BRISTOL-MYERS SQUIBB COMPANY Patent applications |
Patent application number | Title | Published |
20160130272 | CRYSTALLINE FORMS OF N,N-DICYCLOPROPYL-4-(1,5-DIMETHYL-1H-PYRAZOL-3-YLAMINO)-6-ETHYL-1-METHYL-- 1,6-DIHYDROIMIDAZO[4,5-D]PYRROLO[2,3-B]PYRIDINE-7-CARBOXIMIDE FOR THE TREATMENT OF MYELOPROLIFERATIVE DISORDERS - Crystalline form, Form N-2, of N,Ndicyclopropyl-4-(1,5-dimethyl-1Hpyrazol-3-ylamino)-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide (Compound I) is provided. Also provided are a pharmaceutical composition and an oral dosage form comprising Form N-2 of Compound I as well as a method of using the Form N-2 of Compound I in the treatment of myeloproliferative disorders, which include polycythaemia vera, thrombocythaemia and primary myelofibrosis. | 05-12-2016 |
20160039780 | BICYCLO [2.2.2] ACID GPR120 MODULATORS - The present invention provides compounds of Formula (I) or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments. | 02-11-2016 |
20160016960 | INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION - The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection. | 01-21-2016 |
20150376229 | TANGENTIAL FLOW FILTRATION BASED PROTEIN REFOLDING METHODS - Provided herein are methods for refolding proteins that are denatured. Exemplary methods comprise solubilizing the denatured protein with a denaturing agent, e.g., a chaotropic agent, and renaturing the protein using a buffer exchanging system, e.g., tangential flow filtration (TFF). | 12-31-2015 |
20150344480 | PYRAZOLE SUBSTITUTED IMIDAZOPYRAZINES AS CASEIN KINASE 1 D/E INHIBITORS - The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents. | 12-03-2015 |
20150336975 | COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION - The present disclosure provides a series of compounds of the formula (I) | 11-26-2015 |
20150329506 | 4,6-DIARYLAMINOTHIAZINES AS BACE1 INHIBITORS AND THEIR USE FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION - Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: (I) wherein R | 11-19-2015 |
20150322089 | QUINUCLIDINE, 1-AZABICYCLO[2.2.1]HEPTANE, 1-AZABICYCLO [3.2.1]OCTANE, and 1-AZABICYCLO[3.2.2]NONANE COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders. | 11-12-2015 |
20150299136 | LXR MODULATORS - Compounds, pharmaceutically acceptable salts, isomers, or prodrugs thereof, of the invention are disclosed, which are useful as modulators of the activity of liver X receptors (LXR). Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed. | 10-22-2015 |
20150284427 | MACROCYCLIC COMPOUNDS FOR INHIBITION OF INHIBITORS OF APOPTOSIS - There are disclosed compounds that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention. | 10-08-2015 |
20150284409 | Hepatitis C Virus Inhibitors - Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed. | 10-08-2015 |
20150283234 | COMBINATION OF ANTI-KIR AND ANTI-CTLA-4 ANTIBODIES TO TREAT CANCER - Provided are methods for clinical treatment of cancer (e.g., solid tumors or hematological malignancies) using an anti-KIR antibody in combination with an anti-CTLA-4 antibody. | 10-08-2015 |
20150218093 | PYRROLONE OR PYRROLIDINONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS - The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are melanin concentrating hormone receptor-1 (MCHR1) antagonists which may be used as medicaments. | 08-06-2015 |
20150203574 | ANTIBODIES TO IL-6 AND THEIR USES - Antibodies and antigen-binding portions thereof that bind to human IL-6 are provided. Also provided are nucleic acids encoding such antibodies and antigen binding portions, methods of making such antibodies and antigen binding portions, compositions comprising such antibodies or antigen binding portions, and uses of such antibodies or antigen binding portions. | 07-23-2015 |
20150183818 | PROCESS FOR PREPARING DIASTEREOMERICALLY ENRICHED PHOSPHORAMIDATE DERIVATIVES OF NUCLEOSIDE COMPOUNDS FOR TREATMENT OF VIRAL INFECTIONS - The present invention is directed to a process for preparing diastereomerically enriched nucleoside phosphoramidates having the formula I: | 07-02-2015 |
20150175641 | PHOSPHORAMIDIC ACID PRODRUGS OF 5-[5-PHENYL-4-(PYRIDIN-2-YLMETHYLAMINO)QUINAZOLIN-2-YL]PYRIDINE-3-SULFONA- MIDE - A compound of structural formula (I), wherein R is H or —PO3H or a pharmaceutically acceptable salt form thereof. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, I | 06-25-2015 |
20150125463 | CANCER IMMUNOTHERAPY BY DISRUPTING PD-1/PD-L1 SIGNALING - The disclosure provides a method for immunotherapy of a cancer patient, comprises administering to the patient an Ab that inhibits signaling from the PD-1/PD-L1 signaling pathway, or a combination of such Ab and an anti-CTLA-4 Ab. This disclosure also provides a method for immunotherapy of a cancer patient comprising selecting a patient who is a suitable candidate for immunotherapy based on an assessment that the proportion of cells in a test tissue sample from the patient that express PD-L1 on the cell surface exceeds a predetermined threshold level, and administering an anti-PD-1 Ab to the selected subject. The disclosure additionally provides rabbit mAbs that bind specifically to a cell surface-expressed PD-L1 antigen in a FFPE tissue sample, and an automated IHC method for assessing cell surface expression in FFPE tissues using the provided anti-PD-L1 Abs. | 05-07-2015 |
20150118244 | ANTI-TUMOR ANTIBODIES AS PREDICTIVE OR PROGNOSTIC BIOMARKERS OF EFFICACY AND SURVIVAL IN IPILIMUMAB-TREATED PATIENTS - Provided herein are prognostic and diagnostic methods and kits for use with the methods. For example, provided herein are methods for determining whether a subject having cancer will respond to a cancer treatment. For example, provided herein are methods for determining whether a subject having advanced melanoma will respond to a treatment with ipilimumab. Methods for determining the length of survival of cancer patients, e.g., melanoma patients, such as melanoma patients treated with ipilimumab, are also provided herein. | 04-30-2015 |
20150071914 | METHODS OF TREATMENT USING CTLA4 MUTANT MOLECULES - The present invention provides soluble CTLA4 mutant molecules which bind with greater avidity to the CD80 and/or CD86 antigen than wild type CTLA4 or non-mutated CTLA4Ig. The soluble CTLA4 molecules have a first amino acid sequence comprising the extracellular domain of CTLA4, where certain amino acid residues within the S25-R33 region and M97-G107 region are mutated. The mutant molecules of the invention may also include a second amino acid sequence which increases the solubility of the mutant molecule. | 03-12-2015 |
20150065505 | PYRIMIDINONE CARBOXAMIDE INHIBITORS OF ENDOTHELIAL LIPASE - The present invention provides compounds of Formula (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments. | 03-05-2015 |
20150051149 | FIBRONECTIN BINDING DOMAINS WITH REDUCED IMMUNOGENICITY - Fibronectin type III (10Fn3) binding domains having novel designs that are associated with reduced immunogenicity are provided. The application describes alternative 10Fn3 binding domains in which certain immunogenic regions are not modified when producing a binder in order to maintain recognition as a self antigen by the host organism. The application also describes 10Fn3 binding domains in which HLA anchor regions have been destroyed thereby reducing the immunogenic contribution of the adjoining region. Also provided are 10Fn3 domains having novel combinations of modified regions that can bind to a desired target with high affinity. | 02-19-2015 |
20150023976 | ANTIBODY POLYPEPTIDES THAT ANTAGONIZE CD40L - Antibody polypeptides that specifically bind human CD40L are provided. The antibody polypeptides do not activate platelets. The antibody polypeptides are useful in the treatment of diseases involving CD40L activation, such as graft-related diseases and autoimmune diseases. The antibody polypeptides may be domain antibodies (dAbs) comprising a single V | 01-22-2015 |
20140349929 | MULTIVALENT FIBRONECTIN BASED SCAFFOLD DOMAIN PROTEINS - The present invention relates to multivalent polypeptides comprising at least two fibronectin scaffold domains connected via a polypeptide linker. The invention also relates to multivalent polypeptides for use in diagnostic, research and therapeutic applications. The invention further relates to cells comprising such proteins, polynucleotide encoding such proteins or fragments thereof, and to vectors comprising the polynucleotides encoding the innovative proteins. | 11-27-2014 |
20140335178 | DOSAGE FORMS OF APIXABAN - The present invention relates to a Factor Xa inhibitor dosage form comprising apixaban in a solubility-improved form wherein the dosage form provides controlled release of apixaban and methods for preventing or treating venous thromboembolisms, deep vein thrombosis and acute coronary syndrome with said dosage form. | 11-13-2014 |
