| Entries |
| Document | Title | Date |
|---|
| 20080207650 | Chemical Compounds 636 - The present invention provides a compound of a formula (I): | 08-28-2008 |
| 20080227797 | Pyridopyrimidine Derivatives as Pde4 Inhibitors for the Treatment of Inflammatory and Immune Diseases - The present invention provides a compound of a formula (I): [Chemical formula should be inserted here. Please see paper copy] wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE4 mediated disease state. | 09-18-2008 |
| 20080255160 | MAPK/ERK KINASE INHIBITORS - Compounds of the following formula are provided for use with MEK: | 10-16-2008 |
| 20080255161 | 3-HYDROQUINAZOLIN-4-ONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS - The present invention discloses 3-hydroquinazolin-4-one derivatives for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cancer, cardiovascular disease, diabetes, obesity, metabolic syndrome and the like. | 10-16-2008 |
| 20080275069 | Quinazoline Derivative - This invention provides a compound or its pharmaceutically-acceptable salt of formula (I) | 11-06-2008 |
| 20080287472 | Fungicides - Fungicidal compositions comprising derivatives of pyridopyrimidines having the general formula (1): | 11-20-2008 |
| 20090005401 | Novel Compounds - This invention relates to a novel group of 8-Alkyl/Aryl-4-aryl-2-N-(alkylamino)-N″-substituted-N′-cyanoguanidino-8H-pyrido[2,3-d]pyrimidin-7-one compounds, processes for the preparation thereof, the use thereof in treating CSBP/p38 kinase mediated diseases and pharmaceutical compositions for use in such therapy. | 01-01-2009 |
| 20090023756 | SUBSTITUTED QUINAZOLINES AS PDE10 INHIBITORS - The invention pertains to substituted quinazoline compounds of structures (I) and (II) that serve as effective phosphodiesterase (PDE) inhibitors. The invention also relates to compounds which are selective inhibitors of PDE-10. The invention further relates to intermediates for preparation of such compounds; pharmaceutical compositions comprising such compounds; and the use of such compounds in methods for treating certain central nervous system (CNS) or other disorders. The invention relates also to methods for treating neurodegenerative and psychiatric disorders, for example psychosis and disorders comprising deficient cognition as a symptom. (I, II). | 01-22-2009 |
| 20090030020 | 7H-Pyrido[3,4-D]Pyrimidin-8-Ones, Their Manufacture and Use as Protein Kinase Inhibitors - Objects of the present invention are the compounds of formula I | 01-29-2009 |
| 20090048276 | Inhibitors of Fatty Acid Synthase (Fas) - The instant invention provides for compounds which comprise substituted 3-aryl-4-hydroxyquinolin-2(1H)-ones that inhibit FAS activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting FAS activity by administering the compound to a patient in need of treatment of cancer. | 02-19-2009 |
| 20090069348 | Use of Inhibitors of the Renin-Angiotensin System - It has been found that an inhibitor of the renin-angiotensin system is useful for the treatment or prevention of a condition associated with hypoxia or impaired metabolic function or efficiency. In particular, it may be used in connection with therapy of stroke or its recurrence, the acute treatment of myocardial infarction, and the treatment or prevention of wasting or cachexia, and is thus useful in treatment of the symptoms and signs of ageing. It may also be used to enhance function in healthy subjects. | 03-12-2009 |
| 20090105283 | 3-HYDROQUINAZOLIN-4-ONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS - The present invention discloses 3-hydroquinazolin-4-one derivatives for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cancer, cardiovascular disease, diabetes, obesity, metabolic syndrome and the like. | 04-23-2009 |
| 20090163522 | Derivatives of Pyrido[2,3-d]pyrimidine, the Preparation Thereof, and the Therapeutic Application of the Same - The invention relates to derivatives of pyrido[2,3-d]pyrimidine, to the preparation thereof, and to the therapeutic application of the same. | 06-25-2009 |
| 20090215799 | HETEROCYCLIC SUBSTITUTED BISARYLUREA DERIVATIVES - The present invention relates to heterocyclic substituted bisarylurea derivatives of formula I, the use of the compounds of formula I as inhibitors of one or more kinases, the use of the compounds of formula I for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient. | 08-27-2009 |
