3-substituted-6-aryl pyridines

US7863454B2 · kind B2 · utility

Assignee

• Novartis International Pharmaceutical, Ltd. · BM

Inventors

• Alan Hutchison · Madison, US
• Jun Yuan · Guilford, US
• Kyungae Lee · Newton, US
• George D. Maynard · Clinton, US
• Bertrand L. Chenard · Waterford, US
• Nian Liu · North Branford, US
• Qin Guo · Branford, US
• Zihong Guo · Southbury, US
• Peter Hrnciar · Lexington, US

Key dates

• Filing date: Mar 3, 2008
• Grant date: Jan 4, 2011
• Expiry date: Jul 27, 2028

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C40B40/00
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

3-substituted-6-aryl pyridines of Formula I are provided:wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.