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US 11,142,531 B2Granted
Cyano substituted heteroarylpyrimidinone derivative, preparation method and use thereof
AssigneeZhejiang Hisun Pharmaceutical Co., Ltd.
InventorsHejun Lv, Dongliang Guan, Mingxiao Chen, Jinglu Wang, Lin Qian
Life of this patent
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Abstract
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.
Claims21
A compound as shown in Formula (I):
- or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof,
- wherein
- X is selected from —NH—, —O— or —S—;
- L1 is selected from alkylene, cycloalkylene or heterocyclylene;
- R1 is selected from hydrogen atom, alkyl, halogen, alkoxy or cyano, wherein the alkyl or alkoxy is optionally further substituted by one or more substituent groups selected from halogen, hydroxy, cyano, nitro, alkoxy, cycloalkyl, heterocyclyl, aryl, heteroaryl, —NR8R9, —C(O)NR8R9, —C(O)R6, —OC(O)R6, —S(O)qNR8R9, —NR8S(O)2R9 or —NR8C(O)R9;
- R2 is selected from hydrogen atom, hydroxy, halogen, nitro, cyano, alkyl, alkoxy, cycloalkyl, heterocyclyl, aryl, heteroaryl, —NR8R9, —C(O)NR8R9, —C(O)R6, —OC(O)R6, —S(O)qNR8R9, —NR8S(O)2R9 or —NR8C(O)R9, wherein the alkyl, alkoxy, 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, —NR10R11, —C(O)NR10R11, —C(O)R12, —C(O)OR12 or —NR10C(O)R11;
- R3 is selected from aryl or heteroaryl, wherein the aryl or heteroaryl is optionally further substituted by one or more substituent groups selected from R7;
- R4 and R5 are each independently selected from hydrogen atom, alkyl, —OR6, —SR6, —NR8R9, —C(O)NR8R9, —C(O)R6, —OC(O)R6, —S(O)qNR8R9, —NR8S(O)2R9 or —NR8C(O)R9;
- or, R4 and R5, together with the atom to which they are attached, form a C3-8 saturated or partly unsaturated cycloalkyl, or form a C4-8 saturated or partly unsaturated heterocyclyl having one or more heteroatoms selected from N, O and S(O)q, wherein the cycloalkyl or heterocyclyl is optionally further substituted by one or more substituent groups selected from hydroxy, halogen, nitro, cyano, alkyl, alkoxy, cycloalkyl, heterocyclyl, aryl, heteroaryl, —NR8R9, —C(O)NR8R9, —C(O)R6, —OC(O)R6, —S(O)qNR8R9, —NR8S(O)2R9 or —NR8C(O)R9;
- R7 is each independently selected from hydrogen atom, hydroxy, halogen, cyano, nitro, alkyl, alkoxy, cycloalkyl, heterocyclyl, aryl, heteroaryl, —NR8R9, —C(O)NR8R9, —C(O)R6, —OC(O)R6, —S(O)qNR8R9, —NR8S(O)2R9 or —NR8C(O)R9, wherein the alkyl, alkoxy, cycloalkyl, heterocyclyl, aryl or heteroaryl is optionally further substituted by a substituent group selected from hydroxy, halogen, nitro, cyano, alkyl, alkoxy, cycloalkyl, heterocyclyl, aryl, heteroaryl, —NR8R9, —C(O)NR8R9, —C(O)R6, —OC(O)R6, —S(O)qNR8R9, —NR8S(O)2R9 or —NR8C(O)R9;
- R6, R8 and R9 are each independently selected from hydrogen atom, alkyl, —OR12, cyano, hydroxy, halogen, 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, —NR10R11, —C(O)NR10R11, —C(O)R12, —C(O)OR12 or —NR10C(O)R11;
- or, R8 and R9, together with the N atom to which they are attached, form a C4-8 heterocyclyl, wherein the C4-8 heterocycle comprises one or more atoms selected from N, O and S(O)q, and the C4-8 heterocycle is optionally further substituted by one or more substituent groups selected from hydroxy, halogen, nitro, cyano, alkyl, alkoxy, cycloalkyl, heterocyclyl, aryl, heteroaryl, ═O, —NR10R11, —C(O)NR10R11, —C(O)R12, —C(O)OR12 or —NR10C(O)R11;
- R10, R11 and R12 are each independently 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;
- and
- q is 0, 1 or 2.
12 more elements
Dependencies are inferred from the claim text.