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    • 2. 发明授权
    • Tri-substituted (aryl or heteroaryl) derivatives and pharmaceutical
compositions containing the same
    • 三取代(芳基或杂芳基)衍生物和含有它们的药物组合物
    • US5622977A
    • 1997-04-22
    • US474214
    • 1995-06-07
    • Graham J. WarrellowEwan C. BoydRikki P. AlexanderJohn C. Head
    • Graham J. WarrellowEwan C. BoydRikki P. AlexanderJohn C. Head
    • C07C43/235C07C59/72A61K31/44C07D213/04C07D405/10C07D409/10
    • C07C43/235C07C59/72
    • Compounds of the general formula (1) ##STR1## are described wherein Y is halogen or --OR.sup.1, where R.sup.1 is a substituted or unsubstituted alkyl; X is --O--, --S-- or --N(R.sup.8)--, where R.sup.8 is hydrogen or alkyl; R.sup.2 is substituted or unsubstituted alkyl, alkenyl, cycloalkyl or cycloalkenyl; R.sup.3 is hydrogen, halogen or --OR.sup.9, where R.sup.9 is hydrogen or substituted or unsubstituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl, or formyl, carboxamido or thiocarboxamido; R.sup.4 and R.sup.5, which may be the same or different, are each --(CH.sub.2).sub.n Ar, where Ar is a monocyclic or bicyclic aryl group or monocyclic or bicyclic heteroaryl and n is integer of 0 to 3; R.sup.6 is hydrogen or substituted or unsubstituted alkyl; R.sup.7 is hydrogen or substituted or unsubstituted alkyl; and the salts, solvates, hydrates and N-oxides thereof. Compounds according to the invention are potent, selective and orally active PDE IV inhibitors and are useful in the prophylaxis and treatment of asthma and other diseases.
    • 其中Y为卤素或-OR 1,其中R 1为取代或未取代的烷基; X是-O - , - S-或-N(R 8) - ,其中R 8是氢或烷基; R2是取代或未取代的烷基,烯基,环烷基或环烯基; R3是氢,卤素或-OR9,其中R9是氢或取代或未取代的烷基,烯基,烷氧基烷基或烷酰基,或甲酰基,甲酰氨基或硫代羧酰胺基; R 4和R 5可以相同或不同,各自为 - (CH 2)n Ar,其中Ar为单环或双环芳基或单环或双环杂芳基,n为0至3的整数; R6是氢或取代或未取代的烷基; R7是氢或取代或未取代的烷基; 及其盐,溶剂合物,水合物和N-氧化物。 根据本发明的化合物是有效的,选择性和口服活性的PDE IV抑制剂,并且可用于预防和治疗哮喘和其它疾病。