发明授权
US06169097A 1-(1,2-Disubstituted piperidinyl)-4-substituted piperidine derivatives
失效
1-(1,2-二取代哌啶基)-4-取代的哌啶衍生物
- 专利标题: 1-(1,2-Disubstituted piperidinyl)-4-substituted piperidine derivatives
- 专利标题(中): 1-(1,2-二取代哌啶基)-4-取代的哌啶衍生物
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申请号: US09102295申请日: 1998-06-22
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公开(公告)号: US06169097A公开(公告)日: 2001-01-02
- 发明人: Frans Eduard Janssens , François Maria Sommen , Dominique Louis Nestor Ghislaine Surleraux , Yves Emiel Maria Van Roosbroeck
- 申请人: Frans Eduard Janssens , François Maria Sommen , Dominique Louis Nestor Ghislaine Surleraux , Yves Emiel Maria Van Roosbroeck
- 优先权: EP9520365 19951227
- 主分类号: A61K31445
- IPC分类号: A61K31445
摘要:
The present invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; p is 0, 1 or 2; ═Q is ═O or ═NR3; X is a covalent bond or a bivalent radical of formula —O—, —S—, —NR3—; R1 is Ar1; Ar1C1-6alkyl or di(Ar1)C1-6alkyl, wherein each C1-6alkyl group is optionally substituted with hydroxy, C1-4alkyloxy, oxo or a ketalized oxo substituent of formula —O—CH2—CH2—O— or —O—CH2—CH2—CH2—O—; R2 is Ar2; Ar2C1-6alkyl; Het or HetC1-6alkyl; R3 is hydrogen or C1-6alkyl; R4 is hydrogen; C1-4alkyl; C1-4aklyloxyC1-4alkyl; hydroxyC1-4alkyl; carboxyl; C1-4aklyloxycarbonyl or Ar3; R5 is hydrogen; hydroxy; Ar3; Ar3C1-6alkyloxy; di(Ar3)C1-6alkyloxy; Ar3C1-6alkylthio; di(Ar3)C1-6alkylthio; Ar3C1-6alkylsulfoxy; di(Ar3)C1-6alkylsulfoxy; Ar3C1-6alkylsulfonyl; di(Ar3)C1-6alkylsulfonyl; —NR7R8; C1-6alkyl substituted with —NR7R8; or a radical of formula (a-1) or (a-2); R4 and R5 may also be taken together; R6 is hydrogen; hydroxy; C1-6alkyloxy; C1-6alkyl or Ar3C1-6alkyl; Ar1, Ar2 and Ar3 are phenyl or substituted phenyl; Ar2 is also naphtalenyl; and Het is an optionally substituted monocyclic or bicyclic heterocycle; as substance P antagonists; their preparation, compositions containing them and their use as a medicine.
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