申请人:A.H. ROBINS COMPANY, INCORPORATED
公开号:EP0295010A1
公开(公告)日:1988-12-14
Compounds of general formula I
wherein,
Ar represents a 1-naphthyl group, a 2-naphthyl group, a 2,3-dihydro-1 H-inden-4(or 5)-yl group, a 2-furanylmethyl group, a 2-pyridinyl group, a phenyl group or a phenyl substituted by one to three substituents wherein the or each substituent independently represents a loweralkyl group, a loweralkoxy group, a diloweralkylamino group, a cyano group, a loweralkylthio group, a loweralkylsulfinyl group, a loweralkylsulfonyl group, an acyl group, an acylamino group, an aminocarbonyl group, a diloweral- kylaminoloweralkoxy group, a trifluoromethyl group, a nitro group or a halogen atom;
X represents a thio group, a sulfinyl group, a sulfonyl group or an oxygen atom;
d represents zero or one;
B represents a carbonyl group, a thioxomethyl group or a cyanoiminomethyl group;
each of n, m and p independently represents an integer from 2 to 6 inclusive;
each of Z and W independently represent an R group or a
group with the proviso that when Z represents R, W represents a -(CH2)m-NR1R2 group and when Z represents (CH2)m-NR1R2, W represents R;
each of R, R1, R2, R3 and R4 independently represents a hydrogen atom, a loweralkyl group, a cycloalkyl group, a phenyl group or a phenylloweralkyl group wherein phenyl may be substituted by one to three radicals wherein each radical independently represents a loweralkyl group, a loweralkoxy group, a cyano group, a trifluoromethyl group, a nitro group or a halogen atom or
each of R1 and R2, and R3 and R4 may, together with the adjacent nitrogen atom form the heterocyclic ring structure 1-homopiperidinyl, 1-piperidinyl, 4-morpholinyl, 1-pyrrolidinyl, 1-piperazinyl, or 4-substituted-1-piperazinyl;
with the further proviso that some meanings given for the symbols must not be realized simultaneously, as indicated specifically in claim 1, or the pharmaceutically acceptable salts thereof are useful in the treatment of cardiac arrhythmia.
通式 I 的化合物
其中
Ar 代表 1-萘基、2-萘基、2,3-二氢-1 H-茚-4(或 5)-基、2-呋喃甲基、2-吡啶基、苯基或被一至三个取代基取代的苯基,其中或每个取代基独立地代表低级烷基、一个低级烷氧基、一个低级烷氨基、一个氰基、一个低级烷硫基、一个低级烷基亚磺基、一个低级烷基磺酰基、一个酰基、一个酰氨基、一个氨基羰基、一个低级烷氨基低级烷氧基、一个三氟甲基、一个硝基或一个卤原子;
X 代表硫代基团、亚砜基团、磺酰基团或氧原子;
d 代表 0 或 1;
B 代表羰基、硫氧甲基或氰亚氨基甲基;
n、m 和 p 各自独立地代表 2 至 6(含 6)的整数
Z和W各自独立地代表一个R基团或一个
但当 Z 代表 R 时,W 代表-(CH2)m-NR1R2 基团;当 Z 代表 (CH2)m-NR1R2 时,W 代表 R;
R、R1、R2、R3 和 R4 各自独立地代表氢原子、低级烷基、环烷基、苯基或苯基低级烷基,其中苯基可被一至三个基团取代,每个基团独立地代表低级烷基、低级烷氧基、氰基、三氟甲基、硝基或卤素原子或
R1 和 R2 以及 R3 和 R4 中的每一个可与相邻的氮原子一起形成杂环结构 1-高哌啶基、1-哌啶基、4-吗啉基、1-吡咯烷基、1-哌嗪基或 4-取代-1-哌嗪基;
进一步的但书是,如权利要求 1 中特别指出的,符号的某些含义不得同时实现,或其药学上可接受的盐类可用于治疗心律失常。