2-aminoindans as selective dopamine D3 ligands

US5708018A · kind A · utility

Assignee

• Pharmacia & Upjohn Company LLC · US

Inventors

• Susanne R. Haadsma-Svensson · Portage, US
• Bengt R. Andersson · Göteborg, SE
• Clas Sonesson · Lindome, SE
• Chiu-Hong Lin · Kalamazoo, US
• R. Nicholas Waters · Göteborg, SE
• Kjell A. I. Svensson · Alingsås, SE
• Per A. E. Carlsson · Göteborg, SE
• Lars O. Hansson · Gothenburg, SE
• N. Peter Stjernlof · Mölndal, SE

Key dates

• Filing date: Feb 2, 1996
• Grant date: Jan 13, 1998
• Expiry date: Feb 2, 2016

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2602/08
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Compounds and their pharmaceutically acceptable salts suitable for treating central nervous system disorders associated with the dopamine D3 receptor activity of Formula I: ##STR1## wherein R.sub.1 and R.sub.2 are independently chosen from hydrogen, C.sub.1 -C.sub.8 alkyl, OCH.sub.3, OH, OSO.sub.2 CF.sub.3, OSO.sub.2 CH.sub.3, SOR.sub.5, CO.sub.2 R.sub.5, CONH.sub.2, CONR.sub.5 R.sub.6, COR.sub.5, CN, SO.sub.2 NH.sub.2, SO.sub.2 NR.sub.5 R.sub.6, SO.sub.2 R.sub.5, --OCO--(C.sub.1 -C.sub.6 alkyl), --NCO--(C.sub.1 -C.sub.6 alkyl), --CH.sub.2 O--(C.sub.1 -C.sub.6 alkyl), --CH.sub.2 OH, --CO-Aryl, --NHSO.sub.2 -Aryl, --NHSO.sub.2 --(C.sub.1 -C.sub.6 alkyl), phthalimide, thiophenyl, pyrrol, pyrrolinyl, oxazolyl, or R.sub.1 and R.sub.2 together form --O(CH.sub.2).sub.1-2 O-- or --(CH.sub.2).sub.3-6 -- (except that only one of R.sub.1 and R.sub.2 can be hydrogen or OH in any such compound); R.sub.3 and R.sub.4 are independently chosen from C.sub.2 -C.sub.4 alkenyl, C.sub.3 -C.sub.8 alkynyl, C.sub.3 -C.sub.8 cycloalkyl, --(CH.sub.2).sub.p -- thienyl (where p is 1-4), or C.sub.1 -C.sub.8 alkyl (except where R.sub.1 or R.sub.2 are hydrogen or OH or where both R.sub.1 and R.sub.2 are OCH.sub.…