOR THE PREPARATION OF INTERMEDIATES USEFUL FOR THE MANUFACTURE NEP INHIBITORS (Fri, 21 Jun 2013)
<p id="p-0001" num="0000">The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising -amino- -biphenyl- -methylalkanoic acid, or acid ester, backbone, such as N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.</p>
>> read more

Substituted indole derivatives (Fri, 21 Jun 2013)
<p id="p-0001" num="0000">The present invention relates to substituted indole derivatives, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.</p>
>> read more

Use of inhibitors of the activity or function of PI3K (Fri, 21 Jun 2013)
The invention relates to new uses of PI3K inhibitors, wherein said inhibitors have an inhibitory action on the PI3K isoform delta for the treatment of immunopathology in a subject suffering from a disease or disorder selected from malaria, leishmaniasis, trypanosomiasis, toxoplasmosis and/or neurocysticercosis, via functional inhibition of TLR9 of the infected subject.
>> read more

METHOD OF DETECTING THE PRESENCE OF AN ANTIBODY IN A SAMPLE (Fri, 21 Jun 2013)
Methods for detecting in a sample the presence of an antibody to a conjugate of an antigen associated with a first carrier by a first association are disclosed. The method comprises contacting a conjugate of the antigen associated with a second carrier by a second association with said sample under conditions that allow binding of the antibody to the antigen; and introducing an agent to detect the presence of the antibody bound to said antigen. The first association and the second association are covalent associations and the first association is different from the second association. Also provided are kits, multiwell plates and conjugates that are useful in the method and further uses of the method. Also provided is a method of releasing a batch of a vaccine comprising a conjugate of an antigen associated with a first carrier by a first association and antibodies useful in this method.
>> read more

CONTACT LENSES WITH ENZYMATICALLY DEGRADABLE COATINGS THEREON (Fri, 14 Jun 2013)
<p id="p-0001" num="0000">The invention is related to a disposable contact lens comprising a top coating which is made of a hydrophilic polymeric material including dangling hydrophilic polymer chains covalently linked to the hydrophilic polymeric material through oligo-caprolactone linkages susceptible to enzymatic degradation in the eyes. The top coating is stable to lens processing/storage and confers lubricity to the lens. However, it slowly is degraded during the lens wear due to the action of enzymes (e.g., Lipase) in tear film. The loss in lubricity will be experienced as a drop in comfort for the lens wearer and thereby serves as the built-in compliance features of the disposable contact lens.</p>
>> read more

ADJUVANTING MENINGOCOCCAL FACTOR H BINDING PROTEIN (Fri, 14 Jun 2013)
<p id="p-0001" num="0000">Factor H binding protein (fHBP) has been proposed for use in immunising against serogroup B meningococcus (‘MenB’). This antigen can be efficiently adsorbed to an aluminium hydroxyphosphate adjuvant by (i) ensuring that adsorption takes place at a pH which is equal to or below the adjuvant's point of zero charge (PZC), and/or (ii) selecting a fHBP and adjuvant with an isoelectric point/PZC within the range of 5.0 to 7, and/or (iii) selecting a fHBP with an isoelectric point above the adjuvant's PZC and using a buffer to bring the pH to within 1.2 pH units of the PZC. The adsorption is particularly useful for compositions which include multiple fHBP variants, and also in situations where an aluminium hydroxide adjuvant should be avoided. Buffered pharmaceutical compositions can include at least two different meningococcal fHBP antigens, both of which are at least 85% adsorbed to aluminium hydroxyphosphate adjuvant.</p>
>> read more

PYRROLOPYRIMIDINE COMPOUNDS AS INHIBITORS OF CDK4/6 (Fri, 14 Jun 2013)
<p id="p-0001" num="0000">The invention is directed to novel pyrrolopyrimidine compounds of formula (I) wherein R<sup>1</sup>, R<sup>2Y</sup>, R<sup>4</sup>, R<sup>8</sup>-R<sup>11</sup>, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="43.18mm" wi="69.85mm" file="US20130150342A1-20130613-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> read more

ANTIBODIES FOR EPIDERMAL GROWTH FACTOR RECEPTOR 3 (HER3) DIRECTED TO DOMAIN III AND DOMAIN IV OF HER3 (Fri, 14 Jun 2013)
The present invention relates to antibodies or fragments thereof that bind to a non-linear epitope within domain 3 of the HER3 receptor and inhibit both ligand-dependent and ligand-independent signal transduction. The invention also relates antibodies or fragments thereof that bind to amino acid residues within domains 3-4 of HER3 and inhibit both ligand-dependent and ligand-independent signal transduction; and compositions and methods of use of such antibodies or fragments thereof.
>> read more

CYCLIC UREA DERIVATIVES AS ANDROGEN RECEPTOR ANTAGONISTS (Fri, 14 Jun 2013)
The present invention is directed to compounds of formula (I) wherein R1, R2, R3, and A are defined herein. The present invention also provides for pharmaceutical compositions comprising a compound of formula (I) as well as to the use of such compounds as androgen receptor antagonists for the treatment of diseases and conditions mediated by the androgen receptor, such as prostate cancer.
>> read more

COMPOSITIONS AND METHODS FOR ENHANCED GENERATION OF HEMATOPOIETIC STEM/PROGENITOR CELLS (Fri, 14 Jun 2013)
The present invention relates to methods, kits and compositions for expansion of hematopoietic stem/progenitor cells and providing hematopoietic function to human patients in need thereof. In one aspect, it relates to kits and compositions comprising a Notch agonist and an aryl hydrocarbon receptor antagonist. Also provided herein are methods for expanding the hematopoietic stem/progenitor cells using kits and compositions comprising a Notch agonist and an aryl hydrocarbon receptor antagonist. The hematopoietic stem/progenitor cells expanded using the disclosed kits, compositions and methods include human umbilical cord blood stem/progenitor cells, placental cord blood stem/progenitor cells and peripheral blood stem cells. The present invention also relates to administering hematopoietic stem/progenitor cells expanded using a combination of a Notch agonist and an aryl hydrocarbon receptor antagonist to a patient for short-term and/or long-term in vivo repopulation benefits.
>> read more

