C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 235/26 (2006.01) A61K 31/404 (2006.01) A61K 31/416 (2006.01) A61K 31/4184 (2006.01) A61K 31/4192 (2006.01) A61K 31/423 (2006.01) A61K 31/428 (2006.01) A61P 29/00 (2006.01) C07D 209/34 (2006.01) C07D 231/56 (2006.01) C07D 235/06 (2006.01) C07D 249/18 (2006.01) C07D 263/58 (2006.01) C07D 277/62 (2006.01)
Patent
CA 2610354
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.
L'invention concerne un composé de la formule (I) dans laquelle A=B=Dreprésente 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 ou N=CR9-S; X1 représente CR1 ou N; X2 et X3 représentent chacun indépendamment CR8 ou N; R1, R6, R8, R9 et R10 représentent chacun indépendamment hydrogène, halogène, hydroxy, (C1-C6)alkyle, (C1,-C6)alcoxy, hydroxy(C1-C6)alcoxy, (C1-C6)alcoxy-(C1-C6)alkyle, (C1-C6)alcoxy-(C1-C6)alcoxy, halo(C1-C6)alkyle, (C1-C6)alkylthio, (C1-C6)alkylsulfinyle ou (C1-C6)alkylsulfonyle; R2, R3, R4, et R5 représentent chacun indépendamment hydrogène, (C1-C6)alkyle, halogène, halo(C1-C6) alkyle, ou hydroxy(C1-C6)alkyle; et R7 représente halogène, (C1-C6)alkyle, halo(C1-C6)alkyle, (C1-C6)alcoxy, hydroxy(C1-C6)alcoxy, (C1-C6)alcoxy-(C1-C6)alkyle, (C1-C6)alcoxy-(C1-C6)alcoxy, [(C1-C6)alkyle]NH- ou [(C1-C6)alkyle]2N-; ou un sel de celui-ci pharmaceutiquement acceptable, pour autant que: (i) lorsque A=B=D représente NR10-N=N ou N=N-NR10, alors R2 représente (C1-C6)alkyle, halogène, halo(C1-C6) alkyle ou hydroxy(C1-C6)alkyle; ou (ii) lorsque A=B=D représente NR10-N=N ou N=N-NR10, et R2 (C1-C6)alkyle, alors R7 représente halogène, (C1-C6)alkyle, (C1-C6)aIcoxy, hydroxy(C1-C6)alcoxy, (C1-C6)alcoxy-(C1-C6)alkyle, (C1-C6)alcoxy(C1-C6)alcoxy, [(C1-C6)alkyle]NH- ou [(C1-C6)alkyle]2N-. Ces composés sont utilisés dans le traitement d'états pathologiques provoqués par une suractivation du récepteur VR1 tel que la douleur, ou analogue chez les mammifères. L'invention concerne également une composition pharmaceutique renfermant le composé précité.
Inoue Tadashi
Kawashima Tadashi
Nagayama Satoshi
Shishido Yuji
Pfizer Inc.
Torys Llp
LandOfFree
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