公开(公告)号：US4308270A

公开(公告)日：1981-12-29

申请号：US196034

申请日：1980-10-10

申请人： Kalman Takacs ,  Antal Simay ,  Ilona Kiss nee Ajzert ,  Peter L. Nagy ,  Maria Hetyey nee Papp ,  Marian Escery nee Puskas ,  Jozsef Szegy ,  Sandor Virag ,  Sandor J. Nagy

发明人： Kalman Takacs ,  Antal Simay ,  Ilona Kiss nee Ajzert ,  Peter L. Nagy ,  Maria Hetyey nee Papp ,  Marian Escery nee Puskas ,  Jozsef Szegy ,  Sandor Virag ,  Sandor J. Nagy

IPC分类号： A61K31/535 ,  A61P7/10 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P29/00 ,  C07D273/04 ,  C07D413/06

CPC分类号： C07D273/04 ,  Y10S514/821 ,  Y10S514/869

摘要： The invention concerns new compounds of the general formula (I) ##STR1## wherein R.sup.1 is hydrogen or phenyl optionally substituted by one or more of the following substituents: alkyl having 1 to 4 carbon atoms, halogen, alkoxy having 1 to 4 carbon atoms or nitro;R.sup.2 is alkyl having 1 to 4 carbon atoms, cycloalkyl having 5 to 7 carbon atoms or phenyl, optionally substituted with one or more of the following groups: alkyl having 1 to 4 carbon atoms, halogen, alkoxy having 1 to 4 carbon atoms or nitro; or R.sup.2 is a naphthyl group;R.sup.3 is alkyl having 1 to 4 carbon atoms, acyl or hydrogen;R.sup.4 hydrogen or alkyl having 1 to 4 carbon atoms;R.sup.5 is cycloalkyl having 5 to 7 carbon atoms, alkyl having 1 to 6 carbon atoms, phenyl-(C.sub.1-4 -alkyl) in which the phenyl moiety may optionally be substituted with alkoxy having 1 to 4 carbon atoms, halogen or nitro;or R.sup.4 and R.sup.5 together represent a group of the general formula (V) ##STR2## wherein R.sup.6 is hydrogen or alkoxy having 1 to 4 carbon atoms, m and n stand for 0, 1 or 2and acid addition and quaternary salts thereof.The compounds of the general formula (I) are potent peripheral vasodilators and hypotensive agents. They increase the coronary blood flow and in addition to their slight antiinflammatory and diuretic acidivity possess strong antiarrhythmic properties.A process for the preparation of these compounds and pharmaceutical compositions containing them are also within the scope of the invention.

摘要翻译： 本发明涉及通式（I）的新化合物其中R 1为氢或任选被一个或多个下述取代基取代的苯基：具有1-4个碳原子的烷基，卤素，具有1-4个碳原子的烷氧基 碳原子或硝基; R 2是具有1至4个碳原子的烷基，具有5至7个碳原子的环烷基或苯基，任选被一个或多个下列基团取代：具有1至4个碳原子的烷基，卤素，具有1至4个碳原子的烷氧基或硝基 ; 或R 2为萘基; R3是具有1-4个碳原子的烷基，酰基或氢; R4是氢或具有1-4个碳原子的烷基; R5是具有5至7个碳原子的环烷基，具有1至6个碳原子的烷基，苯基部分可任选地被具有1至4个碳原子的烷氧基取代的苯基 - （C 1-4 - 烷基），卤素或硝基; 或者R 4和R 5一起表示通式（V）的基团，其中R 6是氢或具有1至4个碳原子的烷氧基，m和n代表0,1或2，酸加成和季盐 其中。 通式（I）的化合物是有效的外周血管扩张剂和降压药。 它们增加冠状动脉血流量，除了其轻微的抗炎和利尿酸性之外，具有强烈的抗心律失常性质。 制备这些化合物的方法和含有它们的药物组合物也在本发明的范围内。