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1. 发明申请

WO1993003013A1 INDOLINE DERIVATIVES HAVING AN AMIDE FUNCTION, THEIR PREPARATION, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：具有酰胺官能团的吲哚衍生物，其制备物和含有它们的药物组合物
公开(公告)号：WO1993003013A1
公开(公告)日：1993-02-18
申请号：PCT/FR1992000758
申请日：1992-07-31
申请人： ELF SANOFI
发明人： ELF SANOFI , WAGNON, Jean , PLOUZANE, Claude , SERRADEIL-LEGAL, Claudine , NISATO, Dino , TONNERRE, Bernard
IPC分类号： C07D209/42
CPC分类号： C07D401/06 , C07D209/42 , C07D401/12 , C07D403/06 , C07D417/06
摘要： The invention relates to compounds of formula (I), wherein R1 is a halogen atom, C1-C4 alkyl, hydroxyl, C1-C4 alkoxy, a group benzyloxy, cyano, trifluoromethyl, nitro or amino; R2 is C1-C6 alkyl, C3-C7 cycloalkyl, C5-C7 cycloalcen, a phenyl unsubstituted or substituted one or a plurality of times, C1-C4 alkoxy, halogen, a group trifluoromethyl, a group amino, or R2 is a nitrophenyl unsubstituted or substituted one or a plurality of times; R3 is a hydrogen atom; R4 is a carbamyl group having the formula CONR6R7; R5 is C1-C4 alkyl; naphtyl-1; naphtyl-2; dimethylamino-5 naphtyl-1; a phenyl unsubstituted or substituted one or a plurality of times, or R5 is nitrophenyl unsubstituted or substituted one or a plurality of times; R6 is C1-C6 alkyl, or R6 is similar to R7; R7 is a group piperidin-4-yl; a group azetidin-3-yl, said groups being substituted or unsubstituted on the nitrogen by C1-C4 alkyl, by a benzyloxycarbonyl or by an alkoxycarbonyl in C1-C4; a group (CH2)r itself substituted by a group pyridyl-2, -3 or -4, by a group hydroxyl, by an amino group free or substituted by one or two substituants; or R6 and R7 form together with the nitrogen atom to which they are linked a heterocycle selected amongst: morpholin, thiomorpholin, thiazolidin or 2,2-dimethylthiazolidin unsubstituted or substituted by R8, piperazin unsubstituted or substituted in 4 by a group R''8, an unsaturated mononitrogenated cycle with 5 links substituted by R8 or a saturated mononitrogenated cycle with 3, 4, 5, 6 or 7 links substituted by R8 and R9; R8 is R'8 or a group (CH2)r itself substituted by hydroxyl or by a free amino or substituted by one or two C1-C4 alkyls; R'8 is a group (CH2)q itself substituted by a carboxyl group, a group C1-C4 alkoxycarbonyl, a benzyloxycarbonyl group, a group carbamoyl free or substituted by a hydroxyl or by one or two C1-C4 alkyls, or a group aminocarbothioyl free or substituted by one or two C1-C4 alkyls; R''8 is R'8 or a group (CH2)2NH2 free or substituted by one or two C1-C4; R9 is hydrogen, halogen, a group (CH2)rOR10, a group (CH2)rNR11R12, a group (CH2)sCONR11R'11, a group azido; R10 is hydrogen, C1-C4 alkyl, mesyl or tosyl; R11, R'11 and R12 are each hydrogen or C1-C4 alkyl or R11 is hydrogen and R12 is C1-C4 alkoxycarbonyl or benzyloxycarbonyl; n is 0, 1 or 2; m is 0, 1, or 2; q is 0, 1, 2 or 3; r is 0, 1, 2 or 3 with the provision that r is different from 0 when R8 or R9 is in the alpha position of the intracyclic amidic nitrogen; s is 0 or 1; as well as its optional salts. These compounds are useful in the treatment of affections of the central nervous system, the cardiovascular system and the gastric system in human beings and animals.

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