Piperidine compounds for use as ccr-3 inhibitors
    4.
    发明授权
    Piperidine compounds for use as ccr-3 inhibitors 失效
    用作ccr-3抑制剂的哌啶化合物

    公开(公告)号:US06670379B2

    公开(公告)日:2003-12-30

    申请号:US10332642

    申请日:2003-04-17

    IPC分类号: A61F31445

    摘要: Compounds of formula (I) in free or salt form, where Ar1 is phenyl substituted by one or more halogen atoms, Ar2 is phenyl or naphthyl which is unsubstituted or substituted by one or more substituents selected from halogen, cyano, hydroxy, nitro, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy or C1-C8-alkoxycarbonyl, R1 is hydrogen or C1-C8-alkyl optionally substituted by hydroxy, C1-C8-alkoxy, acyloxy, N(R2)R3, halogen, carboxy, C1-C8-alkoxycarbonyl, —CON(R4)R5 or by a monovalent cyclic organic group, R2 and R3 are each independently hydrogen or C1-C8-alkyl, or R2 is hydrogen and R3 is acyl or —SO2R6, or R2 and R3 together with the nitrogen atom to which they are attached denote a 5 or 6-membered heterocyclic group, R4 and R5 are each independently hydrogen or C1-C8-alkyl, or R4 and R5 together with the nitrogen atom to which they are attached denote a 5 or 6-membered heterocyclic group, R6 is C1-C8-alkyl, C1-C8-haloalkyl, or phenyl optionally substituted by C1-C8-alkyl, and n is 1, 2, 3, or 4, with the proviso that when Ar1 is p-chlorophenyl and R1 is hydrogen, R2 is not phenyl or p-nitrophenyl. The compounds are useful as pharmaceuticals.

    摘要翻译: 游离或盐形式的式(I)化合物,其中Ar 1是被一个或多个卤素原子取代的苯基,Ar 2是未取代的或被一个或多个选自卤素,氰基的取代基取代的苯基或萘基 ,羟基,硝基,C 1 -C 8 - 烷基,C 1 -C 8 - 卤代烷基,C 1 -C 8 - 烷氧基或C 1 -C 8 - 烷氧基羰基,R 1是氢或任选被羟基取代的C 1 -C 8烷基, 烷氧基,酰氧基,N(R 2)R 3,卤素,羧基,C 1 -C 8 - 烷氧基羰基,-CON(R 4)R 5或一价环状有机基团R 2 和R 3各自独立地为氢或C 1 -C 8烷基,或R 2为氢,R 3为酰基或-SO 2 R 6,或R 2和R 3与 它们所连接的氮原子表示5或6元杂环基团,R 4和R 5各自独立地为氢或C 1 -C 8 - 烷基,或R 4和R 5与 它们所连接的氮原子表示5或6元杂环基,R 6是C 1 -C 8 - 烷基,C 1 -C 8 - 卤代烷基或任选取代的苯基 由C 1 -C 8烷基构成,n为1,2,3或4,条件是当Ar 1为对氯苯基且R 1为氢时,R 2不为苯基或p - 硝基苯基。 这些化合物可用作药物。