- Pyrazolopyridine compound and use thereof
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The present invention relates to a pyrazolopyridine compound and use thereof, and further relates to a pharmaceutical composition comprising the pyrazolopyridine compound. The pyrazolopyridine compound or the pharmaceutical composition can be used as a so
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- AMINO-QUINOLINES AS KINASE INHIBITORS
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Disclosed are compounds having the formula:wherein R 1 , R 2 , R 3 and Z are as defined herein, and methods of making and using the same.
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- BICYCLIC PYRIDINE AND PYRIMIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT, AMELIORATION OR PREVENTION OF INFLUENZA
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The present invention relates to a compound having the formula (I), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, codrug, cocrystal, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which is useful in treating, ameloriating or preventing influenza.
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- PYRIMIDINE AND PYRIDINE DERIVATIVES AND USE IN TREATMENT, AMELIORATION OR PREVENTION OF INFLUENZA THEREOF
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Provided herein is a compound of formula (I), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, codrug, cocrystal, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which is useful in treating, ameliorating or preventing influenza.
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- AMINO-QUINOLINES AS KINASE INHIBITORS
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Disclosed are compounds having the formula: wherein R1, R2, R3 and Z are as defined herein, and methods of making and using the same.
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- AMINO-QUINOLINES AS KINASE INHIBITORS
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Disclosed are compounds having the formula: wherein R1, R2, R3 and Z are as defined herein, and methods of making and using the same.
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- AMINO QUINAZOLINES AS KINASE INHIBITORS
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Disclosed are compounds having the formula (Formula I)): wherein R1, R2, R3 and Z are as defined herein, and methods of making and using the same.
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- FLUOROALKYL-SUBSTITUTED PYRAZOLOPYRIDINES AND USE THEREOF
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The present application relates to novel fluoroalkyl-substituted pyrazolopyridines, to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prophylaxis of diseases and to their use for production of medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders.
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- BICYCLIC AZA HETEROCYCLES, AND USE THEREOF
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The present application relates to novel bicyclic azaheterocycles, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.
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- HETEROARYL-SUBSTITUTED PYRAZOLOPYRIDINES AND USE THEREOF AS SOLUBLE GUANYLATE CYCLASE STIMULATORS
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The present application relates to novel heteroaryl-substituted pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for t
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- SUBSTITUTED ANNULATED PYRIMIDINES AND TRIAZINES, AND USE THEREOF
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The present application relates to novel substituted fused pyrimidines and triazines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
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- RING-FUSED PYRIMIDINES AND TRIAZINES AND USE THEREOF FOR THE TREATMENT AND/OR PROPHYLAXIS OF CARDIOVASCULAR DISEASES
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The present application relates to novel fused pyrimidines and triazines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
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- MODULATORS OF THE GPR119 RECEPTOR AND THE TREATMENT OF DISORDERS RELATED THERETO
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The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, and N-oxides thereof,that are useful as single pharmaceutical agents or in combination with one or more additional pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing secretion of an incretin; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.
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Page/Page column 106; 107
(2013/04/25)
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- RING-FUSED 4-AMINOPYRIMIDINES AND USE THEREOF AS STIMULATORS OF SOLUABLE GUANYLATE CYCLASES
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The present application relates to novel fused 4-aminopyrimidines, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for th
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- USE OF STIMULATORS AND ACTIVATORS OF SOLUBLE GUANYLATE CYCLASE FOR TREATING SICKLE-CELL ANEMIA AND CONSERVING BLOOD SUBSTITUTES
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The present invention relates to the novel use of stimulators and activators of soluble guanylate cyclase for the treatment of sickle cell anemia and for the preservation of blood substitutes. The present invention furthermore relates to the use of stimulators and activators of soluble guanylate cyclase in combination with PDE5 inhibitors for the treatment of sickle cell anemia and for the preservation of blood substitutes.
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- Substituted annellated pyrimidines and use thereof
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The present application relates to novel substituted annellated pyrimidines, methods for production thereof, use thereof alone or in combinations for treating and/or preventing diseases and use thereof for the production of medicinal products for treating
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- INHIBITORS OF INFLUENZA VIRUSES REPLICATION
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Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
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- AMINO QUINAZOLINES AS KINASE INHIBITORS
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Disclosed are compounds having the formula (Formula (I)): wherein R1, R2, R3, and Z are as defined herein, and methods of making and using the same.
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- Substituted 5-fluoro-1H-pyrazolopyridines and their use
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The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
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- INHIBITORS OF INFLUENZA VIRUSES REPLICATION
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Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
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- INHIBITORS OF INFLUENZA VIRUSES REPLICATION
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Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
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- A modified approach to C-14-labeled 2-(3,4-difluorophenoxy)-5- fluoronicotinic acid and other halogen-substituted analogs
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A modified approach to a carbon-14-labeled pyridine ring system was developed based on the electrocyclic ring-closure of 1,4,4-trisubstituted butadiene. The new method was applied to prepare 2-(3,4-difluorophenoxy)-5- fluoro-[2-14C] nicotinic a
- Zhang, Yinsheng,Jian, Zhigang,Stolle, Wayne T.
