Back to results
US 5,478,933 AGranted
Benzodiazepine derivatives and their use as antagonists of cholecystokinin and/or gastrin receptors
AssigneeMerck Sharpe & Dohme Ltd.
InventorGraham A. Showell
Life of this patent
Estimating the term…
Abstract
Disclosed are new benzodiazepine compounds which are useful as cholecystokinin and gastrin receptor antagonists and are useful in the treatment of anxiety, panic and pain.
Claims6
A compound of formula (I), or a salt or prodrug thereof:
- ##STR16## wherein:
- each of W and Z represents a nitrogen atom or a group CH;
- one of X and Y represents a carbonyl group and the other represents a group NH, with the proviso that the system W-X-Y-Z contains no nitrogen-nitrogen bonds;
- R.sup.1 represents H, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, cyclopropylmethyl, (CH.sub.2 ).sub.q -imidazolyl, (CH.sub.2).sub.q triazole, (CH.sub.2).sub.q tetrazole (where q is 1, 2 or 3 ), CH.sub.2 CO.sub.2 R.sup.5 (where R.sup.5 is C.sub.1-4 alkyl) or CH.sub.2 CONR.sup.6 R.sup.7 (where R.sup.6 and R.sup.7 each independently represents H or C.sub.1-4 alkyl, or R.sup.6 and R.sup.7 together form a chain (CH.sub.2).sub.p where p is 4 or 5);
- R.sup.2 represents C.sub.1-6 alkyl, halo, (CH.sub.2).sub.r -tetrazolyl, optionally substituted in the tetrazolyl ring by C.sub.1-4 alkyl, (CH.sub.2).sub.r -triazolyl, (CH.sub.2).sub.r -imidazolyl, CONR.sup.6 R.sup.7, SO(C.sub.1-6 alkyl), SO.sub.2 (C.sub.1-6 alkyl), CONHSO.sub.2 R.sup.8, SO.sub.2 NHCOR.sup.8 (where R.sup.8 is C.sub.1-6 alkyl, optionally substituted aryl, 2,2-difluorocyclopropane or trifluoromethyl), SONHR.sup.9 (where R.sup.9 is a nitrogen containing heterocycle), cyano, B(OH).sub.2 or (CH.sub.2).sub.r CO.sub.2 H, where r is zero, 1 or 2;
- R.sup.3 represents C.sub.1-6 alkyl or halo;
- m is 0, 1 or 2;
- and
- n is 0, 1, 2 or 3.
6 more elements
Dependencies are inferred from the claim text.