DUBOIS, Laurent,EVANNO, Yannick,MALANDA, André,MALOIZEL, Christian
申请号:
EP08761774.2
公开号:
EP2125787B1
申请日:
2008.01.17
申请国别(地区):
EP
年份:
2017
代理人:
摘要:
N-(Benzo-heterocyclyl)-1-heteroaryl-1H-indole-2-carboxamide derivatives (I) are new. Indole derivatives of formula (I) and their acid addition salts, hydrates and solvates are new. X 1-X 4H, halo, alkyl, cycloalkyl, cycloalkyl-(1-3C) alkyl, fluoroalkyl, alkoxy, fluoroalkoxy, CN, CONR 1R 2, NO 2, NR 1R 2, alkylthio, alkylsulfinyl, alkylsulfonyl, SO 2NR 1R 2, NR 3COR 4, NR 3SO 2R 5 or aryl (optionally substituted (os) by one or more of alkyl, cycloalkyl, cycloalkyl-(1-3C) alkyl, fluoroalkyl, alkoxy, fluoroalkoxy, CN or NO 2); W' : benzo-fused 5-7 membered heterocycle, (i) containing 1-3 of S, O and/or N as heteroatom(s), (ii) bonded to the N of (I) via the benzo ring, (iii) os on C of the heterocyclic ring by one or more of alkyl, cycloalkyl, cycloalkyl-(1-3C) alkyl, fluoroalkyl, alkoxy, cycloalkoxy, cycloalkyl-(1-3C) alkoxy, aryl, arylalkyl, = O or thio and (iv) os on N by R 6 if the N is adjacent to = O or in other cases by R 7; Y' : heteroaryl (os by one or more of halo, alkyl, cycloalkyl, cycloalkyl-(1-3C) alkyl, fluoroalkyl, OH, alkoxy, fluoroalkoxy, CN, CONR 1R 2, NO 2, NR 1R 2, alkylthio, SH, alkylsulfinyl, alkylsulfonyl, cycloalkylsulfinyl, cycloalkylsulfonyl, SO 2NR 1R 2, NR 3COR 4, NR 3SO 2R 5, aryl or arylalkyl (where aryl moieties are os as in X 1-X 4); R 1, R 2H, alkyl, cycloalkyl, cycloalkyl-(1-3C) alkyl, arylalkyl or aryl; or NR 1R 2azetidino, pyrrolidone, piperidino, azepino, morpholino, thiomorpholino, piperazino or homopiperazino (all os by alkyl, cycloalkyl, cycloalkyl-(1-3C) alkyl, arylalkyl or aryl); R 3, R 4H, alkyl, arylalkyl or aryl; R 5alkyl, arylalkyl or aryl; R 6H, alkyl, cycloalkyl, cycloalkyl-(1-3C) alkyl, fluoroalkyl, arylalkyl, alkylcarbonyl, cycloalkyl-(1-3C) alkylcarbonyl, fluoroalkylcarbonyl, cycloalkylcarbonyl, arylcarbonyl, arylalkylcarbonyl, alkylsulfonyl, fluoroalkylsulfonyl, cycloalkylsulfonyl, cycloalkyl-(1-3C) alkylsulfonyl, arylsulfonyl or aryl; ring S and N atoms in W' and Y' are optionally in oxidized form; unless specified