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US 2016/0237072 A1Published application
Oxazolidinones as modulators of mglur5
AssigneeBristol-Myers Squibb Company
InventorsAndrew P. Degnan, Darrell Maxwell, Matthew D. Hill, Haiquan Fang, Michael F. Parker, Fukang Yang, Joanne J. Bronson, John E. Macor
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Abstract
The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, agonists and partial agonists for the mGluR5 receptor and may be useful for the treatment of various disorders of the central nervous system.
Claims15
A compound of formula I
- where:
- R1 is hydrogen or alkyl;
- R2 is hydrogen or alkyl;
- R3 is
- R4 is cyano, alkyl, haloalkyl, cycloalkyl, hydroxy, alkoxy, haloalkoxy, or thioalkyl, where alkyl, haloalkyl, and cycloalkyl are substituted with 0-3 substituents selected from halo, alkyl, haloalkyl, hydroxy, and alkoxy;
- or R4 is a bridged [1-4.1-4.0-3]bicycloalkyl;
- or R4 is alkylcarbonylamino, haloalkylcarbonylamino, cycloalkanonyl, valerolactamyl, oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydropyranyloxy, phenyl, or phenoxy;
- or R4 is amino, alkylamino, dialkylamino, azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, homopiperidinyl, homopiperazinyl, or homomorpholinyl;
- or R4 is pyrazolyl, isoxazolyl, isothiazolyl, imidazolyl, oxazolyl, thiazolyl, triazolyl, oxadiazolyl, thiadiazolyl, or indazolyl, and is substituted with 0-2 substituents selected from halo and alkyl;
- L is a bond, alkylene, or hydroxyalkylene;
- Ar1 is phenyl, pyridinyl, pyrazinyl, pyrimidinyl, or pyridazinyl, and is substituted with 1 R3 substituent and with 0-3 substituents selected from cyano, halo, alkyl, haloalkyl, alkoxy, and haloalkoxy;
- and
- Ar2 is phenyl, pyridinyl, pyrazinyl, pyrimidinyl, pyridazinyl, pyrrolyl, furanyl, thienyl, pyrazolyl, isoxazolyl, isothiazolyl, imidazolyl, oxazolyl, thiazolyl, triazolyl, oxadiazolyl, thiadiazolyl, tetrazolyl, or benzimidazolyl, and is substituted with 0-3 substituents selected from cyano, halo, alkyl, haloalkyl, hydroxy, alkoxy, haloalkoxy, and phenyl;
- or a pharmaceutically acceptable salt thereof.
11 more elements
Dependencies are inferred from the claim text.