| 摘要 |
Compounds of the formula (1) : <CHEM> and pharmaceutically acceptable salts are described, wherein X is O or S; R<1> is C1-6alkyl, C2-6alkenyl, C3-5cycloalkylC1-4alkyl, or C1-4alkyl substituted by 1 to 3 fluoro groups; R<2> is hydrogen, -CN, -CONR<5>R<6>, -CO2R<7>, 5-tetrazolyl, -NO2, -NH2 or -NHCOR<8> wherein R<5> to R<8> are independently hydrogen or C1-4alkyl; R<3> is hydrogen or C1-4alkyl; R<4> is hydrogen or C1-4alkyl; and R is halo, C1-4alkyl, C1-4alkoxy, cyano, -CONR<9>R<1><0>, -CO2R<1><1>, -S(0)nC1-4alkyl, -NO2, -NH2, -NHCOR<1><2>, or -SO2NR<1><3>R<1><4> wherein n is 0, 1 or 2 and R<9> to R<1><4> are independently hydrogen or C1-4alkyl; with the proviso that R<1> is not methyl when R<2> is -CO2H, -CO2CH2CH3 or -CN, X is 0, R<3> is hydrogen, R<4> is hydrogen or methyl and R is 6-methoxy. These compounds have bronchodilator, anti-allergic, vasodilator and anti-inflammatory activities. Pharmaceutical compositions are described as are methods of use. Processes for the preparation of the compounds of the formula (1) are described. |