| 20090215800 | Enzyme and Receptor Modulation - Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator. | 08-27-2009 |
| 20090325985 | Diketopiperidine Derivatives as HIV Attachment Inhibitors - Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, diketopiperidine derivatives that possess unique antiviral activity are provided. These compounds are useful for the treatment of HIV and AIDS. | 12-31-2009 |
| 20100035902 | 5-ARYL-SUBSTITUTED DIHYDROPYRIDOPYRIMIDINES AND DIHYDROPYRIDAZINES AND USE THEREOF AS MINERAL CORTICOID ANTAGONISTS - The present application relates to novel aryl-substituted heterobicyclic compounds, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders. | 02-11-2010 |
| 20100093771 | Compound having bicyclic pyrimidine structure and pharmaceutical composition comprising the same - The present invention relates to a bicyclic pyrimidine compound of the following formula (I) or a salt thereof. | 04-15-2010 |
| 20100120800 | AGENT FOR PREVENTING RECURRENCE OF CEREBROVASCULAR DISORDER AND AGENT FOR AMELIORATING TROUBLES FOLLOWING CEREBROVASCULAR DISORDER AND INHIBITING PROGRESS THEREOF - There is provided an agent for preventing the recurrence of cerebrovascular disorder and an agent for ameliorating troubles following cerebrovascular disorder and inhibiting the progress thereof which contain a compound having an angiotensin II antagonistic activity, a prodrug thereof or a salts thereof. | 05-13-2010 |
| 20100130517 | NEW 4,8-DIPHENYL-POLYAZANAPHTHALENE DERIVATIVES - New inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) are disclosed herein, as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy. | 05-27-2010 |
| 20100179173 | SUBSTITUTED FUSED PYRIMIDINES AS ANTAGONISTS OF GPR105 ACTIVITY - Fused pyrimidine compounds of structural formula (I) are effective as antagonists of the biological activity of the GPR105 protein. They are useful for the treatment, control or prevention of disorders responsive to antagonism of this receptor, such as diabetes, particularly, Type 2 diabetes, insulin resistance, hyperglycemia, lipid disorders, obesity, atherosclerosis, and Metabolic Syndrome. | 07-15-2010 |
| 20100204252 | METHODS OF TREATING HYPERTENSION WITH AT LEAST ONE ANGIOTENSIN II RECEPTOR BLOCKER AND CHLORTHALIDONE - The present invention relates to a method of treating hypertension in a subject or patient needing treatment thereof by administering to said subject or patient at least one angiotensin II receptor blocker in combination with chlorthalidone. | 08-12-2010 |
| 20110015213 | QUINAZOLINE DERIVATIVES - Quinazoline derivatives of the following formula: | 01-20-2011 |
| 20110034487 | CXCR3 ANTAGONISTS - Compounds, compositions and methods that are useful in the treatment of inflammatory and immune conditions and diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of a chemokine receptor. The subject methods are useful for the treatment of inflammatory and immunoregulatory disorders and diseases, such as multiple sclerosis, rheumatoid arthritis, transplant rejection and type I diabetes. | 02-10-2011 |
| 20110065733 | MAPK/ERK KINASE INHIBITORS - Compounds of the following formula are provided for use with MEK: | 03-17-2011 |
| 20110105539 | 2'-HALOBIPHENYL-4-YL INTERMEDIATES IN THE SYNTHESIS OF ANGIOTENSIN II ANTAGONISTS - A process for obtaining 2′-halo-4-methylbiphenyls is described, which comprises reacting 4 halotoluene with a 1,2-dihalobenzene in the presence of elemental metal such as magnesium, lithium or zinc, wherein 0 to 0.9 molar, particularly 0 to 0.2 molar excess of 4-halotoluene in regard to 1,2-dihalobenzene is used, and arised organometal intermediates are quenched by elemental mental halogen. In addition, the coupling of arised 2′-halo-4-methylbiphenyls with 2-(1-propyl)-4-methyl-6-(1′-methylbenzimidazole-2-il)benzimidazole to afford 3′-(2′-halo-biphenyl-4-ylmethyl)-1,7′-dimethyl-2′-propyl-1H,3′H-[2,5′]bibenzoimidazolyl, which can be further converted to organometallic compound and said organometallic compound is further reacted with formic acid derivative, such as N,N-dimethylformamide, alkylformiate or carbon dioxide to obtain telmisartan, is also described. Further described is use of in line analytics for monitoring the aforementioned reactions, process for preparing a pharmaceutical composition and/or dosage for, or use in preparing a medicament. | 05-05-2011 |
