公开(公告)号：US4365064A

公开(公告)日：1982-12-21

申请号：US196583

申请日：1980-10-14

申请人： Kalman Takacs ,  Ilona Kiss nee Ajzert ,  Antal Simay ,  Peter Literati Nagy ,  Maria Hetyey nee Papp ,  Marian Ecsery nee Puskas ,  Laszlo Szekeres ,  Gyula Papp ,  Sandor Viragh ,  Eva Udvardy

发明人： Kalman Takacs ,  Ilona Kiss nee Ajzert ,  Antal Simay ,  Peter Literati Nagy ,  Maria Hetyey nee Papp ,  Marian Ecsery nee Puskas ,  Laszlo Szekeres ,  Gyula Papp ,  Sandor Viragh ,  Eva Udvardy

IPC分类号： C07D413/06 ,  A61K20060101 ,  A61K31/41 ,  A61K31/415 ,  A61K31/42 ,  A61K31/435 ,  A61K31/47 ,  A61K31/475 ,  A61P9/08 ,  C07D20060101 ,  C07D217/00 ,  C07D217/04 ,  C07D217/16 ,  C07D271/00 ,  C07D271/06 ,  C07D273/04 ,  C07D401/06

CPC分类号： A61K31/41 ,  A61K31/415 ,  A61K31/42 ,  A61K31/435 ,  A61K31/47 ,  A61K31/475 ,  C07D217/00 ,  C07D217/04 ,  C07D217/16 ,  C07D271/00 ,  C07D271/06 ,  C07D273/04 ,  C07D401/06 ,  C07D413/06 ,  Y10S514/929 ,  Y10S514/96 ,  Y10S514/962

摘要： The invention concerns new compounds of the formula (I) ##STR1## wherein R.sup.1 is hydrogen, phenyl or phenyl substituted with at least one 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, phenyl, or phenyl substituted with at least one alkyl having 1 to 4 carbon atoms, halogen, alkoxy having 1 to 4 carbon atoms or nitro;R.sup.3 is alkoxy having 1 to 4 carbon atoms or hydrogen,R.sup.4 is hydrogen, alkyl having 1 to 4 carbon atoms unsubstituted or substituted with alkoxy having 1 to 4 carbon atoms, benzyloxy or cyano, phenyl, or phenyl substituted with at least one alkyl having 1 to 4 carbon atoms, halogen, alkoxy having 1 to 4 carbon atoms or nitro, or phenyl-(C.sub.1-4 alkyl)-alkyl, in which the phenyl moiety may bear an alkoxy substituent having 1 to 4 carbon atoms or a halogen;m and n are each 0, 1 or 2 or a pharmaceutically acceptable acid addition or quaternary salt thereof.The compounds are potent vasodilators and exert a favorable influence on the extremital blood flow. They also show a heart function influencing activity.Methods for the preparation of said compounds and pharmaceutical compositions containing them are also the subject of the invention.

摘要翻译： 本发明涉及新的式（I）化合物，其中R 1是氢，苯基或被至少一个具有1-4个碳原子的烷基取代的苯基，卤素，具有1-4个碳原子的烷氧基 或硝基; R2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，苯基或被至少一个具有1至4个碳原子的烷基取代的苯基，卤素，具有1至4个碳原子的烷氧基或硝基; R3为具有1-4个碳原子的烷氧基或氢，R4为氢，未取代或未被取代或未被取代或未被取代的具有1-4个碳原子的烷氧基的烷基，苄氧基或氰基，苯基或被至少一个具有至少一个烷基 1至4个碳原子，卤素，具有1至4个碳原子的烷氧基或硝基，或苯基 - （C 1-4烷基） - 烷基，其中苯基部分可以带有具有1至4个碳原子的烷氧基取代基或卤素; m和n各自为0,1或2，或其药学上可接受的酸加成盐或季盐。 这些化合物是有效的血管扩张剂，对前列腺血流量有很好的影响。 它们也显示出影响活动的心脏功能。 制备所述化合物的方法和含有它们的药物组合物也是本发明的主题。

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。

公开(公告)号：US4187220A

公开(公告)日：1980-02-05

申请号：US829148

申请日：1977-08-30

申请人： Kalman Takacs ,  Peter N. Literati ,  Ilona Kiss nee Ajzert ,  Antal Simay ,  Matyas Szentivanyi ,  Sandor Virag ,  Katalin Farago

发明人： Kalman Takacs ,  Peter N. Literati ,  Ilona Kiss nee Ajzert ,  Antal Simay ,  Matyas Szentivanyi ,  Sandor Virag ,  Katalin Farago

IPC分类号： C07C259/14 ,  C07C259/18 ,  C07D211/28 ,  C07D213/42 ,  C07D215/12 ,  C07D217/14 ,  C07D231/12 ,  C07D295/088 ,  C07D295/14 ,  C07D401/12 ,  C07D403/12