20140335170 | Reduced Mass Metformin Formulations - The present invention relates to metformin extended release (XR) formulations with improved compactability to provide reduced mass tablets, granulations, and capsules. | 11-13-2014 |
20140309229 | METHODS FOR SELECTING AND TREATING CANCER IN PATIENTS WITH IGF-1R/IR INHIBITORS - The present invention relates generally to the field of pharmacogenomics, and more specifically to methods and procedures to determine drug sensitivity in patients to allow the identification of individualized genetic profiles which will aid in selecting cancer patients that are responsive to IGF-1R/IR inhibition. | 10-16-2014 |
20140273094 | METHODS OF ENHANCING PROTEIN QUALITY AND QUANTITY BY YEAST FED-BATCH FERMENTATION - The present invention describes a method for producing an antibody in | 09-18-2014 |
20140273093 | METHODS OF PRODUCING ANTIBODIES IN YEAST - The present invention describes a method for producing an antibody in | 09-18-2014 |
20140243524 | ARYL- AND HETEROARYL-SUBSTITUTED TETRAHYDROISOQUINOLINES AND USE THEREOF TO BLOCK REUPTAKE OF NOREPINEPHRINE, DOPAMINE, AND SEROTONIN - The compounds of the present invention are represented by the chemical structure found in Formula (I): | 08-28-2014 |
20140235608 | PYRIDINEDIONE CARBOXAMIDE INHIBITORS OF ENDOTHELIAL LIPASE - The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments. | 08-21-2014 |
20140235574 | ARIPIPRAZOLE COMPLEX FORMULATION AND METHOD - An aripiprazole formulation is provided which includes the antipsychotic agent aripiprazole in the form of an inclusion complex in a β-cyclodextrin, preferably, sulfobutyl ether β-cyclodextrin (SBECD), which in the form of an injectable produces reversible generally minimal to mild irritation at the intramuscular injection site. A method for minimizing or reducing irritation caused by aripiprazole at an intramuscular injection site and a method for treating schizophrenia employing the above formulation are also provided. | 08-21-2014 |
20140221484 | GENETIC POLYMORPHISMS ASSOCIATED WITH CARDIOVASCULAR DISORDERS AND DRUG RESPONSE, METHODS OF DETECTION AND USES THEREOF - The present invention is based on the discovery of genetic polymorphisms that are associated with cardiovascular disorders, particularly acute coronary events such as myocardial infarction and stroke, and genetic polymorphisms that are associated with responsiveness of an individual to treatment of cardiovascular disorders with statin. In particular, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by such nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and proteins, and methods of using the nucleic acid and proteins as well as methods of using reagents for their detection. | 08-07-2014 |
20140221357 | PYRROLINONE CARBOXAMIDE COMPOUNDS USEFUL AS ENDOTHELIAL LIPASE INHIBITORS - The present invention provides compounds of Formula (I) or Formula (III): [INSERT CHEMICAL STRUCTURE HERE] (I) [INSERT CHEMICAL STRUCTURE HERE] (III) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments. | 08-07-2014 |
20140221338 | NOVEL MACROCYCLES AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (Ia): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same. | 08-07-2014 |
20140213588 | PYRROLINONE CARBOXAMIDE COMPOUNDS USEFUL AS ENDOTHELIAL LIPASE INHIBITORS - The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments. The disclosure also provides a novel method of treating diseases or conditions related to the activity of endothelial lipase by use of compounds according to Formula (II): as defined in the specification and compositions comprising any of the compounds. | 07-31-2014 |
20140194598 | B7-RELATED NUCLEIC ACIDS AND POLYPEPTIDES USEFUL FOR IMMUNOMODULATION - The present invention provides nucleic acids encoding B7-related factors that modulate the activation of immune or inflammatory response cells, such as T-cells. Also provided are expression vectors and fusion constructs comprising nucleic acids encoding B7-related polypeptides, including BSL1, BSL2, and BSL3. The present invention further provides isolated B7-related polypeptides, isolated fusion proteins comprising B7-related polypeptides, and antibodies that are specifically reactive with B7-related polypeptides, or portions thereof. In addition, the present invention provides assays utilizing B7-related nucleic acids, polypeptides, or peptides. The present invention further provides compositions of B7-related nucleic acids, polypeptides, fusion proteins, or antibodies that are useful for the immunomodulation of a human or animal subject. | 07-10-2014 |
20140193438 | ENEDIYNE COMPOUNDS, CONJUGATES THEREOF, AND USES AND METHODS THEREFOR - Enediyne compounds having a structure according to formula (I), where R | 07-10-2014 |
20140193430 | COMPOSITIONS AND METHODS FOR REGULATING NK CELL ACTIVITY - The present invention relates to novel compositions and methods for regulating an immune response in a subject. More particularly, the invention relates to specific antibodies that regulate the activity of NK cells and allow a potentiation of NK cell cytotoxicity in mammalian subjects. The invention also relates to fragments and derivatives of such antibodies, as well as pharmaceutical compositions comprising the same and their uses, particularly in therapy, to increase NK cell activity or cytotoxicity in subjects. | 07-10-2014 |
20140187488 | METHODS FOR MAINTAINING PEGYLATION OF POLYPEPTIDES - Described herein are methods for maintaining PEGylation and inhibiting dePEGylation of polypeptides, such as fibronectin-based scaffold proteins, during storage. | 07-03-2014 |
20140179896 | INHIBITORS OF TYPE 2 VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTORS - The present disclosure relates to novel vascular endothelial growth factor receptor (VEGFR)-binding polypeptides and methods for using these polypeptides to inhibit biological activities mediated by vascular endothelial growth factors (VEGFs). The present disclosure also provides various improvements relating to single domain binding polypeptides. | 06-26-2014 |
20140179711 | PROCESS FOR PREPARING 2-AMINOTHIAZOLE-5-AROMATIC CARBOXAMIDES AS KINASE INHIBITORS - The invention relates to processes for preparing compounds having the formula, | 06-26-2014 |
20140179551 | METHODS FOR THE SELECTION OF BINDING PROTEINS - This application provides an improved screening method for the selection of target-binding proteins having desirable biophysical properties. The method combines mRNA display and yeast surface display in a way that takes advantage of the desirable attributes of both processes. | 06-26-2014 |
20140163081 | LXR MODULATORS - Compounds, pharmaceutically acceptable salts, isomers, or prodrugs thereof, of the invention are disclosed, which are useful as modulators of the activity of liver X receptors (LXR). Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed. | 06-12-2014 |
20140163002 | CYCLIC P1 LINKERS AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same. | 06-12-2014 |
20140161808 | ANTIBODIES THAT BIND NOVEL PCSK9 VARIANTS - The present invention provides novel polynucleotides encoding PCSK9b and PCSK9c polypeptides, fragments and homologues thereof. Also provided are vectors, host cells, antibodies, and recombinant and synthetic methods for producing said polypeptides. The invention further relates to diagnostic and therapeutic methods for applying these novel PCSK9b and PCSK9c polypeptides to the diagnosis, treatment, and/or prevention of various diseases and/or disorders related to these polypeptides. The invention further relates to screening methods for identifying agonists and antagonists of the polynucleotides and polypeptides of the present invention. | 06-12-2014 |
20140154268 | ALPHA5-BETA1 ANTIBODIES AND THEIR USES - The present disclosure provides isolated monoclonal antibodies, particularly human monoclonal antibodies, or antigen binding portions thereof, that specifically bind to integrin α5β1 with high affinity. Nucleic acid molecules encoding the antibodies of the disclosure, expression vectors, host cells and methods for expressing the antibodies of the disclosure are also provided. Immunoconjugates, bispecific molecules and pharmaceutical compositions comprising the antibodies or antigen binding portions thereof are also provided. The disclosure also provides methods for treating various cancers using the anti-α5β1 antibodies or antigen binding portions thereof described herein. | 06-05-2014 |