ANTIBODIES FOR EPIDERMAL GROWTH FACTOR RECEPTOR 3 (HER3) (Fri, 14 Jun 2013)
This invention relates to antibodies or fragments thereof which interact with HER family of receptors, e.g., HER3 receptor. In particular, it relates to antibodies or fragments thereof that recognize a conformational epitope of HER3 receptor comprising residues from both domains 2 and 4 resulting in inhibition of both ligand-dependent and ligand-independent signal transduction; and allow ligand binding (e.g., neuregulin), whilst preventing ligand-induced activation of signal transduction. These antibodies or fragments can be used to treat a number of diseases or disorders characterized by increased levels of HER3 expression (e.g., esophageal cancer). These antibodies or fragments can be used to treat a number of diseases or disorders characterized by the antibodys or fragments ability to decrease tissue weight (e.g., prostate or uterine weights) or to induce atrophy of tissue (e.g., atrophy of male breast). Alternatively, these antibodies or fragments can be used to treat a disorder characterized by increased levels of HER3 expression in an esophageal tract, gastric cancer or head and neck cancer.
>> read more

CONTACT LENSES WITH ENZYMATICALLY DEGRADABLE COATINGS THEREON (Fri, 14 Jun 2013)
The invention is related to a disposable contact lens comprising a top coating which is made of a hydrophilic polymeric material including dangling hydrophilic polymer chains covalently linked to the hydrophilic polymeric material through oligo-caprolactone linkages susceptible to enzymatic degradation in the eyes. The top coating is stable to lens processing/storage and confers lubricity to the lens. However, it slowly is degraded during the lens wear due to the action of enzymes (e.g., Lipase) in tear film. The loss in lubricity will be experienced as a drop in comfort for the lens wearer and thereby serves as the built-in compliance features of the disposable contact lens.
>> read more

ANTIBODIES FOR EPIDERMAL GROWTH FACTOR RECEPTOR 3 (HER3) DIRECTED TO DOMAIN II OF HER3 (Fri, 14 Jun 2013)
The present invention relates to antibodies or fragments thereof that target an epitope of a HER3 receptor residing in domain 2 of the HER3 receptor to block both ligand-dependent and ligand-independent signal transduction and tumor growth; and compositions and methods of use thereof.
>> read more

CONJUGATED VI SACCHARIDES (Fri, 07 Jun 2013)
<p id="p-0001" num="0000">Two Vi conjugates have been prepared by carbodiimide-mediated synthesis, using adipic acid dihydrazide derivatized CRM<sub>197 </sub>(a non-toxic variant of diphtheria toxin) and tetanus toxoid, as carrier proteins.</p>
>> read more

NOVEL TRIFLUOROMETHYL-OXADIAZOLE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE (Fri, 07 Jun 2013)
The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or diabetes/metabolic syndrome via inhibition of HDAC4.
>> read more

Pyrazolopyrrolidine compounds (Fri, 07 Jun 2013)
The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
>> read more

Salts of 4-methyl N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide (Fri, 31 May 2013)
<p id="p-0001" num="0000">Salts of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide are prepared by various processes.</p>
>> read more

NUCLEIC ACIDS AND PROTEINS FROM STREPTOCOCCUS GROUPS A AND B (Fri, 24 May 2013)
<p id="p-0001" num="0000">The invention provides proteins from group B <i>streptococcus </i>(<i>Streptococcus agalactiae</i>) and group A <i>streptococcus </i>(<i>Streptococcus pyogenes</i>), including amino acid sequences and the corresponding nucleotide sequences. Data are given to show that the proteins are useful antigens for vaccines, immunogenic compositions, and/or diagnostics. The proteins are also targets for antibiotics.</p>
>> read more

BENZONAPTHYRIDINE COMPOSITIONS AND USES THEREOF (Fri, 17 May 2013)
<p id="p-0001" num="0000">The present invention generally relates to compositions comprising benzonapthyridine small molecule immune potentiators (SMIPs) that are capable of stimulating or modulating an immune response in a subject that has had pre- or post-exposure to a pathogen such as hemorrhagic fever virus. Also provided are methods of preparing and using the SMIP compositions of the invention.</p>
>> read more

2,3,5-Trisubstituted Thiophene Compounds and Uses Thereof (Fri, 17 May 2013)
<p id="p-0001" num="0000">The present invention provides a compound of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.69mm" wi="69.85mm" file="US20130123252A1-20130516-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.</p>
>> read more

CARRIER MOLECULE COMPRISING A SPR0096 AND A SPR2021 ANTIGEN (Fri, 17 May 2013)
The invention provides a conjugate comprising an antigen and a carrier molecule, wherein the carrier molecule comprises a spr0096 antigen and a spr2021 antigen. spr0096 and spr2021 are Streptococcus pneumoniae antigens. The conjugate may be used in a method for raising an immune response in a mammal, the method comprising administering the conjugate to the mammal. Also provided are pharmaceutical compositions, particularly vaccines, comprising the conjugate.
>> read more

TETRAHYDRO-PYRIDO-PYRIMIDINE DERIVATIVES (Thu, 16 May 2013)
The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R<sp>1</sp>, R<sp>2</sp> and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
>> read more