CPC分类号： C07D231/12 ,  C07C259/14 ,  C07C259/18 ,  C07D211/28 ,  C07D213/42 ,  C07D215/12 ,  C07D217/14 ,  C07D295/088

摘要： A compound effective in the treatment of diabetic angiopathy, i.e. a selective .beta.-receptor blocker has the formula ##STR1## wherein: R.sup.2 is a hydrogen or alkyl having one to five carbon atoms, R.sup.3 is alkyl having one to five carbon atoms, cycloalkyl or phenyl optionally substituted with hydroxyl or phenyl, or R.sup.2 and R.sup.3 together form a five- to eight-membered ring optionally containing also other heteroatoms and/or fused with an other ring, preferably phenyl, naphthyl, quinolyl, isoquinolyl, pyridyl, pyrazolyl, R.sup.5 is hydrogen or alkyl having one to four carbon atoms, cycloalkyl or phenyl optionally substituted with halogen, alkoxy having one to four carbon atoms or alkyl having one to four carbon atoms, R.sup.6 is hydrogen, alkyl having one to four carbon atoms or phenyl, m=0, 1 or 2, and n=0, 1 or 2.

摘要翻译： 治疗糖尿病性血管病的化合物，即选择性β-受体阻断剂具有下式（I）其中：R 2是氢或具有1至5个碳原子的烷基，R 3是具有1至5个碳原子的烷基 任选地被羟基或苯基取代的环烷基或苯基，或者R 2和R 3一起形成任选地还含有其它杂原子和/或与另一个环稠合的五至八元环，优选苯基，萘基，喹啉基，异喹啉基，吡啶基， 吡唑基，R5是氢或具有1-4个碳原子的烷基，环烷基或任选被卤素取代的苯基，具有1-4个碳原子的烷氧基或具有1-4个碳原子的烷基，R6是氢，具有1-4个碳原子的烷基或 苯基，m = 0,1或2，n = 0,1或2。

公开(公告)号：US4308399A

公开(公告)日：1981-12-29

申请号：US54791

申请日：1979-07-05

申请人： Kalman Takacs ,  Peter N. Literati ,  Ilona Kiss nee Ajzert ,  Antal Simay ,  Matyas Szentivanyi ,  Sandor Virag ,  Katalin Farago

发明人： Kalman Takacs ,  Peter N. Literati ,  Ilona Kiss nee Ajzert ,  Antal Simay ,  Matyas Szentivanyi ,  Sandor Virag ,  Katalin Farago

IPC分类号： C07C259/14 ,  C07C259/18 ,  C07D211/28 ,  C07D213/42 ,  C07D215/12 ,  C07D217/14 ,  C07D231/12 ,  C07D295/088 ,  C07D295/14 ,  C07D401/12 ,  C07D403/12

CPC分类号： C07D231/12 ,  C07C259/14 ,  C07C259/18 ,  C07D211/28 ,  C07D213/42 ,  C07D215/12 ,  C07D217/14 ,  C07D295/088

摘要： A compound effective in the treatment of diabetic angiopathy, i.e. a selective .beta.-receptor blocker has the formula ##STR1## wherein: R.sup.2 is a hydrogen or alkyl having one to five carbon atoms,R.sup.3 is alkyl having one to five carbon atoms, cycloalkyl or phenyl optionally substituted with hydroxyl or phenyl, or R.sup.2 and R.sup.3 together form a five- to eight-membered ring optionally containing also other heteroatoms and/or fused with another ring, preferably phenyl, naphthyl, quinolyl, isoquinolyl, pyridyl, pyrazolyl,R.sup.5 is hydrogen or alkyl having one to four carbon atoms, cycloalkyl or phenyl optionally substituted with halogen, alkoxy having one to four carbon atoms or alkyl having one to four carbons,R.sup.6 is hydrogen, alkyl having one to four carbon atoms or phenyl, m=0, 1 or 2, and n=0, 1 or 2.

摘要翻译： 治疗糖尿病性血管病的化合物，即选择性β-受体阻断剂具有下式（I）其中：R 2是氢或具有1至5个碳原子的烷基，R 3是具有1至5个碳原子的烷基 ，任选被羟基或苯基取代的环烷基或苯基，或者R 2和R 3一起形成任选地还含有其它杂原子和/或与另一个环稠合的五至八元环，优选苯基，萘基，喹啉基，异喹啉基，吡啶基，吡唑基 R5是氢或具有1-4个碳原子的烷基，环烷基或任选被卤素取代的苯基，具有1-4个碳原子的烷氧基或具有1-4个碳原子的烷基，R6是氢，具有1-4个碳原子的烷基或苯基， m = 0,1或2，n = 0,1或2。