Patent ID: 8288376
Filing Date: 2012-10-16
Classification: A61P,C07D

Abstract:
1. A method of modulating the activity of TRPV1 receptors comprising administering to a patient a modulatory amount of a compound of formula (I): or pharmaceutically acceptable salt thereof in which: A is, with the C—N bond of the benzimidazole unit with which it is fused, a 4- to 7-membered monocyclic heterocycle or monocyclic heteroaryl, containing from one to three heteroatoms selected from O, S and N, including the nitrogen atom of the benzimidazole unit; P is an 8-, 9-, 10- or 11-membered bicyclic heterocycle or bicyclic heteroaryl, containing from 1 to 6 heteroatoms selected from N, O and S; P being linked to the -C(Y)- group by a carbon atom; with the proviso that, when A is a 7-membered saturated heterocycle, P is other than 2,3-dihydro-1,4-benzodioxane, the 1-benzopyran-2-one or isoindole; R1 is substituted on P one to four times and each R1 may be identical or different, R1 being selected from hydrogen, halogen, oxo, thio, C said heteroaryl or aryl of R1 being optionally substituted with one or more substituents R with the proviso that, when R1 is attached to a nitrogen atom of P, then R1 is not halogen, oxo, thio, cyano, nitro, SF Y is an oxygen or sulphur atom; R2 is hydrogen, halogen, C R3 is substituted on a carbon atom of A, each R3 may be substituted 1 to 3 times on a carbon atom of A, each R3 substituted on a carbon atom of A may be identical or different, said R3 substituted on a carbon atom of A being selected from hydrogen, halogen, C or R3 is substituted on a nitrogen atom of A, each R3 may be substituted once or twice on a nitrogen atom of A and may be identical or different, said R3 substituted on a nitrogen atom of A being selected from hydrogen, halogen, C R or R R or R R or R R the sulphur atom(s) of the heterocycle A may be in oxidized form (S(O) or S(O) the nitrogen atom(s) may be in oxidized form (N-oxide); and with the proviso that 2-(2-chlorophenyl)-1,3-dioxo-N-(7,8,9,10-tetrahydro-6H-azepino[1,2-a]benzimidazol-3-yl)isoindoline-5-carboxamide is excluded.