Isoquinoline derivatives as therapeutic agents

US5807868A · kind A · utility

Assignee

• Knoll, Inc. · DE

Inventors

• Bruce Sargent · Nottingham, GB
• David Johnston · Nottingham, GB
• Andrew Philip Crew · North Babylon, US

Key dates

• Filing date: Dec 21, 1995
• Grant date: Sep 15, 1998
• Expiry date: Dec 21, 2015

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D409/08
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Tetrahydroisoquinoline compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof, in which: R.sub.1 represents one or more substituents selected from H, halo, hydroxy, alkyl (optionally substituted by hydroxy), alkoxy, alkylthio, alkylsulphinyl, alkyl-sulphonyl, nitro, cyano, polyhaloalkyl, polyhaloalkoxy, phenyl (optionally substituted by one or more of halo, alkyl or alkoxy), or R.sub.1 is optionally alkylated carbamoyl; PA1 R.sub.2 represents a saturated or unsaturated aliphatic group optionally substituted by hydroxy or alkoxy; PA1 E represents an alkylene chain optionally substituted by one or more alkyl groups; PA1 and G represents (a) optionally substituted saturated or unsaturated alicyclic group containing 3 to 8 carbon atoms, or (b) optionally substituted saturated or unsaturated aliphatic chain containing 1 to 12 carbon atoms, or (c) optionally substituted 5 or 6 membered heterocyclic ring containing one or more N or O atoms or SO.sub.n groups in which n is 0, 1 or 2; PA1 and O-acylated derivatives thereof which provide lipophilic esters have utility in analgesia or in the treatment of psychoses (e.g. schizophrenia), Parkinson's disease, Lesch-Nyan sy…