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US 5,688,943 AGranted
Benzodiazepine derivatives useful as CCK-receptor antagonists
AssigneeYamanouchi Pharmaceutical Co., Ltd.
InventorsHamish Ryder, Graeme Semple, David Alan Kendrick, Michael Szelke, Masato Satoh, Mitsuaki Ohta, Keiji Miyata, Akito Nishida
Life of this patent
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Abstract
This invention relates to benzodiazepine derivatives which are useful as drugs exhibiting antagonism at the gastrin and/or CCK-B receptor, and to their production.
Claims16
A benzodiazepine compound of formula I, or a pharmaceutically acceptable salt thereof:
- ##STR7## wherein:
- (a) R.sup.1 is --CH.sub.2 CHOH(CH.sub.2 ).sub.a R.sup.4 or a ketone group --CH.sub.2 CO(CH.sub.2 ).sub.a R.sup.5 in which a is 0 or 1, or a group --CH.sub.2 COC(CH.sub.3 ).sub.2 --R.sup.5 ;
- R.sup.4 and R.sup.5 are selected from (C.sub.l -C.sub.8)alkyl groups;
- (C.sub.3 -C.sub.8)cycloalkyl and adamantyl groups, which may be unsubstituted or substituted by one or two (C.sub.1 -C.sub.8)alkyl groups;
- and groups of formulae II and III;
- ##STR8## in which R.sup.6 is H or (C.sub.1 C.sub.8)alkyl or --CO--(C.sup.1-C.sub.6)alkyl and b is 1 or 2;
- (b) R.sup.2 and R.sup.3 are independently selected from 5-and 6-membered aromatic carbocyclic and 5-and 6-membered heterocyclic groups with one heteroatom selected from the group consisting of N, O and S, where R.sup.2 and R.sup.3 each may have 1 or 2 substituents selected from the group consisting of a halogen atom, an amino group, a hydroxyl group, a nitro group, a cyano group, an alkyl group, an alkoxy group, a hydroxyamino group, an alkylamino group and a dialkylamino group, a carbamoyl group, a formylamino group, an alkylaminoalkyl group, a dialkylaminoalkyl group, a --(CH.sub.2).sub.c --CO.sub.2 H group in which c is 0-2 and a --(CH.sub.2 ).sub.c --CO.sub.2 H in which c is 0-2, wherein alkyl portions of the recited groups consist of 1 to 6 carbon atoms;
- and
- (c) W and X are selected independently from halogen and hydrogen atoms and (C.sub.1 -C.sub.8)alkyl and (C.sub.1 -C.sub.8)alkoxy groups.
6 more elements
Dependencies are inferred from the claim text.