02-04-2020 дата публикации
Номер: US20200102322A1
Автор:
Hejun LV,
Dongliang GUAN,
Mingxiao CHEN,
Jinglu WANG,
Lin QIAN,
LV HEJUN,
GUAN DONGLIANG,
CHEN MINGXIAO,
WANG JINGLU,
QIAN LIN,
LV, Hejun,
GUAN, Dongliang,
CHEN, Mingxiao,
WANG, Jinglu,
QIAN, Lin
The present invention relates to a cyano-substituted heteroarylpyrimidinone derivative represented by formula (I), a preparation method therefor and a use thereof as a therapeutic agent, in particular a use as an acetyl-CoA carboxylase (ACC) inhibitor, and the definition of each substituent in formula (I) is the same as the definition in the description. 5. The compound according to claim 1 , wherein Ris selected from methyl or trifluoromethyl.6. The compound according to claim 1 , wherein:{'sup': 2', '12', '8', '9, 'Ris selected from tetrazolyl, —C(O)ORor —C(O)NRR;'}{'sup': '8', 'Ris selected from hydrogen atom or alkyl;'}{'sup': 9', '12, 'Ris selected from cyano or —OR; and'}{'sup': '12', 'Ris selected from hydrogen atom, alkyl, alkenyl, cycloalkyl, heterocyclyl, aryl or heteroaryl, wherein the alkyl, cycloalkyl, heterocyclyl, aryl or heteroaryl is optionally further substituted by one or more substituent groups selected from hydroxy, halogen, nitro, cyano, alkyl, alkoxy, cycloalkyl, heterocyclyl, aryl, heteroaryl, carboxylic acid or carboxylic ester.'}8. The compound according to claim 1 , wherein Ris selected from tetrahydropyranyl.9. The compound according to claim 1 , wherein Ris selected from alkoxy or halogen claim 1 , wherein the alkoxy is optionally further substituted by halogen or cycloalkyl; and Ris preferably methoxy claim 1 , ethoxy claim 1 , fluoro claim 1 , trifluoromethyl claim 1 , difluoromethoxy claim 1 , fluoroethoxy or cyclopropyl methoxy.15. A pharmaceutical composition claim 1 , comprising an effective amount of the compound according to claim 1 , and optionally pharmaceutically acceptable carrier claim 1 , excipient or a combination thereof.16. A method for inhibiting ACC in a subject in need thereof claim 1 , comprising administering to the subject a therapeutically effective amount of the compound according to or the pharmaceutical composition according to .17. (canceled)18. A method for preventing or treating ACC-related diseases or ...
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