IP Library Granted Patent US 8,609,852
Granted Patent B2
US 8,609,852 · App. 13/558,537 · Granted Dec 17, 2013

Thiazolyl mGluR5 antagonists and methods for their use

Inventors: Nicholas D. Cosford (San Diego, CA); Thomas J. Seiders (San Diego, CA); Joseph E. Payne (Oceanside, CA); Jeffrey R. Roppe (Temecula, CA); Dehua Huang (San Diego, CA); Nicholas D. Smith (San Diego, CA); Steve F. Poon (South Pasadena, CA); Chris King (Carlsbad, CA); Brian W. Eastman (San Diego, CA); Bowei Wang (San Diego, CA); Jeannie M. Arruda (LaJolla, CA); Jean-Michel Vernier (Laguna Niguel, CA); Xiumin Zhao (San Diego, CA)
Assignee: Merck Sharp & Dohme Corp.
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Quick Facts
Patent No.
US 8,609,852
App. No.
13/558,537
Granted
Dec 17, 2013
Kind
B2
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.

Claims (3)

1. A compound which is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition which comprises the compound of claim 1 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient.

Assignments (1)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
Continuity (4)
Continuation 13016304 · Jan 28, 2011
Continuation 11664902
Provisional Application 60616805 · Oct 7, 2004
Related Publication 20120289696A1 · Nov 15, 2012