Thiazolyl mGluR5 antagonists and methods for their use

US8609852B2 · kind B2 · utility

Assignee

• Merck Sharp & Dohme LLC · US

Inventors

• Nicholas D. P. Cosford · San Diego, US
• Thomas Jon Seiders · San Diego, US
• Joseph E. Payne · San Diego, US
• Jeffrey Roger Roppe · Temecula, US
• Dehua Huang · San Diego, US
• Nicholas D. Smith · San Diego, US
• Steve F. Poon · South Pasadena, US
• Chris King · Seattle, US
• Brian Walter Eastman · San Diego, US
• Bowei Wang · Westfield, US
• Jeannie M. Arruda · San Diego, US
• Jean-Michel Vernier · Laguna Niguel, US
• Xiumin Zhao · San Diego, US

Key dates

• Filing date: Jul 26, 2012
• Grant date: Dec 17, 2013
• Expiry date: Jul 26, 2032

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D471/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.