The Upjohn Co.

Pharmacia & Upjohn Company

William H Darlington

Arthur Glenn Romero

Chiu-Hong Lin

Susanne R Haadsma-Svensson

Montford F Piercey

Michael D Ennis

Robert B McCall

Kerry Anne Cleek

Jeffrey A Leiby

This invention is therapeutically useful 2-aminotetralins and pharmaceutically acceptable acid addition salts thereof of the formula

Therapeutically useful 2-aminotetralin derivatives

Compounds and their pharmaceutically acceptable salts suitable for treating central nervous system disorders associated with the dopamine D3 receptor activity of structural Formula I: ##STR1##

Aryl substituted bicyclic amines as selective dopamine D3 ligands

This invention is therapeutically useful 2-aminotetralins and pharmaceutically acceptable acid addition salts thereof of the formula ##STR1## R, R.sub.1 to R.sub.5 and p are as defined in the specification, these compounds are useful to treat central nervous system disorders, hypertension, diabetes, sexual impotency and to control appetite.

This invention is therapeutically useful tetralins and pharmaceutically acceptable acid addition salts thereof of the formula I: ##STR1## wherein X is --(CH.sub.2).sub.n -- or --C(R.sub.1)(H)--; R is C.sub.1 -C.sub.8 alkyl; and R.sub.1 and R.sub.2 are the same or different and are selected from the group consisting of hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.8) alkynyl, aryl and benzyl. These compounds are useful to treat central nervous system disorders and are unexpectedly resistant to metabolism by the liver and have superior oral plasma bioavailability.

Carboxamido-(1,2N)-carbocyclic-2-aminotetralin derivatives

Substituted 1-(alkoxyphenyl)piperazines are disclosed as partial dopamine agonists useful in the treatment of dopaminergic dysregulation. The compounds 1-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]-3-phenyl-2-imidazolidinone and 1-(3-chlorophenyl)-3-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]-2-imidaz olidinone, are preferred in the treatment of Parkinsonism, schizophrenia, and drug addiction.

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Kalamazoo, MI, United States of America

William H Darlington