20140141024 | COMBINATION OF ANTI-CTLA4 ANTIBODY WITH DIVERSE THERAPEUTIC REGIMENS FOR THE SYNERGISTIC TREATMENT OF PROLIFERATIVE DISEASES - Compositions and methods are disclosed which are useful of the treatment and prevention of proliferative disorders. | 05-22-2014 |
20140135318 | SUBSTITUTED SULFONAMIDES USEFUL AS ANTIAPOPTOTIC BCL INHIBITORS - Disclosed are compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein: W and Q and G are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bcl-2 family antiapoptotic proteins for the treatment of cancer; and pharmaceutical compositions comprising such compounds. | 05-15-2014 |
20140128365 | PYRIDONE/HYDROXYPYRIDINE 11-BETA HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS - Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: | 05-08-2014 |
20140121155 | Crystal Forms of Saxagliptin and Processes for Preparing Same - Physical crystal structures of a compound of the formula I: | 05-01-2014 |
20140120163 | COATED TABLET FORMULATION AND METHOD - A coated tablet formulation is provided which includes a medicament such as the DPP4-inhibitor, saxaglipitin | 05-01-2014 |
20140113892 | LACTAM-CONTAINING COMPOUNDS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS - The present application describes lactam-containing compounds and derivatives thereof of Formula I: | 04-24-2014 |
20140113370 | FC FUSION PROTEINS COMPRISING NOVEL LINKERS OR ARRANGEMENTS - The application provides Fc fusion proteins having novel arrangements. In one embodiment, the application provides Fc fusion proteins comprising a | 04-24-2014 |
20140107020 | FIBRONECTIN BASED SCAFFOLD DOMAIN PROTEINS THAT BIND TO MYOSTATIN - The present invention relates to fibronectin-based scaffold domain proteins that bind to myostatin. The invention also relates to the use of these proteins in therapeutic applications to treat muscular dystrophy, cachexia, sarcopenia, osteoarthritis, osteoporosis, diabetes, obesity, COPD, chronic kidney disease, heart failure, myocardial infarction, and fibrosis. The invention further relates to cells comprising such proteins, polynucleotides encoding such proteins or fragments thereof, and to vectors comprising the polynucleotides encoding the proteins. | 04-17-2014 |
20140105896 | FIBRONECTIN BASED SCAFFOLD DOMAIN PROTEINS THAT BIND TO MYOSTATIN - The present invention relates to fibronectin-based scaffold domain proteins that bind to myostatin. The invention also relates to the use of these proteins in therapeutic applications to treat muscular dystrophy, cachexia, sarcopenia, osteoarthritis, osteoporosis, diabetes, obesity, COPD, chronic kidney disease, heart failure, myocardial infarction, and fibrosis. The invention further relates to cells comprising such proteins, polynucleotides encoding such proteins or fragments thereof, and to vectors comprising the polynucleotides encoding the proteins. | 04-17-2014 |
20140100365 | BISFLUOROALKYL-1,4-BENZODIAZEPINONE COMPOUNDS - Disclosed are compounds of Formula (I) or prodrugs thereof; | 04-10-2014 |
20140099707 | ANTIBODY POLYPEPTIDES THAT ANTAGONIZE CD40L - Antibody polypeptides that specifically bind human CD40L are provided. The antibody polypeptides do not activate platelets. The antibody polypeptides are useful in the treatment of diseases involving CD40L activation, such as graft-related diseases and autoimmune diseases. The antibody polypeptides may be domain antibodies (dAbs) comprising a single V | 04-10-2014 |
20140099317 | ANTIBODY POLYPEPTIDES THAT ANTAGONIZE CD40 - Antibody polypeptides that specifically bind a novel epitope of human CD40 are provided. The antibody polypeptides do not exhibit CD40 agonist activity. The antibody polypeptides are useful in the treatment of diseases involving CD40 activation, such as autoimmune diseases. The antibody polypeptides may be domain antibodies (dAbs) comprising a single V | 04-10-2014 |
20140094595 | Protein Scaffolds for Antibody Mimics and Other Binding Proteins - Disclosed herein are proteins that include an immunoglobulin fold and that can be used as scaffolds. Also disclosed herein are nucleic acids encoding such proteins and the use of such proteins in diagnostic methods and in methods for evolving novel compound-binding species and their ligands. | 04-03-2014 |
20140093511 | OPTIMIZATION OF ANTIBODIES THAT BIND LYMPHOCYTE ACTIVATION GENE-3 (LAG-3), AND USES THEREOF - The present invention provides isolated monoclonal antibodies that specifically bind LAG-3, and have optimized functional properties compared to previously described anti-LAG-3 antibodies, such as antibody 25F7 (US 2011/0150892 A1). These properties include reduced deamidation sites, while still retaining high affinity binding to human LAG-3, and physical (i.e., thermal and chemical) stability. Nucleic acid molecules encoding the antibodies of the invention, expression vectors, host cells and methods for expressing the antibodies of the invention are also provided, as well as immunoconjugates, bispecific molecules and pharmaceutical compositions comprising the antibodies. The present invention also provides methods for detecting LAG-3, as well as methods for treating stimulating immune responses using an anti-LAG-3 antibody of the invention. Combination therapy, in which the antibodies are co-administered with at least one additional immunostimulatory antibody, is also provided. | 04-03-2014 |
20140088109 | N-((1R,2S,5R)-5-(TERT-BUTYLAMINO)-2-((S)-3-(7-TERT-BUTYLPYRAZOLO[1,5-A][1,- 3,5]TRIAZIN-4-YLAMINO)-2-OXOPYRROLIDIN-1-YL)CYCLOHEXYL)ACETAMIDE, A DUAL MODULATOR OF CHEMOKINE RECEPTOR ACTIVITY, CRYSTALLINE FORMS AND PROCESSES - The present invention provides a novel antagonist: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin -1-yl)cyclohexyl)acetamide: | 03-27-2014 |
20140079778 | Pharmaceutical Formulations Including An Amine Compound - The present invention relates to solid, semisolid, or liquid formulations comprising water soluble antioxidants that prevent or reduce formic acid and/or formyl species generation in the dosage form during the manufacturing process and/or during shelf-life storage. The formulations of the present invention prevent or reduce formation of N-formyl impurities (and gelatin crosslinking) during the manufacturing process and/or during shelf-life storage. | 03-20-2014 |
20140079702 | ANTAGONISTS OF IL-6 TO RAISE ALBUMIN AND/OR LOWER CRP - The present invention is directed to therapeutic methods using IL-6 antagonists such as antibodies and fragments thereof having binding specificity for IL-6 to improve survivability or quality of life of a patient in need thereof. In preferred embodiments these patients will comprise those exhibiting (or at risk of developing) an elevated serum C-reactive protein level or a reduced serum albumin level prior to treatment. In another preferred embodiment, the patient's Glasgow Prognostic Score will be increased and survivability will preferably be improved. | 03-20-2014 |
20140065164 | IP-10 ANTIBODY DOSAGE ESCALATION REGIMENS - In certain embodiments, the present invention provides a method of treating an IP10-related disease in a subject, comprising: (a) administering to the subject a predetermined dosage of an anti-IPIO antibody; (b) detecting the level of the anti-IPIO antibody in a sample of the subject; and (c) if the level of the anti-IPIO antibody from step (b) is below a threshold exposure level, increasing the dosage of the anti-IPIO antibody in the subject such that the IP-10 related disease in the subject is treated. | 03-06-2014 |
20140038893 | TARGETED THERAPEUTICS BASED ON ENGINEERED PROTEINS THAT BIND EGFR - The present invention relates to single domain proteins that bind to epidermal growth factor receptor (EGFR). The invention also relates to single domain proteins for use in diagnostic, research and therapeutic applications. The invention further relates to cells comprising such proteins, polynucleotide encoding such proteins or fragments thereof, and to vectors comprising the polynucleotides encoding the innovative proteins. | 02-06-2014 |
20140031337 | AZOLOTRIAZINONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS - The present application provides compounds that are useful as MCHR1 antagonists, especially for the treatment of obesity, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I | 01-30-2014 |
20140012007 | 4-PYRIDINONE COMPOUNDS AND THEIR USE FOR CANCER - Disclosed herein is a process for preparing a compound of Formula (I), comprising the steps of: (a) reacting an aniline compound of Formula (II) and an carboxylic acid compound of Formula (III) or an activated carboxylic acid compound thereof, to provide a compound of Formula (IV); and (b) converting said protected amine group attached to said compound of Formula (IV) to an amine group to provide said compound of Formula (I); wherein PAm is a protected amine group. Processes to prepare the compounds of Formulae (II), (III), and (IV) are also disclosed. | 01-09-2014 |
