公开(公告)号：EP0202774A3

公开(公告)日：1989-03-15

申请号：EP86302934.4

申请日：1986-04-18

申请人： RICHTER GEDEON VEGYESZETI GYAR R.T.

发明人： Szántay, Csabe ,  Sóti, Ferenc ,  Incze, Maria ,  Balogh, Zsuzsanna ,  Szombathelyi, Zsolt ,  Kárpáti, Egon ,  Kiss, Béla ,  Csomor, Katalin ,  Laszlovszky, Istvan ,  Lapis, Erzsébet ,  Forgács, Lilla ,  Kuthi, Csaba ,  Szporny, László

IPC分类号： C07D471/14 ,  A61K31/44

CPC分类号： C07D401/06 ,  C07D209/16 ,  C07D471/14

摘要： The invention relates to new racemic and optically active 1,12b-disubstituted octahydroindolo[2,3- alquinolizine derivatives of formula (I)
wherein
R 1 and R 2 are the same or different and represent hydrogen, halogen, nitro, alkyl having from 1 to 6 carbon atoms, alkoxy having from 1 to 6 carbon atoms or hydroxyl, R" and R 5 are the same or different and represent hydrogen, alkyl having from to 6 carbon atoms or aralkyl having from 1 to 6 carbon atoms in the alkyl moiety, R 4 is alkyl having from 1 to 6 carbon atoms, aryl or aralkyl having from 1 to 6 carbon atoms in the alkyl moiety, and R 6 is an electron attracting substituent, and cis and trans isomers and acid addition salts thereof. The compounds are pharmaceutically active, in particular they show an outstanding cardiovascular, e.g. selective peripheral vasodilating activity. Some of these compounds are valuable intermediates in the preparation of other, pharmaceutically active compounds.

公开(公告)号：EP0202774A2

公开(公告)日：1986-11-26

申请号：EP86302934.4

申请日：1986-04-18

申请人： RICHTER GEDEON VEGYESZETI GYAR R.T.

发明人： Szántay, Csabe ,  Sóti, Ferenc ,  Incze, Maria ,  Balogh, Zsuzsanna ,  Szombathelyi, Zsolt ,  Kárpáti, Egon ,  Kiss, Béla ,  Csomor, Katalin ,  Laszlovszky, Istvan ,  Lapis, Erzsébet ,  Forgács, Lilla ,  Kuthi, Csaba ,  Szporny, László

IPC分类号： C07D471/14 ,  A61K31/44

CPC分类号： C07D401/06 ,  C07D209/16 ,  C07D471/14

摘要： The invention relates to new racemic and optically active 1,12b-disubstituted octahydroindolo[2,3- alquinolizine derivatives of formula (I)
wherein

R 1 and R 2 are the same or different and represent hydrogen, halogen, nitro, alkyl having from 1 to 6 carbon atoms, alkoxy having from 1 to 6 carbon atoms or hydroxyl,
R" and R 5 are the same or different and represent hydrogen, alkyl having from to 6 carbon atoms or aralkyl having from 1 to 6 carbon atoms in the alkyl moiety,
R 4 is alkyl having from 1 to 6 carbon atoms, aryl or aralkyl having from 1 to 6 carbon atoms in the alkyl moiety, and
R 6 is an electron attracting substituent, and cis and trans isomers and acid addition salts thereof.

The compounds are pharmaceutically active, in particular they show an outstanding cardiovascular, e.g. selective peripheral vasodilating activity. Some of these compounds are valuable intermediates in the preparation of other, pharmaceutically active compounds.

摘要翻译： 本发明涉及式（I）的新的外消旋和旋光活性的1,12b-二取代的八氢吲哚并[2,3-喹喔啉衍生物，其中R 1和R 2相同或不同且代表氢，卤素，硝基，具有1至6 碳原子，具有1至6个碳原子的烷氧基或羟基，R“和R5相同或不同，代表氢，烷基部分具有6至6个碳原子的烷基或具有1至6个碳原子的芳烷基，R4是 具有1至6个碳原子的烷基，在烷基部分具有1至6个碳原子的芳基或芳烷基，并且R 6是吸电子取代基，以及其顺式和反式异构体及其酸加成盐。 特别是它们表现出优异的心血管功能，例如选择性的外周血管舒张活性。这些化合物中的一些是制备其它药物活性化合物的有价值的中间体。