LOW DENSITY LIPOPROTEIN-RELATED PROTEIN 6 (LRP6) - HALF LIFE EXTENDER CONSTRUCTS (Sat, 11 May 2013)
The present invention relates to LRP6 constructs that bind to LRP6 receptor. The LRP6 constructs comprise at least one LRP6 binding moiety and a half-life extender molecule such that the LRP6 construct inhibit the Wnt signaling pathway without potentiation of the Wnt signal. The LRP6 constructs also have an increased half-life to provide more time for the therapeutic benefit.
>> read more

(Fri, 03 May 2013)

>> read more

Production of ophthalmic devices based on photo-induced step growth polymerization (Fri, 03 May 2013)
<p id="p-0001" num="0000">The invention provide a new lens curing method for making hydrogel contact lenses. The new lens curing method is based on actinically-induced step-growth polymerization. The invention also provides hydrogel contact lenses prepared from the method of the invention and fluid compositions for making hydrogel contact lenses based on the new lens curing method. In addition, the invention provide prepolymers capable of undergoing actinically-induced step-growth polymerization to form hydrogel contact lenses.</p>
>> read more

NOVEL PURINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE (Fri, 03 May 2013)
The invention relates to PI3K inhibitors of the formula (I) • in which all of the variables are as defined in the specification, to their preparation, to their medical use, in particular to their use in the treatment of cancer and neurodegenerative disorders, and to medicaments comprising them.
>> read more

IMIDAZOQUINOXALINE COMPOUNDS AS IMMUNOMODULATORS (Fri, 26 Apr 2013)
<p id="p-0001" num="0000">The invention provides novel compositions comprising imidazoquinoxaline compounds of formula (I) and analogs thereof. Also provided are methods of administering the compositions in an effective amount to enhance the immune response of a subject. Further provided are novel compositions and methods of administering the compositions in combination with (an) other agent(s).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.46mm" wi="30.90mm" file="US20130101622A1-20130425-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> read more

HOMOGENOUS SUSPENSION OF IMMUNOPOTENTIATING COMPOUNDS AND USES THEREOF (Fri, 26 Apr 2013)
<p id="p-0001" num="0000">The present invention generally relates to homogeneous suspensions of small molecule immune potentiators (SMIPs) that are capable of stimulating or modulating an immune response in a subject in need thereof. The homogeneous suspensions may be used in combinations with various antigens or adjuvants for vaccine therapies.</p>
>> read more

Pyrido[2,3-b]pyrazine compounds useful as IP receptor agonist (Fri, 26 Apr 2013)
<p id="p-0001" num="0000">The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed. Examples of compounds of the invention include the compounds according to Formula Ia, or a pharmaceutically acceptable salt thereof, and the compounds of the examples.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.69mm" wi="55.71mm" file="US08754085-20140617-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> read more

QUINAZOLINE DERIVATIVES AS PI3K MODULATORS (Fri, 26 Apr 2013)
The invention relates to substituted quinazoline derivative of the formula (I), wherein A, X1, X2, X3, X4 and R5 are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
>> read more

Small molecule immunopotentiators and assays for their detection (Thu, 25 Apr 2013)
The invention provides immunostimulatory compositions comprising a small molecule immuno-potentiator (SMIP) compound and methods of administration thereof. Also provided are methods of administering a SMIP compound in an effective amount to enhance the immune response of a subject to an antigen. Further provided are novel compositions and methods of administering SMIP compounds alone or in combination with another agent for the treatment of cancer, infectious diseases and/or allergies/asthma. In a further aspect, the invention relates generally to methods of screening for small molecule immuno-modulatory compositions.
>> read more

METHOD FOR MAKING UV-ABSORBING OPHTHALMIC LENSES (Fri, 19 Apr 2013)
<p id="p-0001" num="0000">Described herein is a cost-effective and time-efficient method for making UV-absorbing contact lenses. In contrast to the conventional method for making UV-absorbing contact lenses which involves copolymerizing a lens forming composition including a UV-absorbing vinylic monomer, a method of the invention involves dipping a contact lens in a solution of UV-absorbing polymer comprising carboxyl-containing monomeric units and UV-absorbing monomeric units to form a UV-absorbing coating on the contact lens.</p>
>> read more

ArylSulfonamide Based Matrix Metalloprotease Inhibitors (Fri, 19 Apr 2013)
<p id="p-0001" num="0000">The present invention provides a compound of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="36.32mm" wi="52.41mm" file="US20130096105A1-20130418-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.</p>
>> read more

IMIDAZOQUINOLINE COMPOUNDS (Fri, 19 Apr 2013)
<p id="p-0001" num="0000">The invention provides novel compositions comprising imidazoquinoline compounds. Also provided are methods of administering the compositions in an effective amount to enhance the immune response of a subject. Further provided are novel compositions and methods of administering the compositions in combination with (an)other agent(s).</p>
>> read more

SUBSTITUTED AMINOPROPIONIC DERIVATIVES AS NEPRILYSIN INHIBITORS (Fri, 19 Apr 2013)
<p id="p-0001" num="0000">The present invention provides a compound of formula I′;</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.44mm" wi="69.68mm" file="US20130096127A1-20130418-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, wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>5</sup>, B<sup>1</sup>, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.</p>
>> read more

HETEROARYL COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS (Fri, 19 Apr 2013)
<p id="p-0001" num="0000">The present invention provides compounds of Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="16.43mm" wi="50.46mm" file="US20130096149A1-20130418-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, and X are as defined herein. The compounds of Formula (I) and pharmaceutical compositions thereof are useful for the treatment of cancer, and B-Raf-associated diseases.</li> </ul> </li> </ul> </p>
>> read more

Process for preparation of optically active compounds using transfer hydrogenation (Fri, 19 Apr 2013)
<p id="p-0001" num="0000">A catalytic process for the preparation of optically active compounds and their conversion thereafter to desired drug substances. In particular, the process relates to the preparation of (S)-3-(1-Dimethylamino-ethyl)-phenol using asymmetric catalytic reduction and transfer hydrogenation, thereby providing an improved route to forming drug substances such as rivastigimine and rivastigimine hydrogen tartrate.</p>
>> read more

