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NEW DERIVATIVES AS MIMETICS OF LEPTIN RECEPTOR MODULATORS
专利权人:
АстраЗенека АБ (SE)
发明人:
ХИГГИНБОТТОМ Майкл (GB),СИМПСОН Айан (GB),ХОРТОН Джеймс (GB),ТИЗАК Чарлз (GB),ХОРГАН Энн Вьет-Анх (GB)
申请号:
RU2010148900/04
公开号:
RU2010148900A
申请日:
2009.06.04
申请国别(地区):
RU
年份:
2012
代理人:
摘要:
1. The compound of formula (I) !! or its pharmaceutically acceptable salt, solvate, hydrate, geometric isomer, tautomer or optical isomer, where! each R1 is independently selected from C1-4 alkyl, C1-4 alkoxy, halogen, cyano, and CF3; ! R2 is C1-6 alkyl (optionally substituted with one or more substituents selected from hydroxy, halogen and cyano) or - [C (R4A) (R4B)] m-R5; ! R3 is hydrogen, C1-4 alkyl or fluoro-C1-4 alkyl; ! each of R4A and R4B is independently selected from hydrogen, halogen, hydroxy, C1-4 alkyl, fluoro-C1-4 alkyl, and hydroxy-C1-4 alkyl; ! R5 is C3-8cycloalkyl, C6-10aryl, heterocyclyl or heteroaryl, each of which is optionally substituted with one or more substituents selected from hydroxy, halogen, cyano, nitro, CF3 and C1-4 alkyl; ! m is 0, 1 or 2; and! n is 0, 1, 2, 3 or 4; ! provided that the compound is not selected from:! - pyridin-4-ylmethyl-bis (2-chloroethyl) carbamate; ! - (2,6-dichloropyridin-4-yl) methyldimethylcarbamate; ! - (2,6-dichloropyridin-4-ylmethylpropylcarbamate;! - pyridin-4-ylmethylmethylcarbamate;! - pyridin-4-ylmethylisopropylcarbamate;! - Pyridin-4-ylmethyl- [3- (trifluoromethyl) phenyl] carbamate;! 4-ylmethyl- (5-chloro-2-methoxyphenyl) carbamate;! - pyridin-4-ylmethyl- (2-methoxyphenyl) carbamate;! - pyridin-4-ylmethyl- (2,6-dimethylphenyl) carbamate;! - pyridine -4-ylmethyl- (2,4,6-trimethylphenyl) carbamate;! - pyridin-4-ylmethyl- (5-chloro-2,4-dimethoxyphenyl) carbamate;! - pyridin-4-ylmethyl- (2-methyl- 5-nitrophenyl) carbamate;! - pyridin-4-ylmethyl- (3-ethylphenyl) carbamate;! - pyridin-4-ylmethyl- (2,4-di etilfenil) carbamate; - pyridin-4-ilmetil- (3,4,5-trimethoxyphenyl) carbamate; - pyridin-4-ylmethyl (methyl) carbamate; - pyridin-4-ylmethylpyridine-3-ylcarbamate;1. Соединение формулы (I) !! или его фармацевтически приемлемые соль, сольват, гидрат, геометрический изомер, таутомер или оптический изомер, где ! каждый R1 независимо выбран из С1-4алкила, С1-4алкокси, галогена, циано и CF3; ! R2 представляет со
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