申请人:AMERICAN HOME PRODUCTS CORPORATION
公开号:EP0039190A1
公开(公告)日:1981-11-04
The invention concerns a compound of formula I
in which R1 and R2 are hydrogen, or R1 and R2 together form a chain of the formula
wherein R6, R7, R8 and R9 each is hydrogen or lower alkoxy; R3 is one of the following
or
wherein R10 is hydrogen or at least one substituent selected from halo, lower alkyl, lower alkoxy, hydroxy, 1-oxo (lower) alkoxy or NR"R12 wherein R" and R12 each is hydrogen or lower alkyl; A is 0, S or NR13 wherein R13 is hydrogen or lower alkyl; R4 and R5 each is hydrogen or lower alkyl; and n is 1 or 2; or a therapeutically acceptable acid addition salt thereof, the term "lower alkyl" as used herein means straight chain alkyl radicals containing from 1 to 6 carbon atoms and branched chain alkyl radicals containing from 3 to 4 carbon atoms, the term "lower alkoxy" as used herein means straight chain alkoxy radicals containing from 1 to 6 carbon atoms and branched chain alkoxy radicals containing 3 to4 carbon atoms and the term "1-oxo(lower)alkoxy" as used herein means straight chain 1-oxoalkoxy radicals containing from 2 to 6 carbon atoms and branched chain 1-oxoalkoxy radicals containing 4 to 6 carbon atoms.
Processesforthe preparation of compounds of formula I and their use in pharmaceutical compositions and for the treatment of hypertension are also described.
本发明涉及一种式 I 的化合物
其中 R1 和 R2 为氢,或 R1 和 R2 共同形成一条式链
其中 R6、R7、R8 和 R9 各为氢或低级烷氧基; R3 为下列之一
或
其中 R10 是氢或至少一个选自卤代、低级烷基、低级烷氧基、羟基、1-氧代(低级)烷氧基或 NR "R12 的取代基,其中 R" 和 R12 各自是氢或低级烷基;A 是 0、S 或 NR13,其中 R13 是氢或低级烷基;R4 和 R5 各自是氢或低级烷基;n 是 1 或 2;或其治疗上可接受的酸加成盐,本文所用术语 "低级烷基 "是指含有 1 至 6 个碳原子的直链烷基和含有 3 至 4 个碳原子的支链烷基、本文所用术语 "低级烷氧基 "是指含有 1 至 6 个碳原子的直链烷氧基和含有 3 至 4 个碳原子的支链烷氧基,本文所用术语 "1-氧代(低级)烷氧基 "是指含有 2 至 6 个碳原子的直链 1-氧代烷氧基和含有 4 至 6 个碳原子的支链 1-氧代烷氧基。
还描述了式 I 化合物的制备过程及其在药物组合物和治疗高血压中的用途。