20140011700 | THREE-DIMENSIONAL STRUCTURE OF H1N1 NUCLEOPROTEIN IN COMPLEX WITH ANTIVIRAL COMPOUNDS - The binding mode of the antiviral compounds have been characterized through a variety of biophysical and structural studies, elaborating on the proposed aggregation mechanism of action. We demonstrate the direct binding of these antiviral compounds to NP using thermal shift enhancement assay (TSE) and NMR. In addition, we have completed a detailed analysis of the oligomerization mechanism of action using dynamic light scattering, analytical ultracentrifugation, and surface plasmon resonance (SPR). Structure determination using x-ray crystallography confirmed the proposed compound-induced oligomerization mechanism of action. The co-crystal structure revealed that two compounds bound in an anti-parallel fashion bridging two NP monomers, inducing a novel non-native NP oligomer. Taken together, our data suggest a complex binding mode in which the compounds bind NP specifically in stoichiometric fashion inducing the formation of an NP oligomer without obstructing the RNA binding pocket or interfering with the native NP homo-oligomerization. | 01-09-2014 |
20130345123 | SUBSTITUTED ADIPIC ACID AMIDES AND USES THEREOF - The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein A is a five to eight membered monocyclic or a nine to twelve membered bicyclic heterocyclic ring, as further defined herein; Y is S, CH | 12-26-2013 |
20130330406 | Bilayer Tablet Formulations - The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations. | 12-12-2013 |
20130315911 | BISPECIFIC ANTIBODIES AND METHODS OF USING THE SAME - The present invention relates to antagonizing the activity of IL-17A, IL-17F and IL-23 using bispecific antibodies that comprise a binding entity that is cross-reactive for IL-17A and IL-17F and a binding entity that binds IL-23p19. The present invention relates to novel bispecific antibody formats and methods of using the same. | 11-28-2013 |
20130310393 | SUBSTITUTED BENZIMIDAZOLE AND IMIDAZOPYRIDINE COMPOUNDS USEFUL AS CYP17 MODULATORS - Disclosed are heteroaryl compounds of Formula (I), (I), or pharmaceutically acceptable salts thereof, wherein Z is CH or N; W is CR | 11-21-2013 |
20130310317 | TARGETED THERAPEUTICS BASED ON ENGINEERED PROTEINS FOR TYROSINE KINASES RECEPTORS, INCLUDING IGF-IR - The present invention provides innovative proteins that bind to insulin-like growth factor-I receptor (IGF-IR), as well as other important proteins. The invention also provides innovative proteins in pharmaceutical preparations and derivatives of such proteins and the uses of same in diagnostic, research and therapeutic applications. The invention further provides cells comprising such proteins, polynucleotide encoding such proteins or fragments thereof, and vectors comprising the polynucleotides encoding the innovative proteins. | 11-21-2013 |
20130296325 | HIGH DRUG LOAD TABLET FORMULATION OF [(1R), 2S]-2-AMINOPROPIONIC ACID 2-[4-(4-FLUORO-2-METHYL-1H-INDOL-5-YLOXY)-5-METHYLPYRROLO[2,1-f][1,2,4]TR- IAZIN-6-YLOXY]-1-METHYLETHYL ESTER - The present invention is directed to a high drug load tablet formulation of [(1R),2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-1-methylethyl ester, and to methods of using the formulation in the treatment of cancer. The tablet is obtained by means of a wet granulation process. | 11-07-2013 |
20130288372 | FIBRONECTIN BASED SCAFFOLD DOMAIN PROTEINS THAT BIND IL-23 - The present invention relates to fibronectin based scaffold domain protein that bind interleukin 23 (IL-23). The invention also relates to the use of the innovative proteins in therapeutic applications to treat autoimmune diseases. The invention further relates to cells comprising such proteins, polynucleotide encoding such proteins or fragments thereof, and to vectors comprising the polynucleotides encoding the innovative proteins. | 10-31-2013 |
20130281657 | MACROCYCLES AND MACROCYCLE STABILIZED PEPTIDES - The invention provides methods of preparing macrocycles including macrocycle stabilized peptides (MSPs). Macrocycles and MSPs are prepared according to nucleophilic capture of an iminoquinomethide type intermediate generated from a suitably substituted 2-amino-thiazol-5-yl carbinol. The preferred nucleophile may be selected from an electron rich aromatic moiety in the case of macrocycles and, in the case of MSPs, at least one amino acid comprises an electron rich aromatic moiety. In addition, the concept can be extended to other related 5-membered heterocyclic systems in place of the thiazole, such as imidazole or oxazole. The conditions for the generation of the corresponding iminoquinomethide type intermediates may be similar or different than the conditions used for the 2-amino-thiazol-5-yl carbinol. | 10-24-2013 |
20130280266 | ANTIBODIES TO IL-6 AND THEIR USES - Antibodies and antigen-binding portions thereof that bind to human IL-6 are provided. Also provided are nucleic acids encoding such antibodies and antigen binding portions, methods of making such antibodies and antigen binding portions, compositions comprising such antibodies or antigen binding portions, and uses of such antibodies or antigen binding portions. | 10-24-2013 |
20130253023 | POLYCYCLIC LPA1 ANTAGONIST AND USES THEREOF - Described herein is the LPA1 antagonist 1-{4′-[3-methyl-4-((R)-1-phenyl-ethoxycarbonylamino)-isoxazol-5-yl]-bi-phenyl-4-yl}-cyclopropanecarboxylic acid (Compound 1), or pharmaceutically acceptable salts thereof. Also described are methods of preparing the LPA1 antagonist, or pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions suitable for administration to a mammal that include the LPA1 antagonist, or pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating LPA-dependent or LPA-mediated diseases or conditions. | 09-26-2013 |
20130251713 | METHODS FOR TREATING JUVENILE RHUMATOID ARTHRITIS BY ADMINISTERING A SOLUBLE CTLA4 MOLECULE - The present invention relates to compositions and methods for treating autoimmune diseases, such as juvenile rheumatoid arthritis, by administering to a subject a CTLA4 molecule that block endogenous B7 molecules from binding their ligands. | 09-26-2013 |
20130237555 | Aryl Ether-Base Kinase Inhibitors - The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1. | 09-12-2013 |
20130237499 | Inhibitors of Human Immunodeficiency Virus Replication - The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection. | 09-12-2013 |
20130231324 | SPIRO BICYCLIC DIAMINE DERIVATIVES AS HIV ATTACHMENT INHIBITORS - Compounds of Formula I, including pharmaceutically acceptable salts thereof: | 09-05-2013 |
20130230518 | METHODS FOR TREATING SJOGRENS SYNDROME BY ADMINISTERING A SOLUBLE CTLA4 MOLECULE - The present invention relates to compositions and methods for treating autoimmune diseases, such as Sjogren's syndrome, by administering to a subject a CTLA4 molecule that block endogenous B7 molecules from binding their ligands. | 09-05-2013 |
20130225636 | N-(5S,6S,9R)-5-AMINO-6-(2,3-DIFLUOROPHENYL)-6,7,8,9-TETRAHYDRO-5H-CYCLOHEP- TA[B]PYRIDIN-9-YL-4-(2-OXO-2,3-DIHYDRO-1H-IMIDAZO[4,5-B]PYRIDIN-1-YL)PIPER- IDINE-1-CARBOXYLATE SALT - Disclosed is a hemisulfate salt of Compound (I): | 08-29-2013 |
20130225635 | FUSED BICYCLIC DIAMINE DERIVATIVES AS HIV ATTACHMENT INHIBITORS - Compounds of Formula I, including pharmaceutically acceptable salts thereof: | 08-29-2013 |
20130225551 | JAK2 INHIBITORS AND THEIR USE FOR THE TREATMENT OF MYELOPROLIFERATIVE DISEASES AND CANCER - The present invention provides compounds of formula I | 08-29-2013 |
20130224812 | Process for Resolving Cyclopropyl Diesters - The present disclosure provides a method for the stereospecific hydrolysis of racemic 1,1-dialkyloxycarbonylcyclopropanes. | 08-29-2013 |
20130224296 | Drug Formulations Using Water Soluble Antioxidants - The present invention relates to solid, semisolid, or liquid formulations comprising water soluble antioxidants that prevent or reduce formic acid and/or formyl species generation in the dosage form during the manufacturing process and/or during shelf-life storage. The formulations of the present invention prevent or reduce formation of N-formyl impurities (and gelatin cross-linking) during the manufacturing process and/or during shelf-life storage. | 08-29-2013 |
20130216541 | STABLE SUBCUTANEOUS PROTEIN FORMULATIONS AND USES THEREOF - The present invention relates generally to stable formulations comprising CTLA4Ig molecules, including lyophilized, and liquid formulations for administration via various routes including, for example, routes such as intravenous (IV) and subcutaneous (SC) for treating immune system diseases and tolerance induction. | 08-22-2013 |
