Pyrazolopyridine derivatives as selective cox-2 inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 471/04 (2006.01) A61K 31/435 (2006.01) C07D 221/00 (2006.01) C07D 231/00 (2006.01)

Patent

CA 2349567

The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof in which : R0 and R1 are independently selected from H, halogen, C1-6alkyl, C1-6alkoxy, or C1-6alkoxy substituted by one or more fluorine atoms; R2 is H, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1- 6alkyl, C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms; and R3 is C1-6alkyl or NH2. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.

L'invention concerne des composés de formule (I) et les dérivés pharmaceutiquement acceptables de ceux-ci. Dans cette formule: R?0¿ et R?1¿ sont indépendamment choisis parmi H, halogène, alkyleC¿1-6?, alkoxyC¿1-6?, ou alkoxyC¿1-6? substitué par un ou plusieurs atomes de fluor; R?2¿ représente H, alkyleC¿1-6?, alkyleC¿1-6? substitué par un ou plusieurs atomes de fluor, alkoxyC¿1-6?, hydroxyalkyleC¿1-6?, alkyleSC¿1-6?, C(O)H, alkyleC(O)C¿1-6?, alkylsulphonyleC¿1-6?, ou alkoxyC¿1-6? substitué par un ou plusieurs atomes de fluor; et R?3¿ désigne alkyleC¿1-6? ou NH¿2?. Ces composés de formule (I) sont des inhibiteurs puissants et sélectifs de COX-2 et peuvent donc être utilisés pour traiter la douleur, la fièvre, les inflammations, ainsi que diverses affections et maladies.

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