Amino substituted pyrazolo[1,5,-a]-1,5-pyrimidines and pyrazolo[1,5-a]-1,3,5-triazines

US6476038B1 · kind B1 · utility

Assignees

• Neurogen Corporation · US
• PFIZER INC. · US

Inventors

• James Darrow · Wallingford, US
• Stéphane De Lombaert · Madison, US
• Charles A. Blum · Guilford, US
• Jennifer Tran · Guilford, US
• Mark Giangiordano · Branford, US
• David A. Griffith · Sudbury, US
• Philip A. Carpino · Groton, US

Key dates

• Filing date: Sep 29, 2000
• Grant date: Nov 5, 2002
• Expiry date: Sep 29, 2020

Classification

• Technology area (CPC G): Physics
• CPC primary: G01N2333/70571
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Disclosed are compounds of the formula: where R1, R2, R3, R4, R5, R6, and X are defined herein. These compounds are selective modulators of NPY1 receptors. These compounds are useful in the treatment of a number of CNS disorders, metabolic disorders, and peripheral disorders, particularly eating disorders and hypertension. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided.Compounds of the invention are also useful as probes for the localization of NPY1 receptors and as standards in assays for NPY1 receptor binding. Methods of using the compounds in receptor localization studies are given.