申请人:Schering Corporation
公开号:US05393755A1
公开(公告)日:1995-02-28
Novel polycylic guanine derivatives of the formula: ##STR1## wherein J is oxygen or sulfur, R.sup.1 is hydrogen, alkyl or alkyl substituted with aryl or hydroxy; R.sup.2 is hydrogen, aryl, heteroaryl, cycloalkyl, alkyl or alkyl substituted with aryl, heteroaryl, hydroxy, alkoxy, amino, monoalkyl amino or dialkylamino, or --(CH.sub.2).sub.m TCOR.sup.20 wherein m is an integer from 1 to 6, T is oxygen or --NH-- and R.sup.20 is hydrogen, aryl, heteroaryl, alkyl or alkyl substituted with aryl or heteroaryl; R.sup.3 is hydrogen, halo, trifluoromethyl, alkoxy, alkylthio, alkyl, cycloalkyl, aryl, aminosulfonyl, amino, monoalkylamino, dialkylamino, hydroxyalkylamino, aminoalkylamino, carboxy, alkoxycarbonyl or aminocarbonyl or alkyl substituted with awl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino; R.sup.a, R.sup.b, R.sup.c, and R.sup.d are defined in the specification; and n is zero or one. The compounds of formulas (I) and (I') are useful as antihypertensive, muscle relaxant and bronchodilating agents.
新颖的多环鸟嘌呤衍生物的化学式为:##STR1## 其中J为氧或硫,R.sup.1为氢,烷基或烷基取代芳基或羟基;R.sup.2为氢,芳基,杂环芳基,环烷基,烷基或烷基取代芳基,杂环芳基,羟基,烷氧基,氨基,单烷基氨基或二烷基氨基,或--(CH.sub.2).sub.m TCOR.sup.20,其中m为1到6的整数,T为氧或--NH--,R.sup.20为氢,芳基,杂环芳基,烷基或烷基取代芳基或杂环芳基;R.sup.3为氢,卤素,三氟甲基,烷氧基,硫烷基,烷基,环烷基,芳基,氨基磺酰基,氨基,单烷基氨基,二烷基氨基,羟基烷基氨基,氨基烷基氨基,羧基,烷氧羰基或氨基羰基或烷基取代芳基,羟基,烷氧基,氨基,单烷基氨基或二烷基氨基;R.sup.a,R.sup.b,R.sup.c和R.sup.d在规范中有定义;n为零或一。化合物的化学式(I)和(I')可用作降压、肌肉松弛和扩张支气管剂。