- 专利标题: Derivatives of n-(1h-indazolyl)-and n-(1h-indolyl)-urea as well as related compounds as modulators of the vanilloid-1 receptor (vr1) for treatment of pain
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申请号: US10571544申请日: 2004-09-16
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公开(公告)号: US20070078156A1公开(公告)日: 2007-04-05
- 发明人: Stephen Fletcher , Gregory Hollingworth , Brian Jones , Richard Moyes , Lauren Rogers
- 申请人: Stephen Fletcher , Gregory Hollingworth , Brian Jones , Richard Moyes , Lauren Rogers
- 优先权: GB0322016.7 20030919
- 国际申请: PCT/GB04/03968 WO 20040916
- 主分类号: A61K31/4745
- IPC分类号: A61K31/4745 ; C07D498/04 ; C07D491/04 ; C07D471/02
摘要:
Compounds of formula (I): wherein A, B and D are each C, N, O or S; E is C or N; the dotted circle within the five-membered ring indicates that the ring may be unsaturated or partially saturated; R1 is halogen, hydroxy, C1-6 alkyl, haloC1-6 alkyl, hydroxyC1-6 alkyl, C1-6 alkoxy, halo C1-6 alkoxy, hydroxyC1-6 alkoxy, C3-7 cycloalkyl, C3-5 cycloalkylC1-4 alkyl, NR7R8, C1-6 alkyl substituted with NR7R8, C,1-6 alkoxy substituted with NR7R8, oxo, cyano, SO2NR7R8, CONR7R8, NHCOR9 or NHSO2R9; R2 is halogen, hydroxy, C1-6 alkyl, halo C1-6 alkyl, hydroxyC1-6 alkyl, C1-6 alkoxy, halo C1-6 alkoxy, hydroxyC1-6 alkoxy, C 3-7 cycloalkyl, C3-5 cycloalkylC1-4 alkyl, NR7R8, C1-6 alkyl substituted with NR7R8, C1-6, alkoxy substituted with NR7R8, cyano, SON2R7R8, CONR7R8, NHCOR9, or NHSO2R9; R3 and R4 are each independently hydrogen, C1-6, alkyl, phenyl or halophenyl; R5 and R6 are, at each occurrence, independently hydrogen, C1-6 alkyl, phenyl, halophenyl or carboxy; X is an oxygen or sulfur atom; Y is an aryl, heteroaryl, carbocyclyl or fused-carbocyclyl group; n is either zero or an integer from 1 to 3; p is either zero or an integer from, 1 to 4; and q is either zero or an integer from 1 to 3; the other substituents are defined in claim 1; are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).
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