| 20110118287 | Bicycloheteroaryl Compounds As P2X7 Modulators and Uses Thereof - Bicycloheteroaryl compounds are disclosed that have formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others. | 05-19-2011 |
| 20110118288 | PHARMACEUTICAL COMPOSITION FOR TREATING HYPERTENSION AND METABOLIC SYNDROME AND USE THEREOF - The present invention provides a pharmaceutical composition comprising the following active ingredients: 1) an angiotensin II receptor antagonist or a pharmaceutically acceptable salt thereof, 2) pioglitazone or a pharmaceutically acceptable salt thereof; and 3) rosuvastatin or a pharmaceutically acceptable salt thereof. The present invention also provides use of the pharmaceutical composition in preparing a medicament for treating hypertension or metabolic syndrome. The pharmaceutical composition of the present invention can treat hypertension or metabolic syndrome, while effectively controlling the incidence of associated cardiovascular diseases and more potently improving survival prognosis in hypertensive patients. When blood pressure is lowered to desired level, the risk factors such as cardiovascular diseases are rectified, metabolic disorders and prognosis of patients are improved, and survival rate of hypertensive patients is raised. | 05-19-2011 |
| 20110263619 | PHARMACEUTICAL FORMULATIONS AND USE THEREOF IN THE PREVENTION OF STROKE, DIABETES AND/OR CONGESTIVE HEART FAILURE - The present invention relates to use of an inhibitor of the renin-angiotensin system (RAS) or a pharmaceutically acceptable derivative thereof, such as ramipril or ramiprilat, in the prevention of stroke, diabetes and/or congestive heart failure (CHF). | 10-27-2011 |
| 20120059019 | Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 03-08-2012 |
| 20120095028 | 3-OXA-7-AZABICYCLO[3.3.1]NONANES - Compounds of Formula (I) that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein. | 04-19-2012 |
| 20120196879 | 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-fluorophen-}-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. | 08-02-2012 |
| 20120245187 | HETEROBICYCLIC CARBOXAMIDES AS INHIBITORS FOR KINASES - The invention relates to novel organic compounds of formula (I) | 09-27-2012 |
| 20120264770 | HSP90 INHIBITORS - The invention relates to HSP90 inhibiting compounds consisting of the formula: | 10-18-2012 |
| 20120283278 | 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-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. | 11-08-2012 |
| 20120283279 | COMBINATION - 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 mTOR inhibitor, 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 mTOR is beneficial, e.g. cancer. | 11-08-2012 |
| 20120322817 | 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. | 12-20-2012 |
| 20130005750 | HETEROBICYCLIC CARBOXAMIDES AS INHIBITORS FOR KINASES - The invention relates to novel organic compounds of formula (I) | 01-03-2013 |
| 20130005751 | HETEROBICYCLIC CARBOXAMIDES AS INHIBITORS FOR KINASES - The invention relates to novel organic compounds of formula (I) | 01-03-2013 |
| 20130109705 | COMBINATION | 05-02-2013 |
| 20130165456 | 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-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethy; -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, to a human in need thereof. | 06-27-2013 |
| 20130172370 | PHARMACEUTICAL COMPOSITION FOR USE IN THE TREATMENT OF GLAUCOMA - The present invention relates to a compound which is an antagonist of CXCR3 or an inhibitor of the CXCR3 receptor expression for the treatment of glaucoma. | 07-04-2013 |
| 20130197016 | DOSING REGIMES FOR THE TREATMENT OF OCULAR VASCULAR DISEASE - The use of vascular endothelial growth factor receptor 2 inhibitors or a pharmaceutically acceptable salt thereof for the treatment of ocular vascular disease is provided. Dosing regimes, including once weekly administration, of certain VEGF-R2 inhibitors are provided which deliver therapeutically effective concentrations of the VEGF-R2 compounds in ocular tissues for at least one week for the treatment of ocular vascular disease. | 08-01-2013 |
