Merck + Co., Inc.

James B Hoffman

Mark G Bock

Doug W Hobbs

Daniel F Veber

Roger M Freidinger

Ben E Evans

Peter D Williams

Douglas J Pettibone

Kevin F Gilbert

Debra S Perlow

Joseph M Pawluczyk

George F Lundell

Jill M Erb

The invention is directed to a series of novel piperazinylcamphorsulfonyl compounds where the camphor ring is substituted by amides, amines, alkanes, alkenes, alkylamines, halogens, hydroxy, carboxy, alkoxycarbonyl and heterocyclic tings. Such compounds are oxytocin antagonists useful in the treatment of preterm labor, dysmenorrhea and for the stoppage of labor preparatory to cesarean delivery.

Piperazinylcamphorsulfonyl oxytocin antagonists

Compounds of the formula: ##STR1## where R.sup.1 is hydrogen or hydroxy and R.sup.2 is a substituted amino group, a substituted heterocyclic ring or a substituted alkyl. These compounds are oxytocin and vasopressin antagonists useful in the treatment of preterm labor, dysmenorrhea and for the stoppage of labor preparatory to cesarean delivery, timing of parturition, uterine hyperactivity, endometriosis, hypertension, congestive heart failure, hyponatremia and cognitive disorders. Also disclosed are pharmaceutical compositions containing these compounds, methods of their use and methods of their preparation.

Amide-substituted derivatives of spiroindanylcamphorsulfonyl oxytocin

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King of Prussia, PA, United States of America

James B Hoffman