20130210857 | Inhibitors of Human Immunodeficiency Virus Replication - The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection. | 08-15-2013 |
20130210787 | C-3 CYCLOALKENYL TRITERPENOIDS WITH HIV MATURATION INHIBITORY ACTIVITY - Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-3 cycloalkenyl triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II, III and IV: | 08-15-2013 |
20130210703 | FIBRONECTIN BASED SCAFFOLD DOMAIN PROTEINS THAT BIND PCSK9 - The present invention relates to fibronectin based scaffold domain proteins that bind PCSK9. The invention also relates to the use of the innovative proteins in therapeutic applications to treat atherosclerosis, hypercholesterolemia and other cholesterol related diseases. The invention further relates to cells comprising such proteins, polynucleotides encoding such proteins or fragments thereof, and to vectors comprising the polynucleotides encoding the innovative protein. | 08-15-2013 |
20130209494 | ENEDIYNE COMPOUNDS, CONJUGATES THEREOF, AND USES AND METHODS THEREFOR - Enediyne compounds having a structure according to formula (I), where R | 08-15-2013 |
20130204012 | Process For Preparing Dipeptidyl Peptidase IV Inhibitors And Intermediates Therefor - A process for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV is provided which employs a BOC-protected amine of the structure | 08-08-2013 |
20130203992 | METHODS FOR THE PREPARATION OF HIV ATTACHMENT INHIBITOR PIPERAZINE PRODRUG COMPOUND - A method for making the compound | 08-08-2013 |
20130203775 | Novel Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 08-08-2013 |
20130203758 | Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 08-08-2013 |
20130203748 | Inhibitors of Human Immunodeficiency Virus Replication - The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection. | 08-08-2013 |
20130197202 | ANTI-CD80 ANTIBODY - The present invention discloses a method for assaying the binding of L104EA29YIg to a receptor. The receptor is preferably CD86 or CD80. The present invention also discloses antibodies to be used in the assay, as well as hybridomas expressing the antibodies. | 08-01-2013 |
20130196871 | Fibronectin Binding Domains with Reduced Immunogenicity - Fibronectin type III ( | 08-01-2013 |
20130195865 | METHOD OF PREVENTING THE DEVELOPMENT OF RHEUMATOID ARTHRITIS IN SUBJECTS WITH UNDIFFERENTIATED ARTHRITIS - The invention relates to methods and compositions for treating undifferentiated arthritis (UA) and/or preventing the development of rheumatoid arthritis (RA) in subjects with UA by administering to a subject in need thereof an effective amount of soluble CTLA4 molecule. | 08-01-2013 |
20130190481 | HUMAN ANTIBODIES THAT BIND MESOTHELIN, AND USES THEREOF - The present disclosure provides isolated monoclonal antibodies that specifically bind to mesothelin with high affinity, particularly human monoclonal antibodies. Preferably, the antibodies bind human mesothelin. In certain embodiments, the antibodies are capable of internalizing into mesothelin-expressing cells or are capable of mediating antigen dependent cellular cytotoxicity. The invention further provides anti-mesothelin antibodies that can inhibit the binding of mesothelin to the ovarian cancer antigen CA125. Nucleic acid molecules encoding the antibodies of this disclosure, expression vectors, host cells and methods for expressing the antibodies of this disclosure are also provided. Antibody-partner molecule conjugates, bispecific molecules and pharmaceutical compositions comprising the antibodies of this disclosure are also provided. This disclosure also provides methods for detecting mesothelin, as well as methods for treating cancers, such as mesotheliomas, pancreatic cancers and ovarian cancers, using an anti-mesothelin antibody of this disclosure. | 07-25-2013 |
20130190361 | SUBSTITUTED OXADIAZOLE COMPOUNDS - Disclosed are compounds of Formula (I): | 07-25-2013 |
20130184284 | DIAMINOCYCLOHEXANE COMPOUNDS AND USES THEREOF - The present invention provides compounds of Formula (I): | 07-18-2013 |
20130184279 | N-((3-BENZYL)-2,2-(BIS-PHENYL)-PROPAN-1-AMINE DERIVATIVES AS CETP INHIBITORS FOR THE TREATMENT OF ATHEROSCLEROSIS AND CARDIOVASCULAR DISEASES - Compounds of formula Ia and Ib | 07-18-2013 |
20130184262 | DIAMINOCYCLOHEXANE COMPOUNDS AND USES THEREOF - The present invention provides compounds of Formula (I): | 07-18-2013 |
20130184212 | FIBRONECTIN BASED SCAFFOLD PROTEINS HAVING IMPROVED STABILITY - The present application provides fibronectin based scaffold proteins associated with improved stability. The application also relates to stable formulations of fibronectin based scaffold proteins and the use thereof in diagnostic, research and therapeutic applications. The application further relates to cells comprising such proteins, polynucleotides encoding such proteins or fragments thereof, and to vectors comprising such polynucleotides. | 07-18-2013 |
20130183269 | Hepatitis C Virus Inhibitors - The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein. | 07-18-2013 |
20130178462 | COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION - The present disclosure provides a series of compounds of the formula (I) | 07-11-2013 |
20130177562 | METHODS OF ANTAGONIZING SIGNAL TRANSDUCTION IN DORSAL ROOT GANGLION CELLS - Use of antagonists to IL-31 are used to treat inflammation and pain by inhibiting, preventing, reducing, minimizing, limiting or minimizing stimulation in neuronal tissues. Such antagonists include antibodies and fragments, derivative, or variants thereof. Symptoms such as pain, tingle, sensitization, tickle associated with neuropathies are ameliorated. | 07-11-2013 |
20130165447 | Inhibitors of PDE10 - PDE10 inhibitors having the general formula (I) | 06-27-2013 |
20130164345 | Co-Processing Method and Formulations for HIV Attachment Inhibitor Prodrug Compound and Excipients - A process for the production of a formulation of HIV attachment inhibitor piperazine tris salt prodrug compound involves dissolving the prodrug compound in a solvent to form a solution; adding a first quantity of a first anti-solvent to the solution; then dispersing a first quantity of HPMC in the solution; adding a second quantity of the first anti-solvent to the solution; dispersing a second quantity of HPMC in the solution; then adding a second anti-solvent to the solution so as to crystallize the compound with the HPMC and thereby form the formulation, wherein the second anti-solvent is a combination of acetone and isopropyl acetate (IPAC). The formulation is then washed, and dried. | 06-27-2013 |
20130161848 | PROCESS FOR MAKING STERILE ARIPIPRAZOLE OF DESIRED MEAN PARTICLE SIZE - A process is provided for making sterile aripiprazole having an average particle size less than 100 microns but preferably greater than 25 microns employing an impinging jet crystallization procedure. The resulting bulk aripiprazole of desired particle size may be used to form a sterile freeze-dried aripiprazole formulation, which upon constitution with water and intramuscular injection releases aripiprazole over a period of at least about one week and up to about eight weeks. | 06-27-2013 |
20130157948 | BISPECIFIC EGFR/IGFIR BINDING MOLECULES - The present invention relates to bispecific molecules comprising an EGFR binding domain and a distinct IGFIR binding domain for use in diagnostic, research and therapeutic applications. The invention further relates to cells comprising such proteins, polynucleotide encoding such proteins or fragments thereof, and vectors comprising the polynucleotides encoding the innovative proteins. Exemplary bispecific molecules include antibody-like protein dimers based on the tenth fibronectin type III domain. | 06-20-2013 |
20130156768 | COMBINATION OF ANTI-CTLA4 ANTIBODY WITH BRAF INHIBITORS FOR THE SYNERGISTIC TREATMENT OF PROLIFERATIVE DISEASES - Compositions and methods are disclosed which are useful of the treatment and prevention of proliferative disorders. | 06-20-2013 |
20130150371 | Inhibitors of PDE10 - PDE10 inhibitors having the general formula (I) | 06-13-2013 |
20130144042 | B7-RELATED NUCLEIC ACIDS AND POLYPEPTIDES USEFUL FOR IMMUNOMODULATION - The present invention provides nucleic acids encoding B7-related factors that modulate the activation of immune or inflammatory response cells, such as T-cells. Also provided are expression vectors and fusion constructs comprising nucleic acids encoding B7-related polypeptides, including BSL1, BSL2, and BSL3. The present invention further provides isolated B7-related polypeptides, isolated fusion proteins comprising B7-related polypeptides, and antibodies that are specifically reactive with B7-related polypeptides, or portions thereof. In addition, the present invention provides assays utilizing B7-related nucleic acids, polypeptides, or peptides. The present invention further provides compositions of B7-related nucleic acids, polypeptides, fusion proteins, or antibodies that are useful for the immunomodulation of a human or animal subject. | 06-06-2013 |
