GLAXOSMITHKLINE LLC Patent applications |
Patent application number | Title | Published |
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 |
20160106756 | BENZODIAZEPINES FOR TREATING SMALL CELL LUNG CANCER - The present invention relates to the use of a benzodiazepine compound, and its use in the treatment of cancer, particularly small cell lung cancer. | 04-21-2016 |
20160022781 | METHODS FOR ADMINISTERING HYPOGLYCEMIC AGENTS - The present invention relates to methods of administering hypoglycemic agents and/or GLP-1 agonists. | 01-28-2016 |
20160017343 | HOST CELLS AND METHODS OF USE - The present invention relates to genetically modified host cells, in particular yeast cells, comprising at least one isolated polynucleotide encoding a Killer Expression protease (Kex2p) or a fragment and/or variant thereof which has at least one Kex2p functional activity and at least one isolated polynucleotide encoding a Protein Disulfide-Isomerase (Pdi1) or a fragment and/or variant thereof which has at least one Pdi functional activity. Also provided herein are genetically modified host cells comprising at least one isolated polynucleotide encoding a Killer Expression protease (Kex2p) or a fragment and/or variant thereof which has at least one Kex2p functional activity, at least one isolated polynucleotide encoding a Protein Disulfide-Isomerase (Pdi1) or a fragment and/or variant thereof which has at least one Pdi1 functional activity and at least one isolated polynucleotide encoding a Endoplasmic Reticulum Oxidoreductin (Ero1) or a fragment and/or variant thereof which has at least one Ero1 functional activity. | 01-21-2016 |
20150352121 | COMBINATION - A novel combination comprising the PI3K-β inhibitor 2-methyl-1-{[2-methyl-3-(trifluoromethyl)phenyl]methyl}-6-(4-morpholinyl)-1H-benzimidazole-4-carboxylic acid, or a pharmaceutically acceptable salt thereof, with 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, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of PI3K-β and/or B-Raf is beneficial, eg. cancer. | 12-10-2015 |
20150322082 | NOVEL COMPOUNDS AS DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS - This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, genetic (Type 1, Type 5 hyperlipidemia) and acquired forms of hypertriglyceridemia or hyperlipoproteinemia-related disorders, caused by but not limited to lipodystrophy, hypothyroidism, medications (beta blockers, thiazides, estrogen, glucocorticoids, transplant) and other factors (pregnancy, alcohol intake), hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, cardiovascular outcomes, angina, excess hair growth (including syndromes associated with hirsutism), nephrotic syndrome, fibrosis such as myocardial, renal and liver fibrosis, hepatitis C virus infection and acne or other skin disorders. | 11-12-2015 |
20150273057 | Combination - 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, and/or 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 an EGFR inhibitor suitably cetuximab (Erbitux) or erlotinib; 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 EGFR is beneficial, eg. cancer. | 10-01-2015 |
20150272952 | Combination - The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine, or a pharmaceutically acceptable hydrate and/or salt thereof, and N-{(1S)-2-amino-1-[(3,4-difluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-furancarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof. | 10-01-2015 |
20150272950 | COMBINATION - The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof, and N-{(1S)-2-amino-1-[(3,4-difluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-furancarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof. | 10-01-2015 |
20150218142 | Derivatives of Betulin - The present invention relates to compounds characterized by having a structure according to the following Formula I: | 08-06-2015 |
20150216868 | Method of Adjuvant Cancer Treatment - The present invention provides a method of providing adjuvant treatment to a human patient which comprises administering to such a patient therapeutically effective doses of dabrafenib and trametinib for a time period sufficient to increase relapse-free survival (RFS). | 08-06-2015 |
