Diphenylsulphoximine muscarinic receptor antagonists

C - Chemistry – Metallurgy – 07 – D

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C07D 211/56 (2006.01) A61K 31/135 (2006.01) A61K 31/40 (2006.01) A61K 31/445 (2006.01) C07C 381/10 (2006.01) C07D 207/09 (2006.01) C07D 207/14 (2006.01) C07D 211/28 (2006.01) C07D 213/53 (2006.01) C07D 241/12 (2006.01) C07D 333/22 (2006.01) C07D 401/02 (2006.01) C07D 405/06 (2006.01) C07D 409/02 (2006.01)

Patent

CA 2072127

2072127 9110648 PCTABS00006 Compounds of formula (I), wherein R and R1 are H or C1-C4 alkyl; and X is a group of formulae (II) or (III), wherein either R2 is H or C1-C4 alkyl and R3 is C1-C4 alkyl, or R2 and R3 represent -(CH2)r- wherein r is from 2 to 5; R4 is C1-C4 alkyl; X1 is a direct link, O or S; R5 is mono or disubstituted phenyl wherein the substituents are H, halo, C1-C4 alkyl, C1-C4 alkoxy, -(CH2)sOH, -(CH2)sNR8R9, -CONR10R11, -SO2NH2 or -OCO(C1-C4 alkyl), or adjacent substituents may form a fused ring; or R5 is thienyl, pyridinyl or pyrazinyl; R8 and R9 are H or C1-C4 alkyl, or R8 is hydrogen and R9 is -SO2(C1-C4 alkyl), -CONR10R11, -CO(C1-C4 alkyl) or -SO2NH2; R10 and R11 are hydrogen or C1-C4 alkyl; m is 1, 2 or 3; n is 0, 1 or 2; p is 0 or 1; and s is 0, 1 or 2, (with certain provisos); are gastrointestinal and bladder selective muscarinic receptor antagonists of utility for example in irritable bowel syndrome.

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