Muscarinic receptor antagonists

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 211/34 (2006.01) A61K 31/445 (2006.01) C07D 405/06 (2006.01) C07D 405/10 (2006.01)

Patent

CA 1328454

Abstract "Muscarinic Receptor Antagonists" A compound or the formula:- Image --- (I) or a pharmaceutically acceptable salt thereof, wherein Y is a direct link, -CH2-, -(CH2)2-, -CH2O- or -CH2S-; R is -CN or -CONH2; and R1 is a group of the formula:- Image , Image or Het where R2 and R3 are each independently H, C1-C4 alkyl, C1-C4 alkoxy, -(CH2)nOH, halo, trifluoromethyl, cyano, -(CH2)nNR4R5, -CO(C1-C4 alkyl), -OCO(C1-C4 alkyl), -CH(OH)(C1-C4 alkyl), -C(OH)(C1-C4 alkyl)2, -SO2NH2, -(CH2)nCONR4R5 or -(CH2)nCOO(C1-C4 alkyl); R4 and R5 are each independently H or C1-C4 alkyl; n is 0, 1 or 2; X and X1 are each independently O or CH2; m is 1, 2 or 3; and "Het" is pyridyl, pyrazinyl or thienyl. The compounds are muscarinic receptor antagonists useful in the treatment of diseases associated with the altered motility and/or tone of smooth muscle, especially irritable bowel syndrome.

615036

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