20150158951 | ANTIBODY FORMULATIONS - This invention relates to a shear and temperature stable antibody formulations that are more stable than compared to a standard formulation (such as 30 mM citrate, 100 mM NaCl, pH 6.5). The present invention's shear and temperature stable antibody formulations show reduced precipitation when subjected to stress conditions but the standard formulation had aggregated. This result was unpredictable because thermodynamically the two formulations are similar as seen by their DSC (differential scanning calorimeter) profiles. | 06-11-2015 |
20150148343 | CHROMENONE ANALOGS AS SIRTUIN MODULATORS - The present invention relates to novel sirtuin-modulating compounds, corresponding pharmaceutical compositions comprising a sirtuin-modulating compound, alone and/or in combination with another therapeutic agent, and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. | 05-28-2015 |
20150126522 | ENHANCER OF ZESTE HOMOLOG 2 INHIBITORS - This invention relates to novel substituted benzamides according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers. | 05-07-2015 |
20150094321 | COMBINATION - The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering 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 N-{(1S)-2-amino-1-[(3,4-difluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-furancarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof. | 04-02-2015 |
20150093356 | THROMBOPOIETIN MIMETICS - Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative. | 04-02-2015 |
20150079030 | 3'-[(2Z)-[1-(3,4-DIMETHYLPHENYL)-1,5-DIHYDRO-3-METHYL-5-OXO-4H-PYRAZOL-4-Y- LIDENE]HYDRAZINO]-2'-HYDROXY-[1,1'-BIPHENYL]-3-CARBOXYLIC ACID bis-(MONOETHANOLAMINE) - An improved thrombopoietin mimetic, the bis-(monoethanolamine) salt of 3′-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2′-hydroxy-[1,1′-biphenyl]-3-carboxylic acid. | 03-19-2015 |
20140343056 | AZAINDAZOLES - Herein are disclosed azaindazoles of formula (I) | 11-20-2014 |
20140336175 | PURINE DERIVATIVES FOR USE IN THE TREATMENT OF ALLERGIC, INFLAMMATORY AND INFECTIOUS DISEASES - The present invention relates to compounds of formula (I): | 11-13-2014 |
20140288099 | COMPOSITION - Compound (I), and pharmaceutically acceptable salts thereof, are inducers of human interferon. Certain discrete and particular dosages of Compound (I) may be particularly useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and allergic asthma. | 09-25-2014 |
20140275107 | CANCER TREATMENT METHOD - Invented is a method of treating cancer or a pre-cancerous syndrome in a mammal, including a human, in need thereof which comprises the administration of an effective amount of a non-peptide thrombopoietin (TPO) receptor agonist to such mammal, suitably a human. | 09-18-2014 |
20140249156 | Treatment Of Blood Lipid Abnormalities And Other Conditions - There is provided a method of treatment of a patient suffering from blood lipid abnormality comprises the administration of a GPR119 agonist. | 09-04-2014 |
20140249147 | Substituted Bicyclic Aza-Heterocycles and Analogues as Sirtuin Modulators - Provided herein are novel substituted bicyclic aza-heterocycle sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided, are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 09-04-2014 |
20140249143 | Compounds And Methods For Enhancing Innate Immune Responses - Provided are certain compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections. | 09-04-2014 |
20140234253 | Combination Treatments For Hepatitis C - The present invention features methods and pharmaceutical compositions for the treatment of Hepatitis C in a human in need thereof comprising administering a compound of Formula (I), (II), (III), (IV), (V), or (VI) described herein or a pharmaceutically acceptable salt thereof in combination with one or more additional Hepatitis C therapeutic agents. | 08-21-2014 |
20140187566 | PHARMACEUTICAL COMBINATION OF MEK INHIBITOR AND B-RAF INHIBITORS - A novel combination comprising 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, with 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, 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 is beneficial, eg. cancer. | 07-03-2014 |
20140187545 | Pyrazolopyrimidine Derivatives As PI3 Kinase Inhibitors - PI3Kβ selective compounds having the structure | 07-03-2014 |
20140171626 | PROTEIN PURIFICATION - Processes for the purification of NY-ESO-1 related polypeptides, as well as polypeptides produced by these processes are provided herein; a composition comprising pure and stable NY-ESO-1 is also provided. | 06-19-2014 |
