Merck Sharp & Dohme Corp. Patent applications |
Patent application number | Title | Published |
20160136172 | SUBSTITUTED BENZOFURAN COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES - The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. | 05-19-2016 |
20160130659 | COMPOSITIONS AND METHODS FOR TREATING CANCER - The instant invention relates to methods for the treatment of B-cell lymphomas and leukemia by administering a SYK inhibitor. In another embodiment, the invention relates to a method for treating a patient diagnosed with a B-cell lymphoma or leukemia, comprising administering a SYK inhibitor, wherein the B-cells of said patient to be treated are characterized by elevated expression levels of CD86. | 05-12-2016 |
20160130574 | METHODS OF MEASURING GENE EXPRESSION IN FACS-SORTED CELLS - Improved methods of measuring gene expression in intracellularly immunostained FACS-sorted cell populations are provided. Exemplary methods involve fixing cells with formalin and permeabilizing with mild detergent in the presence of ribonucleoside vanadyl complex prior to FACS sorting, followed by RNA extraction in the presence of de-crosslinking agents. The resulting RNA is suitable for gene expression analysis. The method allows for analysis of the gene expression pattern specifically associated with any sortable cell population or subpopulation. | 05-12-2016 |
20160130327 | CMV NEUTRALIZING ANTIGEN BINDING PROTEINS - The present invention is directed to antigen binding proteins including, but not limited to, monoclonal antibodies and antigen binding fragments thereof, that specifically bind to and preferably neutralize human cytomegalovirus (CMV). Also encompassed by the invention are antigen binding proteins that have been humanized. The antigen binding proteins of the invention are useful as a therapeutic agent for treating and/or preventing CMV infections in a patient in need thereof. | 05-12-2016 |
20160130273 | Process for Making CGRP Receptor Antagonists - The invention encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, which are CGRP receptor antagonists useful for the treatment of migraine. | 05-12-2016 |
20160130259 | SUBSTITUTED BENZOFURAN COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES - The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. | 05-12-2016 |
20160122380 | CYCLIC PHOSPHONATE SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES - The present invention relates to Cyclic Phosphonate Substituted Nucleoside Derivatives of Formula (I): (structure) and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein, as well as to compositions and methods of using the Cyclic Phosphonate Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient. | 05-05-2016 |
20160122350 | PROCESS FOR THE PREPARATION OF CHIRAL TERT-BUTYL 4-((1R,2S,5R)-6-(BENZYLOXY)-7-OXO-1,6-DIAZABICYCLO[3.2.1]OCTANE-2-CARBOXA- MIDO)PIPERIDINE-1-CARBOXYLATE DERIVATIVES AND (2S,5R)-7-OXO-N-PIPERIDIN-4-YL-6-(SULFOXY)-1,6-DIAZABICYCLO[3.2.1]OCTANE-- 2-CARBOXAMIDE - A process for the preparation of N-protected 6-(piperidin-4-ylcarbamoyl)piperidin-3-yl sulfonates of Formula (III): which comprises contacting a lactone of Formula (II): with an azacycloalkylamine of formula (II-Am): followed by contact with a sulfonyl halide of formula (II-Su): R | 05-05-2016 |
20160108059 | FUSED TRICYCLIC HETEROCYCLIC COMPOUNDS AS HIV INTEGRASE INHIBITORS - The present invention relates to Fused Tricyclic Heterocycle Derivatives of Formula (I), and pharmaceutically acceptable salts thereof, wherein R | 04-21-2016 |
20160108048 | IMIDAZOLE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG - The present invention relates to Imidazole Derivatives of Formula (I), and pharmaceutically acceptable salts thereof, wherein A, B, Y, R | 04-21-2016 |
20160106835 | COMBINATION THERAPIES FOR CANCER - A novel combination comprising a B-Raf inhibitor, particularly N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl; -2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, and a PD-1 antagonist; pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and/or B-Raf and/or immune modulation through PD-1 is beneficial, e.g., cancer. | 04-21-2016 |
20160102073 | 2-HYDROXYMETHYL-SUBSTITUTED OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to 2-hydroxymethyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 04-14-2016 |
20160082005 | PROCESS OF MAKING AND USING PHARMACEUTICAL FORMULATIONS OF ANTINEOPLASTIC AGENTS - In its several embodiments, this invention discloses a pharmaceutical formulation comprising at least one antineoplastic agent or a pharmaceutically acceptable salt thereof, and at least one dissolution enhancing agent sufficient to substantially dissolve said at least one antineoplastic agent in at least one aqueous diluent, wherein said dissolution enhancing agent is urea, L-histidine, L-threonine, L-asparagine, L-serine, L-glutamine or mixtures thereof; a lyophilized powder comprising said pharmaceutical formulation, and articles of manufacture thereof. | 03-24-2016 |
20160075684 | ALPHA 7 NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS AND USES THEREOF-III - The present invention relates to chemical compounds useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (α7 nAChR). | 03-17-2016 |
20160075656 | QUINOLINE AMIDE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to quinoline amide compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositious comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | 03-17-2016 |
20160075650 | CRYSTALLINE POLYMORPHIC FORMS OF AN ANTIDIABETIC COMPOUND - The present invention relates to polymorphic forms of a compound of formula A: | 03-17-2016 |
20160075645 | AMIDATION PROCESS - This invention describes an amidation process whereby perfluorinated amino acids can be activated and treated with an amine in the presence of a coupling agent and a pyridine derivative to yield amides, without loss of optical purity. | 03-17-2016 |
20160068597 | FDF03 ANTIBODIES AND USES THEREOF - The present invention relates to methods for identifying and using modulators of FDF03 biological activity in vitro and in vivo that are useful in the treatment of cancer. | 03-10-2016 |
20160068532 | NOVEL COMPOUNDS THAT ARE ERK INHIBITORS - Disclosed are the ERK inhibitors of formula (I) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I). This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier. This invention also provides a method of inhibiting ERK (i.e., inhibiting the activity of ERK2) in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of formula (I). | 03-10-2016 |
20160068514 | HALO AND TRIFLUOROMETHYL SUBSTITUTED OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to halo and trifluoromethyl substituted compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 03-10-2016 |
20160068510 | HYDROXY-SUBSTITUTED OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to hydroxy compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 03-10-2016 |
20160060272 | 4-PYRIDONE DERIVATIVE COMPOUNDS AND USES THEREOF AS HIV INTEGRASE INHIBITORS - The present invention relates to 4-Pyridone Compounds of Formula (I); and pharmaceutically acceptable salts and prodrugs thereof, wherein A, R | 03-03-2016 |
20160060256 | THIAZOLE-SUBSTITUTED AMINOPYRIMIDINES AS SPLEEN TYROSINE KINASE INHIBITORS - The invention provides certain thiazole-substituted aminopyrimidine compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R5, R6, and the subscripts r, s, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk). | 03-03-2016 |
20160046581 | Factor XIa Inhibitors - The present invention provides a compound of Formula (I) | 02-18-2016 |
20160045526 | 2'-DISUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES - 2′-disubstituted substituted nucleoside derivatives of formula (I) and pharmaceutically acceptable salts thereof are disclosed: (1), wherein A is N | 02-18-2016 |