Substituted carbamoylmethylamino acetic acid derivatives as novel NEP inhibitors (Fri, 19 Apr 2013)
<p id="p-0001" num="0000">The present invention provides a compound of formula I;</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="41.23mm" wi="68.07mm" file="US08642635-20140204-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>, R<sup>6</sup>, A<sup>1</sup>, A<sup>2</sup>, X<sup>1</sup>, s and m are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. </p>
>> read more

NOVEL OXAZINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE (Fri, 19 Apr 2013)
The invention relates to novel oxazine derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.
>> read more

METHOD FOR MAKING UV-ABSORBING OPHTHALMIC LENSES BY COATING (Fri, 19 Apr 2013)
Described herein is a cost-effective and time-efficient method for making UV-absorbing contact lenses. In contrast to the conventional method for making UV-absorbing contact lenses which involves copolymerizing a lens forming composition including a UV-absorbing vinylic monomer, a method of the invention involves dipping a contact lens in a solution of UV-absorbing polymer comprising carboxyl-containing monomeric units and UV-absorbing monomeric units to form a UV-absorbing coating on the contact lens.
>> read more

BIPHENYL SUBSTITUTED 1,3-DIHYDRO-BENZOIMIDAZOL-2-YLIDENEAMINE DERIVATIVES (Fri, 12 Apr 2013)
<p id="p-0001" num="0000">The invention relates to new derivatives of formula (I),</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="36.32mm" wi="69.85mm" file="US20130090342A1-20130411-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of one or more IGF-1R mediated disorders or diseases.</p>
>> read more

CARBAMATE/ UREA DERIVATIVES CONTAINING PIPERIDIN AND PIPERAZIN RINGS AS H3 RECEPTOR INHIBITORS (Fri, 12 Apr 2013)
The invention relates to compound of the formula I (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation and to medicaments comprising it for traeting diseases connected to tehinhibition of H3 receptor.
>> read more

PIPERIDINYL SUBSTITUTED 1,3-DIHYDRO-BENZOIMIDAZOL-2-YLIDENEAMINE DERIVATIVES (Fri, 05 Apr 2013)
<p id="p-0001" num="0000">The invention relates to new derivatives of formula (I),</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="34.04mm" wi="69.85mm" file="US20130085161A1-20130404-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of one or more IGF-1R mediated disorders or diseases.</p>
>> read more

3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES AS INHIBITORS OF MUTANT IDH (Fri, 05 Apr 2013)
The invention is directed to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R6 are defined herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formual (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.
>> read more

6 - SUBSTITUTED 3 - (QUINOLIN- 6 - YLTHIO) - [1,2,4] TRIAZOLO [4, 3 -A] PYRADINES AS TYROSINE KINASE (Fri, 22 Mar 2013)
The invention relates to compounds of formula (I) and salts thereof: Formula (I) wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
>> read more

METHODS FOR MAKING SACCHARIDE-PROTEIN GLYCOCONJUGATES (Fri, 22 Mar 2013)
The invention provides a process for the reductive amination of a carbonyl group at the reducing terminus of a polysaccharide, wherein the reductive amination is carried out at a pH between 4 and 5. The invention also provides a process for preparing a conjugate of a polysaccharide and a carrier molecule, comprising the steps of: (a) coupling the polysaccharide to a linker, to form a polysaccharide-linker compound in which the free terminus of the linker is an ester group; and (b) reacting the ester group with a primary amine group in the carrier molecule, to form a polysaccharide-linker-carrier molecule conjugate in which the linker is coupled to the carrier molecule via an amide linkage. The invention also provides a process for reducing contamination of a polysaccharide-linker compound with unreacted linker, comprising a step of precipitating unreacted linker under aqueous conditions at a pH of less than 5. The invention also provides polysaccharide-linker-carrier molecule conjugates and intermediate compounds obtained or obtainable by these processes.
>> read more

Pyridine amide derivatives (Fri, 22 Mar 2013)
The present invention provides pyridine amide derivatives which re¬ store or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.
>> read more

PYRIDINE AMIDE DERIVATIVES (Fri, 22 Mar 2013)
The present invention provides pyridine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.
>> read more

PYRIDINE/PYRAZINE AMIDE DERIVATIVES (Fri, 22 Mar 2013)
The present invention provides pyridine/pyrazine amide derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed. Formula (I):
>> read more

HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF CYSTIC FIBROSIS (Fri, 22 Mar 2013)
The present invention provides pyridin-oxadiazole/thiadiazole derivatives of Formula I wherein A is N or CR 4a; and (ii) or (iii) which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.
>> read more

N-SUBSTITUTED HETEROCYCLYL CARBOXAMIDES (Fri, 22 Mar 2013)
A compound of Formula I and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, Ra, A, B, D and E are all as defined herein. The compounds modulate the activity of CFTR and are useful in the treatment of inflammatory or obstructive airways diseases or mucosal hydration, including, for example cystic fibrosis. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
>> read more

COMPOSITIONS AND METHODS OF USE FOR THERAPEUTIC LOW DENSITY LIPOPROTEIN - RELATED PROTEIN 6 (LRP6) MULTIVALENT ANTIBODIES (Fri, 15 Mar 2013)
<p id="p-0001" num="0000">The present disclosure relates to an antibody or antigen binding fragment having at least two receptor binding do mains for two different binding sites of LRP6 and compositions and methods of use thereof.</p>
>> read more

Imidazole derivatives as aldosterone synthase inhibitors (Fri, 15 Mar 2013)
<p id="p-0001" num="0000">The present invention provides a compound of formula (I) or pharmaceutically acceptable salt thereof, wherein the variables R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>7 </sup>and p are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="40.98mm" wi="69.85mm" file="US08575160-20131105-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> read more

