申请人:SmithKline Beecham Corporation
公开号:US06498166B1
公开(公告)日:2002-12-24
The invention provides the compounds of formula (I)
wherein:
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 halogen, CN, CONR4R5, CO2H, CO2C1-6alkyl, or NHSO2R4;
R3 is C1-6alkyl or NH2; and
R4 and R5 are independently selected from H, C1-6alkyl, phenyl, phenyl substituted by one or more atoms or groups (selected from halogen, C1-6alkyl, C1-6alkoxy, or C1-6alkoxy substituted by one or more fluorine atoms), or together with the nitrogen atom to which they are attached form a saturated 4 to 8 membered ring; and
pharmaceutically acceptable derivatives thereof.
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.
该发明提供了公式(I)的化合物,其中:R0和R1独立选择自H,卤素,C1-6烷基,C1-6烷氧基或C1-6烷氧基,其被一个或多个氟原子取代;R2是卤素,CN,CONR4R5,CO2H,CO2C1-6烷基或NHSO2R4;R3是C1-6烷基或NH2;R4和R5独立选择自H,C1-6烷基,苯基,被一个或多个原子或基团(选择自卤素,C1-6烷基,C1-6烷氧基或C1-6烷氧基,其被一个或多个氟原子取代)取代的苯基,或与它们所附着的氮原子一起形成饱和的4至8成员环;以及其药学上可接受的衍生物。公式(I)的化合物是COX-2的有效和选择性抑制剂,并可用于治疗各种疾病的疼痛,发热,炎症。