Muscarinic receptor antagonists

Details Muscarinic receptor antagonists Muscarinic receptor antagonists

1995-04-24

1999-08-03

Chang, Ceila

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514252, 514318, 514326, 514331, 544238, 546193, 546213, 546230, 546239, A61K 31445, C07D21134

Patent

active

059325941

ABSTRACT:
A compound of the formula: or a pharmaceutically acceptable salt thereof,
wherein Y is a direct link, --(CH.sub.2 --, --(CH.sub.2).sub.2 --, --CH.sub.2 O-- or CH.sub.2 S--; R is --CN or --CONH.sub.2 ;
and R.sup.1 is a group of the formula: ##STR1## where R.sup.2 and R.sup.3 are each independently H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, --(CH.sub.2).sub.n OH, halo, trifluoromethyl, cyano, --(CH.sub.2).sub.n NR.sup.4 R.sup.5, --CO(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.4 alkyl), --CH(OH) (C.sub.1 -C.sub.4 alkyl), --C(OH) (C.sub.1 -C.sub.4 alkyl).sub.2, --SO.sub.2 NH.sub.2, --(CH.sub.2).sub.n CONR.sup.4 R.sup.5 or --(CH.sub.2).sub.n COO(C.sub.1 -C.sub.4 alkyl; R.sub.4 and R.sup.5 are each independently H or C.sub.1 -C.sub.4 alkyl; n is 0, 1 or 2;
and "Het" is pyridyl, pyrazinyl or thienyl.
The compounds are muscarinic receptor antagonists usedful in the treatment of diseases associated with the altered motility and/or tone of smooth muscle, especially irritable bowel syndrome.

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