IP Library Granted Patent US 7,879,882
Granted Patent B2
US 7,879,882 · App. 11/664,902 · Granted Feb 1, 2011

Thiazolyl mglur5 antagonists and methods for their use

Assignee: Merck Sharp & Dohme Corp.
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Quick Facts
Patent No.
US 7,879,882
App. No.
11/664,902
Granted
Feb 1, 2011
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 (4)

1. A compound which is:

or a pharmaceutically acceptable salt thereof;

with the proviso that the compound does not comprise any radioisotopes at a level beyond their natural abundance.

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

Assignments (5)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
CHANGE OF NAME Recorded Aug 29, 2012
From: SCHERING CORPORATION
To: MERCK SHARP & DOHME CORP.
Reel/Frame 028866/0511 →
MERGER Recorded Aug 27, 2012
From: MERCK SHARP & DOHME CORP.
To: SCHERING CORPORATION
Reel/Frame 028850/0515 →
CHANGE OF NAME Recorded Jan 26, 2010
From: MERCK & CO., INC.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 023906/0803 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 15, 2008
From: COSFORD, NICHOLAS D.; SEIDERS, THOMAS J.; PAYNE, JOSEPH; ROPPE, JEFFREY R.; HUANG, DEHUA; SMITH, NICHOLAS D.; POON, STEVE F.; KING, CHRIS; EASTMAN, BRIAN W.; WANG, BOWEL; ARRUDA, JEANNIE M.; VERNIER, JEAN-MICHEL; ZHAO, XIUMIN
To: MERCK & CO., INC.
Reel/Frame 021242/0696 →
Continuity (2)
Provisional Application 60616805 · Oct 7, 2004
Related Publication 20090203903A1 · Aug 13, 2009