20140155410 | PYRAZOLYLAMINOPYRIDINES AS INHIBITORS OF FAK - The present invention relates to a compound of formula (I): | 06-05-2014 |
20140148437 | NOVEL COMPOUNDS AS DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS - This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, genetic (Type 1, Type 5 hyperlipidemia) and acquired forms of hypertriglyceridemia or hyperlipoproteinemia-related disorders, caused by but not limited to lipodystrophy, hypothyroidism, medications (beta blockers, thiazides, estrogen, glucocorticoids, transplant) and other factors (pregnancy, alcohol intake), hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, cardiovascular outcomes, angina, excess hair growth (including syndromes associated with hirsutism), nephrotic syndrome, fibrosis such as myocardial, renal and liver fibrosis, hepatitis C virus infection and acne or other skin disorders. | 05-29-2014 |
20140142321 | Benzimidazole Derivatives As PI3 Kinase Inhibitors - This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer. | 05-22-2014 |
20140142155 | METHOD OF TREATING THROMBOCYTOPENIA - Invented is a method of treating thrombocytopenia in a human in need thereof which comprises the administration of a therapeutically effective amount of a 3′-{N′-[1-(3,4-Dimethylphenyl)-3-methyl-5-oxo-1,5-dihydropyrazol-4-ylidene]hydrazino}-2′-hydroxybiphenyl-3-carboxylic acid to such human. | 05-22-2014 |
20140113916 | TRPV4 ANTAGONISTS - The present invention relates to spirocarbamate analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists. | 04-24-2014 |
20140107131 | PYRAZOLYLAMINOPYRIDINES AS INHIBITORS OF FAK - The present invention relates to a compound of formula (I): | 04-17-2014 |
20140100258 | METHODS FOR TREATING DEGENERATIVE DISEASES/INJURIES - Invented is a method of treating cardiovascular disease/injury, in a mammal, including a human, in need thereof which comprises the administration of a therapeutically effective amount of a non-peptide TPO receptor agonist to such mammal. | 04-10-2014 |
20140100234 | QUINOLINE DERIVATIVES AS PI3 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives. | 04-10-2014 |
20140100213 | TRIAZOLONES AS FATTY ACID SYNTHASE INHIBITORS - This invention relates to the use of triazolone derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones in the treatment of cancer. | 04-10-2014 |
20140080889 | Statin and Omega-3 Fatty Acids for Lipid Therapy - A method and composition for lipid therapy. In some embodiments, the method comprises providing a subject group having a baseline triglyceride level of 200 to 499 mg/dl and being at or near its low-density lipoprotein cholesterol (LDL-C) level goal, and reducing the triglyceride level and the non-high-density lipoprotein cholesterol (non-HDL-C) level of the subject group as compared to treatment with a 3-hydroxy-3-methyl glutaryl coenzyme A (HMG CoA) inhibitor alone, by administering to the subject group an effective amount of an HMG CoA inhibitor and a composition comprising omega-3 fatty acids. | 03-20-2014 |
20140080851 | Benzene Sulfonamide Thiazole and Oxazole Compounds - The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents. | 03-20-2014 |
20140073679 | CRYSTALLINE N--5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide hydrochloride - An improved AKT inhibiting compound, crystalline N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide hydrochloride. | 03-13-2014 |
20140066516 | Novel Method - The present invention is directed to a novel method for reducing intrapatient variability in pharmaceutically active agent which is suitably not absorbed in the stomach, such as paracetamol, containing formulations in patients having gastric dysmotility, or a method of improving analgesia in a diabetic patient, or improving absorption of an active agent is a patient with gastric dysmotility, which methods comprises administering orally to said patient in need thereof a pharmaceutical dosage form comprising a first active agent, calcium carbonate, at least one first binding agent, and at least one disintegrating agent as intragranular components in the form of a granulate, and as an extragranular component at least one hydrophilic colloid, an optionally a second binding agent, calcium carbonate, a super disintegrant, and a second active agent. | 03-06-2014 |
