The present invention is directed to a new class of cyclic guanidines of the formula:
in which Q is represented by a substituent selected from the group consisting of (CH₂)n in which n is an integer from 2-10,
A is a substituent selected from the group consisting of -NH-(CH₂)m in which m is an integer from 0-5, a piperidino substituent, or a piperazino substituent; both Ar and Ar₁ are each independently represented by a phenyl ring, each of which may be optionally substituted with up to 3 substituents, each selected from the group consisting of halogen, alkyl, alkoxy, hydroxy, and trifluoromethyl; and R is represented by either hydrogen or an alkyl; R₁ is represented by hydrogen or an alkyl; the tautomers, and optical isomers thereof; and the pharmaceutically acceptable acid addition salts thereof; with the provisos that: 1) when Q is represented by (CH₂)2,3,or ₄ , then A is not represented by NH-(CH₂)o; and 2) when Q is represented by (CH₂)₂ and R is an alkyl; then A is not NH-(CH₂), and to their use as calcium antagonists.
本发明涉及一类新的环
鸟苷,其式如下
其中 Q 代表选自 (CH₂)n 组的取代基,其中 n 为 2-10 的整数、
A 是选自由 -NH-(CH₂)m (其中 m 为 0-5 的整数)、
哌啶取代基或
哌嗪取代基组成的取代基;Ar 和 Ar₁ 均各自独立地由苯基环代表,每个苯基环可任选被最多 3 个取代基取代,每个取代基均选自由卤素、烷基、烷氧基、羟基和三
氟甲基组成的组;R₁由氢或烷基表示;R₁由氢或烷基表示;其同素异形体和光学异构体;以及其药学上可接受的酸加成盐;但有以下条件:1) 当 Q 由 (CH₂)2、3 或 ₄ 表示时,则 A 不是 NH-(CH₂)o;以及 2) 当 Q 由 (CH₂)₂ 表示且 R 是烷基时,则 A 不是 NH-(CH₂),并将它们用作
钙拮抗剂。