Benzodiazepin derivatives useful as CCK-receptor antagonists

Details Benzodiazepin derivatives useful as CCK-receptor antagonists Benzodiazepin derivatives useful as CCK-receptor antagonists

1997-06-06

1999-10-05

Shah, Mukund J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

540509, A61K 3155, C07D24310

Patent

active

059624515

ABSTRACT:
A benzodiazepine derivative of formula (I), or a pharmaceutically acceptable salt thereof, 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 and R.sup.4 and R.sup.5 are selected from alkyl and cycloalkyl groups and saturated heterocyclic groups optionally substituted at a hetero-atom; (b) R.sup.2 and R.sup.3 are independently selected from aromatic carbocyclic and heterocylic residues; and (c) W and X are selected independently from halogen and hydrogen atoms and alkyl and alkoxy groups. These compounds are gastrin and/or CCK-B receptor antagonists. ##STR1##

REFERENCES:
patent: 4820834 (1989-04-01), Evans et al.
patent: 5206234 (1993-04-01), Bock et al.
Lotti et al., "A new potent and selective non-peptide gastrin antagonist and brain cholecystokinin . . . ", European Jnl. of Pharm., 162:273-280, 1989.
Bock, et al., "Development of 1,4-Benzodiazepine Cholecystokinin Type B Antagonists", Jnl. Med. Chem., 36:4276-4292, 1993.
Bock, et al., "Benzodiazepine Gastrin and Brain Cholecystokinin Receptor Ligands: L-356,260", Jnl. Med. Chem., 32:13-16, 1989.

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