20160040252 | METHODS AND COMPOSITIONS FOR TREATING CANCER - The invention is directed to methods, reagents, and kits for the detection of MAPK/ERK pathway mutations in a patient diagnosed for cancer. In one embodiment, the invention comprises a sensitive and selective method to identify mutations to the BRAF, KRAS, and NRAS genes in a single reaction. In another aspect of this embodiment, the invention comprises primers and C probes for the detection of the BRAF, KRAS, and NRAS mutations using a single nucleotide primer extension assay. In another embodiment the invention is used to identify and select patients amenable for treatment with an ERK inhibitor. | 02-11-2016 |
20160040201 | Biocatalytic Transamination Process - A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: | 02-11-2016 |
20160040124 | ADAPTED LEPIDOPTERAN INSECT CELLS FOR THE PRODUCTION OF RECOMBINANT PROTEINS - The present invention relates to the use of increased culture pH, relative to standard insect cell culture conditions, during baculovirus infection of lepidopteran insect cells to enable production of recombinant chikungunya (CHIKV) virus like particles (VLPs). The invention further relates to adapted insect cell lines derived from insect cells such as Sf21, which can grow robustly at elevated culture pH, the use of said cell lines to recombinantly produce pH sensitive proteins in the correct conformation and increase expression of recombinant proteins relative to standard insect cell lines. In some embodiments of the invention, the cells are useful for recombinant production of CHIKV VLPs. The invention also relates to a method for the production of a pH-adapted lepidopteran insect cell line. In some embodiments of said method, the cell line is produced and/or maintained in reduced phosphate serum-free insect cell media. | 02-11-2016 |
20160024091 | INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL - The present invention provides compounds of Formula I | 01-28-2016 |
20160017036 | CELL LINE 3M - The present invention provides, inter alia, an isolated cell line, 3M as well as methods for making such a cell line and methods of using such a cell line, e.g., to produce a protein such as an immunoglobulin. | 01-21-2016 |
20160016975 | C2-AZASPIRO IMINOTHIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE - In its many embodiments, the present invention provides certain C2-azaspiro substituted iminothiazine dioxide compounds. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed. | 01-21-2016 |
20160016947 | SUBSTITUTED PYRIDIZINONE DERIVATIVES AS PDE10 INHIBITORS - The present invention is directed to substituted pyridizinone compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction. | 01-21-2016 |
20160016935 | 2-PYRIDYLOXY-4-ETHER OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to 2-pyridyloxy-4-ether compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-ether compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 01-21-2016 |
20160016923 | S-IMINO-S-OXO-IMINOTHIADIAZINE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE - In its many embodiments, the present invention provides certain S-imino-S-oxo iminothiadiazine compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein R | 01-21-2016 |
20160016921 | S-IMINO-S-OXO-IMINOTHIAZINE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE - In its many embodiments, the present invention provides certain S-imino-S-oxo iminothiazine compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein R | 01-21-2016 |
20160002259 | INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL - The present invention provides compounds of Formula I | 01-07-2016 |
20160000721 | GASTRO-RETENTIVE FORMULATIONS - The present invention relates to pharmaceutical compositions of the poorly soluble drugs, and pharmaceutically acceptable salts thereof, in a controlled-release gastric retained oral dosage form. Such compositions are formulated so as to deliver the majority of the incorporated drug into the stomach and upper gastrointestinal tract, with restricted drug delivery in the lower gastrointestinal tract. The dosage forms have multiple layers including an active layer with a first swellable polymer with raltegravir incorporated therein and a non-active layer with a second swellable polymer having a similar molecular weight or a higher molecular weight as the swellable polymer in the active layer. | 01-07-2016 |
20150374795 | O-GLYCOSYLATED CARBOXY TERMINAL PORTION (CTP) PEPTIDE-BASED INSULIN AND INSULIN ANALOGUES - Compositions and formulations comprising insulin or insulin analogues comprising a carboxy terminal portion (CTP) peptide comprising amino acids 112-188 to 142 of the beta subunit of human chorionic gonadotropin (hCGβ) or a partial variant thereof that includes at least one O-glycosylation site of the CTP peptide, wherein the CTP peptide of the CTP peptide-based insulin or insulin analogue is O-glycosylated are described. In particular embodiments, the O-glycosylated insulin analogues are produced in vivo and in further embodiments, the O-glycosylated CTP-based insulin analogues comprise predominantly mannotriose and mannotetrose O-glycans or predominantly mannose O-glycans. | 12-31-2015 |
20150368344 | MDL-1 LIGAND - The invention provides methods for modulation interactions between MDL-1 and its binding partner, Gal9. Also provided are methods to screen for modulators of MDL-1/Gal9 interaction. | 12-24-2015 |
20150368269 | Factor IXa Inhibitors - The present invention provides a compound of Formula (I) | 12-24-2015 |
20150368247 | 2,6,7 SUBSTITUTED PURINES AS HDM2 INHIBITORS - The present invention provides 2,6,7 substituted purines as described herein or a pharmaceutically acceptable salt thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same. | 12-24-2015 |
20150368246 | TETRACYCLIC HETEROCYCLE COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF HEPATITIS C - The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. I | 12-24-2015 |
20150361101 | TETRACYCLIC HETEROCYCLE COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF HEPATITIS C - The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. | 12-17-2015 |
20150361098 | HETEROBICYCLO-SUBSTITUTED [1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES - Disclosed are compounds of Formula G1 (structurally represented): where “RG3” “Rd1” to “Rd4”, “n”, “m”, “p”, “W”, “X”, “Y”, and “Z” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions. | 12-17-2015 |
20150353570 | BTK INHIBITORS - The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders. | 12-10-2015 |
20150353565 | BTK INHIBITORS - The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or pharmaceutically acceptable salts thereof. Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders. | 12-10-2015 |
20150353553 | 2,6,7,8 SUBSTITUTED PURINES AS HDM2 INHIBITORS - The present invention provides 2,6,7,8 Substituted Purines as described herein or a pharmaceutically acceptable salt thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same. | 12-10-2015 |
20150353535 | THIAZOLE-SUBSTITUTED AMINOPYRIDINES AS SPLEEN TYROSINE KINASE INHIBITORS - The invention provides certain thiazole-substituted aminopyridine compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R | 12-10-2015 |
20150353498 | SUBSTITUTED ISOQUINOLINES AS CRTH2 RECEPTOR MODULATORS - The invention provides certain substituted isoquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters. The invention also provides pharmaceutical compositions comprising for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function. | 12-10-2015 |
20150344500 | C2,C6 OXACYCLIC-FUSED THIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE - In its many embodiments, the present invention provides certain C2-ring-substituted iminothiazine compounds, including compounds Formula (I): (structurally represented) or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and, wherein R1, R2, R3, R4, X, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed. | 12-03-2015 |
