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    • 5. 发明申请
    • SUBSTITUTED N-SULFONYLAMINOPHENYLETHYL-2-PHENOXY ACETAMIDE COMPOUNDS
    • 取代的N-磺酰氨基苯乙烯基-2-苯氧基乙酰胺化合物
    • WO2006095263A8
    • 2007-11-08
    • PCT/IB2006000539
    • 2006-02-24
    • PFIZER JAPAN INCPFIZERHANAZAWA TAKESHIHIRANO MISATOINOUE TADASHINAGAYAMA SATOSHINAKAO KAZUNARISHISHIDO YUJITANAKA HIROTAKA
    • HANAZAWA TAKESHIHIRANO MISATOINOUE TADASHINAGAYAMA SATOSHINAKAO KAZUNARISHISHIDO YUJITANAKA HIROTAKA
    • C07D295/08A61K31/18A61K31/353A61K31/4453A61P25/00C07C311/08C07D311/58
    • C07C311/08
    • This invention provides a compound of the formula (I), wherein R 1 represents (C 1 -C 6 )alkyl; R 2 represents a hydrogen atom, a halogen atom, a hydroxy group, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkyl; R 3 represents a halogen atom, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkoxy-(C 1 ­-C 6 )alkyll, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl, (C 1 -C 6 )alkylthio, (C 1 -C 6 )alkylsulfinyl, (C 1 ­C 6 )alkyllsulfonyl, [(C 1 -C 6 )alkyl]NH-, or [(C 1 -C 6 ) alkyl] 2 N-; R 4 represents a halogen atom, (C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkoxy, (C 1­ -C 6 )alkoxy-(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkoxy, [(C 1 -C 6 )alkyl]NH-, or [(C 1 -C 6 )alkyl] 2 N-; R 5 represents a halogen atom, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkoxy-(C 1 ­-C 6 )alkyll, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl, (C 1 -C 6 )alkylthio, (C 1 -C 6 )alkylsulfinyl, (C 1 -­C 6 )alkyIsulfonyl, [(C 1 -C 6 )alkyl]NH-, [(C 1 -C 6 ) alkyl] 2 N-, H 2 N-(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkyl-NH-(C 1 -C 6 )alkoxy, [(C 1 -C 6 )alkyl] 2 N(C 1 -C 6 )alkoxy, H 2 N-(C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, (C 1 -C 6 )alkyl-NH-(C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, or [(C 1 -C 6 )alkyl] 2 N(C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl; and *indicates a chiral centre; or a pharmaceutically acceptable salt or solvate thereof. These compounds are useful for the treatment of disease conditions caused by overactivation of VR1 receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.
    • 本发明提供式(I)化合物,其中R 1表示(C 1 -C 6 -C 6)烷基; R 2表示氢原子,卤素原子,羟基,(C 1 -C 6 -C 6)烷基,(C 1 -C 6) (C 1 -C 6)烷基,(C 1 -C 6)烷基,(C 1 -C 6)烷基,(C 1 -C 6) C 1 -C 6烷氧基 - (C 1 -C 6 -C 6)烷基或卤代(C 1 -C 6 - ç 6 )烷基; R 3表示卤素原子,(C 1 -C 6 -C 6)烷基,(C 1 -C 6 - (C 1 -C 6)烷氧基,(C 1 -C 6)烷氧基,(C 1 -C 6)烷氧基, (C 1 -C 6)烷基,(C 1 -C 6)烷基,(C 1 -C 6)烷基, )烷氧基 - (C 1 -C 6 -C 6)烷氧基,卤素(C 1 -C 6 -C 6)烷基, (C 1 -C 6 -C 6)烷硫基,(C 1 -C 6 -C 6)烷基亚磺酰基,(C 2 N-; R 5表示卤素原子,(C 1 -C 6 -C 6)烷基,(C 1 -C 6 - (C 1 -C 6)烷氧基,(C 1 -C 6)烷氧基,(C 1 -C 6)烷氧基, (C 1 -C 6)烷基,(C 1 -C 6)烷基,(C 1 -C 6)烷基, )烷氧基 - (C 1 -C 6 -C 6)烷氧基,卤素(C 1 -C 6 -C 6)烷基, (C 1 -C 6 -C 6)烷硫基,(C 1 -C 6 -C 6)烷基亚磺酰基,(C C 6 -C 6烷基) C 1 -C 6烷基] N 2 - , - N - (C 1 -C 6) C 1 -C 6烷氧基,(C 1 -C 6 -C 6)烷基-NH-(C 1 -C 6) -C 6 -C 6烷氧基,[(C 1 -C 6 -C 6)烷基] N 2 N(C < C 1 -C 6 -C 6烷氧基,H 2 N - (C 1 -C 6) )烷氧基 - (C 1 -C 6 -C 6)烷基,(C 1 -C 6 -C 6)烷基-NH - (C 1 -C 6 -C 6)烷氧基 - (C 1 -C 6 -C 6)烷基或[( ç 1 -C 6 )烷基] 2 N(ç 1 -C 6 )烷氧基 - (C 1 < / SUB> -C 6 )烷基; 和*表示手性中心; 或其药学上可接受的盐或溶剂合物。 这些化合物可用于治疗由哺乳动物中VR1受体过度活化引起的疼痛等疼痛引起的疾病状况。 本发明还提供了包含上述化合物的药物组合物。