20130143270 | PRODUCTION AND PURIFICATION OF IL-29 - The expression vectors and methods using an | 06-06-2013 |
20130142805 | COMBINATION OF ANTI-CTLA4 ANTIBODY WITH DIVERSE THERAPEUTIC REGIMENS FOR THE SYNERGISTIC TREATMENT OF PROLIFERATIVE DISEASES - Compositions and methods are disclosed which are useful of the treatment and prevention of proliferative disorders. | 06-06-2013 |
20130142754 | Hepatitis C Virus Inhibitors - Hepatitis C virus inhibitors having the general formula (I) | 06-06-2013 |
20130131074 | PYRIDONE AND PYRIDAZONE ANALOGUES AS GPR119 MODULATORS - Novel compounds of structure Formula I: | 05-23-2013 |
20130131064 | Quinuclidine Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligands - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders. | 05-23-2013 |
20130131051 | COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION - Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: | 05-23-2013 |
20130131049 | COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION - Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: | 05-23-2013 |
20130129819 | Pharmaceutical Formulations Containing An SGLT2 Inhibitor - Pharmaceutical formulations are provided which are in the form of capsules or tablets for oral use and which include a medicament dapagliflozin or its propylene glycol hydrate | 05-23-2013 |
20130129671 | Tripeptides Incorporating Deuterium as Inhibitors of Hepatitis C Virus - Hepatitis C virus inhibitors having the general formula (I) | 05-23-2013 |
20130123503 | Process for Synthesizing Substituted Isoquinolines - The present disclosure generally relates to a process for synthesizing optionally substituted 1-chloro-4-methoxyisoquinolines. The present disclosure also relates to intermediates useful in this process. | 05-16-2013 |
20130121957 | Hepatitis C Virus Inhibitors - The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection. | 05-16-2013 |
20130116237 | [6,6] AND [6,7]-BICYCLIC GPR119 G PROTEIN-COUPLED RECEPTOR AGONISTS - Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: | 05-09-2013 |
20130115193 | Hepatitis C Virus Inhibitors - The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection. | 05-09-2013 |
20130115190 | Hepatitis C Virus Inhibitors - Hepatitis C virus inhibitors having the general formula (I) | 05-09-2013 |
20130108612 | POLYNUCLEOTIDES ENCODING NOVEL PCSK9 VARIANTS | 05-02-2013 |
20130102615 | THIOAMIDE, AMIDOXIME AND AMIDRAZONE DERIVATIVES AS HIV ATTACHMENT INHIBITORS - A compound of Formula I, including pharmaceutically acceptable salts thereof: | 04-25-2013 |
20130102589 | Novel Compound for the Treatment of Hepatitis C - The present invention provides (1aR,12bS)-8-cyclohexyl-11-fluoro-N-((1-methylcyclopropyl)sulfonyl)-1a-((3-methyl-3,8-diazabicyclo[3.2.1]oct-8-yl)carbonyl)-1,1a,2,12b-tetrahydrocyclopropa[d]indolo[2,1-a][2]benzazepine-5-carboxamide (formula I), including pharmaceutically acceptable salts, as well as compositions and methods of using the compound. The compound has activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 04-25-2013 |
20130096305 | DEUTERATED HIV ATTACHMENT INHIBITORS - Deuterated piperazine and piperidine HIV attachment inhibitor compounds are set forth. The present invention provides compounds of Formula I, the pharmaceutically acceptable salts and/or solvates (e.g., hydrates) thereof, their pharmaceutical formulations, and their use in patients suffering from or susceptible to a virus such as HIV. The compounds of Formula I, their pharmaceutically acceptable salts and/or solvates are effective antiviral agents, particularly as inhibitors of HIV. They are useful for the treatment of HIV and AIDS. | 04-18-2013 |
20130096130 | CGRP Receptor Antagonists - The disclosure generally relates to the novel compounds of formula I, including pharmaceutically acceptable salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD). | 04-18-2013 |
20130095109 | ANTIBODY POLYPEPTIDES THAT ANTAGONIZE CD40L - Antibody polypeptides that specifically bind human CD40L are provided. The antibody polypeptides do not activate platelets. The antibody polypeptides are useful in the treatment of diseases involving CD40L activation, such as graft-related diseases and autoimmune diseases. The antibody polypeptides may be domain antibodies (dAbs) comprising a single V | 04-18-2013 |
20130095066 | Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 04-18-2013 |
20130095063 | Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 04-18-2013 |
20130089517 | HOMOGENEOUS PREPARATIONS OF IL-28 AND IL-29 - Homogeneous preparations of IL-28A, IL-28B, and IL-29 have been produced by mutating one or more of the cysteine residues in the polynucleotide sequences encoding the mature proteins. The cysteine mutant proteins can be shown to either bind to their cognate receptor or exhibit biological activity. One type of biological activity that is shown is an antiviral activity. | 04-11-2013 |
20130085147 | Hepatitis C Virus Inhibitors - The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein. | 04-04-2013 |
20130085138 | Selective NR2B Antagonists - The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system. | 04-04-2013 |
20130079338 | Selective NR2B Antagonists - The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system. | 03-28-2013 |
20130078214 | Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 03-28-2013 |
20130072465 | NOVEL BETULINIC ACID DERIVATIVES WITH ANTIVIRAL ACTIVITY - Compounds of Formula I: | 03-21-2013 |
20130064831 | IMMUNOTHERAPEUTIC DOSING REGIMENS AND COMBINATIONS THEREOF - The invention described herein relates to therapeutic dosing regimens and combinations thereof for use in enhancing the therapeutic efficacy of immunotherapeutic agents e.g. CTLA-4 antagonists such as Ipilimumab or Tremelimumab in combination with one or more chemotherapeutic agents in cancer patients. | 03-14-2013 |
20130060027 | TETRAHYDROISOQUINOLINES AND INTERMEDIATES THEREFOR - Disclosed are processes for preparing tetrahydroisoquinolines, intermediates useful in the preparation of tetrahydroisoquinolines, processes for preparing such intermediates, and a crystalline form of 6-[(4S)-2-methyl-4-(naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine. Also disclosed are pharmaceutical compositions comprising tetrahydroisoquinolines, methods of using tetrahydroisoquinolines in the treatment of depression and other conditions and methods for obtaining the crystalline form. | 03-07-2013 |
20130059858 | BENZOFURANYL ANALOGUES AS GPR119 MODULATORS - Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, where-in A, L, m, n, o, p, R | 03-07-2013 |
20130053345 | BICYCLIC HETEROARLY ANALOGUES AS GPR119 MODULATORS - Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein A, D, Di, E, J, L, n, Q, R | 02-28-2013 |
20130045981 | ARIPIPRAZOLE COMPLEX FORMULATION AND METHOD - An aripiprazole formulation is provided which includes the antipsychotic agent aripiprazole in the form of an inclusion complex in a β-cyclodextrin, preferably, sulfobutyl ether β-cyclodextrin (SBECD), which in the form of an injectable produces reversible generally minimal to mild irritation at the intramuscular injection site. A method for minimizing or reducing irritation caused by aripiprazole at an intramuscular injection site and a method for treating schizophrenia employing the above formulation are also provided. | 02-21-2013 |
20130045980 | IMIDAZOPYRIDAZINYL COMPOUNDS - Disclosed are imidazopyridazinyl compounds of Formula (I): (I), or pharmaceutically salts and prodrugs thereof, wherein R | 02-21-2013 |
20130045245 | APIXABAN FORMULATIONS - Compositions comprising crystalline apixaban particles having a D | 02-21-2013 |
20130035318 | C-17 AND C-3 MODIFIED TRITERPENOIDS WITH HIV MATURATION INHIBITORY ACTIVITY - Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 and C-3 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: | 02-07-2013 |
20130034606 | IMMEDIATE RELEASE TABLET FORMULATIONS - The present invention provides an immediate release pharmaceutical formulation which includes a tablet or capsule formulation comprising metformin and the sodium dependent glucose transporter (SGLT2) inhibitor dapagliflozin or its propylene glycol hydrate. The present invention also provides methods of preparing the formulations and methods of treating diseases or disorders associated with SGLT2 activity employing these formulations. | 02-07-2013 |
