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11. 发明授权

US4036841A Indolo[2,3.alpha.]quinolizine derivatives 失效
标题翻译：吲哚洛尔{8 2,3 {60 {9喹嗪衍生物
公开(公告)号：US4036841A
公开(公告)日：1977-07-19
申请号：US575038
申请日：1975-05-06
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
IPC分类号： C07D459/00 , C07D471/14
CPC分类号： C07D471/14 , Y10S514/929
摘要： Compounds of the formula ##STR1## wherein R.sub.1 stands for hydrogen or an acyl group, andR.sub.2 stands for an alkyl group are disclosed.A process for making the above compounds is also disclosed. The compounds are useful as vasodilatating agents for example.
摘要翻译：公开了其中R1代表氢或酰基，R2代表烷基的式“IMAGE”的化合物。

12. 发明授权

US4549020A Eburnane oxime ethers 失效
标题翻译：伊本安肟醚
公开(公告)号：US4549020A
公开(公告)日：1985-10-22
申请号：US508437
申请日：1983-06-27
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Sapi , Maria Zajer nee Balazs , Bela Kiss , Elemer Ezer , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Sapi , Maria Zajer nee Balazs , Bela Kiss , Elemer Ezer , Egon Karpati , Laszlo Szporny
IPC分类号： A61K31/435 , A61P25/02 , A61P25/20 , C07D461/00
CPC分类号： C07D461/00
摘要： The invention relates to optically active or racemic eburnane-oxime ethers of the formulae (Ia) and/or ##STR1## wherein R represents an alkyl group having 1 or 2 carbon atoms,R.sup.2 represents an alkyl group having 1 to 6 carbon atoms,and the configuration of the hydrogen in the 3-position and the R.sup.2 group is .alpha.,.alpha. and/or .beta.,.beta. or .alpha.,.beta. and/or .beta.,.alpha. and acid addition salts thereof.The new compounds show valuable pharmaceutical activities, thus are potent CNS-tranquillants, smooth muscle relaxants, sedatives and hypnotic agents, and can therefore be employed as active ingredients of pharmaceutical compositions, which are also within the scope of the present invention.
摘要翻译：本发明涉及式（Ia）和/或其中R表示具有1或2个碳原子的烷基的式（Ia）和/或其中R 1表示烷基的光学活性或外消旋的桦烷 - 肟醚，具有1至6个碳原子的基团，并且3-位和R2基团中的氢的构型是α，α和/或β，β或α，β和/或β，α和其酸加成盐。新化合物显示出有价值的药物活性，因此是有效的CNS-镇定剂，平滑肌松弛剂，镇静剂和催眠剂，因此可用作药物组合物的活性成分，其也在本发明的范围内。

13. 发明授权

US4456607A 9-Bromo-hexahydro- and octahydro-indolo[2,3 a]quinolizines and use for increasing blood circulation 失效
标题翻译： 9-溴 - 六氢 - 和八氢 - 吲哚并[2,3-a]喹嗪并用于增加血液循环
公开(公告)号：US4456607A
公开(公告)日：1984-06-26
申请号：US269722
申请日：1981-06-02
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Lajos Dancsi , Tibor Keve , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Lajos Dancsi , Tibor Keve , Egon Karpati , Laszlo Szporny
IPC分类号： C07D209/16 , C07D209/42 , C07D461/00 , C07D471/14 , C07D471/22 , A61K31/475 , C07D459/00
CPC分类号： C07D471/14 , C07D209/16 , C07D209/42 , C07D461/00
摘要： New salts of the formula XIIIa and XIIIb are disclosed ##STR1## wherein R.sup.2, R.sup.3 and R.sup.5 are each C.sub.1 to C.sub.6 alkyl and A.sup.- is an anion of a pharmaceutically acceptable acid. Furthermore new compounds of the formula XIVa and XIVb are disclosed: ##STR2## wherein R.sup.2 and R.sup.3 are as defined above. The new salts and compounds are intermediates in the preparation of 10-bromo-vincaminic acid esters. In addition the new salts and compounds have the ability to increase blood circulation and to decrease blood flow resistance in an animal subject while at the same time maintaining a steady pulse rate and blood pressure.
摘要翻译：公开了式XIIIa和XIIIb的新盐，其中R 2，R 3和R 5各自为C 1至C 6烷基，且A为药学上可接受的酸的阴离子。此外，还公开了新的式XIVa和XIVb的化合物：其中R2和R3如上所定义。新的盐和化合物是制备10-溴 - 长春胺酸酯的中间体。此外，新的盐和化合物具有增加动物受试者的血液循环和降低血流阻力的能力，同时保持稳定的脉率和血压。

