Aventis Pharmaceuticals Inc.

Sanofi

Bin Cao

Keith John Harris

Raymond W Kosley, Jr

Hazel Joan Dyke

Charles J Gardner

Rosy Sher

Timothy A Gillespy

Ryan E Hartung

Sathapana Kongsamut

Elsa Amandine Dechaux

Sungtaek Lim

David Stefany

Vieroslava Gurunian

Ray Boffey

Joacy C Aguiar

Jr Raymond W Kosley

Ray Argenta Discovery Ltd Boffey

The present invention relates to a series of substituted dihydro and tetrahydro oxazolopyrimidinones, specifically, to a series of 2-substituted-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-ones and 2-substituted-2,3,5,6-tetra-hydro-oxazolo[3,2-a]pyrimidin-7-ones of formula (I): Wherein p, n, X, Y, R, R, R, R, R, R, Rand Rare as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.

Substituted dihydro and tetrahydro oxazolopyrimidinones, preparation and use thereof

The present invention is directed to a compound of Formula (I) wherein Cy, Cy, L, L, and Rare as defined herein, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds according to Formula (I) in admixture with a pharmaceutically acceptable carrier, and a method of treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like by administering to said patient a pharmaceutically effective amount of a compound according to Formula (I).

2,6-substituted-4-monosubstitutedamino-pyrimidine as prostaglandin D2 receptor antagonists

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Bedminster, NJ, United States of America

Bin Cao