20140066459 | TETRAHYDROQUINOLINE DERIVATIVES USEFUL AS BROMODOMAIN INHIBITORS - Tetrahydroquinoline compounds pharmaceutical compositions containing such compounds and their use in therapy. | 03-06-2014 |
20140065213 | Sustained Release Paracetamol Formulations - The present invention is directed to twice daily sustained release pharmaceutical composition of paracetamol having an immediate release phase of paracetamol and a sustained release phase of paracetamol, said composition having unique and advantageous pharmacokinetic properties and a pharmaceutical composition comprising only a sustained release phase of paracetamol having unique and advantageous pharmacokinetic properties. | 03-06-2014 |
20140057980 | CALCILYTIC COMPOUNDS - Novel calcilytic compounds and methods of using them are provided. | 02-27-2014 |
20140056928 | NOVEL COMPOUNDS - Compounds of formula (I) and salts thereof: | 02-27-2014 |
20140045834 | 7-(3,5-Dimethyl-4-Isoxazolyl)-8-(Methyloxy)-1H-Imidazo[4,5-C]Quinoline Derivatives - Novel quinoline compounds pharmaceutical compositions containing such compounds and their use in therapy. | 02-13-2014 |
20140044727 | FORMULATIONS WITH REDUCED VISCOSITY - The present invention is directed to a method for reducing the viscosity of a formulation containing acetate and a therapeutic protein and formulations made using the claimed method. | 02-13-2014 |
20140044717 | LYOPHILIZED FORMULATIONS - The invention is directed to a method for producing a polypeptide composition comprising: combining a polypeptide with a volatile additive to form a liquid mixture and lyophilizing the liquid mixture to obtain a lyophilized polypeptide composition. | 02-13-2014 |
20140039006 | Tetrahydroquinoline Derivatives Useful As Bromodomain Inhibitors - Tetrahydroquinoline derivatives, pharmaceutical compositions containing such compounds and to their use in therapy. | 02-06-2014 |
20140038982 | CANCER TREATMENT METHOD - Invented is a method of treating cancer or a pre-cancerous syndrome in a mammal, including a human, in need thereof which comprises the administration of an effective amount of a non-peptide thrombopoietin (TPO) receptor agonist to such mammal, suitably a human. | 02-06-2014 |
20140037759 | Antacid Tablet - Aspects of the present invention are directed to an oral antacid tablet comprising at least about 60% by weight directly compressible granulated calcium carbonate and an intense flavoring. The tablet may have a hardness of at least about 22 Strong-Cobb units and the tablet may have a mass of between about 500 mg and about 1,000 mg. Tablets of the present invention reduce or eliminate heartburn symptoms and also freshen breath. | 02-06-2014 |
20140037726 | NOVEL PHARMACEUTICAL COMPOSITION - Disclosed are novel pharmaceutical compositions containing 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 dimethyl sulfoxide solvate, methods of using the compositions in therapy and processes for preparing the same. | 02-06-2014 |
20140037580 | 3'-[(2Z)-[1-(3,4-DIMETHYLPHENYL)-1,5-DIHYDRO-3-METHYL-5-OXO-4H-PYRAZOL-4-Y- LIDENE]HYDRAZINO]-2'-HYDROXY-[1,1'-BIPHENYL]-3-CARBOXYLIC ACID bis-(MONOETHANOLAMINE) - An improved thrombopoietin mimetic, the bis-(monoethanolamine) salt of 3′-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2′-hydroxy-[1,1′-biphenyl]-3-carboxylic acid. | 02-06-2014 |
20140031336 | Tetrahydroquinoline Derivatives Useful As Bromodomain Inhibitors - Tetrahydroquinoline compounds, pharmaceutical compositions containing such compounds and their use in therapy. | 01-30-2014 |
20140024666 | PROLYL HYDROXYLASE INHIBITORS - The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) | 01-23-2014 |
20140024664 | NOVEL ADENINE DERIVATIVES - Compounds of formula (I): | 01-23-2014 |
20140023655 | FORMULATIONS WITH REDUCED VISCOSITY - The present invention is directed to a method for reducing the viscosity of a formulation containing citrate and a therapeutic protein and formulations made using the claimed method. | 01-23-2014 |
20140018534 | Benzimidazole Derivatives As PI3 Kinase Inhibitors - This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kβ, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer. | 01-16-2014 |
20140018525 | BUFFER SYSTEM FOR PROTEIN PURIFICATION - The invention is directed to a method for producing a polypeptide composition comprising: combining a polypeptide with a volatile additive to form a liquid mixture and lyophilizing the liquid mixture to obtain a lyophilized polypeptide composition. | 01-16-2014 |
