- COMBINATIONS OF DIACYLGLYCEROL ACYLTRANSFERASE 2 INHIBITORS AND ACETYL-COA CARBOXYLASE INHIBITOR
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Described herein are pharmaceutical compositions comprising 2-{5-[(3-ethoxypyridin-2-yl)oxy]pyridin-3-yl}-N-[(3S,5S)-5-fluoropiperidin-3-yl]pyrimidine-5-carboxamide, or pharmaceutically acceptable salt thereof, for treatment of liver disease and diseases related thereto. Also described are compositions comprising 2-{5-[(3-ethoxypyridin-2-yl)oxy]pyridin-3-yl}-N-[(3S,5S)-5-fluoropiperidin-3-yl]pyrimidine-5-5 carboxamide, or pharmaceutically acceptable salt thereof and 4-(4-(1-Isopropyl-7-oxo-1,4,6,7-tetrahydrospiro[indazole-5,4'-piperidine]-1'-carbonyl)-6-methoxypyridin-2-yl)benzoic acid, or pharmaceutically acceptable salt thereof, for treatment of liver disease and diseases related thereto.
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Page/Page column 65; 124-126
(2021/09/04)
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- COMBINATIONS FOR TREATMENT OF NAFLD/NASH AND RELATED DISEASES
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A method for treating fatty liver disease and related diseases or disorders with a therapeutically effective amount of a composition comprising from about 25 mg to about 1200 mg of (S)-2-(5-((3-ethoxypyridin-2-yl)oxy)pyridin-3-yl)-N-(tetrahydrofuran-3-yl)pyrimidine-5- carboxamide or a pharmaceutically acceptable salt thereof, and from about 5 mg to about 40 mg of 4-(4-(1-Isopropyl-7-oxo-1,4,6,7-tetrahydrospiro[indazole-5,4'-piperidine]-1'-carbonyl)-6- methoxypyridin-2-yl)benzoic acid or a pharmaceutically acceptable salt thereof.
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Page/Page column 42-43
(2021/09/04)
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- Combinations For Treatment Of NASH/NAFLD And Related Diseases
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The combination of (S)-2-(5-((3-ethoxypyridin-2-yl)oxy)pyridin-3-yl)-N-(tetrahydrofuran-3-yl)pyrimidine-5-carboxamide or pharmaceutically acceptable salt thereof, and 4-(4-(1-Isopropyl-7-oxo-1,4,6,7-tetrahydrospiro[indazole-5,4′-piperidine]-1′-carbonyl)-6-methoxypyridin-2-yl)benzoic acid or pharmaceutically acceptable salt thereof, for treatment of diseases, including non-alcoholic steatohepatitis (NASH), in mammals are described herein.
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Paragraph 0314-0315
(2020/03/23)
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- COMBINATIONS COMPRISING BENZODIOXOL AS GLP-1R AGONISTS FOR USE IN THE TREATMENT OF NASH/NAFLD AND RELATED DISEASES
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In part, the invention provides a new combination comprising (1) a GLP-1R agonist and (2) an ACC inhibitor or a DGAT2 inhibitor, or a KHK inhibitor or FXR agonist. The invention further provides new methods for treating diseases and disorders, for example, fatty liver, nonalcoholic fatty liver disease, nonalcoholic steatohepatitis, nonalcoholic steatohepatitis with liver fibrosis, nonalcoholic steatohepotitis with cirrhosis, and nonalcoholic steatohepatitis with cirrhosis and with hepatocellular carcinoma or with a metabolic-related disease, obesity, and type 2 diabetes, for example, using the new combination described herein.
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Page/Page column 244; 245
(2020/12/07)
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- CRYSTALLINE 2-AMINO-2-(HYDROXYMETHYL)PROPANE-1,3-DIOL SALT OF 4-(4-(1-ISOPROPYL-7-OXO-1,4,6,7-TETRAHYDROSPIRO[INDAZOLE-5,4'-PIPERIDINE]-1'-CARBONYL)-6-METHOXYPYRIDIN-2-YL)BENZOIC ACID
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The invention provides the tris salt of 4-(4-(1-isopropyl-7-oxo-1,4,6,7- tetrahydrospiro[indazole-5,4'-piperidine]-1'-carbonyl)-6-methoxypyridin-2-yl)benzoic acid as a crystalline anhydrous or tri-hydrate; as well as polymorphs, pharmaceutical compositions, dosage forms, and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase (ACC) enzyme(s) in an animal.
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Page/Page column 17
(2019/06/11)
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- SUBSTITUTED HETEROARYL COMPOUNDS AND METHODS OF USE
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The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof. They are useful in preventing, managing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.
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Paragraph 0440; 0466
(2017/03/28)
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- Substituted heteroaryl compounds and composition thereof, and applicaitons of compounds and composition
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The invention provides substituted heteroaryl compounds and a composition thereof, and applicaitons of the compounds and the composition. The compounds are compounds represented by the formula (I) or the formula (II) or stereoisomers, tautomers, nitrogen oxides, solvates, metabolites, pharmaceutically acceptable salts or prodrugs of the compounds represented by the formula (I) or the formula (II). The invention also provides the pharmaceutical composition comprising the compounds; the compounds and the pharmaceutical composition can adjust the activity of protein kinase, and are used for prevention, processing, treatment and remission of diseases or disorders mediated by the protein kinase.