| 20130203786 | SUBSTITUTED SEVEN-MEMBERED HETEROCYCLIC COMPOUNDS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OF DIABETES - The present invention is directed to novel amino-substituted seven-membered heterocyclic compounds 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. | 08-08-2013 |
| 20130203787 | HYDRATE OF 1--5,5-DIFLUORO-PIPERIDIN-2-ONE TARTRATE - The present invention relates to 1.5 hydrate of of 1-{(2S)-2-amino-4-[2,4-bis (trifluoromethyl)-5,8-dihydropyrido[3,4-d]pyrimidin-7(6H)-yl]-4-oxobutyl}-5,5-di-fluoropiperidin-2-one tartrate, a process for preparing the same, and a pharmaceutical composition for inhibiting DPP-IV, which comprises said compound as the active component. | 08-08-2013 |
| 20130217710 | METHODS FOR TREATING CANCER - Methods are provided for treating a human having cancer comprising detecting at least one mutation in a Ras protein or a gene encoding at least one Ras protein from at least one tumor cell from said human and treating said human having at least one mutation in at least one Ras protein or a gene encoding at least one Ras protein with a pharmaceutical composition comprising at least one MEK inhibitor comprising a compound of Structure (I): | 08-22-2013 |
| 20130317047 | PHARMACEUTICAL FORMULATIONS AND USE THEREOF IN THE PREVENTION OF STROKE, DIABETES AND/OR CONGESTIVE HEART FAILURE - The present invention relates to use of an inhibitor of the renin-anglotensin system (RAS) or a pharmaceutically acceptable derivative thereof, such as ramipril or ramiprilat, in the prevention of stroke, diabetes and/or congestive heart failure (CHF). | 11-28-2013 |
| 20140088122 | METHOD OF TREATMENT OF AGE-RELATED MACULAR DEGENERATION (AMD) - The present invention relates generally to the field of treatment and prophylaxis of retinal degenerative diseases. More particularly, the present invention contemplates a method for preventing, reducing the risk of development of, or otherwise treating or ameliorating the symptoms of, age-related macular degeneration (AMD) or related retinal conditions in mammals and in particular humans. The present invention further provides therapeutic compositions enabling dose-dependent or dose-specific administration of agents useful in the treatment and prophylaxis of age-related macular degeneration or related retinal degenerative conditions. | 03-27-2014 |
| 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 |
| 20140303195 | COMBINATION - 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 mTOR inhibitor, 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 mTOR is beneficial, e.g. cancer. | 10-09-2014 |
| 20140309243 | 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-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. | 10-16-2014 |
| 20140323506 | 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-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethy;-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, to a human in need thereof. | 10-30-2014 |
| 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 |
| 20150111904 | 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 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. melanoma. | 04-23-2015 |
| 20150126533 | ADMINISTRATION OF A RAF INHIBITOR AND A MEK INHIBITOR IN THE TREATMENT OF MELANOMA - Disclosed are methods for the treatment of non-BRAFV600E mutant melanoma in patients in need of such treatment. The methods comprise administering to such a patient a MEK inhibitor such as (R)-3-(2,3-dihydroxypropyl)-6-fluoro-5-((2-fluoro-4-iodophenyl)amino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione (TAK-733) and a RAF inhibitor selected from N-{7-cyano-6-[4-fluoro-3-({[3-(trifluoromethyl)phenyl]acetyl}amino)phenoxy]-1,3-benzothiazol-2-yl}cyclopropanecarboxamide (TAK-632) and (R)-2-(1-(6-amino-5-chloropyrimidine-4-carboxamido)ethyl)-N-(5-chloro-4-(trifluoromethyl)pyridin-2-yl)thiazole-5-carboxamide (MLN2480). Also disclosed are medicaments for use in the treatment of such melanoma. | 05-07-2015 |
| 20150148356 | COMPOUNDS FOR DRY SKIN AND ANTI-AGEING APPLICATION - The present invention relates to the cosmetic use, as agent for preventing and/or treating an aesthetic defect in the skin and/or its appendages that is associated with an imbalance in the differentiation and/or proliferation of the cells of an epidermis, of an effective amount of at least one compound represented by one of the general formulae, (Ia) or (Ib) | 05-28-2015 |