PHARMACEUTICAL COMPOSITIONS COMPRISING AN AROMATASE INHIBITOR (Fri, 15 Mar 2013)
The present invention relates to low-dose pharmaceutical compositions comprising the aromatase inhibitor 4,4'-[fluoro-(1-H-1,2,4-triazol-1-yl)methylene]bisbenzonitrile, as the active ingredient in a suitable carrier. The present invention also relates to a process for their preparation and to their use as medicaments.
>> read more

USE OF AN AROMATASE INHIBITOR FOR THE TREATMENT OF HYPOGONADISM AND RELATED DISEASES (Fri, 15 Mar 2013)
This invention relates to a method of increasing testosterone levels and treating hypogonadism and related diseases with the aromatase inhibitor 4,4'-[fluoro-(1-H-1,2,4-triazol-1-yl)methylene]bisbenzonitrile. The present invention further relates to a method of increasing testosterone levels and treating hypogonadism and related diseases with the aromatase inhibitor 4,4'-[fluoro-(1-H-1,2,4-triazol-1-yl)methylene]bisbenzonitrile in a particular dosing regimen. The invention also relates to pharmaceutical compositions comprising said aromatase inhibitor 4,4'-[fluoro-(1-H-1,2,4-triazol-1-yl)methylene]bisbenzonitrile, optionally in combination with other active ingredients. Furthermore, the present invention relates to kits comprising said pharmaceutical compositions together with instructions how to administer them.
>> read more

BENZOTHIAZOLONE COMPOUND (Fri, 15 Mar 2013)
The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form(I) a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.
>> read more

COMPOSITIONS AND METHODS OF USE FOR THERAPEUTIC LOW DENSITY LIPOPROTEIN - RELATED PROTEIN 6 (LRP6) MULTIVALENT ANTIBODIES (Fri, 08 Mar 2013)
<p id="p-0001" num="0000">The present disclosure relates to antibodies targeting LRP6 and compositions and methods of use thereof.</p>
>> read more

COMPOUNDS AND COMPOSITIONS AS PDGFR KINASE INHIBITORS (Fri, 08 Mar 2013)
The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of PDGFR (PDGFRα, PDGFRβ) kinases or c-kit and PDGFR (PDGFRα, PDGFRβ) kinases.
>> read more

BICYCLIC HETEROCYCLE DERIVATIVES FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION (Fri, 08 Mar 2013)
Bicyclic heterocyclic derivatives of formula (I) useful in inhibiting PDGF receptor mediated biological activity. Wherein A is and R1, R1a, R2, R3, R4, R5, R6 and X are as defined herein.
>> read more

2 -AMINO-4 -(PYRIDIN-2-YL)-5, 6-DIHYDRO-4H-1, 3-OXAZINE DERIVATIVES AND THEIR USE AS BACE-1 AND/OR BACE - 2 INHIBITORS (Fri, 01 Mar 2013)
The invention relates to novel oxazine derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.
>> read more

UV-absorbers for ophthalmic lens materials (Fri, 22 Feb 2013)
<p id="p-0001" num="0000">Novel UV absorbing monomers are disclosed. The UV absorbers are particularly suitable for use in intraocular lens materials.</p>
>> read more

UV-ABSORBERS FOR OPHTHALMIC LENS MATERIALS (Fri, 22 Feb 2013)
Novel UV absorbing monomers are disclosed. The UV absorbers are particularly suitable for use in intraocular lens materials.
>> read more

JAK P13K/mTOR COMBINATION THERAPY (Fri, 15 Feb 2013)
Provided herein is a combination therapy comprising a JAK kinase inhibitor and a dual PBK/mTOR inhibitor, as well as methods of treating various cancers through the use of such a combination therapy.
>> read more

UV-absorbers for ophthalmic lens materials (Fri, 08 Feb 2013)
<p id="p-0001" num="0000">Dihydroxybenzotriazole UV absorbing compounds that are particularly useful in ophthalmic devices are disclosed.</p>
>> read more

Pharmaceutical Composition Comprising Cyclic Somatostatin Analogues (Fri, 08 Feb 2013)
<p id="p-0001" num="0000">The present invention describes parenteral pharmaceutical compositions comprising a somatostatin analogue and novel somatostatin analogues.</p>
>> read more

Aryl pyridine as aldosterone synthase inhibitors (Fri, 08 Feb 2013)
<p id="p-0001" num="0000">The present invention provides a compound of formula I;</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="40.81mm" wi="69.85mm" file="US08519142-20130827-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. </p>
>> read more

KALLIKREIN 7 MODULATORS (Fri, 01 Feb 2013)
<p id="p-0001" num="0000">The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.</p>
>> read more

Pyrirnidinyl aryl urea derivatives being FGF inhibitors (Fri, 01 Feb 2013)
<p id="p-0001" num="0000">The invention relates to heteroaryl aryl ureas of the formula IA,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.77mm" wi="65.45mm" file="US08759517-20140624-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein the radicals and symbols have the meanings as defined herein, the use of such compounds in the treatment of protein kinase dependent diseases; to pharmaceutical preparations comprising said heteroaryl aryl ureas, to processes for the manufacture of such novel compounds and to methods of treatment comprising the use of such heteroaryl aryl ureas. </p>
>> read more

PYRAZOLINE DERIVATIVES AND THEIR USE AS SELECTIVE ANDROGEN RECEPTOR MODULATORS (Fri, 01 Feb 2013)
The invention relates to a compound of formula (I) in free form or in pharmaceutically acceptable salt form (I), in which the substituents are as defined in the specification; to compounds of formula (I) for use as androgen receptor modulators. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
>> read more