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Paragraph 0813; 0814; 0815; 0934; 0935; 0936
(2017/07/31)
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- Substituted heteroaryl compounds and compositions and uses thereof
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The invention provides a substituted heteroaryl compound and a composition thereof, and applications of the compound and the composition. The compound is a compound as shown in a formula I, or stereoisomer, tautomer, oxynitride, solvate, metabolite, pharmaceutically-acceptable salt or prodrug of the compound as shown in the formula I. The invention also provides a pharmaceutical composition containing the above-mentioned compound; and the above-mentioned compound and the pharmaceutical composition are capable of adjusting the activity of JAK kinases and are applied in prevention, treatment, therapy and alleviation of JAK kinase mediated diseases or disorders.
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Paragraph 0536; 0537; 0538
(2017/12/27)
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- Substituted heteroaryl compounds and compositions and uses thereof
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The invention provides a substituted ceteroary compound as well as a composition and a purpose thereof. The substituted ceteroary compound is a compound shown as a formula (I) or a stereoisomer, a tautomer, a nitrogen oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug of the pharmaceutically acceptable salt of the compound shown as the formula (I) and is used for regulating diseases or disorders mediated by one kind or various kinds of Janus kinase activities. The invention also provides a medicine composition containing the compound and a method of treating or alleviating the disease or disorder degree of a patient by inhibiting the Janus kinase activity.
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Paragraph 0588; 0589; 0590
(2018/01/04)
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- Spiro aryl phosphorus oxide or sulfide
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The invention discloses a spiro aryl phosphorus oxide or sulfide as ALK inhibitor, and in particular discloses a compound shown in a formula (I) as an ALK inhibitor or a pharmaceutically acceptable salt thereof.
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- SUBSTITUTED HETEROARYL COMPOUNDS AND METHODS OF USE
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The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof useful in preventing, treating or lessening the severity of a JAK-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of JAK-mediated disease.
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Paragraph 0346
(2016/12/22)
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- SUBSTITUTED HETEROARYL COMPOUNDS AND METHODS OF USE
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The present invention provides new heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof useful in preventing, treating or lessening the severity of JAK-mediated diseases. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of JAK-mediated diseases.
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Paragraph 358
(2015/07/07)
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- SUBSTITUTED HETEROARYL COMPOUNDS AND METHODS OF USE
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The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof useful in preventing, treating or lessening the severity of a protein-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.
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Paragraph 0363
(2015/11/24)
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- USE OF ACETYL-COA CARBOXYLASE INHIBITORS FOR TREATING ACNE VULGARIS
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The present invention relates to methods of treating and/or preventing acne in patients comprising the step of administering to patients in need of such treatment a therapeutically effective amount of an ACC inhibitor or a pharmaceutically acceptable salt thereof.
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Page/Page column 41
(2015/03/28)
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- N1-PYRAZOLOSPIROKETONE ACETYL-CoA CARBOXYLASE INHIBITORS
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The invention provides a compound of Formula (I) Z N N O N O A1R2 R1 R3R 3 L A 2 (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3,Z, A1, L and A 5 2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
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Page/Page column 42-43
(2012/04/17)
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- SUBSTITUTED ACETYL-COA CARBOXYLASE INHIBITORS
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The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein G is R1, R2 and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
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Page/Page column 17
(2012/11/07)
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- N1-PYRAZOLOSPIROKETONE ACETYL-COA CARBOXYLASE INHIBITORS
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The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions there-of; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl- CoA carboxylase enzyme(s) in an animal
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Page/Page column 19; 20
(2011/05/16)
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- N2-PYRAZOLOSPIROKETONE ACETYL-COA CARBOXYLASE INHIBITORS
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The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of said compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl- CoA carboxylase enzyme(s) in an animal.
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Page/Page column 42
(2011/06/16)
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- Substituted Spiroamine Compounds
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Substituted spiroamine compounds corresponding to the formula (I) In which m, n, o, p, Q, r, s, t, R1, R2, R3, R4a, R4b, R5a, R5b, R6a, R6b, R7, R8, R9, R10 and R11 have defined meanings; a process for the preparation of such compounds, pharmaceutical compositions containing such compounds and the use of substituted spiroamines for the treatment or inhibition of pain and/or other conditions mediated by the bradykinin 1 receptor.
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- Substituted Spiro-amide Compounds
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Substituted spiro-amide compounds corresponding to formula I in which R5 through R8, D, X, Y and Z have defined meanings, processes for preparing such spiro-amide compounds, pharmaceutical compositions containing such compounds, and methods of using such spiro-amide compounds for treating and/or inhibiting disorders or disease states mediated at least in part by the bradykinin 1 receptor.
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Page/Page column 127
(2010/10/19)
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- FUSED TRICYCLIC PYRAZOLO[1, 5-A]PYRIMIDINES, METHODS FOR PREPARATION AND USES THEREOF
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Fused, tricyclic pyrazolo{1,5-a]pyrimidine compounds of formula A or of formula B: and pharmaceutically acceptable salts thereof are described, which selectively inhibit Raf kinase activity and are useful for treating disorders mediated by certain Raf kinases.
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