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

US5486611A · kind A · utility

Assignee

• The Upjohn Co. · US

Inventors

• Chiu-Hong Lin · Kalamazoo, US
• Susanne R. Haadsma-Svensson · Portage, US
• Robert McCall · Kalamazoo, US
• Arthur Glenn Romero · Kalamazoo, US
• William H. Darlington · Kalamazoo, US
• Michael Ennis · Mattawan, US

Key dates

• Filing date: Oct 28, 1993
• Grant date: Jan 23, 1996
• Expiry date: Oct 28, 2013

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D221/10
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

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.