| 20150299188 | HETEROCYCLIC COMPOUND - Provided is a compound having a superior FLAP inhibitory action and useful as a prophylactic or therapeutic agent for arteriosclerosis and the like, and a salt thereof. The present invention relates to a compound represented by the formula | 10-22-2015 |
| 20150328320 | Novel Pharmaceutical Composition - Disclosed are novel pharmaceutical formulations 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. | 11-19-2015 |
| 20150352117 | 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-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethy;-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, to a human in need thereof. | 12-10-2015 |
| 20150368242 | NOVEL TETRAHYDROPYRIDOPYRIMIDINONE DERIVATIVE - An object is to provide a novel compound having a higher MGAT2 inhibitory activity than conventional compounds. A compound represented by the following general formula (I) or a pharmaceutically acceptable salt thereof is provided. | 12-24-2015 |
| 20160008368 | Combination | 01-14-2016 |
| 20160022680 | Combinations for treatment of cancer - The current disclosure relates to pharmaceutical combinations and compositions useful in the treatment of certain types of cancer. The disclosure also relates to method of treatment these certain types of cancer. In particular, the disclosure relates to the combined use of inhibitors of MEK, EGFR and ERBB2 in the treatment of KRAS-mutant lung cancer, and KRAS-mutant colon cancer. | 01-28-2016 |
| 20160039812 | SUBSTITUTED BICYCLIC DIHYDROPYRIMIDINONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY - Substituted bicyclic dihydropyrimidinones of formula 1 | 02-11-2016 |
| 20160039815 | PYRIDO[3,4-d]PYRIMIDINE-2,4(1H,3H)-DIONE DERIVATIVES - This invention relates to novel Pyrido[3,4-d]pyrimidine-2,4(1H,3H)-dione derivatives of Formula (I): | 02-11-2016 |
| 20160046624 | PYRIDO[2,3-d]PYRIMIDINE-2,4(1H,3H)-DIONE DERIVATIVES - This invention relates to novel Pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione derivatives of Formula (I): | 02-18-2016 |
| 20160075708 | ANTI-ANGIOGENESIS COMPOUND, INTERMEDIATE AND USE THEREOF - Disclosed are an anti-abnormal proliferation of angiogenesis compound represented by formula I, use and intermediate thereof. The compound has good effect against abnormal proliferation of angiogenesis, and the activity of the compound is produced by inhibiting VEGFR2. The compound can be used for treating diseases, such as wet macular degeneration, inflammation, malignant tumor and the like, caused by abnormity of angiogenesis and protein kinases such as VEGFR2, FGFR2 and the like. | 03-17-2016 |
| 20160102090 | SUBSTITUTED 3-BENZYLQUINOXALIN-4(3H)-ONE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF MUSCARINIC ACETYCHOLINE RECEPTOR M1 - In one aspect, the invention relates to 3-benzylquinazolin-4(3H)-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M | 04-14-2016 |
| 20160136132 | A PHARMACEUTICAL COMBINATION FOR THE TREATMENT OF MELANOMA - The present invention relates to a pharmaceutical combination comprising a cyclin dependent kinase (CDK) inhibitor represented by a compound of formula I (as described herein) or a pharmaceutically acceptable salt thereof; and at least one anticancer agent selected from a BRAF inhibitor or a MEK inhibitor, for use in the treatment of melanoma. The present invention also relates to a method for the treatment of melanoma comprising administering to a subject in need thereof, a therapeutically effective amount of a CDK inhibitor and a therapeutically effective amount of at least one anticancer agent selected from a BRAF inhibitor or a MEK inhibitor. | 05-19-2016 |
| 20160143910 | METHODS OF TREATING CANCER AND PREVENTING CANCER DRUG RESISTANCE - Provided herein are methods of treating and/or preventing cancer drug resistance using antagonists of KDM5. | 05-26-2016 |
| 20160143913 | 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-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. | 05-26-2016 |
| 20160175286 | SELECTIVE AT2 RECEPTOR AGONISTS FOR USE IN TREATMENT OF CACHEXIA | 06-23-2016 |
| 20220133730 | Compositions and Methods for the Prevention and Treatment of Hearing Loss - Method, kit and pharmaceutical compositions using an inhibitor of EGFR signaling for prevention or treatment of hearing loss are described. | 05-05-2022 |
