发明名称 INDOLE DERIVATIVES
摘要 The invention provides compounds of the general formula (I): <CHEM> or a physiologically acceptable salt or a solvate (e.g. hydrates) thereof in which R<1> represents a hydrogen atom or a halogen atom or a group selected from C1-6 alkyl, C2-6 alkenyl, fluoroC1-6alkyl, -CHO, -CO2H or -COR<4>; R<2> represents a hydrogen atom or a halogen atom or the group Ar; R<3> represents a hydrogen atom or a group selected from C1-6 alkyl, C3-6alkenyl, C1-6alkoxy, -COR<4>, -SO2R<4> or the group Ar; R<4> represents a group selected from C1-6 alkyl, C2-6 alkenyl, C1-6 alkoxy or the group -NR<1><2>R<1><3>; Ar represents the group <CHEM> R<5> represents a group selected from -CO2H, -NHSO2CF3 or a C-linked tetrazolyl group; R<6> and R<7> which may be the same or different each independently represent a hydrogen atom or a halogen atom or a C1-6alkyl group; Het represents an N-linked imidazolyl group substituted at the 2-position by a C1-6alkyl, C2-6alkenyl or a C1-6alkylthio group, the imidazolyl group optionally being substituted by one or two further substituents selected from a halogen atom or a group selected from cyano, nitro, C1-6alkyl, C2-6alkenyl, fluoroC1-6alkyl, -(CH2)mR<8>, -(CH2)nCOR<9>, or -(CH2)pNR<1><0>COR<1><1>; or Het represents an N-linked benzimidazolyl group substituted at the 2-position by a C1-6alkyl, C2-6alkenyl or a C1-6alkylthio group; R<8> represents a hydroxy or C1-6alkoxy group; R<9> represents a hydrogen atom or a group selected from hydroxy, C1-6alkyl, C1-6alkoxy, phenyl, phenoxy or the group -NR<1><2>R<1><3>; R<1><0> represents a hydrogen atom or a C1-6alkyl group; R<1><1> represents a hydrogen atom or a group selected from C1-6alkyl, C1-6alkoxy, phenyl, phenoxy or the group -NR<1><2>R<1><3>; R<1><2> and R<1><3> which may be the same or different each independently represent a hydrogen atom or a C1-4alkyl group or -NR<1><2>R<1><3> forms a saturated heterocyclic ring which has 5 or 6 ring members and may optionally contain in the ring one oxygen atom; m represents an integer from 1 to 4; n represents an integer from 0 to 4; and p represents an integer from 1 to 4; provided that one of R<2> and R<3> represents the group Ar, and that when R<2> represents the group Ar, R<3> represents a hydrogen atom or a group selected from C1-6 alkyl, C3-6 alkenyl, C1-6alkoxy -COR<4> or -SO2R<4>, and that when R<3> represents the group Ar, R<2> represents a hydrogen atom or a halogen atom. The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.
申请公布号 AU6666990(A) 申请公布日期 1991.05.23
申请号 AU19900066669 申请日期 1990.11.16
申请人 GLAXO GROUP LIMITED 发明人 BARRY CLIVE ROSS;DAVID MIDDLEMISS;DAVID IAN CARTER SCOPES;TORQUIL IAIN MACLEAN JACK;KEVIN STUART CARDWELL;MICHAEL DENNIS DOWLE
分类号 A61K31/40;A61P9/00;A61P9/10;A61P9/12;C07D209/10;C07D209/26;C07D209/30;C07D403/06;C07D403/14;C07D521/00 主分类号 A61K31/40
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