20150343157 | MEDICATION INJECTOR WITH NEAR-EMPTY ALERT - A medication injector that has an alert indicator that alerts the user when the medication injector is approaching near the end of its medication supply is disclosed. The alert indicator gives the user an opportunity to make preparations to obtain additional medication for the injector if there is an insufficient amount of medication in the injector to enable the user to dispense the required dosage amount with the next injection. Initially, the alert indicator is not visible to the user, but becomes visible to the user when the injector is near empty. | 12-03-2015 |
20150342931 | SPIROCYCLIC CETP INHIBITORS - Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis. The chemical compounds that are disclosed cholesterol ester transfer protein (CETP) and are expected to have utility in raising HDL-C, lowering LDL-C, and in the treatment and prevention of atherosclerosis. | 12-03-2015 |
20150337013 | NOVEL ANTIBACTERIAL AGENTS FOR THE TREATMENT OF GRAM POSITIVE INFECTIONS - The present invention relates to novel lipopeptide compounds, pharmaceutical compositions of these compounds and methods of using these compounds as antibacterial compounds. The compounds of the invention are particularly useful against a variety of bacteria, including resistant strains. The compounds are useful as antibacterial agents against | 11-26-2015 |
20150336991 | NOVEL GLUCOKINASE ACTIVATOR COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS, AND METHODS OF TREATMENT - Novel pyridine-2-carboxamide derivatives of formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are effective as glucokinase activating agents. Pharmaceutical compositions and methods of treatment are also included. | 11-26-2015 |
20150336946 | NOVEL 2-PYRIDINECARBOXAMIDE DERIVATIVES, COMPOSITIONS CONTAINING SUCH COMPOUNDS, AND METHODS OF TREATMENT - Novel pyridine-2-carboxamide derivatives of formula I and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are effective as glucokinase activating agents. Pharmaceutical compositions and methods of treatment are also included. The present invention relates to novel pyridine-2-carboxamide derivatives and salts thereof which are effective as glucokinase activating agents. Moreover, it relates to compositions containing such compounds, and methods of treatment. | 11-26-2015 |
20150335648 | HETEROCYCLE-SUBSTITUTED TETRACYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES - The present invention relates to novel Heterocycle-Substituted Tetracyclic Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, A′, R | 11-26-2015 |
20150329612 | PROCESS FOR PURIFYING INSULIN AND ANALOGUES THEREOF - A process is described for purifying insulin and insulin analogues that comprises high-pressure liquid chromatography with an acidic cation exchange medium performed under low to moderate pressure at an elevated temperature. | 11-19-2015 |
20150329562 | Factor IXa Inhibitors - The present invention provides a compound of Formula (I) | 11-19-2015 |
20150329557 | Inhibitors of the Renal Outer Medullary Potassium Channel - The present invention provides compounds of Formula I | 11-19-2015 |
20150329548 | SUBSTITUTED PYRROLOPYRIMIDINES AS HDM2 INHIBITORS - The present invention provides substituted pyrrolopyrimidines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same. | 11-19-2015 |
20150329539 | 4-PYRIDINONETRIAZINE DERIVATIVES AS HIV INTEGRASE INHIBITORS - The present invention relates to 4-Pyridinonetriazine Derivatives of Formula (I); and pharmaceutically acceptable salts thereof, wherein A, X, Y, R | 11-19-2015 |
20150329531 | AMINO-PYRIMIDINE-CONTAINING SPLEEN TYROSINE KINASE (SYK) INHIBITORS - The invention provides certain amino-pyrimidine-containing compounds. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase. | 11-19-2015 |
20150329521 | PROCESS FOR MAKING REVERSE TRANSCRIPTASE INHIBITORS - The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1H)-one derivatives. The compounds synthesized by the processes of the invention are HIV reverse transcriptase inhibitors useful for inhibiting reverse transcriptase, HIV replication and the treatment of human immunodeficiency virus infection in humans. | 11-19-2015 |
20150322074 | 4-FLUOROPIPERIDINE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to 4-fluoropiperidine compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 11-12-2015 |
20150322056 | Factor IXa Inhibitors - The present invention provides a compound of Formula (I) | 11-12-2015 |
20150322041 | 2-PYRIDYLOXY-4-NITRILE-4-SUBSTITUTED OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to 2-pyridyloxy-3-nitrile-4-substituted compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-3-nitrile-4-substituted compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 11-12-2015 |
20150322040 | 3-ESTER-4 SUBSTITUTED OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to 3-ester-4-substituted compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 3-ester-4-substituted compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 11-12-2015 |
20150322039 | 2-PYRIDYLAMINO-4-NITRILE-PIPERIDINYL OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to 2-pyridylamino-4-nitrile-piperidinyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridylamino-4-nitrile-piperidinyl compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 11-12-2015 |
20150320733 | INDAZOLE COMPOUNDS AS ALDOSTERONE SYNTHASE INHIBITORS - This invention relates to indazole compounds of the structural formula: (structure represented) or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment or amelioration of conditions that could be treated by inhibiting aldosterone synthase. | 11-12-2015 |
20150320724 | METHODS OF TREATING DIABETES BY ADMINISTERING A GLUCAGON RECEPTOR ANTAGONIST IN COMBINATION WITH A CHOLESTEROL ABSORPTION INHIBITOR - Use of a glucagon receptor antagonist in combination with a cholesterol absorption inhibitor for the treatment of diabetes and related conditions is disclosed. | 11-12-2015 |
20150315226 | DISULFIDE MASKED PRODRUG COMPOSITIONS AND METHODS - The present invention relates to disulfide masked prodrug compounds, compositions and methods that are amenable to bioactivation by a reducing agent such as glutathione. Such disulfide based compounds, compositions, and methods can be useful, for example, in providing novel prodrugs for use as therapeutics. | 11-05-2015 |
20150315221 | NUCLEOSIDE KINASE BYPASS COMPOSITIONS AND METHODS - The present invention relates to disulfide masked prodrug compounds, compositions and methods that are amenable to bioactivation by a reducing agent such as glutathione. Such disulfide based compounds, compositions, and methods can be useful, for example, in providing novel prodrugs for use as therapeutics. | 11-05-2015 |
20150315141 | Thrombin Inhibitors - Compounds of the invention, which may be useful in inhibiting thrombin and associated thrombotic occlusions, have the following structure: | 11-05-2015 |
20150307850 | CONDITIONAL REPLICATING VIRAL VECTORS - The present invention relates to a cytomegalovirus (CMV) which has been recombinantly altered to express a heterologous polypeptide and to allow for external control of viral replication. The heterologous polypeptide may be a polypeptide of interest such as an antigen, antibody or immune modulator. The CMV vectors of the invention are replication defective, or chemically controllable replication capable, or replication competent. The present invention also relates to uses of the CMV vectors such as inducing an immune response to an antigen or expressing an antibody or immune modulator in vivo. Compositions comprising the CMV expressing the heterologous polypeptide are also encompassed by the present invention. | 10-29-2015 |
20150307591 | ON-COLUMN REFOLDING AND PURIFYING OF LIPOPROTEINS - Provided are methods of refolding and purifying lipoproteins on a chromatography column. In particular methods of refolding ApoL1 polypeptides using a hydrophobic interaction column (HIC). The present invention provides methods for the purification of an active form of a human lipoprotein, such as ApoL1. More particularly, the present invention relates to a method for renaturing an inclusion body of proteins expressed in a large quantity in | 10-29-2015 |