TETRAHYDROPYRIDO-PYRIDINE AND TETRAHYDROPYRIDO-PYRIMIDINE COMPOUNDS AND USE THEREOF AS C5A RECEPTOR MODULATORS (Fri, 01 Feb 2013)
The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
>> read more

Crystalline forms of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide (Fri, 25 Jan 2013)
<p id="p-0001" num="0000">Crystalline forms of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide free base and salts thereof are prepared by various processes.</p>
>> read more

Peptidomimetic sulfamide compounds and antiviral uses thereof (Fri, 25 Jan 2013)
<p id="p-0001" num="0000">The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.</p>
>> read more

SALTS OF AZA-BICYCLIC DI-ARYL ETHERS AND METHODS TO MAKE THEM OR THEIR PRECURSORS (Fri, 25 Jan 2013)
The present invention relates to salts of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza- bicyclo[2.2.2]octane, to methods for making them or their precursors, to pharmaceutical compositions comprising them, and to their use as medicaments.
>> read more

SALTS OF AZA-BICYCLIC DI-ARYL ETHERS AND METHODS TO MAKE THEM OR THEIR PRECURSORS (Fri, 25 Jan 2013)
The present invention relates to salts of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza- bicyclo[2.2.2]octane, to methods for making them or their precursors, to pharmaceutical compositions comprising them, and to their use as medicaments.
>> read more

NOVEL 2-PIPERIDIN-1-YL-ACETAMIDE COMPOUNDS FOR USE AS TANKYRASE INHIBITORS (Fri, 25 Jan 2013)
The present invention provides for compounds of formula (I), wherein R1-R5 and L are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
>> read more

Heteroaryl derivatives as DGAT1 inhibitors (Thu, 24 Jan 2013)
The invention relates to compounds of formula (I): where A is selected from: and R 1 , R 2 , R 3 , R 4 , R 5 , R 10a , R 10b , M, Z, r and s are as defined in the description, useful for treating disorders mediated by acyl coA-diacylglycerol acyl transferase 1 (DGAT1), for example glucose tolerance, Type II diabetes or obesity. The invention also provides pharmaceutical compositions comprising such compounds.
>> read more

Substituted imidazole derivates (Fri, 18 Jan 2013)
<p id="p-0001" num="0000">The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds. The compounds of the invention have the following general formula:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="21.51mm" wi="31.41mm" file="US08735599-20140527-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> read more

4 - PIPERIDINYL COMPOUNDS FOR USE AS TANKYRASE INHIBITORS (Fri, 18 Jan 2013)
The present invention provides for compounds of formula (I).The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
>> read more

NOVEL PYRROLO PYRIMIDINE DERIVATIVES (Fri, 18 Jan 2013)
The present invention describes new pyrrolo pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel pyrrolo pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors.
>> read more

4-OXO-3,5,7,8-TETRAHYDRO-4H-PYRANO {4,3-D} PYRMINIDINYL COMPOUNDS FOR USE AS TANKYRASE INHIBITORS (Fri, 18 Jan 2013)
The present invention provides for compounds of formula (I) wherein R1 and R2 are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
>> read more

TYROSINE LIGATION PROCESS (Fri, 18 Jan 2013)
A process is provided for preparing a conjugate of Formula (I-A) or (I) comprising a polypeptide (or a protein) containing n number of tyrosine units, where n is an integer greater than or equal to 1, dispersed within the amino acid chain having an amino terminus end (A1) and an acid terminus end (A2) of the protein or polypeptide (either the amino or acid terminus end can be the at least one tyrosine unit) and having a weight average molecular weight equal to or greater than 10,000 Daltons (10 kDa), wherein the conjugate comprises a number m of tyrosine conjugates (modified tyrosine residues) as depicted in Formula (I-A) or (I), where m is at least one and is less than or equal to n: where X, Lg, L and R are as defined herein.
>> read more

NOVEL TRIFLUOROMETHYL-OXADIAZOLE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE (Fri, 18 Jan 2013)
The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, (I) in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or metabolic syndrome via inhibition of HDAC4.
>> read more

Heterobicyclic carboxamides as inhibitors for kinases (Fri, 11 Jan 2013)
<p id="p-0001" num="0000">The invention relates to novel organic compounds of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.44mm" wi="69.85mm" file="US08501756-20130806-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumor diseases and ocular neovascular diseases. </p>
>> read more

Phenylacetic acid derivatives (Fri, 11 Jan 2013)
<p id="p-0001" num="0000">Compounds of formula (I) pharmaceutically acceptable salts thereof; and pharmaceutically acceptable esters thereof; which are useful for the treatment of COX-2 dependent disorders.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="39.20mm" wi="69.85mm" file="US08586782-20131119-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> read more

Kinesin inhibitors as cancer therapeutics (Fri, 11 Jan 2013)
<p id="p-0001" num="0000">The invention provides novel compounds having a substituted imidazole ring, and methods of using such compounds for the treatment of certain disorders such as hematological cancers and solid tumors. The compounds of the invention are tri-substituted imidazole derivatives that inhibit KSP. These compounds are also useful for the treatment of drug resistant tumors, such as solid tumors that express elevated levels of P-glycoprotein.</p>
>> read more

Treating diseases mediated by blockade of the epithelial sodium channel with pyrazine-2-carboxamide derivatives (Fri, 11 Jan 2013)
<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="29.13mm" wi="69.85mm" file="US08697687-20140415-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in free or salt or solvate form, where R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6</sup>, R<sup>7</sup>, R<sup>8</sup>, R<sup>9</sup>, R<sup>10 </sup>and R<sup>11 </sup>have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described. </p>
>> read more

Crystalline forms of 4-methyl-n-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide free base (Thu, 10 Jan 2013)
Crystalline forms of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethylphenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide free base are prepared by various processes.
>> read more