14. 发明授权

US4089856A 1-Ethyl-1-(alkoxycarbonylethyl)-octahydro-indolo[2,3-a]quinolizines 失效
标题翻译： 1-乙基-1-（烷氧基羰基乙基） - 八氢 - 吲哚并[{2,3-a {9 quinolizines
公开(公告)号：US4089856A
公开(公告)日：1978-05-16
申请号：US699084
申请日：1976-06-23
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
IPC分类号： C07D471/04 , A61K31/435 , A61P9/06 , A61P9/08 , A61P9/12 , C07D471/14 , C07D459/00
CPC分类号： C07D471/14
摘要： Racemic and optically active 1-alkyl-1,2,3,4,6,7,12,12b-octahydro-indolo[2,3-a]quinolizines of vasodilatory and haemodynamic effect are disclosed.
摘要翻译：公开了血管扩张和血液动力学作用的外消旋和光学活性的1-烷基-1,2,3,4,6,7,12,12b-八氢 - 吲哚并[2,3-a]喹嗪。

15. 发明授权

US4057551A Indolo[2,3-a]quinolizines 失效
标题翻译：吲哚并[8-2,3-a {9 quinolizines
公开(公告)号：US4057551A
公开(公告)日：1977-11-08
申请号：US614240
申请日：1975-09-17
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
IPC分类号： C07D471/04 , A61K31/437 , C07D471/14 , C07D471/02 , C07D455/02
CPC分类号： C07D471/14 , Y10S514/929
摘要： New compounds of the general formula (I) ##STR1## wherein R stands for an alkyl group, have been prepared by reducing a compound of the general formula (II) ##STR2## wherein R stands for alkyl, B stands for H.sub.2 O or an X.sup.- anion derived from an acid, and if B is an X.sup.- anion, A represents hydrogen, whereas if B is H.sub.2 O, A represents an electron pair. If desired, the racemic compounds of the general formula (I) can be resolved to yield the corresponding optically active isomers. The free bases of the general formula (I) can be converted into their pharmaceutically acceptable salts, or the salts can be treated with an alkaline agent to yield the free bases.The compounds of the general formula (I) can be used in the therapy primarily as vasodilatating agents.
摘要翻译：通式（I）的新化合物其中R代表烷基的化合物是通过还原通式（II）的化合物（II）制备的，其中R代表烷基，B 代表H 2 O或衍生自酸的X阴离子，如果B是X-阴离子，则A表示氢，而如果B是H 2 O，则A表示电子对。如果需要，可以拆分通式（I）的外消旋化合物，得到相应的旋光异构体。通式（I）的游离碱可以转化为其药学上可接受的盐，或者盐可以用碱剂处理以产生游离碱。

