C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 263/30 (2006.01) A61K 31/42 (2006.01) A61K 31/435 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/55 (2006.01) A61K 31/675 (2006.01) C07D 263/34 (2006.01) C07D 263/38 (2006.01) C07D 263/46 (2006.01) C07D 263/48 (2006.01) C07D 413/00 (2006.01) C07D 413/06 (2006.01) C07D 413/10 (2006.01) C07D 471/04 (2006.01) C07D 487/04 (2006.01) C07D 521/00 (2006.01) C07F 9/653 (2006.01)
Patent
CA 2221692
A class of substituted oxazoles is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (I), wherein R is selected from hydrido, halo, mercapto, hydroxyl, carboxyalkylthio, carboxyalkylthioalkyl, carboxyalkoxy, carboxyalkoxyalkyl, haloalkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkoxy, aryloxy, aralkoxy, alkylamino, aminocarbonyl, alkoxyalkyl, carboxy(haloalkyl), alkyl, hydroxyalkyl, haloalkyl, alkenyl, hydroxyalkenyl, alkynyl, hydroxyalkynyl, cycloalkyl, cycloalkylalkyl, aminoalkyl, hydroxyalkoxyalkyl, alkylcarbonyl, phosphonylalkyl, amino acid residue, heterocyclylalkyl, cyanoalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, carboxy, carboxyalkyl, arylthioalkyl, aminocarbonylalkyl, alkylcarbonylaminoalkyl, alkoxycarbonylaminoalkyl, aralkoxycarbonylaminoalkyl, aryl, heteroaryl, aralkyl, aryloxyalkyl, aralkoxyalkyl, heteroaryloxyalkyl and heteroarylalkoxyalkyl; wherein R1 is selected from cycloalkyl, cycloalkenyl, aryl and heterocyclyl, wherein R1 is optionally substituted at a substitutable position by alkyl, alkylamino, alkoxy and halo; wherein R2 is selected from alkyl and amino; and wherein R3 is selected from hydrido and alkyl.
L'invention se rapporte à une classe d'oxazoles substitués destinés à être utilisés dans le traitement d'inflammations ou de troubles liés à des inflammations. Des composés d'intérêt particulier sont définis par la formule (I) dans laquelle R est sélectionné parmi hydrido, halo, mercapto, hydroxyle, carboxyalkylthio, carboxyalkylthioalkyle, carboxyalcoxy, carboxyalcoxyalkyle, haloalcoxy, alkylthio, alkylsulfinyle, alkylsulfonyle, alcoxy, aryloxy, aralcoxy, alkylamino, aminocarbonyle, alcoxyalkyle, carboxy(haloalkyle), alkyle, hydroxyalkyle, haloalkyle, alcényle, hydroxyalcényle, alkynyle, hydroxyalkynyle, cycloalkyle, cycloalkylalkyle, aminoalkyle, hydroxyalcoxyalkyle, alkylcarbonyle, phosphonylalkyle, un résidu aminoacide, hétérocyclylalkyle, cyanoalkyle, alcoxycarbonyle, alcoxycarbonylalkyle, carboxy, carboxyalkyle, arylthioalkyle, aminocarbonylalkyle, alkylcarbonylaminoalkyle, alcoxycarbonylaminoalkyle, aralcoxycarbonylaminoalkyle, aryle, hétéroaryle, aralkyle, aryloxyalkyle, aralcoxyalkyle, hétéroaryloxyalkyle et hétéroarylalcoxyalkyle; où R<1> est sélectionné parmi cycloalkyle, cycloalcényle, aryle et hétérocyclyle, R<1> étant éventuellement substitué à une position substituable par alkyle, alkylamino, alcoxy et halo; où R<2> est sélectionné parmi alkyle et amino; et où R<3> est sélectionné parmi hydrido et alkyle.
Bertenshaw Stephen
Brown David L.
Devadas Balekudru
Graneto Matthew
Hwang-Fun Lu
G.d. Searle & Co.
Osler Hoskin & Harcourt Llp
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