20150307533 | SPIROCYCLIC SULFONES AS GAMMA SECRETASE INHIBITORS - Disclosed herein are compounds of Formula (I), wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease. | 10-29-2015 |
20150307489 | PYRIMIDINE PDE10 INHIBITORS - The present invention is directed to pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction. | 10-29-2015 |
20150307488 | CYCLOPROPYL IMIDAZOPYRIDINE PDE10 INHIBITORS - The present invention is directed to substituted cyclopropyl imidazopyridine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction. | 10-29-2015 |
20150307479 | CYCLOBUTYL BENZIMIDAZOLES AS PDE 10 INHIBITORS - The present invention is directed to substituted cyclobutyl benzimidazole compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction. | 10-29-2015 |
20150307465 | Iminothiadiazine Dioxide Compounds as BACE Inhibitors, Compositions and Their Use - In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): | 10-29-2015 |
20150307464 | THERAPEUTIC THIAZOLIDINONE COMPOUNDS - Thiazolidinone compounds, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. | 10-29-2015 |
20150306091 | ALDOSTERONE SYNTHASE INHIBITORS - This invention relates to tricyclic triazole compounds or their pharmaceutically acceptable salts. The inventive compounds selectively inhibit aldosterone synthetase. This invention also provides for pharmaceutical compositions comprising the above-cited compounds or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthetase. | 10-29-2015 |
20150299648 | IMPROVED CULTIVATION MEDIA AND PROCESS FOR IMPROVED PROTEIN PRODUCTION BY PICHIA STRAINS - The present invention provides optimized cell culture media and fed-batch cultivation processes to improve the viability and volumetric production of heterologous proteins in | 10-22-2015 |
20150299243 | 2'-ALKYNYL SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES - The present invention relates to 2′-Alkynyl Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2, R3 and R4 are as defined herein. The present invention also relates to compositions comprising at least one 2′-Alkynyl Substituted Nucleoside Derivative, and methods of using the 2′-Alkynyl Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient. | 10-22-2015 |
20150299227 | INHIBITORS OF CATECHOL O-METHYL TRANSFERASE AND THEIR USE IN THE TREATMENT OF PSYCHOTIC DISORDERS - The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved. | 10-22-2015 |
20150299224 | INHIBITORS OF IRAK4 ACTIVITY - The present invention relates to compounds which modulate interleukin-1 (IL-1) receptor-associated kinase 4 (IRAK4) and are useful in the prevention or treatment of inflammatory, cell proliferative and immune-related conditions and diseases. Specifically, provided herein are inhibitors of IRAK4 of Formula I and pharmaceutical compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases. | 10-22-2015 |
20150299198 | Inhibitors of the Renal Outer Medullary Potassium Channel - The present invention provides compounds of Formula I | 10-22-2015 |
20150299167 | Regioselective N-2 Arylation of Indazoles - A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: | 10-22-2015 |
20150299125 | PRODRUG BIPYRIDYLAMINOPYRIDINES AS SYK INHIBITORS - The present invention provides compounds of Formula (I), which are prodrugs of trans-4-[(1R)-(6-{[4-(difluoromethyl)pyridin-2-yl]amino}-4-methyl-2,3′-bipyridin-6′-yl)-1-hydroxyethyl]cyclohexanecarboxylic acid, a potent inhibitor of Syk. The compounds are useful in the treatment and prevention of diseases mediated by the enzyme, such as asthma, COPD, rheumatoid arthritis and cancer. | 10-22-2015 |
20150291683 | MODIFIED APOL1 POLYPEPTIDES - Modified ApoL1 polypeptides are provided, in particular, the modified polypeptides are expressed without an N-terminal or f-Methionine in bacterial cells. Also provided is a method of recombinantly producing the modified polypeptide. | 10-15-2015 |
20150291561 | SUBSTITUTED PYRIDONE DERIVATIVES AS PDE10 INHIBITORS - The present invention is directed to substituted pyridinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction. | 10-15-2015 |
20150291558 | 2-PYRIDYLOXY-3-SUBSTITUTED-4-NITRILE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to 2-pyridyloxy-3-substituted-4-nitrile compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-3-substituted-4-nitrile compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 10-15-2015 |
20150290325 | LIQUID FORMULATIONS FOR TNFR:Fc FUSION PROTEINS - The invention provides stable liquid formulations for a recombinant biopharmaceutical protein comprising a soluble form of the human p75 TNF receptor fused to an Fe domain of a human immunoglobulin protein (TNFR:Fc). Typically, biopharmaceutical proteins such as monoclonal antibodies (mAbs) and immunoglobulin fusion proteins (e.g., immunoadhesion proteins) are produced by recombinant DNA technology in mammalian cell expression systems. In order to guarantee the reproducible clinical performance of a biopharmaceutical product, manufacturers have to deliver a product of consistent and reproducible quality. | 10-15-2015 |
20150290135 | PROCESS FOR MAKING AGGLOMERATES USING ACOUSTIC MIXING TECHNOLOGY - Described herein is a process for preparing agglomerates comprising: (i) providing a dry powder mixture of one, two, or three active pharmaceutical agent(s), and at least one excipient; and (ii) applying acoustic energy to said dry powder mixture to form agglomerates. | 10-15-2015 |
20150284389 | N-SUBSTITUTED INDAZOLE SULFONAMIDE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS - Disclosed are compounds of Formula A | 10-08-2015 |
20150284379 | TRICYCLIC SUBSTITUTED THIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS AND THEIR USE - In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): (I) and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein the middle ring (referred to herein as “ring B”) of the tricyclic substituent is an optionally substituted 6-membered ring, and each of the remaining variables shown in the formula are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed. | 10-08-2015 |
20150284376 | MINERALOCORTICOID RECEPTOR ANTAGONISTS - The present invention is directed to compounds of the Formula I | 10-08-2015 |
20150284368 | SECONDARY ALCOHOL SUBSTITUTED TRIAZOLES AS PDE10 INHIBITORS - The present invention is directed to secondary alcohol substituted triazole compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction. | 10-08-2015 |
20150274767 | 4'-SUBSTITUTED NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS - The present invention is directed to 4′-substituted nucleoside derivatives of Formula I | 10-01-2015 |
20150274739 | 2'-CYANO SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES - Compounds of Formula (I) are disclosed, wherein R | 10-01-2015 |
20150274716 | TRICYCLIC SUBSTITUTED THIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS AND THEIR USE - In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein the middle ring (referred to herein as “ring B”) of the tricyclic substituent is an optionally substituted 5-membered ring, and each of the remaining variables shown in the formula are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed. | 10-01-2015 |
20150274708 | INHIBITORS OF IRAK4 ACTIVITY - The present invention relates to inhibitors of IRAK4 of Formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases. | 10-01-2015 |
20150274672 | SUBSTITUTED SPIROPIPERIDINYL COMPOUNDS USEFUL AS GPR120 AGONISTS - The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing diabetes, hyperlipidemia, obesity, inflammation related disorders, and related diseases and conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR120. Pharmaceutical compositions and methods of treatment are also included. | 10-01-2015 |
20150266897 | HCV NS3 Protease Inhibitors - The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections. | 09-24-2015 |