20130345243 | 1H-PYROLLO[3,2-D]PYRIMIDINEDIONE DERIVATIVES - The present invention relates to pyrimidinedione compounds of formula (I), | 12-26-2013 |
20130345212 | QUINOLINONE DERIVATIVES - The present invention relates to compounds of the formula (I), | 12-26-2013 |
20130345200 | INDOLES - Herein are disclosed indoles of formula (I) | 12-26-2013 |
20130345120 | PEPTIDE DEFORMYLASE INHIBITORS - The present invention relates to a compound of Formula (I): | 12-26-2013 |
20130310562 | Bicyclic Heteroaromatic Compounds As Protein Tyrosine Kinase Inhibitors - A pharmaceutical formulation comprising the compound of formula | 11-21-2013 |
20130289079 | Nicotine Lozenge Composition - The present invention relates to nicotine lozenge compositions comprising reduced levels of buffering agents from traditional nicotine lozenges and which provide optimal oral pH and prompt nicotine absorption in a smaller, more convenient dosage form. | 10-31-2013 |
20130288984 | COMBINATION - The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering a proteasome inhibiting compound, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, and optional additional antineoplastic agents, to a human in need thereof. | 10-31-2013 |
20130231378 | INHIBITORS OF AkT ACTIVITY - Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis. | 09-05-2013 |
20130231282 | METHODS FOR ADMINISTERING HYPOGLYCEMIC AGENTS - The present invention relates to methods of administering hypoglycemic agents and/or GLP-1 agonists. | 09-05-2013 |
20130225489 | METHODS FOR ADMINISTERING HYPOGLYCEMIC AGENTS - The present invention relates to methods of administering hypoglycemic agents and/or GLP-1 agonists. | 08-29-2013 |
20130197221 | Benzimidazole Derivatives As PI3 Kinase Inhibitors - This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer. | 08-01-2013 |
20130184263 | Derivatives of Betulin - The present invention relates to compounds characterized by having a structure according to the following Formula I: | 07-18-2013 |
20130172378 | Combination of BRAF and VEGF Inhibitors - A novel combination comprising the VEGFR inhibitor 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof, with 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, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of VEGFR and/or B-Raf is beneficial. | 07-04-2013 |
20130165415 | CHEMICAL COMPOUNDS - The present invention features compounds that are prodrugs of HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC. | 06-27-2013 |
20130158114 | Calcilytic Compounds - Novel calcilytic compounds and methods of using them are provided. | 06-20-2013 |
20130157977 | Benzimidazole Boronic Acid Derivatives As PI3 Kinase Inhibitors - This invention relates to the use of benzimidazole boronic acid derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazole boronic acids in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazole boronic acid compounds for treating cancer. | 06-20-2013 |
20130150383 | NOVEL COMPOUNDS - The present invention relates to therapeutically active xanthine derivative compounds of Formula (I): | 06-13-2013 |
20130144055 | Benzene Sulfonamide Thiazole And Oxazole Compounds - The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents. | 06-06-2013 |
20130137736 | Methods for Treating Degenerative Diseases/Injuries - Invented is a method of treating degenerative diseases/injuries, in a mammal, including a human, in need thereof which comprises the administration of a therapeutically effective amount of a non-peptide TPO receptor agonist to such mammal. | 05-30-2013 |
20130078213 | THROMBOPOIETIN MIMETICS - Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative. | 03-28-2013 |
20130072690 | Chemical Compounds - Disclosed are compounds of Formula III. Also disclosed are salts of the compounds, pharmaceutical composition comprising the compounds or salts, and methods for treating HCV infection by administration of the compounds or salts. | 03-21-2013 |
20130072507 | COMBINATION - The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine, or a pharmaceutically acceptable hydrate and/or salt thereof, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof. | 03-21-2013 |
20130072487 | PROLYL HYDROXYLASE INHIBITORS - The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) | 03-21-2013 |
