发明名称 SUBSTITUTED ARYLOXY-N-BICYCLOMETHYL ACETAMIDE COMPOUNDS AS VR1 ANTAGONISTS
摘要 This invention provides a compound of the formula (I): whereinA=B=D represents NR10-C(O)-NR9, S-C(O)-NR9, NR9-C(O)-S, NR9-C(O)-O, CR10-C(O)-NR9, 0-C(O)-NR9, NR10-C(O)-CR9, NR10-NR9-C(O), C(O)-NR9-NR10, NR10-N=CR9, N=N-CR9, NR10-CR9=N, N=CR9-NR10, NR10-N=N, N=N-NR10, S-CR9=N or N=CR9-S; X1 represents CR1 or N; X2 and X3 each independently represents CR8 or N; R1, R6, R8, R9 and R10 each independently represents hydrogen, halogen, hydroxy, (C1-C6)alkyl, (C1,- C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1- C6)aikoxy, halo(C1-C6)alkyl, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl or (C1- C6)alkylsulfonyl; R2, R3, R4, and R5 each independently represents hydrogen, (C1-C6)alkyl, halogen, halo(C1-C6) alkyl, or hydroxy(C1-C6)alkyl; and R7 represents halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1- C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, [(C1- C6)alkyl]NH- or [(C1-C6)alkyl]2N-; or a pharmaceutically acceptable salt thereof, provided that: (i) when A=B=D represents NR10-N=N or N=N-NR10, then R2 represents (C1-C6)alkyl, halogen, halo(C1-C6) alkyl or hydroxy(C1-C6)alkyl; or (ii) when A=B=D represents NR10-N=N or N=N-NR10, and R2 represents (C1- C6)alkyl, then R7 represents halogen, (C1-C6)alkyl, (C1-C6)aIkOXy, hydroxy(C1- C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy(C1-C6)alkoxy, [(C1- C6)alkyl]NH- or [(C1-C6)alkyl]2N-. 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.
申请公布号 CA2610354(A1) 申请公布日期 2006.12.07
申请号 CA20062610354 申请日期 2006.05.22
申请人 PFIZER LIMITED 发明人 NAGAYAMA, SATOSHI;SHISHIDO, YUJI;KAWASHIMA, TADASHI;INOUE, TADASHI
分类号 C07D235/26;A61K31/404;A61K31/416;A61K31/4184;A61K31/4192;A61K31/423;A61K31/428;A61P29/00;C07D209/34;C07D231/56;C07D235/06;C07D249/18;C07D263/58;C07D277/62 主分类号 C07D235/26
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