20130034520 | Hepatitis C Virus Inhibitors - The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection. | 02-07-2013 |
20130030178 | METHODS OF MAKING HIV ATTACHMENT INHIBITOR PRODRUG COMPOUND AND INTERMEDIATES - A method for making the compound of Formula I: | 01-31-2013 |
20130030011 | COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION - The present disclosure provides a series of compounds of the formula (I) | 01-31-2013 |
20130030005 | PHARMACEUTICAL FORMULATIONS OF SUBSTITUTED AZAINDOLEOXOACETIC PIPERAZINE DERIVATIVES WITH PROTEASE INHIBITORS - This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. | 01-31-2013 |
20130029954 | C-28 AMINES OF C-3 MODIFIED BETULINIC ACID DERIVATIVES AS HIV MATURATION INHIBITORS - Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-28 amines of C-3 modified betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS. In particular, the following compounds are provided herein, including pharmaceutically acceptable salts thereof: | 01-31-2013 |
20130029939 | NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME - Compounds are provided which are activators of the enzyme glucokinase and thus are useful in treating diabetes and related diseases, which compounds have the structure wherein R | 01-31-2013 |
20130028906 | HUMAN ANTIBODIES THAT BIND MESOTHELIN, AND USES THEREOF - The present disclosure provides isolated monoclonal antibodies that specifically bind to mesothelin with high affinity, particularly human monoclonal antibodies. Preferably, the antibodies bind human mesothelin. In certain embodiments, the antibodies are capable of internalizing into mesothelin-expressing cells or are capable of mediating antigen dependent cellular cytotoxicity. The invention further provides anti-mesothelin antibodies that can inhibit the binding of mesothelin to the ovarian cancer antigen CA125. Nucleic acid molecules encoding the antibodies of this disclosure, expression vectors, host cells and methods for expressing the antibodies of this disclosure are also provided. Antibody-partner molecule conjugates, bispecific molecules and pharmaceutical compositions comprising the antibodies of this disclosure are also provided. This disclosure also provides methods for detecting mesothelin, as well as methods for treating cancers, such as mesotheliomas, pancreatic cancers and ovarian cancers, using an anti-mesothelin antibody of this disclosure. | 01-31-2013 |
20130028905 | HUMAN ANTIBODIES THAT BIND MESOTHELIN, AND USES THEREOF - The present disclosure provides isolated monoclonal antibodies that specifically bind to mesothelin with high affinity, particularly human monoclonal antibodies. Preferably, the antibodies bind human mesothelin. In certain embodiments, the antibodies are capable of internalizing into mesothelin-expressing cells or are capable of mediating antigen dependent cellular cytotoxicity. The invention further provides anti-mesothelin antibodies that can inhibit the binding of mesothelin to the ovarian cancer antigen CA125. Nucleic acid molecules encoding the antibodies of this disclosure, expression vectors, host cells and methods for expressing the antibodies of this disclosure are also provided. Antibody-partner molecule conjugates, bispecific molecules and pharmaceutical compositions comprising the antibodies of this disclosure are also provided. This disclosure also provides methods for detecting mesothelin, as well as methods for treating cancers, such as mesotheliomas, pancreatic cancers and ovarian cancers, using an anti-mesothelin antibody of this disclosure. | 01-31-2013 |
20130028904 | HUMAN ANTIBODIES THAT BIND MESOTHELIN, AND USES THEREOF - The present disclosure provides isolated monoclonal antibodies that specifically bind to mesothelin with high affinity, particularly human monoclonal antibodies. Preferably, the antibodies bind human mesothelin. In certain embodiments, the antibodies are capable of internalizing into mesothelin-expressing cells or are capable of mediating antigen dependent cellular cytotoxicity. The invention further provides anti-mesothelin antibodies that can inhibit the binding of mesothelin to the ovarian cancer antigen CA125. Nucleic acid molecules encoding the antibodies of this disclosure, expression vectors, host cells and methods for expressing the antibodies of this disclosure are also provided. Antibody-partner molecule conjugates, bispecific molecules and pharmaceutical compositions comprising the antibodies of this disclosure are also provided. This disclosure also provides methods for detecting mesothelin, as well as methods for treating cancers, such as mesotheliomas, pancreatic cancers and ovarian cancers, using an anti-mesothelin antibody of this disclosure. | 01-31-2013 |
20130028859 | Hepatitis C Virus Inhibitors - The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection. | 01-31-2013 |
20130023564 | PIPERIDINYL DERIVATIVE AS A MODULATOR OF CHEMOKINE RECEPTOR ACTIVITY - The present application describes the compound of formula (I): | 01-24-2013 |
20130023514 | SUBSTITUTED PYRROLOTRIAZINES AS PROTEIN KINASE INHIBITORS - The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) pyrrolotriazines inhibit protein kinase activity thereby making them useful as anticancer agents. | 01-24-2013 |
20130018325 | FLANGE EXTENDER FOR USE WITH AN INJECTION DEVICE AND METHOD OF ASSEMBLYAANM Schiller; EricAACI WestfieldAAST NJAACO USAAGP Schiller; Eric Westfield NJ USAANM Laskar; Christina JoyAACI Cliffside ParkAAST NJAACO USAAGP Laskar; Christina Joy Cliffside Park NJ USAANM Aon; MitaliAACI Princeton JunctionAAST NJAACO USAAGP Aon; Mitali Princeton Junction NJ USAANM Caizza; RichardAACI VernonAAST NJAACO USAAGP Caizza; Richard Vernon NJ USAANM Bell; JonAACI WaldwickAAST NJAACO USAAGP Bell; Jon Waldwick NJ US - A flange extender for use with an injection device is described. The flange extender includes first and second flange extender pieces and a locking mechanism to lock the first and second flange extender pieces to one another. In one embodiment, the locking mechanism includes each piece having a locking finger extending from the piece and an aperture adapted to receive the locking finger. The first and second flange extender pieces extend in a direction transverse to a main axis of the injection device to thereby provide a surface area for manual manipulation of the injection device during an injection. The first and second flange extender pieces also attach to each other on opposite sides of the injection device. | 01-17-2013 |
20130012723 | METHODS AND COMPOUNDS FOR PRODUCING DIPEPTIDYL PEPTIDASE IV INHIBITORS AND INTERMEDIATES THEREOF - Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided. | 01-10-2013 |
20130012540 | Hepatitis C Virus Inhibitors - This disclosure concerns novel compounds of Formula (I) or as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds. | 01-10-2013 |
20130012519 | Biomarker Identifying the Reactivation of STAT3 After Src Inhibition - A method of identifying cancer or an associated disorder comprising identifying and quantifying STAT3 occurring in a biological sample taken from a subject after administering a SFK inhibitor to said subject. | 01-10-2013 |
20130012436 | FIBRONECTIN BASED SCAFFOLD DOMAIN PROTEINS THAT BIND IL-23 - The present invention relates to fibronectin based scaffold domain protein that bind interleukin 23 (IL-23), specifically the p19 subunit of IL-23. The invention also relates to the use of the innovative proteins in therapeutic applications to treat autoimmune diseases. The invention further relates to cells comprising such proteins, polynucleotide encoding such proteins or fragments thereof, and to vectors comprising the polynucleotides encoding the innovative proteins. | 01-10-2013 |
20130012435 | MULTIVALENT FIBRONECTIN BASED SCAFFOLD DOMAIN PROTEINS - The present invention relates to multivalent polypeptides comprising at least two fibronectin scaffold domains connected via a polypeptide linker. The invention also relates to multivalent polypeptides for use in diagnostic, research and therapeutic applications. The invention further relates to cells comprising such proteins, polynucleotide encoding such proteins or fragments thereof, and to vectors comprising the polynucleotides encoding the innovative proteins. | 01-10-2013 |
20130004457 | Hepatitis C Virus Inhibitors - The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection. | 01-03-2013 |
20120330019 | Hepatitis C Virus Inhibitors - Hepatitis C virus inhibitors are disclosed having the general formula: | 12-27-2012 |
