Purine derivatives having phosphodiesterase IV inhibition activity

US6319928A · kind A · utility

Assignee

• Euro-Celtique S.A. · LU

Inventors

• Mark Chasin · Manalapan, US
• David Cavalla · Cambridge, GB
• Peter Hofer · Liestal, CH
• Peter Wintergerst · Basel, CH
• Andre Gehrig · Basel, CH

Key dates

• Filing date: Oct 14, 1999
• Grant date: Nov 20, 2001
• Expiry date: Oct 14, 2019

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D473/34
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

A compound of the formula: ##STR1## wherein PA1 R.sub.2 is O or S; PA1 R.sub.3, R.sub.6a and R.sub.8 are the same or different and each represent a C.sub.1-8 alkyl which is unbranched or branched and unsubstituted or substituted with OH, alkoxy, CO.sub.2 H, .dbd.NOH, .dbd.NOCONH.sub.2, or .dbd.O; C.sub.3-8 cycloalkyl which is unsubstituted or substituted with OH, alkoxy, CO.sub.2 H, .dbd.NOH, .dbd.NOCONH.sub.2, or .dbd.O; C.sub.4-8 cycloalkylalkyl wherein the cycloalkyl portion is unsubstituted or substituted with OH, alkoxy, CO.sub.2 H, .dbd.NOH, .dbd.NOCONH.sub.2, or .dbd.O; aryl which is unsubstituted or substituted with Cl, NH.sub.2, alkylamino, dialkylamino, amido, C.sub.1 -C.sub.8 alkylamido, C.sub.1 -C.sub.3 dialkylamido, OH, alkoxy, HC.dbd.NOH, HC.dbd.NOCONH.sub.2, C.sub.1 -C.sub.3 alkyl, phenyl or benzyl; aralkyl (C.sub.1-4); heterocyclyl; heterocyclylalkyl (C.sub.1 -C.sub.4); and heteroaryl; PA1 R.sub.6b represents a H or R.sub.6a, or together R.sub.6b, N, and R.sub.6a make a 3 to 8 member ring containing at least one carbon, from one to three nitrogen atoms, from zero to two oxygen atoms, from zero to two sulfur atoms, said ring optionally substituted with alkoxy, CO.sub…