- ISO-CITRATE DEHYDROGENASE (IDH) INHIBITOR
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Disclosed are compounds inhibiting the conversion of α–KG to D-2-HG, pharmaceutically acceptable salts, hydrates, solvates or stereoisomers thereof and pharmaceutical compositions comprising the compounds. The compound and the pharmaceutical composition c
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- NOVEL BENZIMIDAMIDES COMPOUNDS COMPRISING AN OXABORININ RING
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The invention relates to 4-(1-hydroxy-3,4-dihydro-1H-benzo[c][1,2]oxaborinin-3-yl)benzimidamide derivatives and their use in treating diseases and conditions of the skin (for example, Netherton syndrome, rosacea, atopic dermatitis, psoriasis and itch) cau
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- PIPERIDINE COMPOUNDS AS PCSK9 INHIBITORS
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One aspect of the invention relates to a series of new PCSK9 inhibitor compounds comprising piperidine ring structures, including compounds of formula (I) and/or pharmaceutically acceptable salts thereof. Another aspect of the invention relates to methods of treating PCSK9 receptor related diseases comprising administration of one or more compounds of formula (I) or a pharmaceutically acceptable salt thereof.
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- ISOQUINOLINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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A compound of formula (I): wherein the substituents are as defined in the description. Medicinal products containing the same which are useful in treating or preventing pathologies which are the result of activation of the RhoA/ROCK pathway and phosphorylation of the myosin light chain.
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Paragraph 0269; 0270; 0271
(2017/06/12)
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- Synthesis method of 3-fluoro-4-bromo-acetophenone
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The invention relates to a synthesis method of 3-fluoro-4-bromo-acetophenone. The method includes: taking 3-fluoro-4-bromo-benzoyl chloride, dimethylhydroxyamine hydrochloride and methylmagnesium chloride as the raw materials, carrying out aminolysis, ext
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Paragraph 0023; 0024; 0030; 0031; 0037; 0038
(2017/08/27)
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- HEPATITIS C VIRUS INHIBITORS AND USES THEREOF IN PREPARATION OF DRUGS
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A series of hepatitis C virus (HCV) inhibitors and compositions and applications thereof in the preparation of drugs for treating chronic HCV infection. Especially, a series of compounds that are used as NS5A inhibitors, and compositions and uses thereof in the preparations of drugs.
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Paragraph 0477; 0478
(2017/12/17)
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- BTK INHIBITORS
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Provided are Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.
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Page/Page column 115
(2016/07/27)
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- NOVEL AROMATIC COMPOUND AND USE THEREOF
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Provided is a compound showing a bone formation promoting action (and/or bone resorption suppressive action). A compound of the formula (I) or a pharmacologically acceptable salt: [wherein each substituent is as defined in the DESCRIPTION], has low toxicity, shows good pharmacokinetics, has an action to promote bone formation, and is useful for the prophylaxis or To treatment of metabolic bone diseases (osteoporosis, fibrous osteitis (hyperparathyroidism), osteomalacia, Paget's disease that influences the systemic bone metabolism parameter etc.) associated with a decrease in the bone formation ability as compared to the bone resorption capacity.
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Paragraph 0715-0717; 0871-0873
(2016/08/17)
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- HEPATITIS C INHIBITOR COMPOUNDS
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Compounds of Formula (I) and (II) wherein R1, R2, R3, R6, A and A' are defined herein. The compounds are useful as inhibitors of the function of NS5A protein encoded by HCV for the treatment of hepatitis C viral infection.
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Page/Page column 23-24
(2012/05/04)
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- IMIDAZO[1,2-B][1,2,4]TRIAZINES AS C-MET INHIBITORS
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The present invention relates to imidazo[1,2-b][1,2,4]triazines that are inhibitors of c-Met and are useful in the treatment of c-Met associated diseases including cancer.
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- Substituted inmidazoles as bombesin receptor subtype-3 modulators
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Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.
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Page/Page column 31
(2010/02/17)
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- SALTS OF 2-FLUORO-N-METHYL-4-[7-(QUINOLIN-6-YL-METHYL)-IMIDAZO[1,2-b][1,2,4]TRIAZIN-2-YL]BENZAMIDE AND PROCESSES RELATED TO PREPARING THE SAME
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The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.
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Page/Page column 18-19
(2009/12/05)
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- Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors
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Aryldihydropyridazinones and aryldimethylpyrazolones with 2-benzyl vinylogous amide substituents have been identified as potent PDE3B subtype selective inhibitors. Dihydropyridazinone 8a (PDE3B IC50=0.19 nM, 3A IC50=1.3 nM) was selec
- Edmondson, Scott D.,Mastracchio, Anthony,He, Jiafang,Chung, Christine C.,Forrest, Michael J.,Hofsess, Scott,MacIntyre, Euan,Metzger, Joseph,O'Connor, Naphtali,Patel, Kajal,Tong, Xinchun,Tota, Michael R.,Van Der Ploeg, Lex H. T.,Varnerin, Jeff P.,Fisher, Michael H.,Wyvratt, Matthew J.,Weber, Ann E.,Parmee, Emma R.
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p. 3983 - 3987
(2007/10/03)
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- Sulfamoylheteroaryl pyrazole compounds as anti-inflammatory/analgesic agents
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This invention relates to a compound of the formula: or a pharmaceutically acceptable salt thereof, wherein A and R1 are each an optionally substituted 5 to 6-membered heteroaryl, wherein the heteroaryl is optionally fused to a carbocyclic ring or 5 to 6-heteroaryl; R2 is NH2; R3 and R4 are each hydrogen, halo, (C1-C4)alkyl optionally substituted with halo and the like; and X1 to X4 are each hydrogen, halo, hydroxy, (C1-C4)alkyl optionally substituted with halo and the like. These compounds have COX-2 inhibiting activity and thus useful for treating or preventing inflammation or other COX-2 related diseases.
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