Substituted 4-hydroxy-phenylalcanoic acid derivatives with agonist activity to PPAR-gamma

US6294580A · kind A · utility

Assignee

• Glaxo Wellcome Inc. · US

Inventors

• Timothy Mark Willson · Durham, US
• Robert Mook · Chapel Hill, US
• Istvan Kaldor · Durham, US
• Brad Henke · Cary, US
• David Norman Deaton · King of Prussia, US
• Jon Loren Collins · Durham, US
• Jeffrey Edmond COBB · Durham, US
• Marcus Brackeen · Durham, US
• Matthew J. SHARP · Apex, US
• John Mark O'Callaghan · Ashford, GB
• Greg Erickson · Cary, US
• Grady Evan Boswell · Cary, US

Key dates

• Filing date: Aug 25, 1998
• Grant date: Sep 25, 2001
• Expiry date: Aug 25, 2018

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2601/16
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A compound having formula (I), wherein A is selected from the group consisting of: (i) phenyl, wherein said phenyl is optionally substituted by one or more halogen atoms, C.sub.1-6 alkyl, C.sub.1-3 alkoxy, C.sub.1-3 fluoroalkoxy, nitrile, or --NR.sup.7 R.sup.8 where R.sup.7 and R.sup.8 are independently hydrogen or C.sub.1-3 alkyl; (ii) a 5- or 6-membered hetrocyclic group containing at least one heteroatom selected from oxygen, nitrogen and sulfur; and (iii) a fused bicyclic ring (a), wherein ring C represents a heterocyclic group as defined in point (ii) above, which bicyclic ring is attached to group B via a ring atom of ring C; B is selected from the group consisting of: (iv) C.sub.1-6 alkylene; (v) --MC.sub.1-6 alkylene or C.sub.1-6 alkyleneMC.sub.1-6 alkylene, wherein M is O, S, or --NR.sup.2 wherein R.sup.2 represents hydrogen or C.sub.1-3 alkyl; (vi) a 5- or 6-membered heterocyclic group containing at least one nitrogen heteroatom and optionally at least one further heteroatom selected from oxygen, nitrogen and sulfur and optionally substituted by C.sub.1-3 alkyl; and (vii) Het-C.sub.1-6 alkylene, wherein Het represents a heterocyclic group as defined in point (vi) above; A…