abstract |
Muscarinic receptor antagonists, useful especially in the treatment of irritable bowel syndrome, of formula (IA) or (IB) or a pharmaceutically acceptable salt thereof, where R?2 and R3¿ are each independently H, halo or C¿1?-C4 alkyl; m is 0, 1 or 2; n is 1, 2 or 3; Y is a direct link, O or S; with the proviso that when n is 1, Y is a direct link; Het is a group of formula (A) or (B), where p is 0, 1 or 2, q is 1, 2 or 3, and r is 0, 1, 2 or 3, with the proviso that the sum of p, q and r is at least 3, the N atom of 'Het' being attached to the group (CH2)n in formula (IA) and to the H atom in formula (IB); and R?1¿ is a group of formula (a), (b) or Het1, where R?4 and R5¿ are each independently H, C¿1?-C4 alkyl, C1-C4 alkoxy, -(CH2)tOH, halo, trifluoromethyl, cyano, -(CH2)tNR?6R7¿, -CO(C¿1?-C4 alkyl), -OCO(C1-C4 alkyl), CH(OH)(C1-C4 alkyl), -C(OH)(C1-C4 alkyl)2, -SO2NH2, -(CH2)tCONR?6R7¿ or -(CH¿2?)tCOO(C1-C4 alkyl); R?6 and R7¿ are each independently H or C¿1?-C4 alkyl; t is 0, 1 or 2; X and X?1¿ are each independently O or CH¿2?; s is 1, 2 or 3; and Het?1¿ is pyridyl, pyrazinyl or thienyl. |