16. 发明授权

US4057550A Nitrogen-containing polycyclic compounds 失效
标题翻译：含氮多环化合物
公开(公告)号：US4057550A
公开(公告)日：1977-11-08
申请号：US614239
申请日：1975-09-17
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
IPC分类号： C07D471/06 , A61K31/435 , A61K31/4375 , A61K31/439 , A61P9/08 , C07D461/00 , C07D471/02 , C07D455/02
CPC分类号： C07D461/00 , Y10S514/929
摘要： New compounds of the general formula (I) ##STR1## wherein R.sub.1 stands for alkyl and R.sub.2 stands for carboxy, a functional carboxy derivative or a group convertible into carboxy group or a functional derivative thereof, have been prepared by reducing a compound of the general formula ##STR2## wherein R.sub.1 and R.sub.2 each have the same meanings as defined above and X.sup.- represents an anion derived from an acid, and optionally subjecting the obtained compound to hydrolysis. If desired, the racemic compounds of the general formula (I) can be resolved to yield the corresponding optically active isomers. The free bases of the general formula (I) can be converted into their pharmaceutically acceptable salts, or the salts can be treated with an alkaline agent to yield the free bases.The compounds of the general formula (I) can be used in the therapy primarily as vasodilatating agents.
摘要翻译：通式（I）的新化合物其中R1代表烷基，R2代表羧基，官能羧基衍生物或可转化成羧基的基团或其官能衍生物，通过还原化合物通式（II）其中R 1和R 2各自具有与上述相同的含义，并且X代表由酸衍生的阴离子，并且任选地使得到的化合物进行水解。如果需要，可以拆分通式（I）的外消旋化合物，得到相应的旋光异构体。通式（I）的游离碱可以转化为其药学上可接受的盐，或者盐可以用碱剂处理以产生游离碱。

17. 发明授权

US4044012A Indolo-quinolizidine derivatives 失效
标题翻译：吲哚 - 喹嗪啶衍生物
公开(公告)号：US4044012A
公开(公告)日：1977-08-23
申请号：US670243
申请日：1976-03-25
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
IPC分类号： C07D471/14 , C07D459/00
CPC分类号： C07D471/14 , Y10S514/929
摘要： New compounds of the formula ##STR1## are provided wherein R.sub.1 is hydrogen, and R.sub.2 stands for an alkyl group and optically active enanthiomers and pharmaceutically acceptable salts thereof.
摘要翻译：提供新的式“IMAGE”化合物，其中R 1是氢，R 2代表烷基和光学活性的对映异构体及其药学上可接受的盐。

18. 发明授权

US4054571A Nitrogen-containing polycyclic compounds and a process for the preparation thereof 失效
标题翻译：含氮多环化合物及其制备方法
公开(公告)号：US4054571A
公开(公告)日：1977-10-18
申请号：US614151
申请日：1975-09-17
申请人： Csaba Szantay , Lajor Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajor Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
IPC分类号： C07D471/06 , A61K31/4375 , A61K31/4745 , C07D461/00 , C07D471/04
CPC分类号： C07D461/00
摘要： The invention relates to new eburnamenine derivatives of the general formula (I), ##STR1## wherein R.sub.1 stands for an alkyl group,R.sub.2 stands for a carboxy group, a functional carboxy derivative (preferably an ester group) or a group convertable into carboxy group or a functional derivative thereof (preferably cyano group), andX.sup.- is an anion derived from an acid,And the corresponding free bases.These compounds are valuable intermediates of the preparation of eburnamenine derivatives with advantageous therapeutical effects.The above compounds are prepared as follows: a compound of the general formula (II), ##STR2## wherein R.sub.1 has the same meanings as defined above, is reacted with a compound of the general formula (III), ##STR3## wherein R.sub.2 has the same meanings as defined above and Y is halogen, and, if desired, a thus-obtained compound of the general formula (I), wherein R.sub.1 and R.sub.2 each have the same meanings as defined above and X.sup.- is a halide ion, is reacted with an acid, and/or, if desired, a compound of the general formula (I), wherein R.sub.1 and X.sup.- each have the same meanings as defined above and R.sub.2 is cyano or an ester group, is subjected to hydrolysis, and/or, if desired, a compound of the general formula (I), wherein R.sub.1, R.sub.2 and X.sup.- each have the same meanings as defined above, is treated with a base.
摘要翻译：本发明涉及通式（I），其中R1代表烷基，R2代表羧基，官能羧基衍生物（优选酯基）或可转化基团的新颖的本本母胺衍生物羧基或其功能性衍生物（优选氰基），X是衍生自酸的阴离子，和相应的无碱基。

