您的位置: 首页 > 农业专利 > 详情页

DERIVATE VON PYRROLOPYRIDIN-2-CARBOXAMIDEN, IHRE HERSTELLUNG UND IHRE THERAPEUTISCHE ANWENDUNG
专利权人:
SANOFI
发明人:
DUBOIS, LAURENT,EVANNO, YANNICK,MALANDA, ANDRE
申请号:
EP08761773.4
公开号:
EP2106401B1
申请日:
2008.01.17
申请国别(地区):
EP
年份:
2012
代理人:
摘要:
Pyrrolopyridine derivatives (I) are new. Pyrrolo[3,2-b]pyridine, pyrrolo[3,2-c]pyridine, pyrrolo[2,3-c]pyridine or pyrrolo[2,3-b]pyridine derivatives of formula (I) and their N-oxides, salts, solvates and hydrates are new. X : H or 1-4 of halo, R', OR', CN, CONR 1R 2, NO 2, NR 1R 2, SR, SOR, SO 2R, SO 2NR 1R 2, NR 3COR 4, NR 3SO 2R 5, Ar or Ar(1-5C)alkyl; Ar : aryl or heteroaryl optionally substituted with halo, R', OR', NO 2 or CN; R : 1-6C alkyl; R' : R, 3-7C cycloalkyl, (3-7C)cycloalkyl(1-3C)alkyl or 1-6C fluoroalkyl; Y' : halo, R', OH, OR', CN, CONR 1R 2, NO 2, NR 1R 2, SR, 1-6C fluoroalkylthio, SH, SOR", SO 2R", SO 2NR 1R 2, NR 3COR 4, NR 3SO 2R 5, Ar or Ar(1-5C)alkyl; R" : R, 3-7C cycloalkyl or (3-7C)cycloalkyl(1-6C)alkyl; R 1-R 4H, R, 3-7C cycloalkyl or (3-7C)cycloalkyl(1-3C)alkyl, Ar or Ar(1-5C)alkyl, or NR 1R 2 = azetidine, pyrrolidine, piperidine, azepine, morpholine, thiomorpholine, piperazine or homopiperazine optionally substituted with halo, R', OR', NO 2 or CN; R 5R, 3-7C cycloalkyl or (3-7C)cycloalkyl(1-3C)alkyl, Ar or Ar(1-5C)alkyl; W' : phenyl fused to a 5- to 7-membered heterocycle that contains 1-3 heteroatoms (N, O, S) and is optionally C-substituted with R', oxo, thio, Ar, or Ar(1-5C)alkyl, and optionally N-substituted with R 6 when N is adjacent to CO or with R 7 in other cases, where S and N atoms are optionally oxidized; R 6H, R', Ar or Ar(1-5C)alkyl; R 7R', aryl(1-6C)alkyl, COR', aroyl, aryl(1-6C)alkylcarbonyl, SO 2R', arylsulfonyl, aryl(1-6C)alkylsulfonyl or aryl. An independent claim is also included for a process for preparing (I). [Image] ACTIVITY : Analgesic; Antiinflammatory; Antidiabetic; Uropathic; Gynecological; Antipsoriatic; Antipruritic; Virucide; Neuroprotective; Antidepressant. MECHANISM OF ACTION : TRPV1 receptor antagonist. N-(2-methyl-5-benzothiazolyl)-5-fluoro-1-(4-pyridylmethyl)-1H-pyrrolo[2,3-b]pyridine-2-carboxamide gave 50% inhibition of the current induced by capsaicin on dorsal root ganglions at a concentration of 10
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

意 见 箱

匿名:登录

个人用户登录

找回密码

第三方账号登录

忘记密码

个人用户注册

必须为有效邮箱
6~16位数字与字母组合
6~16位数字与字母组合
请输入正确的手机号码

信息补充