Heterobicyclic carboxamides as inhibitors for kinases (Fri, 04 Jan 2013)
<p id="p-0001" num="0000">The invention relates to novel organic compounds of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.44mm" wi="67.39mm" file="US08486954-20130716-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumor diseases and ocular neovascular diseases. </p>
>> read more

Organic compounds (Fri, 04 Jan 2013)
<p id="p-0001" num="0000">The present invention relates to a compound of the formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.25mm" wi="73.74mm" file="US08497286-20130730-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R1, R2, R3, R4 and R5 are as defined in the specification, for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations a compound of that class; a method of treatment comprising administering a compound of that class and a method for its manufacture. </p>
>> read more

Heterobicyclic carboxamides as inhibitors for kinases (Fri, 04 Jan 2013)
<p id="p-0001" num="0000">The invention relates to novel organic compounds of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.90mm" wi="67.65mm" file="US08492393-20130723-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumour diseases and ocular neovascular diseases. </p>
>> read more

Heterobicyclic carboxamides as inhibitors for kinases (Fri, 04 Jan 2013)
<p id="p-0001" num="0000">The invention relates to novel organic compounds of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.53mm" wi="67.39mm" file="US08541432-20130924-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumour diseases and ocular neovascular diseases. </p>
>> read more

Squaramide derivatives as CXCR2 antagonist (Fri, 04 Jan 2013)
<p id="p-0001" num="0000">The present invention relates to compounds of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.57mm" wi="70.61mm" file="US08722925-20140513-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein X, R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4 </sup>and R<sup>5 </sup>are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described. </p>
>> read more

SOLID FORMS AND SALTS OF TETRAHYDRO-PYRIDO-PYRIMIDINE DERIVATIVES (Fri, 04 Jan 2013)
The invention relates to crystalline anhydrous forms, crystalline solvate forms and/or salt forms including crystalline salt forms of {(S)-3-[6-(6-methoxy-5-methyl-pyridin-3-yl)-5,6,7,8- tetrahydro-pyrido[4,3-d]pyrimidin-4-yloxy]-pyrrolidin-1-yl}-(tetrahydro-pyran-4-yl)-methanone or salt forms including crystalline salt forms of 1-{(S)-3-[6-(6-methoxy-5-trifluoromethyl- pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-ylamino]-pyrrolidin-1-yl}-propan-1-on; pharmaceutical compositions and combinations including these forms as well as to methods of using these forms, including their pharmaceutical compositions and combinations for the treatment of diseases.
>> read more

CYCLOHEXYL ISOQUINOLINONE COMPOUNDS (Fri, 28 Dec 2012)
The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
>> read more

3 - IMIDAZOLYL- INDOLES FOR THE TREATMENT OF PROLIFERATIVE DISEASES (Fri, 28 Dec 2012)
The invention relates to 3-heterocyclyl indolyl compounds capable of inhibiting the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively, said compounds having the formula (I), in which: R1, R2, R3 and R4 are as defined in the Summary of the Invention. Due to their activity, the compounds are useful in the treatment of various disorders and diseases mediated by the activity of MDM2 and/or MDM4, or variants thereof, such as inflammatory or proliferative diseases or in the protection of cells.
>> read more

HYDROXY SUBSTITUTED ISOQUINOLINONE DERIVATIVES (Fri, 28 Dec 2012)
The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
>> read more

Oxazine derivatives and their use in the treatment of neurological disorders (Wed, 26 Dec 2012)
<p id="p-0001" num="0000">The invention relates to novel heterocyclic compounds of the formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.65mm" wi="64.43mm" file="US08338413-20121225-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them. </p>
>> read more

Heterocyclic sulfonamide derivatives (Fri, 14 Dec 2012)
<p id="p-0001" num="0000">The present invention relates to compounds:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="102.45mm" wi="61.21mm" file="US08470878-20130625-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and pharmaceutically acceptable salts thereof. The compounds have been demonstrated as inhibitors of MEK and therefore may be useful in the treatment of hyperproliferative diseases like cancer and inflammation. </p>
>> read more

Aryl-pyridine derivatives as aldosterone synthase inhibitors (Fri, 14 Dec 2012)
<p id="p-0001" num="0000">The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5 </sup>and n are defined herein. The invention also relates to a method for manufacturing compounds of the invention, and their therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.60mm" wi="69.85mm" file="US08519134-20130827-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> read more

HETEROCYCLIC SULFONAMIDE DERIVATIVES (Fri, 14 Dec 2012)
The present invention relates to compounds (I) and pharmaceutically acceptable salts thereof. The compounds have been demonstrated as inhibitors of MEK and therefore may be useful in the treatment of hyperproliferative diseases like cancer and inflammation.
>> read more

SILICONE HYDROGEL LENSES WITH NANO-TEXTURED SURFACES (Fri, 14 Dec 2012)
The invention is related to a method for making a silicone hydrogel contact lens having a nano-textured surface which mimics the surface texture of cornea of human eye. A method of the invention comprises creating a prime coating having nano-textures through controlled imbibition and/or depositions of a reactive polymeric coating material and fixing the nano-textures by crosslinking a hydrophilic polymeric material onto the prime coating to form a crosslinked polymeric coating that perserves the nano-textures of the prime coating and provides a nano-textured surface to the contact lens.
>> read more

Salts of benzimidazolyl pyridyl ethers and formulations thereof (Fri, 07 Dec 2012)
<p id="p-0001" num="0000">Salts of benzimidazolyl pyridyl ethers are provided, particularly salts of {1-methyl-5-[2-(5-trifluoromethyl-1H-imidazol-2-yl)-pyridin-4-yloxy]-1H-benzoimidazol-2-yl}-(4-trifluoromethyl-phenyl)amine. Compositions and formulations including such salts and surfactants as well as methods of preparing such compositions and formulations are provided.</p>
>> read more

