887594-13-0Relevant articles and documents
NOVEL PYRIDONE CARBOXYLIC ACID DERIVATIVE OR SALT THEREOF
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Paragraph 2327-2329, (2020/03/09)
It is intended to provide a novel compound having high antitumor activity and low toxicity to normal cells. The present invention provides a pyridone carboxylic acid derivative represented by the following formula (1) or a salt thereof wherein R1 represents a hydrogen atom, a halogen atom or the like; R2 represents a hydrogen atom, a halogen atom or the like; R3 to R6 each represent a hydrogen atom or the like; R7 represents a hydrogen atom or the like; R8 represents a hydrogen atom, a halogen atom, the following formula (a) (wherein Ra1 and Ra2 each represent a hydrogen atom, a hydroxy group, an optionally substituted lower alkyl group or the like) or the like, or R7 and R8 together represent —N—OR10 (wherein R10 represents a hydrogen atom, an optionally substituted lower alkyl group, or an aralkyl group), or R7 and R8 form an optionally substituted 4- to 6-membered saturated hetero ring together with the adjacent carbon atom, or the like; R9 represents a hydrogen atom or the like; X represents a nitrogen atom or the like; and Y represents a nitrogen atom or the like.
SUBSTITUTED PYRAZOLE COMPOUNDS AS SERINE PROTEASE INHIBITORS
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Paragraph 0507, (2017/05/27)
There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin and/or kallikrein, which compounds include substituted pyrazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which diseases or disorders are amenable to treatment or prevention by the inhibition of thrombin and/or kallikrein.
HETEROCYCLIC COMPOUND
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Paragraph 0988; 0989; 0990, (2016/06/28)
The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12)
Patel, Snahel,Harris, Seth F.,Gibbons, Paul,Deshmukh, Gauri,Gustafson, Amy,Kellar, Terry,Lin, Han,Liu, Xingrong,Liu, Yanzhou,Liu, Yichin,Ma, Changyou,Scearce-Levie, Kimberly,Ghosh, Arundhati Sengupta,Shin, Young G.,Solanoy, Hilda,Wang, Jian,Wang, Bei,Yin, Jianping,Siu, Michael,Lewcock, Joseph W.
, p. 8182 - 8199 (2015/11/09)
Recent data suggest that inhibition of dual leucine zipper kinase (DLK, MAP3K12) has therapeutic potential for treatment of a number of indications ranging from acute neuronal injury to chronic neurodegenerative disease. Thus, high demand exists for selective small molecule DLK inhibitors with favorable drug-like properties and good CNS penetration. Herein we describe a shape-based scaffold hopping approach to convert pyrimidine 1 to a pyrazole core with improved physicochemical properties. We also present the first crystal structures of DLK. By utilizing a combination of property and structure-based design, we identified inhibitor 11, a potent, selective, and brain-penetrant inhibitor of DLK with activity in an in vivo nerve injury model.
3-SUBSTITUTED PYRAZOLES AND USE AS DLK INHIBITORS
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, (2014/08/06)
The present invention provides for compounds of Formula (I) and various embodiments thereof, and compositions comprising compounds of Formula (I) and various embodiments thereof. (I) In compounds of Formula I, the groups R1, R2, R3, R4, R5, R6 and R7 have the meaning as described herein. The present invention also provides for methods of using compounds of Formula I and compositions comprising compounds of Formula (I) as DLK inhibitors and for treating neurodegeneration diseases and disorders.
PYRIDONE AND AZA-PYRIDONE COMPOUNDS AND METHODS OF USE
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Page/Page column 239, (2011/11/30)
Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