20150266895 | NOVEL COMPOUNDS THAT ARE ERK INHIBITORS - Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1). | 09-24-2015 |
20150265715 | POSACONAZOLE INTRAVENOUS SOLUTION FORMULATIONS STABILIZED BY SUBSTITUTED BETA-CYCLODEXTRIN - The present invention relates to aqueous solutions useful as pharmaceutical compositions of posaconazole for intravenous administration. These compositions include a solubilizing agent, such as a modified β-cyclodextrin in an acidified solution, which can also include a chelating agent such as disodium edetate (EDTA). In clinical trials, a 200 mg posaconazole dose of the selected composition was found to achieve acceptable pharmacokinetic properties. | 09-24-2015 |
20150260731 | ANTIBODIES, KIT AND METHOD FOR DETECTING AMYLOID BETA OLIGOMERS - This invention is a selective Aβ oligomer kit and immunoassay method capable of reliably and sensitively detecting Aβ oligomers in a biological sample of a patient. In one embodiment the inventive assay uses a pair of anti-Aβ oligomer antibodies, as capture and detection antibodies, to detect and quantify Aβ oligomers. The method can be used to differentiate Alzheimer's disease (AD) patients from non-AD patients and/or to stratify AD patients according to the severity of their disease. | 09-17-2015 |
20150258074 | NOVEL COMPOUNDS THAT ARE ERK INHIBITORS - Disclosed are the ERK inhibitors of formula (1.0), having a pyrazolopyridine base structure, and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0). | 09-17-2015 |
20150253341 | QUANTIFICATION OF TAU IN BIOLOGICAL SAMPLES BY IMMUNOAFFINITY ENRICHMENT AND MASS SPECTROMETRY - The present invention provides a quantitative immunoaffinity LC-MS/MS assay for detection and quantification of Tau protein in a biological sample. | 09-10-2015 |
20150252033 | 2-PYRIDYLOXY-3-ESTER-4-NITRILE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to 2-pyridyloxy-3-ester-4-nitrile compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-3-ester-4-nitrile compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 09-10-2015 |
20150250759 | COMPOSITION FOR INHIBITION OF CATHEPSIN K - The present invention relates to the a method of inhibiting bone resorption in a mammal in need thereof with an oral pharmaceutical composition comprising a cathepsin K inhibitor, or a pharmaceutically acceptable salt thereof, or a mixture thereof, according to a continuous schedule having a dosage interval of once weekly, biweekly, twice monthly or once monthly. | 09-10-2015 |
20150246917 | INHIBITORS OF HEPATITIS C VIRUS REPLICATION - The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. | 09-03-2015 |
20150246902 | SUBSTITUED BENZOFURAN COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES - The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. | 09-03-2015 |
20150239866 | TRIAZOLYL DERIVATIVES AS SYK INHIBITORS - Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer. | 08-27-2015 |
20150232447 | CRYSTALLINE FORM OF A REVERSE TRANSCRIPTASE INHIBITOR - The retrovirus designated human immunodeficiency virus (HIV), particularly the strains known as HIV type-1 (HIV-1) and type-2 (HIV-2), have been etiologically linked to the immunosuppressive disease known as acquired immunodeficiency syndrome (AIDS). HIV seropositive individuals are initially asymptomatic but typically develop AIDS related complex (ARC) followed by AIDS. Affected individuals exhibit severe immunosuppression which makes them highly susceptible to debilitating and ultimately fatal opportunistic infections. The invention is directed to a novel crystalline form of the RT inhibitor 3-chloro-5-({1-[(4-methyl-5 -oxo-4,5-dihydro-1 H-1,2, 4-triazol-3-yl)methyl]-2-oxo-4-(trifluoromethy 1)-1,2-dihydropyridin-3-yl) oxy)benzonitrile used in the treatment HIV infection and AIDS. | 08-20-2015 |
20150232428 | SUBSTITUTED PHENYL-SPLEEN TYROSINE KINASE (SYK) INHIBITORS - The invention provides certain substituted phenyl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R | 08-20-2015 |
20150225365 | INDOLINE COMPOUNDS AS ALDOSTERONE SYNTHASE INHIBITORS - This invention relates to indo line compounds of the structural formula I, or their pharmaceutically acceptable salts, wherein the variables are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase. | 08-13-2015 |
20150218097 | GLYCOSIDASE INHIBITORS AND USES THEREOF - The invention provides compounds of Formula (I) for inhibiting gh cosidases, prodrugs of the compounds, and pharmaceutical compositions comprising the compounds or prodrugs of the compounds. The invention also provides method of treating diseases and disorders related to deficiency or over-expression of O-gh coprotein 2-acetamido-2-deoxy-β-D-glucopyranosidase (O-GlcNAcase), accumulation or deficiency of 2-acetamido-2-deoxy-β-D-glucopyranoside (O-GlcNAc). | 08-06-2015 |
20150209424 | INACTIVATED VARICELLA ZOSTER VIRUS VACCINES, METHODS OF PRODUCTION, AND USES THEREOF - The invention provides an inactivated varicella zoster virus (VZV), and compositions and vaccines comprising said inactivated VZV, wherein the infectivity of the VZV is undetectable and wherein the inactivated VZV induces an immune response against VZV when administered to a patient. In embodiments of the compositions described herein, the VZV is inactivated with gamma radiation. The invention also provides a method of preparing an inactivated VZV vaccine, the method comprising gamma irradiating a sample comprising a VZV using from about 5 kGy to about 50 kGy of gamma radiation. Also provided by the invention herein is a method of treatment of or immunization against HZ or other disease associated with the reactivation of VZV, the method comprising administering to a subject a vaccine or pharmaceutical composition comprising a therapeutically effective amount of an inactivated VZV and a pharmaceutically acceptable carrier, wherein the VZV is inactivated by gamma irradiation. | 07-30-2015 |
20150197772 | MAMMALIAN EXPRESSION VECTOR pUHAB - The present invention relates to the construction and utilization of a new mammalian expression vector that contains a unique multiple cloning site (MCS), designated pUHAB. The pUHAB vector comprises a high copy replication origin (ColE1), a drug resistance gene (TK-Hygromycin), and a human cytomegalovirus promoter operably associated with a unique intron (hCMV/intron). Further, pUHAB comprises a selectable marker conferring resistance to kanamycin in bacterial cells, and a phage f1(+) region. pUHAB can be used to transiently or stably express cloned genes when transfected into mammalian cells. The invention also encompasses kits and host cells and cell lines comprising pUHAB, and methods of producing a recombinant protein using pUHAB. | 07-16-2015 |
20150197531 | SULFONAMIDE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG - The present invention relates to Sulfonamide Derivatives of Formula (I): | 07-16-2015 |
20150197490 | CRYSTALLINE POLYMORPHIC FORMS OF AN ANTIDIABETIC COMPOUND - The present invention relates to polymorphic forms of a compound of formula A: | 07-16-2015 |
20150191461 | PYRAZOLYL DERIVATIVES AS SYK INHIBITORS - The present invention provides novel pyrazole derivatives of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer. | 07-09-2015 |
20150190402 | SOLID DOSAGE FORMULATIONS OF AN OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to a pharmaceutical composition comprising the compound suvorexant, or a pharmaceutically acceptable salt thereof, a concentration-enhancing polymer, and optionally a pharmaceutically acceptable surfactant. The concentration-enhancing polymer is a polymer that forms an amorphous dispersion with suvorexant, that is insoluble or almost completely insoluble in water by (a) dissolving the suvorexant or (b) interacting with the suvorexant in such a way that the suvorexant does not form crystals or crystalline domains in the polymer. A concentration-enhancing polymer is water soluble or readily disperse in water, so that when the polymer is placed in water or an aqueous environment (e.g. fluids in the gastrointestinal (GI) tract or simulated GI fluids), the solubility and/or bioavailability of suvorexant is increased over the solubility or bioavailability in the absence of the polymer. | 07-09-2015 |
