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    • 6. 发明申请
    • SUBSTITUTED N-SULFONYLAMINOBENZYL-2-PHENOXY ACETAMIDE COMPOUNDS
    • 取代的N-磺酰基苯甲酰基-2-苯氧基乙酸酯化合物
    • WO2006051378A1
    • 2006-05-18
    • PCT/IB2005/003321
    • 2005-10-31
    • PFIZER JAPAN INC.PFIZER INC.INOUE, TadashiNAGAYAMA, SatoshiNAKAO, Kazunari
    • INOUE, TadashiNAGAYAMA, SatoshiNAKAO, Kazunari
    • C07D295/08C07D311/58C07C311/08A61K31/4453A61K31/353A61K31/18A61P25/00
    • C07D295/096C07C311/08C07C2601/02C07C2602/08C07C2602/10C07D311/58
    • This invention provides a compound of the formula (I): wherein R 1 represents a (C 1 ,-C 6 )alkyl group; R 2 represents a hydrogen atom, a halogen atom, a hydroxy group, a (C 1 -C 6 ) alkyl group or a (C 1 -C 6 ) alkoxy group; R 3 , R 4 , R 5 and R 6 each independently represents a hydrogen atom, a (C 1 -C 6 ) alkyl, or a halogen atom; R 7 represents a hydrogen atom, a halogen atom, a hydroxy group, a (C 1 -C 6 ) alkyl group optionally substituted with a piperidino group, a (C 1 -C 6 )alkoxy group optionally substituted with a 3-7 membered cycloalkyl ring, a hydroxy(C 1 -C 6 )alkoxy group, a (C 1 -C 8 )alkoxy- (C 1 -C 8 )alkyl group, a (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkoxy group, a halo (C 1 -C 6 )alkyl group, a (C 1 -C 6 )alkylthio group, a (C 1 -C 6 )alkylsulfinyl group or a (C 1 -C 6 )alkylsulfonyl group; R 8 represents a (C 1 -C 6 )alkyl group, a halo(C 1 -C 6 ,)aIkyl group, a (C 1 -C 6 )alkoxy group, a hydroxy(C 1 -C 6 )alkoxy group, a (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl group or a (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkoxy group; or R 7 and R 8 , when adjacent to each other, taken together with the carbon atoms to which they are attached form a 5-8 membered carbocyclic or heterocyclic ring, wherein the carbocyclic ring or the heterocyclic ring is unsubstituted or substituted with one or more substituents selected from the group consisting of a hydroxy group, a (C 1 -C 6 )alkyl group, a (C 1 -C 6 )alkoxy group and a hydroxy(C 1 -C 6 )alkyl group; and R 9 represents a hydrogen atom or a halogen atom; 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 as pain or the like in mammalian. The present invention also provides a pharmaceutical composition comprising the compound of formula (I).
    • 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)烷基或(C 1 -C 6 -C 6)烷基 C 1 -C 6烷氧基; R 3,R 4,R 5和R 6各自独立地表示氢原子,(C 1〜 或者卤素原子; R 7表示氢原子,卤素原子,羟基,(C 1 -C 6 -C 6)烷基,任选被 哌啶子基,任选被3-7元环烷基环取代的(C 1 -C 6 -C 6)烷氧基,羟基(C 1 -C 6 - -C(C 1 -C 6)烷氧基,(C 1 -C 8 - )烷氧基 - (C 1 -C 6 - (C 1 -C 6)烷基,(C 1 -C 6 -C 6)烷氧基 - (C 1 -C 6 - 亚烷基) (C 1 -C 6)烷氧基,卤代(C 1 -C 6 -C 6)烷基,(C 1 -C 6)烷氧基, (C 1 -C 6)烷硫基,(C 1 -C 6)烷基亚磺酰基或(C 1 -C 6 - 烷基磺酰基; R 8表示(C 1 -C 6 -C 6)烷基,卤代(C 1 -C 6 - (C 1 -C 6)烷基,(C 1 -C 6 -C 6)烷氧基,羟基(C 1 -C 6 - C 1 -C 6烷氧基,(C 1 -C 6 -C 6)烷氧基 - (C 1 -C 6 - (C 1 -C 6)烷基或(C 1 -C 6 -C 6)烷氧基 - (C 1 -C 6 - 6个)烷氧基; 或R 7和R 8彼此相邻时,与它们所连接的碳原子一起形成5-8元碳环或杂环,其中 碳环或杂环是未取代的或被一个或多个选自羟基,(C 1 -C 6 -C 6)烷基的取代基取代 ,(C 1 -C 6 -C 6)烷氧基和羟基(C 1 -C 6 -C 6)烷基 组; R 9表示氢原子或卤素原子; 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VR1受体过度活化引起的疾病状况,例如哺乳动物的疼痛等。 本发明还提供包含式(I)化合物的药物组合物。
    • 8. 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
    • WO2006095263A1
    • 2006-09-14
    • PCT/IB2006/000539
    • 2006-02-24
    • PFIZER JAPAN INC.PFIZER INC.HANAZAWA, TakeshiHIRANO, MisatoINOUE, TadashiNAHAYAMA, SatoshiNAKAO, KazunariSHISHIDO, YujiTANAKA, Hirotaka
    • HANAZAWA, TakeshiHIRANO, MisatoINOUE, TadashiNAHAYAMA, SatoshiNAKAO, KazunariSHISHIDO, YujiTANAKA, Hirotaka
    • C07D295/08C07D311/58C07C311/08A61K31/4453A61K31/353A61K31/18A61P25/00
    • 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代表(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 - (C 1 -C 6)烷基,(C 1 -C 6)烷氧基 - (C 1 -C 6 - )烷基,(C 1 -C 6) )烷氧基 - (C 1 -C 6 -C 6)烷氧基,卤代(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 - (C 1 -C 6)烷基,(C 1 -C 6)烷氧基 - (C 1 -C 6 - )烷基,(C 1 -C 6) )烷氧基 - (C 1 -C 6 -C 6)烷氧基,卤代(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 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。