Patent number: 8642603
Abstract: 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, R1, R2, R3, R4, R5, R6, R7 and R8 are 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.
Type:
Grant
Filed:
September 4, 2009
Date of Patent:
February 4, 2014
Assignee:
Sanofi
Inventors:
Bin Cao, Vieroslava Gurunian, Sathapana Kongsamut, Raymond W. Kosley, Jr., Rosy Sher, Ryan E. Hartung
Publication number: 20100075994
Abstract: 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, R1, R2, R3, R4, R5, R6, R7 and R8 are 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.
Type:
Application
Filed:
September 4, 2009
Publication date:
March 25, 2010
Applicant:
SANOFI-AVENTIS
Inventors:
Bin CAO, Vieroslava GURUNIAN, Sathapana KONGSAMUT, Raymond W. KOSLEY, JR., Rosy SHER, Ryan E. HARTUNG
Publication number: 20070129403
Abstract: The present invention provides methods of treating schizophrenia and/or glucoregulatory abnormalities in a patient in need thereof comprising administering to said patient a therapeutically effective amount of a compound of formula I wherein in is 0, 1 or 2; n is 0, 1 or 2; p is 0 or 1; each R is independently hydrogen, halogen, trifluoromethyl, C1-C6alkyl, C1-C6alkoxy, benzyloxy, hydroxy, nitro or amino; each R1 is independently hydrogen, C1-C6alkyl, C1-C6alkenyl, C1-C6alkanoyl, halogen, cyano, —C(O)C1-C6alkyl, —C1-C6alkyleneCN, —C1-C6alkyleneNR?R? wherein R? and R? are each independently hydrogen or C1-C6alkyl, —C1-C6alkyleneOC(O)C1-C6alkyl, or —CH(OH)R4 wherein R4 is hydrogen or C1-C6alkyl; R2 is hydrogen, C1-C6alkyl optionally substituted with halogen, hydroxy or benlzyloxy, C1-C6alkenyl, C1-C6alkynyl, —CO2C1-C6alkyl, or —R5—NR?R? wherein R5 is C1-C6alkylene, C1-C6alkenylene or C1-C6alkynylene and R? and R? are each independently hydrogen, C1-C6alkyl or alternatively the group —NR?R? as a whole
Type:
Application
Filed:
September 29, 2006
Publication date:
June 7, 2007
Applicant:
AVENTIS PHARMACEUTICALS INC.
Inventors:
Craig Smith, David Rampe, Beth Borowsky, Sathapana Kongsamut