Thiazolyl mGluR5 antagonists and methods for their use

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United States of America Patent

PATENT NO 8242143
APP PUB NO 20110230526A1
SERIAL NO

13016304

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Abstract

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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.

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Patent Owner(s)

Patent OwnerAddress
MERCK SHARP & DOHME LLC126 EAST LINCOLN AVENUE RAHWAY NJ 07065

International Classification(s)

Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Arruda, Jeannie M LaJolla, US 35 486
Cosford, Nicholas D San Diego, US 17 330
Eastman, Brian W San Diego, US 8 58
Huang, Dehua San Diego, US 80 686
King, Chris Carlsbad, US 18 522
Payne, Joseph Oceanside, US 6 7
Poon, Steve F Pasadena, US 5 28
Roppe, Jeffrey R Temecula, US 13 65
Seiders, Thomas J San Diego, US 10 111
Smith, Nicholas D San Diego, US 100 994
Vernier, Jean-Michel Laguna Niguel, US 82 846
Wang, Bowei Westfield, US 44 455
Zhao, Xiumin San Diego, US 5 19

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