20150182503 | MINERALOCORTICOID RECEPTOR ANTAGONISTS - The present invention is directed to compounds of the Formula I: as well as pharmaceutically acceptable salts thereof, that may be useful for treating aldosterone-mediated diseases. The invention furthermore relates to specific diastereomers and enantiomers of the compounds, to processes for preparing compounds of the Formula I, to their potential use for the therapy and prophylaxis of the above-mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula I. | 07-02-2015 |
20150158935 | PROTECTIVE VACCINE BASED ON STAPHYLOCOCCUS AUREUS SA2493 PROTEIN - The present invention relates to methods of inducing an immune response to | 06-11-2015 |
20150147337 | CRYSTALLINE ANTI-HUMAN IL-23 ANTIBODIES - Crystalline forms of antibodies to human IL-23, such as antibodies to human IL-23p19, are provided, as well as methods of producing such crystalline forms, and uses of such crystalline forms, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders. In various embodiments, the anti-hulL-23 antibody crystals, such as anti-hulL-23p19 antibody crystals of the present invention are obtainable by batch crystallization methods, vapor diffusion methods, liquid-liquid diffusion methods, and dialysis. In other aspects, the invention relates to suspensions of the crystalline anti-hulL-23 antibodies of the present invention, including those at higher concentrations and lower viscosities than would be possible with a corresponding non-crystalline solution at the same concentration of antibody. In other embodiments, the anti-huiL-23 antibody crystals of the present invention have increased stability, i.e. they maintain biological activity of the anti-huiL-23 antibody, such as anti-huiL-23p 19 antibody, longer than corresponding solution formulations. | 05-28-2015 |
20150141444 | N-METHYL TETRAHYDROQUINOLINE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to N-methyl tetrahydroquinoline compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | 05-21-2015 |
20150141428 | TrkA Kinase Inhibitors, Compositions and Methods Thereof - The present invention is directed to benzyl urea compounds, which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C. | 05-21-2015 |
20150111866 | CYCLIC AMINE SUBSTITUTED HETEROCYCLIC CETP INHIBITORS - Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis. | 04-23-2015 |
20150105354 | HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS - Disclosed are compounds of the formula I | 04-16-2015 |
20150104453 | FDF03 ANTIBODIES AND USES THEREOF - The present invention relates to methods for identifying and using modulators of FDF03 biological activity in vitro and in vivo that are useful in the treatment of cancer. | 04-16-2015 |
20150099771 | PYRIDINE CGRP RECEPTOR ANTAGONISTS - The present invention is directed to pyridine derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved. | 04-09-2015 |
20150099729 | INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL - The present invention provides compounds of Formula I | 04-09-2015 |
20150099715 | FORMULATIONS OF ACADESINE - This invention provides a buffered solution comprising acadesine, as well as compositions, formulations and kits containing said solution. The solution, compositions, formulation, and kits can be used to prevent morbidity/mortality in a patient or to treat an ischaemic condition, a condition regulated by adenosine, or a condition associated with reduced blood flow to a tissue in a patient. | 04-09-2015 |
20150087832 | PROCESS FOR MAKING BETA 3 AGONISTS AND INTERMEDIATES - The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are useful in the treatment of certain disorders, including overactive bladder, urinary incontinence, and urinary urgency. | 03-26-2015 |
20150051227 | PREDICTIVE BIOMARKER USEFUL FOR CANCER THERAPY MEDIATED BY A CDK INHIBITOR - The present invention provides a predictive biomarker whose expression level is useful for identifying patients responsive to a therapeutically effective dose of a CDK inhibitor. In one embodiment of the invention, the predictive biomarker is the ratio of MCL-1 to BCL-xL (MCL-1:BCL-xL ratio) and the CDK inhibitor is SCH 927965 (Dinaciclib). | 02-19-2015 |
20150045346 | SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF - The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc. | 02-12-2015 |
20150044250 | VACCINES AGAINST CLOSTRIDIUM DIFFICILE COMPRISING RECOMBINANT TOXINS - The present invention relates to recombinant | 02-12-2015 |
20150038490 | SPIROPYRROLIDINE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE - The present invention is directed to spiropyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved. | 02-05-2015 |
20150031891 | BIS-QUARTERNARY CINCHONA ALKALOID SALTS AS ASYMMETRIC PHASE TRANSFER CATALYSTS - The invention is directed to novel bis-quarternary cinchona alkaloid salts and the use of bis-quarternary cinchona alkaloid salts in asymmetric phase transfer catalysis. The present invention is directed to novel bis-quarternary cinchona alkaloid salts and the use of bis-quarternary cinchona alkaloid salts in asymmetric phase transfer catalysis. On certain substrates and under specific reaction conditions, the inventors have discovered that the use of bis-quarternary cinchona alkaloid salts in asymmetric phase transfer catalysis surprisingly provides for a more active and efficient process as compared to mono-quarternary catalysts. | 01-29-2015 |
20150024071 | INHIBITORS OF CATECHOL O-METHYL TRANSFERASE AND THEIR USE IN THE TREATMENT OF PSYCHOTIC DISORDERS - The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved. | 01-22-2015 |
20140371138 | INHIBITORS OF HEPATITIS C VIRUS REPLICATION - The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. | 12-18-2014 |
20140350002 | IMIDAZOPYRIDIN-2-ONE DERIVATIVES - The present invention is directed to imidazopyridin-2-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR | 11-27-2014 |
20140349998 | PYRROLOPYRIMIDINES AS JANUS KINASE INHIITORS - The instant invention provides compounds of formula I which are JAK3 inhibitors. Specifically, the compounds of formula I are pyrrolo[2,3-d]pyrimidine derivative compounds. The instant invention also provides methods of treating JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer, by administering the pyrrolo[2,3-d]pyrimidine-derivative compounds of formula I. | 11-27-2014 |
20140349972 | SUBSTITUTED PYRIMIDINES - The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions. | 11-27-2014 |
20140348841 | ANTI-GITR ANTIBODIES - Antibodies to human GITR are provided, as well as uses thereof, e.g., in treatment of proliferative and immune disorders. | 11-27-2014 |
20140343071 | COMPOSITIONS AND METHODS FOR TREATING CANCER - The instant invention provides a method of treating a cancer, selected from the group consisting of breast cancer, melanoma, colorectal cancer, non-small cell lung cancer and ovarian cancer, by administering a combination of a WEE1 inhibitor and a CHK1 inhibitor, wherein the WEE1 inhibitor is MK-1775 or a pharmaceutically acceptable salt thereof, or MK-3652 or a pharmaceutically acceptable salt thereof, and the CHK1 inhibitor is MK-8776 or a pharmaceutically acceptable salt thereof, or SCH900444 or a pharmaceutically acceptable salt thereof. | 11-20-2014 |
20140336196 | PHOSPHORIC ACID SALTS OF SITAGLIPTIN - The present invention relates to novel phosphoric acid salts of 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine, and polymorphs, hydrates and solvates thereof, which are potent inhibitors of dipeptidyl peptidase-IV useful for the prevention and/or treatment of non-insulin dependent diabetes mellitus, also referred to as type 2 diabetes. The present invention also relates to the process for preparing the novel phosphoric acid salts of 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine, as well as pharmaceutical compositions containing the novel phosphoric acid salts, and methods of use thereof for the treatment of diabetes, obesity, and high blood pressure. | 11-13-2014 |
