C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 311/46 (2006.01) A61K 31/18 (2006.01)
Patent
CA 2600409
This invention provides a compound of the formula (I), wherein R1 represents (C1-C6)alkyl; R2 represents a hydrogen atom, a halogen atom, a hydroxy group, (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkyl or halo(C1-C6)alkyl; R3 represents a halogen atom, (C1-C6)alkyl, (C1- C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1~-C6)alkyll, (C1-C6)alkoxy- (C1-C6)alkoxy, halo(C1-C6)alkyl, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl, (C1~C6)alkyllsulfonyl, [(C1-C6)alkyl]NH-, or [(C1-C6) alkyl]2N-; R4 represents a halogen atom, (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-; R5 represents a halogen atom, (C1- C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1~-C6)alkyll, (C1-C6)alkoxy-(C1-C6)alkoxy, halo(C1-C6)alkyl, (C1-C6)alkylthio, (C1- C6)alkylsulfinyl, (C1-~C6)alkyIsulfonyl, [(C1-C6)alkyl]NH-, [(C1-C6) alkyl]2N- , H2N-(C1-C6)alkoxy, (C1-C6)alkyl-NH-(C1-C6)alkoxy, [(C1-C6)alkyl]2N(C1- C6)alkoxy, H2N-(C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkyl-NH-(C1-C6)alkoxy-(C1- C6)alkyl, or [(C1-C6)alkyl]2N(C1-C6)alkoxy-(C1-C6)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.
La présente invention a trait à un composés de formule (I), dans laquelle R1 représente (C1-C6)alkyle; R2 représente un atome d'hydrogène, un atome d'halogène, un groupe hydroxy, (C1-C6)alkyle, (C1-C6)alcoxy, hydroxy(C1-C6)alkyle, (C1-C6)alcoxy-(C1-C6)alkyle ou halo(C1-C6)alkyle; R3 représente un atome d'halogène, (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, (C1-C6)alkylsulfonyle, [(C1-C6)alkyl]NH-, ou [(C1-C6) alkyl]2N-; R4 représente un atome d'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)alkyl]NH-, ou [(C1-C6)alkyl]2N-; R5 représente un atome d'halogène, (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, (C1-C6)alkyIsulfonyle, [(C1-C6)alkyl]NH-, [(C1-C6) alkyl]2N-, H2N-(C1-C6)alcoxy, (C1-C6)alkyl-NH-(C1-C6)alcoxy, [(C1-C6)alkyl]2N(C1-C6)alcoxy, H2N-(C1-C6)alcoxy-(C1-C6)alkyle, (C1-C6)alkyl-NH-(C1-C6)alcoxy-(C1-C6)alkyle, ou [(C1-C6)alkyl]2N(C1-C6)alcoxy-(C1-C6)alkyle; ou un sel ou solvate pharmaceutiquement acceptable de ceux-ci. Ces composés sont utiles pour le traitement de conditions morbides provoquées par une activation excessive du récepteur VR1 telles que la douleur ou analogue chez des mammifères. L'invention a également trait à une composition pharmaceutique comportant ledit composé.
Hanazawa Takeshi
Hirano Misato
Inoue Tadashi
Nahayama Satoshi
Nakao Kazunari
Pfizer Inc.
Torys Llp
LandOfFree
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