Quinoxaline carboxamide derivatives as protein tyrosine kinase inhibitors (Fri, 07 Dec 2012)
<p id="p-0001" num="0000">The invention relates to compounds of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.51mm" wi="74.51mm" file="US08536175-20130917-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein the substituens are as defined in the specification, in free form or in the form of a pharmaceutically acceptable salt, solvate, ester, N-oxide thereof; processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases. </p>
>> read more

Quinoxaline carboxamide derivatives as protein tyrosine kinase inhibitors (Fri, 07 Dec 2012)
<p id="p-0001" num="0000">The invention relates to compounds of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.89mm" wi="73.32mm" file="US08674099-20140318-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein the substituents are as defined in the specification, in free form or in the form of a pharmaceutically acceptable salt, solvate, ester, N-oxide thereof; processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases. </p>
>> read more

3-SPIROCYCLIC PIPERIDINE DERIVATIVES AS GHRELIN RECEPTOR AGONISTS (Fri, 07 Dec 2012)
The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor.
>> read more

Beta-2-adrenoreceptor agonists (Fri, 30 Nov 2012)
<p id="p-0001" num="0000">Compounds of formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.82mm" wi="69.85mm" file="US08436017-20130507-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in free or salt or solvate form, where </p> <p id="p-0003" num="0000">Ar is a group of formula</p> <p id="p-0004" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="20.57mm" wi="69.85mm" file="US08436017-20130507-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0005" num="0000">Y is carbon or nitrogen and R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6</sup>, R<sup>7</sup>, R<sup>8</sup>, R<sup>9</sup>, R<sup>10</sup>, X, n, p, q and r are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of obstructive or inflammatory airways diseases.</p>
>> read more

3-spirocyclic piperidine derivatives as ghrelin receptor agonists (Fri, 30 Nov 2012)
<p id="p-0001" num="0000">The invention relates to derivatives of formula (I),</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.38mm" wi="67.39mm" file="US08546416-20131001-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor. </p>
>> read more

VISIBLE LIGHT ABSORBERS FOR OPHTHALMIC LENS MATERIALS (Thu, 29 Nov 2012)
Azo compounds that block visible light are disclosed. These light absorbers are particularly suitable for use in intraocular lens materials.
>> read more

SUBSTITUTED INDOLE DERIVATIVES FOR THE TREATMENT OF IMMUNOLOGICAL DISORDERS (Fri, 23 Nov 2012)
The present invention relates to substituted indole derivatives, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. (I).
>> read more

Pyridazinyl derivatives as smo inhibitors (Fri, 16 Nov 2012)
<p id="p-0001" num="0000">The present invention relates to compounds of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="20.57mm" wi="73.66mm" file="US08481542-20130709-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">in which R11 and R12 are defined in the Summary of the Invention; capable of inhibiting the Hedgehog and Smo signaling pathway. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the diagnosis and treatment of pathologies relating to the Hedgehog and Smo signaling pathway, for example, tumor formation, cancer, neoplasia and non-malignant hyperproliferative disorders.</li> </ul> </li> </ul> </p>
>> read more

ANTIPYRETICS TO ENHANCE TOLERABILITY OF VESICLE-BASED VACCINES (Fri, 16 Nov 2012)
A method for immunising a human subject, wherein the subject receives (i) an immunogenic composition comprising bacterial vesicles and (ii) an antipyretic, and wherein the immunogenic composition and the antipyretic are administered to the subject within 24 hours of each other. Paracetamol significantly reducesfever rates without negatively affecting the immunogenicity either of a meningococcal vesicle vaccine or of concomitantly-administered antigens.
>> read more

Chimeric, hybrid and tandem polypeptides of meningococcal NMB1870 (Fri, 09 Nov 2012)
<p id="p-0001" num="0000">NMB1870 is a protein in <i>Neisseria meningitidis</i>. Three families of NMB1870 are known. To increase the ability of a NMB1870 protein to elicit antibodies that are cross-reactive between the families, NMB1870 is engineered. Sequences can be substituted from one NMB1870 family into the corresponding position in another family. Proteins of NMB1870 sequences from different families can be joined to each other.</p>
>> read more

PYRAZINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS (Thu, 08 Nov 2012)
The invention relates to novel heterocyclic compounds of the formula (I) in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.
>> read more

Pyridine and pyrazine derivative for the treatment of CF (Fri, 02 Nov 2012)
<p id="p-0001" num="0000">The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.</p>
>> read more

Processes for the manufacture of macrocyclic depsipeptides and new intermediates (Fri, 02 Nov 2012)
<p id="p-0001" num="0000">The invention relates to a method or process for the chemical manufacture of depsipeptides of the formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="44.53mm" wi="68.83mm" file="US08614289-20131224-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein the symbols have the meaning defined in the description, to new intermediates and their manufacture, as well as related invention embodiments. </p>
>> read more

17α-HYDROXYLASE/C17,20-LYASE INHIBITORS (Fri, 02 Nov 2012)
The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds of the present invention have been found to be useful as 17α-hydroxylase/C17,20-lyase inhibitors.
>> read more

DIAZA-SPIRO[5.5]UNDECANES AS OREXIN RECEPTOR ANTAGONISTS (Thu, 01 Nov 2012)
The invention relates to compound of the formula (I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
>> read more

DISUBSTITUTED HETEROARYL-FUSED PYRIDINES (Thu, 01 Nov 2012)
The invention relates to compound of the formula (I′) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
>> read more

PROCESSES FOR THE MANUFACTURE OF MACROCYCLIC DEPSIPEPTIDES AND NEW INTERMEDIATES (Sat, 27 Oct 2012)
The invention relates to a method or process for the chemical manufacture of depsipeptides of the formula (I), wherein the symbols have the meaning defined in the description, to new intermediates and their manufacture, as well as related invention embodiments.
>> read more

Site Search