20140329276 | METHODS FOR INCREASING N-GLYCAN OCCUPANCY AND REDUCING PRODUCTION OF HYBRID N-GLYCANS IN PICHIA PASTORIS STRAINS LACKING ALG3 EXPRESSION - Methods for increasing the yield and N-glycosylation site occupancy of paucimannose or complex N-glycans of recombinant glycoproteins produced in a recombinant host cell lacking dolichyl-P-Man:Man5GlcNAc2-PP-dolichyl alpha-1,3 mannosyltransferase (Alg3p) activity are disclosed. In particular, recombinant host cells are provided that comprise a disruption of the expression of an OS-9 family gene in the host cell. These recombinant host cells may then be used for producing recombinant glycoproteins. In further embodiments, the recombinant host cells further overexpress at least one heterologous single-subunit oligosaccharyltransferase, which in particular embodiments is capable of functionally suppressing the lethal phenotype of a mutation of at least one essential protein of the yeast oligosaccharyltransferase (OTase) complex. | 11-06-2014 |
20140323519 | HETEROCYCLIC COMPOUNDS AS B-RAF INHIBITORS FOR TREATMENT OF CANCER - This invention relates to novel heterocyclic compounds that are useful for treating cancer and other cellular proliferative diseases and/or disorders associated with B-Raf activity. The compounds of the invention may be illustrated by the Formula (I). (Formula (I)) | 10-30-2014 |
20140296222 | IMINOTHIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE - In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): | 10-02-2014 |
20140296221 | IMINOTHIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE - In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): | 10-02-2014 |
20140296205 | SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF - The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc. | 10-02-2014 |
20140296202 | SUBSTITUTED PIPERIDINYL COMPOUNDS USEFUL AS GPR119 AGONISTS - Substituted piperidinyl compounds of the formula (I): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119. | 10-02-2014 |
20140275022 | SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF - The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc. | 09-18-2014 |
20140275017 | CGRP RECEPTOR ANTAGONISTS - Compounds of Formula I: | 09-18-2014 |
20140256818 | NANO-SUSPENSION PROCESS - Described herein is a process for preparing nano-suspensions, wherein the process comprises: providing an admixture of at least one active pharmaceutical compound, an aqueous dispersion medium, and milling media and applying thereto acoustic energy having a frequency of from about 10 hertz to 1000 hertz and which supplies a linear acceleration of from about 10 G′s to about 100 G′s (where “G” is the force of gravity) for a period sufficient to supply a nano-suspension having a D | 09-11-2014 |
20140248279 | USE OF IL-23 AND IL-17 ANTIAGONISTS TO TREAT AUTOIMMUNE OCULAR INFLAMMATORY DISEASE - Novel methods and drug products for treating autoimmune ocular inflammatory disease are disclosed, which involve administration of agents that antagonize one or both of IL-17 and IL-23 activity. | 09-04-2014 |
20140244289 | COLD STORAGE SYSTEM FOR STORING PHARMACEUTICAL PRODUCT CONTAINERS - Intelligent cold storage system for storing pharmaceutical product containers, such as vials, ampules, syringes, bottles, medication tubes, blister packs and cartons, at the point of dispensing. Embodiments of the invention use product identification technology, such as radio-frequency identification (RFID) tags and barcode readers, to uniquely identify containers as they are added to or removed from the cold storage compartment, and automatically retrieve from a local or remote database a variety of details associated with the containers and their contents, such as manufacturing data, expiration dates, time out of refrigeration, inventory levels, safety information, usage statistics, known contraindications and warnings, etc. If the details indicate that there is a problem with a particular pharmaceutical (e.g., that it is counterfeit, expired, suspect, spoiled, recalled or almost depleted), then a message or warning is automatically delivered to a human operator via an attached output device, such as a display screen, speaker or printer. Embodiments of the invention may also be configured to monitor and report temperature faults, power failures and other anomalies associated with the cold storage system or cold storage compartment. | 08-28-2014 |
20140235537 | N-GLYCOSYLATED INSULIN ANALOGUES - Compositions and formulations comprising N-glycosylated insulin analogues are described. In particular embodiments, the glycosylated insulin analogues are produced in vivo and comprise one or more the N-linked N-glycans selected from high mannose or fucosylated or non-fucosylated hybrid, paucimannose, or complex N-glycans. In other embodiments, the N-glycan comprising the high mannose or fucosylated or non-fucosylated hybrid, paucimannose, or complex N-glycan is attached to the insulin analogue in vitro. Examples of N-glycans include but are not limited to a molecule having a structure selected from N-glycans in the group consisting of Man( | 08-21-2014 |
20140234301 | Modulation of PILR to Treat Immune Disorders - The present invention provides methods of using PILRα agonists, or PILRβ antagonists, to treat immune disorders, such as autoimmune and inflammatory disorders, including CNS, joint and gut inflammation. | 08-21-2014 |
20140234296 | STABLE FORMULATIONS OF ANTIBODIES TO HUMAN PROGRAMMED DEATH RECEPTOR PD-1 AND RELATED TREATMENTS - The present invention relates to stable formulations of antibodies against human programmed death receptor PD-1, or antigen binding fragments thereof. The present invention further provides methods for treating various cancers and chronic infections with stable formulations of antibodies against human programmed death receptor PD-1, or antigen binding fragments thereof. | 08-21-2014 |
20140221383 | CETP INHIBITORS - Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: | 08-07-2014 |
20140220027 | 1D05 PCSK9 ANTAGONISTS - Antagonists of human proprotein convertase subtilisin-kexin type 9 (“PCSK9”) are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure. | 08-07-2014 |
20140213584 | SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF - The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc. | 07-31-2014 |
20140212412 | USE OF IL-33 ANTAGONISTS TO TREAT FIBROTIC DISEASE - Methods for treating fibrotic disease, such as idiopathic pulmonary fibrosis and scleroderma, with antagonists of IL-33 are disclosed. | 07-31-2014 |
20140206715 | PREPARATION AND USE OF COMPOUNDS AS PROTEASE INHIBITORS - Disclosed are compounds of the formula I | 07-24-2014 |
20140206675 | IMINOTHIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE - In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): (I) and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R | 07-24-2014 |
20140206665 | SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF - The invention is directed to compounds for selectively inhibiting glycosidases, uses of the compounds and pharmaceutical compositions including the compounds, and methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, and/or accumulation or deficiency of O-GlcNAc. | 07-24-2014 |
20140206640 | 2'-AZIDO SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES - The present invention relates to 2′-Azido Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R | 07-24-2014 |
20140206563 | BIOMARKERS FOR PSORIASIS - A group of polypeptides that are modulated in a psoriatic sample as compared to a normal sample is provided. These polypeptides can be used as biomarkers for diagnosis and monitoring treatment of psoriasis. | 07-24-2014 |