19. 发明授权

US4464534A Process for the preparation of vincaminic acid esters 失效
标题翻译：用于制备长春酸酯的方法
公开(公告)号：US4464534A
公开(公告)日：1984-08-07
申请号：US425866
申请日：1982-09-28
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Kreidl , Andras Nemes , Maria Farkas nee Kirjak , Gyorgy Visky , Laszlo Czibula
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Kreidl , Andras Nemes , Maria Farkas nee Kirjak , Gyorgy Visky , Laszlo Czibula
IPC分类号： C07D461/00 , C07D455/00
CPC分类号： C07D461/00
摘要： The invention relates to a new process for the preparation of apovincaminic acid esters. More particularly, the invention concerns a process for preparing racemic and optionally active vincaminic acid esters of the formula (I) ##STR1## in which R.sup.1 and R.sup.2 independently stand for alkyl having from one to 6 carbon atoms, and 14-epimers thereof.According to the invention an octahydroindolo[2,3-a]quinolizine-oxime ester of the formula (II) ##STR2## in which R.sup.1 and R.sup.2 have the same meaning as defined above, is reacted with an aqueous solution of sulfurous acid or a salt thereof at a temperature of 80.degree. to 110.degree. C. and the 14-epimeric mixture obtained is epimerized or separated in a known manner and if desired, the racemic vincaminic acid esters are resolved.The valuable, pharmaceutically active compounds of the formula (I) can be prepared according to the invention in a considerably improved yield and the undesired side reactions can be suppressed and/or the by-products can easily be converted into other pharmaceutically active materials.
摘要翻译：本发明涉及一种用于制备氨磷酸酯的新方法。更具体地说，本发明涉及一种制备式（I）的外消旋和任选活性的长春胺酸酯的方法，其中R 1和R 2独立代表具有1至6个碳原子的烷基，和14-差向异构体其中。根据本发明，其中R 1和R 2具有与上述相同的含义的式（II）的二氢吲哚并[2,3-a]喹嗪肟酯与其中的亚硫酸酯水溶液酸或其盐，并且所得的14-差向异构体混合物以已知方式进行差向异构化或分离，如果需要，外消旋的长春碱酯被分解。式（I）的有价值的药物活性化合物可以按照本发明以显着提高的产量制备，并且可以抑制不期望的副反应和/或副产物可以容易地转化成其它药物活性物质。

20. 发明授权

US4356305A Process for the preparation of halovincamone derivatives 失效
标题翻译：制备Halovincone酮衍生物的方法
公开(公告)号：US4356305A
公开(公告)日：1982-10-26
申请号：US175384
申请日：1980-08-05
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Lajos Dancsi , Tibor Keve , Ferenc Drexler
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Lajos Dancsi , Tibor Keve , Ferenc Drexler
IPC分类号： A61K31/435 , A61P9/08 , C07D461/00
CPC分类号： C07D461/00
摘要： The invention relates to new halovincamone derivatives of the general formula (I), ##STR1## wherein R is a C.sub.1-6 alkyl group and X is halogen, and pharmaceutically acceptable acid addition salts and optically active isomers thereof. These compounds possess valuable vasodilating effect, and can be applied to advantage in the therapy.The new compounds defined above are prepared according to the invention so that a single epimer or an epimeric mixture of a racemic or optically active halogenated 14-oxo-15-hydroxy-E-homoeburnane derivative of the general formula (II), ##STR2## wherein R and X are as defined above, or an acid addition salt thereof is treated with an oxidizing agent, and, if desired, the resulting compound of the general formula (I) is converted into its pharmaceutically acceptable acid addition salt and/or resolved.
摘要翻译：本发明涉及通式（I）的新的Halovincone酮衍生物，其中R是C 1-6烷基，X是卤素的化合物及其药学上可接受的酸加成盐和旋光异构体。这些化合物具有有价值的血管扩张作用，可用于治疗中的优势。根据本发明制备上述新化合物，使得通式（II）的外消旋或光学活性的卤代14-氧代-15-羟基-E-高拜尔班恩衍生物的单个差向异构体或差向异构体混合物（II）其中R和X如上所定义，或其酸加成盐用氧化剂处理，如果需要，将所得的通式（I）化合物转化为其药学上可接受的酸加成盐和 /或解决。

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