Thienoisoxazolyl-and thienylpyrrazolyl-phenoxy substituted propyl derivatives useful as D4 antagonists

US7125903B1 · kind B1 · utility

Assignee

• Aventis Pharmaceuticals Inc. · US

Inventors

• David M. Fink · Doylestown, US
• Brian S. Freed · Phillipsburg, US
• Nicholas J. Hrib · Somerville, US
• Raymond W. Kosley, Jr. · Bound Brook, US
• George E. Lee · Somerville, US
• Gregory H. Merriman · Somerville, US
• Barbara S. Rauckman · Flemington, US

Key dates

• Filing date: Sep 13, 2000
• Grant date: Oct 24, 2006
• Expiry date: Sep 13, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D495/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The compounds are of the class thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.