Muscarinic receptor antagonists

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 471/08 (2006.01) A61K 31/435 (2006.01) C07D 209/52 (2006.01) C07D 405/06 (2006.01) C07D 451/02 (2006.01) C07D 453/06 (2006.01) C07D 471/18 (2006.01)

Patent

CA 2068527

Muscarinic receptor antagonists, useful especially in the treatment of irritable bowel syndrome, of formula (IA) or (IB) or a pharmaceutically acceptable salt thereof, where R2 and R3 are each independently H,halo or C1-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 R1 is a group of formula (a), (b) or Het1, where R4 and R5 are each independently H, C1-C4 alkyl, C1-C4 alkoxy, -(CH2)tOH, halo, trifluoromethyl, cyano, -(CH2)tNR6R7, -CO(C1-C4 alkyl), -OCO(C1-C4 alkyl), CH(OH)(C1-C4 alkyl), -C(OH)(C1-C4 alkyl)2, -SO2NH2, -(CH2)tCONR6R7 or -(CH2)tCOO(C1-C4 alkyl); R6 and R7 are each independently H or C1-C4 alkyl; t is 0, 1 or 2; X and X1 are each independently O or CH2; s is 1, 2 or 3; and Het1 is pyridyl, pyrazinyl or thienyl.

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