Piperazine-substituted [1,2,4]triazolo[1,5-C]quinazolin-5-amine compounds with A2A antagonist properties

US9676780B2 · kind B2 · utility

Assignee

• Merck Sharp & Dohme LLC · US

Inventors

• Amjad Ali · Freehold, US
• Michael Man-Chu Lo · Rahway, US
• Yeon-Hee Lim · South San Francisco, US
• Andrew Stamford · Madison, US
• Rongze Kuang · Green Brook, US
• Paul Tempest · Brookline, US
• Younong Yu · East Brunswick Township, US
• Michael Y. Berlin · Flemington, US
• Pauline C. Ting · New Providence, US
• Gang Zhou · Bound Brook, US
• Tao Yu · Shanghai, CN
• Christopher W. Boyce · Flemington, US
• Joseph M. Kelly · Sayreville, US
• Jayaram R. Tagat · Westfield, US
• Junying Zheng · New Providence, US
• Xianhai Huang · Hackettstown, US
• Wei Zhou · Scotch Plains, US
• Jae-Hun Kim · Scotch Plains, US
• Nicolas Zorn · Durmenach, FR
• Dong Xiao · Hackettstown, US
• Gioconda V. Gallo · Summit, US
• Walter Won · Alpine, US
• Heping Wu · Edison, US
• Rajan Anand · Wilmington, US
• Qiaolin Deng · Edison, US

Key dates

• Filing date: Dec 20, 2013
• Grant date: Jun 13, 2017
• Expiry date: Feb 12, 2034

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D513/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Disclosed are compounds of Formula A: (structurally represented) where “RG1”, “RG2a”, “RG4”, “RG5”, “MG1”, “n” and “m” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.