申请人:THE DU PONT MERCK PHARMACEUTICAL COMPANY
公开号:EP0373591A2
公开(公告)日:1990-06-20
Compounds of the present invention, are represented by the general formula
wherein R₁ group which may be alkyl of from 1 to about 6 carbon atoms, alkenyl of from 2 to about 6 carbon atoms, alkynyl of from 2 to about 10 carbon atoms, alkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms, halogen, acetamido, amino, nitro, alkylamino of from 1 to about 6 carbon atoms, hydroxy, hydroxyalkyl of from 1 to about 6 carbon atoms, cyano or arylalkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms R₂, R₃ and R₄ are hydrogen or hydroxyl groups or the combination of either hydrogen or hydroxyl groups; W represents alkylene of from 1 to about 10 carbon atoms; and B represents -NHCOR₅, -NHCONR₅R₆, or -NHCOOR₅ wherein R₅ and R₆ may be the same or different and represent hydrogen, alkyl of from 1 to about 6 carbon atoms, alkoxyalkyl wherein the alkyl groups may be the same or different and contain from 1 to about 6 carbon atoms, cycloalkyl of from 3 to about 8 carbon atoms, alkenyl of from 2 to about 6 carbon atoms, alkynyl of from 2 to about 6 carbon atoms, phenyl which may be unsubstituted or substituted with alkyl of 1 to 6 carbon atoms; furanyl, thiophenyl, imidazole, oxazole or indole, aralkyl wherein the alkyl group contains from 1 to about 6 carbon atoms and the aryl group represents phenyl unsubstituted or substituted with alkyl of from 1 to about 6 carbon atoms, or R₅ and R₆ may together with N form a pyrrolidine, piperidine, piperazine, morpholine or thiomorpholine ring and except that R₅ is not hydrogen when B is -NHCOOR₅; or a pharmaceutically acceptable salt thereof. The compounds are useful in the treatment or prophylaxis of cardiac disorders or in the treatment of glaucoma.
本发明的化合物由通式表示
其中 R₁ 基团可以是 1 至约 6 个碳原子的烷基、2 至约 6 个碳原子的烯基、2 至约 10 个碳原子的炔基、烷氧基(其中烷基含有 1 至约 6 个碳原子)、卤素、乙酰胺基、氨基、硝基、1 至约 6 个碳原子的烷基氨基、羟基、1 至约 6 个碳原子的羟烷基、氰基或芳基、R₂、R₃ 和 R₄ 是氢或羟基或氢或羟基的组合;W 代表 1 至约 10 个碳原子的亚烷基;B代表-NHCOR₅、-NHCONR₅R₆或-NHCOOR₅,其中R₅和R₆可以相同或不同,代表氢、1至约6个碳原子的烷基、烷氧基烷基,其中烷基可以相同或不同,含有1至约6个碳原子、3-约 8 个碳原子的环烷基、2-约 6 个碳原子的烯基、2-约 6 个碳原子的炔基、未取代或被 1-6 个碳原子的烷基取代的苯基;呋喃基、噻吩基、咪唑基、噁唑基或吲哚基、芳烷基,其中烷基含有 1 至约 6 个碳原子,芳基代表未取代的苯基或被 1 至约 6 个碳原子的烷基取代的苯基、或 R₅ 和 R₆ 可与 N 一起形成吡咯烷、哌啶、哌嗪、吗啉或硫代吗啉环,但当 B 为 -NHCOOR₅ 时,R₅ 不是氢;或其药学上可接受的盐。这些化合物可用于治疗或预防心脏疾病或治疗青光眼。