20130053407 | PYRROLO [3,2-D] PYRIMIDIN-3-YL DERIVATIVES USED AS ACTIVATORS OF AMPK - Pyrrolopyrimidones compounds of the formula (I), salts thereof, and pharmaceutical compositions containing them are disclosed herein, as well as methods for their use in medicine, for instance as activators of AMPK. | 02-28-2013 |
20130053383 | INDAZOLES - Herein are disclosed indazoles of formula (I) | 02-28-2013 |
20130053317 | METHODS FOR TREATING OR PREVENTING CARDIOVASCULAR DISORDERS AND PROVIDING CARDIOVASCULAR PROTECTION - The present invention provides methods for treating, preventing and/or ameliorating at least one cardiovascular disorder in a human in need thereof comprising administering to said human a pharmaceutical composition comprising at least one polypeptide having at least one GLP-1 activity and/or at least one GLP-1 agonist. | 02-28-2013 |
20130035501 | PROCESS FOR PREPARING BENZOXABOROLES - The present invention is a process comprising contacting a compound of formula 6: | 02-07-2013 |
20130029938 | Chemical Compounds - Compounds of Formula I and methods for treating metabolic disorders are disclosed. | 01-31-2013 |
20130018049 | Azaindole Compounds and Methods for Treating HIV - Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV). | 01-17-2013 |
20130012499 | TRPV4 ANTAGONISTS - The present invention relates to quinoline analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists. | 01-10-2013 |
20120315291 | PURINE DERIVATIVES AND THEIR PHARMACEUTICAL USES - The present invention relates to compounds of formula (I): | 12-13-2012 |
20120315267 | NOVEL USES - The present invention relates to antibodies which multiple antigen specificities and their use in treating human diseases | 12-13-2012 |
20120308609 | 6-AMINO-2--9-[5-(1-PIPERIDINYL)-7,9-DIHYDRO-8H-PURIN-8-ONE MALEATE - The present invention relates to a compound which is 6-amino-2-{[(1S)-1-methylbutyl]oxy}-9-[5-(1-piperidinyl)pentyl]-7,9-dihydro-8H-purin-8-one: | 12-06-2012 |
20120302579 | CANCER TREATMENT METHOD - Invented is a method of treating cancer and pre-cancerous syndromes in a mammal, including a human, in need thereof which comprises the administration of a therapeutically effective amount of a non-peptide TPO receptor agonist to such mammal. | 11-29-2012 |
20120283438 | COMPOUNDS - The present invention includes novel compounds useful in the treatment of various disorders in particular infectious diseases, cancer, and allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, and as vaccine adjuvants. | 11-08-2012 |
20120245180 | COMBINATION - The present invention relates to a method of treating cancer in a mammal and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a novel combination comprising the MEK inhibitor: N-{3-[3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, and the PI3 kinase inhibitor: 2,4-difluoro-N-{2-(methyloxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl}benzenesulfonamide, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same, and methods of using such combinations in the treatment of cancer. | 09-27-2012 |
20120202835 | COMBINATION - The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering 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, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof. | 08-09-2012 |
20120196886 | COMBINATION - The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering 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, and N-{(1S)-2-amino-1-[(3,4-difluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-furancarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof. | 08-02-2012 |
20120172333 | PYRROLO-PYRIDINE DERIVATIVES AS ACTIVATORS OF AMPK - The present invention relates to pyrrolopyridone compounds of the formula (I), | 07-05-2012 |
20120071329 | METHODS FOR IDENTIFYING COMPOUNDS OF INTEREST USING ENCODED LIBRARIES - The present invention provides a method for identifying a compound of interest by screening libraries of molecules which include an encoding oligonucleotide tag. | 03-22-2012 |
20120035193 | 6-AMINO-PURIN-8-ONE COMPOUNDS - Compounds of formula (I): | 02-09-2012 |
20120010244 | INDOLE DERIVATIVES AS IKK2 INHIBITORS - The invention is directed to a certain novel compound which is an inhibitor of kinase activity, in particular IKK2 activity. | 01-12-2012 |
20110301203 | CHEMICAL COMPOUNDS - This invention relates to non-steroidal compounds that are modulators of androgen receptor, and also to the methods for the making and use of such compounds. | 12-08-2011 |
