Indolin-2-one derivatives

Details Indolin-2-one derivatives Indolin-2-one derivatives

1997-11-03

1999-09-14

Morris, Patricia L.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

548483, 548485, C07D20934

Patent

active

059525118

ABSTRACT:
A compound represented by formula (I): ##STR1## wherein R.sub.1 represents a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a nitro group, a trifluoromethyl group, a lower alkylthio group, an acyl group, a carboxyl group, a mercapto group or an amino group; R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, an alkoxy group, an acyl group, an aryl group or a heterocyclic group; R.sub.3 represents a lower alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; R.sub.4 represents a hydrogen atom, a lower alkyl group, an aryl group, a heterocyclic group, --OR.sub.5, --SR.sub.5 or --NR.sub.6 R.sub.7 (wherein R.sub.5, R.sub.6, and R.sub.7 each represent a lower alkyl group, etc.); X and Y each represent --CH.sub.2 --, --NH-- or --O--; and n represents an integer of from 0 to 4, and an intermediate for synthesis thereof are disclosed. The compound of the present invention exhibits selective antagonism against gastrin receptors without causing side effects attributed to CCK-A receptor antagonism and is useful for the treatment and prevention of peptic ulcers, gastritis, reflux esophagitis, and Zollinger-Ellison syndrome, and for the treatment of neoplasm originating in the gastrointestinal system.

REFERENCES:
patent: 4760083 (1988-07-01), Myers et al.
patent: 4876259 (1989-10-01), Myers et al.
Skiles et al., Tetrahedron Letters, 31, No. 50, 7277-7280 (1990).
Otomasu et al., Chem. Pharm. Bull. 23, (7) 1431-1435 (1975).
Joshi et al., Heterocycles, 31, No. 3, 473-477 (1990).
Hino et al., Chem. Pharm. Bull. 8, 839-842 (1960).

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