20140200213 | 2-SPIRO-SUBSTITUTED IMINOTHIAZINES AND THEIR MONO-AND DIOXIDES AS BACE INHIBITORS, COMPOSITIONS AND THEIR USE - In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): | 07-17-2014 |
20140200180 | METHOD FOR PRODUCING PROTEINS IN PICHIA PASTORIS THAT LACK DETECTABLE CROSS BINDING ACTIVITY TO ANTIBODIES AGAINST HOST CELL ANTIGENS - Methods for producing proteins and glycoproteins in | 07-17-2014 |
20140171480 | CRYSTALLINE POLYMORPHIC FORMS OF AN ANTIDIABETIC COMPOUND - The present invention relates to polymorphic forms of a compound of formula A: | 06-19-2014 |
20140171456 | FUSED TRICYCLIC COMPOUNDS AS mTOR INHIBITORS - The present invention relates to certain pyrazolo[1,5-a]pyrrolo[3,2-e]pyrimidine and dipyrazolopyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrrolo[3,2-e]pyrimidine or dipyrazolopyrimidine compounds. | 06-19-2014 |
20140171437 | OXAZOLE DERIVATIVES USEFUL AS INHIBITORS OF FAAH - The present invention is directed to certain oxazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease. | 06-19-2014 |
20140170658 | MAMMALIAN CYTOKINES; RELATED REAGENTS - Purified genes encoding a cytokine or composite cytokine from a mammal, reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding these molecules are provided. Methods of using said reagents and diagnostic kits are also provided. | 06-19-2014 |
20140170154 | ENGINEERED ANTI-IL-23R ANTIBODIES - Antibodies to human IL-23R are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders. | 06-19-2014 |
20140161798 | ANTI-PCSK9 AND METHODS FOR TREATING LIPID AND CHOLESTEROL DISORDERS - The present invention provides compositions and methods for treating disorders of cholesterol and lipid metabolism by administration of an anti-PCSK9 antibody or a peptide inhibitor of PCSK9. | 06-12-2014 |
20140161770 | 2'-CYANO SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF USEFUL FOR THE TREATMENT OF VIRAL DISEASES - The present invention relates to 2′-Cyano Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R | 06-12-2014 |
20140147461 | POLYPEPTIDES FOR INDUCING A PROTECTIVE IMMUNE RESPONSE AGAINST STAPHYLOCOCCUS AUREUS - The present invention features polypeptides comprising an amino acid sequence structurally related to SEQ ID NO: 1 and uses of such polypeptides and compositions thereof. SEQ ID NO: 1 is a full length | 05-29-2014 |
20140147442 | USE OF IL-23 ANTAGONISTS FOR TREATMENT OF INFECTION - Methods and compositions comprising antagonists of IL-23 are provided for the treatment of infections, such as chronic bacterial, viral and fungal infections. | 05-29-2014 |
20140142115 | INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL - This invention relates to compounds having structural Formula I: | 05-22-2014 |
20140141445 | Isolated Mammalian Monocyte Cell Genes; Related Reagents - DNA clones encoding a receptor in the Ig superfamily and a related soluble variant have been isolated from a human monocyte library. The invention provides receptor polypeptides, nucleic acids encoding them, expression vectors, and transformed cells for recombinant production of the polypeptides. | 05-22-2014 |
20140141444 | Isolated Mammalian Monocyte Cell Genes; Related Reagents - DNA clones encoding a receptor in the Ig superfamily and a related soluble variant have been isolated from a human monocyte library. The invention provides receptor polypeptides, nucleic acids encoding them, expression vectors, and transformed cells for recombinant production of the polypeptides. | 05-22-2014 |
20140141012 | ENGINEERED ANTI-TSLP ANTIBODY - The invention relates to binding compounds that specifically bind to human TSLP, as well as uses thereof, e.g., in the treatment of inflammatory disorders and allergic inflammatory response. | 05-22-2014 |
20140140954 | METHODS OF MODULATING CYTOKINE ACTIVITY; RELATED REAGENTS - Provided are methods of modulating cytokine activity, e.g., for the purpose of treating immune and inflammatory disorders, including tumors and cancer. Also provided are methods of administering agonists or antagonists of IL-33 and IL-33 receptor. | 05-22-2014 |
20140128368 | SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS, AND METHODS OF TREATMENT - Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included. | 05-08-2014 |
20140128367 | CYCLOALKYL-FUSED TETRAHYDROQUINOLINES AS CRTH2 RECEPTOR MODULATORS - The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R | 05-08-2014 |
20140128361 | CYCLIC AMIDE BACE-1 INHIBITORS HAVING A BENZAMIDE SUBSTITUENT - Disclosed are compounds of the formula | 05-08-2014 |
20140120037 | METHOD FOR DETECTION OF AMYLOIDS BETA OLIGOMERS IN A FLUID SAMPLE AND USES THEREOF - The invention herein is directed to a selective Aβ oligomer immunoassay capable of reliably and sensitively detecting Aβ oligomers in a biological sample of a patient. In one embodiment the inventive assay uses a pair of anti-Aβ oligomer antibodies, 19.3 and 82E1, to detect and quantify Aβ oligomers in a cerebrospinal fluid (CSF) sample. The inventive assay can be used to differentiate Alzheimer's disease (AD) patients from non-AD patients and/or to stratify AD patients according to the severity of their disease. The inventive assay can also be used as a target engagement assay that can measure bound Aβ oligomers as a surrogate end-point for the assessment of therapeutic efficacy and/or target engagement. | 05-01-2014 |
20140113920 | TRICYCLIC HETEROCYCLES USEFUL AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS - The present invention is directed to novel tricyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved. | 04-24-2014 |
20140112919 | INTERLEUKIN-10 ANTIBODIES - The methods and compositions provided herein relate generally to IL-10 specific antibodies and uses thereof. More specifically, compositions of humanized IL-10 specific antibodies and methods to use such antibodies in modulating the biological activity of IL-10, particularly in autoimmune disorders and pathogen-mediated immunopathology. | 04-24-2014 |
20140107346 | PROCESS FOR PREPARING CHIRAL DIPEPTIDYL PEPTIDASE-IV INHIBITORS - A process for the preparation of pyrazolopyrolidines of structural formula I: and W is or P, wherein in P is an amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process. | 04-17-2014 |
20140107044 | SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF - The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc. | 04-17-2014 |
20140106413 | IMMOBILIZED TRANSAMINASES AND PROCESS FOR MAKING AND USING IMMOBILIZED TRANSAMINASE - The invention is directed to immobilized transaminases and methods of making and using them. | 04-17-2014 |
20140105887 | METHODS FOR MODULATING IL-33 ACTIVITY - Provided herein are methods of modulating IL-33 activity, e.g., for the purpose of treating immune diseases and conditions, as well as methods of screening for compounds capable antagonizing IL-33 signaling. | 04-17-2014 |
20140093875 | MAMMALIAN CYTOKINES; RECEPTORS; RELATED REAGENTS AND METHODS - Nucleic acids encoding mammalian cytokine receptor, e.g., for cytokine IL-B50, purified proteins and fragments thereof. Antibodies, both polyclonal and monoclonal, are also provided. Methods of using the compositions for both diagnostic and therapeutic utilities are described. | 04-03-2014 |
20140093564 | PHARMACEUTICAL COMPOSITIONS OF COMBINATIONS OF DIPEPTIDYL PEPTIDASE-4 INHIBITORS WITH SIMVASTATIN - The present invention is directed to novel pharmaceutical compositions comprising fixed dose combinations of a dipeptidyl peptidase-4 inhibitor (DPP-4 inhibitor), or a pharmaceutically acceptable salt thereof, and simvastatin, or pharmaceutically acceptable salt thereof, methods of preparing such pharmaceutical compositions, and methods of treating Type 2 diabetes and hypercholesterolemia with such pharmaceutical compositions. In particular, the invention is directed to pharmaceutical compositions comprising fixed-dose combinations of sitagliptin phosphate and simvastatin. | 04-03-2014 |