20110269781 | COMPOUNDS - The present invention includes novel compounds useful in the treatment of various disorders in particular infectious diseases, cancer, and allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, and as vaccine adjuvants. | 11-03-2011 |
20110263855 | PROCESSES AND INTERMEDIATES FOR CARBAMOYLPYRIDONE HIV INTEGRASE INHIBITORS - Processes are provided which create an aldehyde methylene, or hydrated or hemiacetal methylene attached to a heteroatom of a 6 membered ring without going through an olefinic group and without the necessity of using an osmium reagent. In particular, a compound of formula (I) can be produced from (II) and avoid the use of an allyl amine: (formulae I and II) where R, P | 10-27-2011 |
20110229500 | PURINE DERIVATIVES FOR USE IN THE TREATMENT OF ALLERGIC, INFLAMMATORY AND INFECTIOUS DISEASES - The present invention relates to compounds of formula (I): | 09-22-2011 |
20110190236 | CHEMICAL COMPOUNDS - The present invention features compounds that are prodrugs of HIIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC. | 08-04-2011 |
20110152303 | Chemical Compounds - Novel diarylpyrimidine derivatives and pharmaceutically acceptable salts, solvates or hydrates thereof, designed to inhibit HIV reverse transcriptase, are provided, and a pharmaceutical composition containing the same, especially an anti-HIV agent. More specifically, novel diarylpyrimidine derivatives that are derivatives of the HIV reverse transcriptase inhibitor TMC278 of formula (1 | 06-23-2011 |
20110152217 | POLYMORPHS OF (S)-3-AMINOMETHYL-7-(3-HYDROXY-PROPOXY)-3H-BENZO[C][1,2]OXABOROL-1-OL - This invention provides, among other things, polymorphs of the hydrochloride salt of (S)-3-aminomethyl-7-(3-hydroxy-propoxy)-3H-benzo[c][1,2]oxaborol-1-ol. | 06-23-2011 |
20110144136 | NOVEL ADENINE DERIVATIVES - The present invention relates to compounds of formula (I): | 06-16-2011 |
20110136763 | TRISUBSTITUTED BORON-CONTAINING MOLECULES - This invention largely relates to 3,4,6-trisubstituted benzoxaborole compounds, and their use for treating bacterial infections. | 06-09-2011 |
20110135671 | PURINE DERIVATIVES FOR USE IN THE TREATMENT OF ALLERGIC, INFLAMMATORY AND INFECTIOUS DISEASES - The present invention relates to compounds of formula (I): | 06-09-2011 |
20110135670 | PURINE DERIVATIVES FOR USE IN THE TREATMENT OF ALLERGIC, INFLAMMATORY AND INFECTIOUS DISEASES - The present invention relates to compounds of formula (I): | 06-09-2011 |
20110131754 | PROCESS - The present invention relates to a process using ultrasonic cutting for the preparation of an oral delivery device comprising a core which includes a pharmaceutically active agent covered by an outer coating which includes one or more openings communicating from the exterior of the device toward the core. | 06-09-2011 |
20110053934 | COMPOUNDS AND METHODS OF TREATMENT - A derivative, which is useful as a ret kinase inhibitor is described herein. The described invention also includes methods of using the same in the treatment of diseases mediated by inappropriate ret kinase activity. | 03-03-2011 |
20110046109 | 2,4,8-TRISUBSTITUTED-8H-PYRIDO[2,3-D]PYRIMIDIN-7-ONE COMPOUNDS AND COMPOSITIONS FOR USE IN THERAPY - Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. | 02-24-2011 |
20110009625 | NOVEL COMPOUNDS - Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. | 01-13-2011 |
20100323329 | Apparatus and Method for Manufacturing Customized Dentures - This disclosure relates to an apparatus and method for digitally utilizing and customizing dental features needed in the manufacture of dentures. | 12-23-2010 |
20100216746 | CHEMICAL COMPOUNDS - The present invention relates to compounds that are a non-nucleoside reverse transcriptase inhibitors, and to processes for the preparation and use of the same. Specifically, the present invention includes methods of using such compounds in the treatment of human immunodeficiency virus infection. | 08-26-2010 |
20100196321 | COMPOUNDS - The present invention features compounds of Formula (I) and (Ia), pharmaceutical compositions and use in the treatment of viral disease: | 08-05-2010 |
20100152175 | Pyridine Derivatives and Their Use in The Treatment of Psychotic Disorders - There are provided according to the invention novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: | 06-17-2010 |