20120329990 | B7-RELATED NUCLEIC ACIDS AND POLYPEPTIDES USEFUL FOR IMMUNOMODULATION - The present invention provides nucleic acids encoding B7-related factors that modulate the activation of immune or inflammatory response cells, such as T-cells. Also provided are expression vectors and fusion constructs comprising nucleic acids encoding B7-related polypeptides, including BSL1, BSL2, and BSL3. The present invention further provides isolated B7-related polypeptides, isolated fusion proteins comprising B7-related polypeptides, and antibodies that are specifically reactive with B7-related polypeptides, or portions thereof. In addition, the present invention provides assays utilizing B7-related nucleic acids, polypeptides, or peptides. The present invention further provides compositions of B7-related nucleic acids, polypeptides, fusion proteins, or antibodies that are useful for the immunomodulation of a human or animal subject. | 12-27-2012 |
20120328570 | Hepatitis C Virus Inhibitors - The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection. | 12-27-2012 |
20120322761 | HETEROCYCLIC CETP INHIBITORS - Compounds of formula Ia and Ib | 12-20-2012 |
20120322749 | TABLETED COMPOSITIONS CONTAINING ATAZANAVIR - Disclosed are compressed tablets containing atazanavir sulfate, optionally with another active agents, e.g., anti-HIV agents, granules that contain atazanavir sulfate and an intragranular lubricant that can be used to make the tablets, compositions comprising a plurality of the granules, processes for making the granules and tablets, and methods of treating HIV. | 12-20-2012 |
20120316126 | Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 12-13-2012 |
20120309770 | Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 12-06-2012 |
20120309745 | HIV Integrase Inhibitors - The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV. | 12-06-2012 |
20120309698 | HIV Integrase Inhibitors - The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV. | 12-06-2012 |
20120309028 | IMMUNOASSAY STANDARDS AND MEASUREMENT OF CLINICAL BIOMARKERS USING INTRA-ASSAY CALIBRATION STANDARDS - The present invention provides novel compositions and methods for creating quantitative standards to calibrate analytes. These compositions and methods enable the creation of standards and calibrators for analyzing analytes and measuring clinical biomarkers. Also provided are kits comprising the novel compositions for use in assays, for example sandwich immunoassays. | 12-06-2012 |
20120302750 | PROCESS FOR PREPARING 2-AMINOTHIAZOLE-5-AROMATIC CARBOXAMIDES AS KINASE INHIBITORS - The invention relates to processes for preparing compounds having the formula, | 11-29-2012 |
20120302747 | PYRROLOTRIAZINE KINASE INHIBITORS - The invention provides compounds of formula I | 11-29-2012 |
20120302571 | CRYSTALLINE FORMS OF (S)-1-(4-(5-CYCLOPROPYL-1H-PYRAZOL-3-YLAMINO)PYRROLO[1,2-f][1,2,4]TRIAZIN- -2-YL)-N-(6-FLUOROPYRIDIN-3-YL)-2-METHYLPYRROLIDINE-2-CARBOXAMIDE - Crystalline forms of (S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrrolo[1,2-f][1,2,4]triazin-2-yl)-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide of the formula (I) are provided. Also provided is a pharmaceutical composition comprising one or more crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol, as well as a method of using one or more crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol in the treatment of cancer and other proliferative diseases. | 11-29-2012 |
20120301490 | IMMUNOCONJUGATES, COMPOSITIONS FOR MAKING THEM, AND METHODS OF MAKING AND USE - An immunoconjugate in which a phosphate-prodrugged DNA minor groove binding agent of formula (I), where X is a nucleophilically displaceable leaving group, is conjugated to an antibody or an antigen binding fragment of an antibody, and compounds that can be used for making such immunoconjugates, and uses of such immunoconjugates. | 11-29-2012 |
20120294936 | REDUCED MASS METFORMIN FORMULATIONS - The present invention relates to metformin extended release (XR) formulations with improved compactability to provide reduced mass tablets, granulations, and capsules. | 11-22-2012 |
20120283184 | INHIBITORS OF TYPE 2 VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTORS - The present disclosure relates to novel vascular endothelial growth factor receptor (VEGFR)-binding polypeptides and methods for using these polypeptides to inhibit biological activities mediated by vascular endothelial growth factors (VEGFs). The present disclosure also provides various improvements relating to single domain binding polypeptides. | 11-08-2012 |
20120283181 | CRYSTAL FORMS OF SAXAGLIPTIN AND PROCESSES FOR PREPARING SAME - Physical crystal structures of a compound of the formula I: | 11-08-2012 |
20120282336 | BILAYER TABLET FORMULATIONS - The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations. | 11-08-2012 |
20120276600 | Process For Preparing Dipeptidyl Peptidase IV Inhibitors And Intermediates Therefor - A process for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV is provided which employs a BOC-protected amine of the structure | 11-01-2012 |
20120270228 | PREDICTORS OF PATIENT RESPONSE TO TREATMENT WITH EGF RECEPTOR INHIBITORS - The present invention provides methods and compositions to facilitate determining whether an EGFR-expressing cancer in an individual is an EGFR inhibitor-responsive cancer, as well as methods for determining the likelihood that a patient having an EGFR-expressing cancer will exhibit a beneficial response to an EGFR inhibitor therapy. The methods generally involve determining a normalized expression level of a gene product that correlates with EGFR inhibitor responsiveness. | 10-25-2012 |
20120263786 | Pharmaceutical Formulations Containing an SGLT2 Inhibitor - Pharmaceutical formulations are provided which are in the form of capsules or tablets for oral use and which include a medicament dapagliflozin or its propylene glycol hydrate | 10-18-2012 |
20120252799 | HETEROCYCLIC AROMATIC COMPOUNDS USEFUL AS GROWTH HORMONE SECRETAGOGUES - Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I | 10-04-2012 |
20120202285 | ANTIBODIES TO IL-6 AND THEIR USES - Antibodies and antigen-binding portions thereof that bind to human IL-6 are provided. Also provided are nucleic acids encoding such antibodies and antigen binding portions, methods of making such antibodies and antigen binding portions, compositions comprising such antibodies or antigen binding portions, and uses of such antibodies or antigen binding portions. | 08-09-2012 |
20120201816 | LACTAM-CONTAINING COMPOUNDS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS - The present application describes lactam-containing compounds and derivatives thereof of Formula I: | 08-09-2012 |
20120201814 | COMPOSITIONS MONOVALENT FOR CD28 BINDING AND METHODS OF USE - Disclosed are domain antibodies that monovalently bind CD28. Domain antibodies that are monovalent for binding of CD28 can inhibit CD28 activity. In one aspect, a domain antibody consists of or comprises a single immunoglobulin variable domain that specifically binds and antagonizes the activity of CD28, in an aspect, without substantially agonizing CD28 activity. In another aspect, the domain antibody is a human domain antibody. The disclosure further encompasses methods of antagonizing CD80 and/or CD86 interactions with CD28 in an individual and methods of treating diseases or disorders involving CD80 and/or CD86 interactions with CD28, the methods involving administering a domain antibody to the individual. | 08-09-2012 |
20120196814 | (R)-1-(4-(4-FLUORO-2-METHYL-1H-INDOL-5-YLOXY)-5-METHYLPYRROLO[2,1-f][1,2,4- ]TRIAZIN-6-YLOXY)PROPAN-2-OL METABOLITES - The present invention is directed to metabolites of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-ol, the compound of formula (I), pharmaceutical compositions thereof, and to methods of using the metabolites and the pharmaceutical compositions in the treatment of cancer. | 08-02-2012 |
20120101262 | PROTEIN PURIFICATION BY CAPRYLIC ACID (OCTANOIC ACID) PRECIPITATION - The invention provides methods for a purifying protein of interest from a mixture comprising the protein of interest and one or more contaminants, including host cell DNA and proteins, by precipitation of the contaminants with caprylic acid. Such methods are particularly useful for purifying antibodies from cell cultures. Moreover, mixtures that have been depleted of contaminants using the methods of the invention can be used directly in downstream chromatography applications (e.g., ion exchange chromatography) without any further purification. These methods lead to manufacturing processes with a minimum number of unit operations and reduce the resource requirements, and thus positively influence the cost of goods for therapeutic protein production. | 04-26-2012 |