发明名称 PYRIMIDINE DERIVATIVES USEFUL AS SELECTIVE COX-2 INHIBITORS
摘要 The invention provides the compounds of formula (I) in which: R1 is selected from the group consisting of H, C1-6alkyl, C1-2alkyl substituted by one to five fluorine atoms, C3-6alkenyl, C3-10cycloalkylC0-6alkyl, C4-12bridged cycloalkyl, A(CR4R5)n and b(CR4R5)n; R2 is C1-2alkyl substituted by one to five fluorine atoms; R3 is selected from the group consisting of C1-6alkyl, NH2 and R7CONH; R4 and R5 are independently selected from H or C1-6alkyl; A is an unsubstituted 5- or 6-membered heteroaryl or an unsubstituted 6-membered aryl, or a 5- or 6-membered heteroaryl or a 6-membered aryl substituted by o ne or more R6; R6 is selected from the group consisting of halogen, C1-6alkyl, C1- 6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6alkoxy substituted by one or more F, NH2SO2 and C1-6alkylSO2; B is selected from th e group consisting of Formula (i) and (ii) and where (iv) defines the point of attachment of the ring; R7 is selected from the group consisting of H, C1- 6alkyl, C1-6alkoxy, C1-6alkylOC1-6alkyl, phenyl, HO2CC1-6alkyl, C1-6alkylOCO C1- 6alkyl, C1-6alkylOCO, H2NC1-6alkyl, C1-6alkylOCONHC1-6alkyl and C1- 6alkylCONHC1-6alkyl; and n is 0 to 4. Compounds of formula (I) are potent an d selective inhibitors of COX-2 and are of use in treatment of the pain, fever and inflammation of variety of conditions and diseases.
申请公布号 CA2448192(A1) 申请公布日期 2002.12.05
申请号 CA20022448192 申请日期 2002.05.23
申请人 GLAXO GROUP LIMITED 发明人 PAYNE, JEREMY JOHN;PEGG, NEIL ANTHONY;NAYLOR, ALAN
分类号 A61K31/505;A61K31/513;A61P29/00;A61P43/00;C07D239/34;C07D401/12;(IPC1-7):C07D239/34 主分类号 A61K31/505
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