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p. 382 - 386
(2012/06/01)
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- THE USE OF sGC STIMULATORS, sGC ACTIVATORS, ALONE AND COMBINATIONS WITH PDE5 INHIBITORS FOR THE TREATMENT OF SYSTEMIC SCLEROSIS (SSc).
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The use of sGC stimulators, sGC activators alone, or in combination with PDE5 inhibitors for the prevention and treatment of fibrotic diseases, such as systemic sclerosis, scleroderma, and the concomitant fibrosis of internal organs.
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- AMINOPYRIMIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES
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The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
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- PYRIMIDINES AND PYRIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES
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The present invention relates to compounds useful as inhibitors of protein kinases, such as inhibitors of GSK-3. The invention provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. The invention provides processes for preparing compounds of the invention. The invention provides methods of identifying compounds useful for treatment of diabetes, diabetic neuropathy, osteoporosis, Alzheimer's disease, Huntington's disease, Parkinson's disease, AIDS-associated dementia, bipolar disorder, amyotrophic lateral sclerosis, multiple sclerosis, schizophrenia, leukocytopenia, cardiomyocyte hypertrophy, stroke, post-stroke, spinal cord injury, traumatic brain injury, Charcot-Marie-Tooth, peripheral nerve regeneration, and rheumatoid arthritis.
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- PROCESS FOR PREPARING 5-FLUORO-1H-PYRAZOLO [3, 4-B] PYRIDIN-3-AMINE AND DERIVATIVES THEREOF
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The present invention relates to a process for the synthesis of 5-fluoro-1H-pyrazolo [3, 4-b]pyridin-3-amine in high yield and purity. The present invention also relates to processes for the synthesis of 5-fluoro-1H-pyrazolo [3, 4- b] ρyridin-3-amine derivatives. These processes are useful for preparing biologically active compounds, particularly certain GSK-3 inhibitors, or derivatives thereof. Reagents and conditi ons : i. Pd ( OAc )2, PPh3, Et3N, H2CO2; i i. 1 ) (COCl )2, CH2Cl2, cat. DMF; 2 ) NH3 (g ), dioxane, i i i. TFAA, Et3N, CH2Cl2, O°C; iv. H2NNH2. H2O, n-butanol, reflux.
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Page/Page column 35-36
(2009/03/07)
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- AMINOPYRIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES
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The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
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- AMINOPYRIMIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES
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The present invention relates to compounds of formula I useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention
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- AMINOPYRIMIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES
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The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
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Page/Page column 56; 58
(2008/12/06)
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- Cinnamamide compounds as metabotropic glutamate receptor antagonists
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The invention relates to compounds of formula I or pharmaceutically acceptable salts or solvates thereof: where R1, R2, R3, A, X, and n are defined in the description. The invention also includes pharmaceutical composition
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Page/Page column 22
(2010/11/26)
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- Bicyclic piperazines as metabotropic glutatmate receptor antagonists
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The invention relates to compounds of formula I or pharmaceutically acceptable salts or solvates thereof: where Ar1, A, Hy, R1, m and n are as defined in the description. The invention also includes pharmaceutical compositions and uses of, and processes of making the compounds, as well as methods of medical treatment of mGluR5-mediated disorders.
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Page/Page column 45
(2008/06/13)
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- Method for producing 3-substituted 2-chloro-5-fluoro-pyridine or its salt
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To provide a method for producing a 3-substituted 2-chloro-5-fluoro-pyridine or its salt in high yield from a readily available material through a short process under mild reaction conditions using a reagent which is easy for handling and simple in the reaction operation. Namely, a method for producing the following compound (2) or its salt which comprises selectively reducing a chlorine atom at the 6-position of the following compound (1) or its salt, is provided. Further, a method for producing the following compound (4) or its salt which comprises substituting a Z1 group of the following compound (2) or its salt obtained by the reduction reaction, by a Z2 group, is provided. Here, Z1 is —CO2R1, etc., and R1 is a hydrogen atom, an alkyl group, an alkenyl group, an aryl group, an aralkyl group or a cycloalkyl group. Z2 is a group different from Z1 and is —CO2R5, etc., and R5 is an alkyl group, an alkenyl group, an aryl group, an aralkyl group or a cycloalkyl group.
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Page/Page column 7
(2010/10/20)
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- AMINO-TETRAZOLES ANALOGUES AND METHODS OF USE
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A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R 5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.
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