A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/416 (2006.01) A61K 31/343 (2006.01) A61K 31/404 (2006.01) A61K 31/4245 (2006.01) A61K 31/428 (2006.01) A61K 31/437 (2006.01) C07C 275/28 (2006.01) C07D 209/08 (2006.01) C07D 209/34 (2006.01) C07D 231/56 (2006.01) C07D 263/56 (2006.01) C07D 275/04 (2006.01) C07D 277/62 (2006.01) C07D 307/79 (2006.01) C07D 471/04 (2006.01)
Patent
CA 2538454
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;. R 1 is halogen, hydroxy, C 1-6 álkyl, haloC 1-6 alkyl, hydroxyC 1-6 alkyl, C 1-6 alkoxy, halo C 1-6 alkoxy, hydroxyC 1-6 alkoxy, C 3-7 cycloalkyl, C 3-5 cycloalkylC 1-4 alkyl, NR7R8, C 1-6 alkyl substituted with NR7R8, C, 1-6 alkoxy substituted with NR7R8, oxo, cyano, SO2NR7R8, CONR7R8, NHCOR9 or NHSO2R 9 ; R2 is halogen, hydroxy, C 1-6 alkyl, halo C 1-6 alkyl, hydroxyC 1-6 alkyl, C 1-6 alkoxy, halo C 1-6 alkoxy, hydroxyC 1-6 alkoxy, C 3-7 cycloalkyl, C 3-5 cycloalkylC 1-4 alkyl, NR7R8, C 1- 6 alkyl substituted with NR7R8, C1-6 , alkoxy substituted with NR7R8, cyano, SON2R7R8, CONR7R8, NHCOR9 , or NHSO2R9; R3and R 4 are each independently hydrogen, C 1-6 ,alkyl, phenyl or halophenyl; R5 and R 6 are, at each occurrence, independently hydrogen, C 1-6 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).
Les composés de la formule (I) sont utiles en tant que composés thérapeutiques, en particulier dans le traitement de la douleur et d'autres états pouvant être améliorées par la modulation de la fonction du récepteur vanilloïde-1 (VR1).
Fletcher Stephen Robert
Hollingworth Gregory John
Jones A. Brian
Moyes Christopher Richard
Rogers Lauren
Merck Sharp & Dohme Limited
Ogilvy Renault Llp/s.e.n.c.r.l.,s.r.l.
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