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1. 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。

2. 发明授权

US4052404A Indolo (2,3-.alpha.)quinolizines 失效
标题翻译：吲哚（2,3'）喹啉
公开(公告)号：US4052404A
公开(公告)日：1977-10-04
申请号：US635092
申请日：1975-11-25
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： C07D459/00 , A61K31/404 , A61K31/435 , A61K31/4375 , A61P9/08 , C07D471/02 , C07D471/14 , C07D455/02
CPC分类号： C07D471/14 , Y10S514/929
摘要： The invention relates to new indolo-quinolizidine derivatives of the general formula (I) or salts or optically active isomers thereof, ##STR1## wherein R stands for an alkyl group, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME, AS WELL AS TO A PROCESS FOR THE PREPARATION THEREOF.The new compounds according to the invention possess vasodilatating and hypotensive effects and can be used in the therapy as medicines. The new compounds according to the invention are completely devoid of harmful side-effects.

3. 发明授权

US4329350A 1,1-Disubstituted octahydro-indolo[2,3-a]quinolizines, process for the preparation thereof and compositions containing same 失效
标题翻译： 1,1-二取代八氢 - 吲哚并[2,3-a]喹嗪，其制备方法和含有它们的组合物
公开(公告)号：US4329350A
公开(公告)日：1982-05-11
申请号：US41192
申请日：1979-05-21
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 , A61K31/437 , A61K31/4375 , A61P9/08 , C07D471/14 , A61K31/40 , C07D455/02
CPC分类号： C07D471/14 , Y10S514/929
摘要： Compounds of the formula: ##STR1## wherein R is alkyl having 1 to 6 carbon atoms;A is substituted or unsubstituted alkyl having 1 to 6 carbon atoms, aralkyl having 7 to 16 carbon atoms wherein the alkyl or aralkyl groups are unbranched in the 1-position or an acyl group derived from an aliphatic or aromatic carboxylic acid;B is hydrogen; orA and B together form an optionally substituted alkylidene having 2 to 8 carbon atoms or an aralkylidene group having 7 to 18 carbon atoms where the alkylidene and aralkylidene groups are unbranched in the 1-position or pharmaceutically acceptable salts thereof are disclosed. The compounds have vasodilating properties.
摘要翻译：下式的化合物：其中R是具有1至6个碳原子的烷基; A是取代或未取代的具有1至6个碳原子的烷基，具有7至16个碳原子的芳烷基，其中烷基或芳烷基在1-位是非支链的，或由脂族或芳族羧酸衍生的酰基; B是氢; 或A和B一起形成任选取代的具有2至8个碳原子的亚烷基或具有7至18个碳原子的芳烷叉基，其中亚烷基和亚烷叉基在1-位或其药学上可接受的盐中是无支链的。该化合物具有血管扩张性质。

4. 发明授权

US4283401A Process for the preparation of 11-bromo-vincaminic acid ester derivatives and their use in protecting animals against cerebral hypoxy 失效
标题翻译：制备11-溴 - 长春胺酸酯衍生物的方法及其在保护动物免受脑缺氧的作用
公开(公告)号：US4283401A
公开(公告)日：1981-08-11
申请号：US56647
申请日：1979-07-11
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： C07D461/00 , C07D471/22 , A61K31/55 , C07D459/00
CPC分类号： C07D461/00
摘要： A novel process for preparing 11-bromo-vincaminic acid esters of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each stand independently from each other for a C.sub.1-6 alkyl group, comprising the steps of treating a 1-alkyl-1-alkoxycarbonylethyl-octahydroindolo-quinolisine of the general formula ##STR2## wherein R.sup.2 is as defined above and R.sup.3 stands for a C.sub.1-6 alkyl group, with a brominating agent and treating the resulting isomeric mixture of the bromo-derivatives with an alkaline agent or treating the corresponding 14-oxo-E-homo-eburnane being unsubstituted in ring A with a brominating agent and nitrosating the resulting 11-bromo-14-oxo-E-homo-eburnane of the general formula ##STR3## wherein R.sup.2 is as defined above, then subjecting the resulting 11-bromo-14-oxo-15-hydroxyimino-E-homoeburnanes to deoxyimination and treating the 14,15-dioxo-derivatives obtained with a base in an alcohol of the general formula R.sup.1 OH, wherein R.sup.1 is as defined above.All the intermediate products are novel and exhibit a therapeutical protecting effect against cerebral hypoxy.
摘要翻译：一种用于制备通式为“IMAGE”的11-溴 - 长春胺酸酯的新方法，其中R 1和R 2各自独立地为C 1-6烷基独立地包括如下步骤：将1-烷基-1-烷氧基羰基乙基其中R 2如上所定义，R 3表示C 1-6烷基，与溴化剂反应，并用碱处理所得到的溴代衍生物的异构体混合物或处理环A中未取代的相应的14-氧代-E-均 - 异丁苯与溴化剂并亚硝化所得的通式为“IMAGE”的11-溴-14-氧代-E-均 - 胡烷，其中R2如上定义，然后将所得的11-溴代-14-氧代-15-羟基亚氨基-E-高硼烷进行脱氧亚胺化处理，并用在通式为R 1 OH的醇中用碱获得的14,15-二氧代衍生物进行脱氧，其中R1如上定义。所有的中间产物都是新颖的，并且对脑缺氧具有治疗保护作用。

5. 发明授权

US4278682A Vasodilating method of treatment using a indolo-quinolizine-monoester, diester or nitrile 失效
标题翻译：使用吲哚 - 喹诺酮单酯，二酯或腈的血管扩张治疗方法
公开(公告)号：US4278682A
公开(公告)日：1981-07-14
申请号：US26345
申请日：1979-04-02
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： C07D455/02 , A61K31/435 , A61K31/439 , A61P9/08 , C07D471/14 , A61K31/445
CPC分类号： C07D471/14 , Y10S514/929
摘要： Vasodilating octahydro-indolo[2,3-a]quinolizine derivatives of the formula ##STR1## wherein Q is hydrogen or an A--CH.sub.2 --CH.sub.2 -- group and A is cyano or --COOR, wherein R is C.sub.1-6 alkyl.
摘要翻译：其中Q为氢或A-CH2-CH2-基团且A为氰基或-COOR的式为“IMAGE”的血管扩张型八氢 - 吲哚并[2,3-a]喹嗪衍生物，其中R为C1-6烷基。

6. 发明授权

US4173642A Vasodilating 1,1-di-(2-methoxycarbonyl-ethyl)-1,2,3,4,5,6,12,12b-octahydro-indolo[2,3 -a]quinolizine 失效
标题翻译：血管舒张1,1-二（2-甲氧基羰基 - 乙基）-1,2,3,4,5,6,12,12b-八氢 - 吲哚并[2,3-a]喹嗪
公开(公告)号：US4173642A
公开(公告)日：1979-11-06
申请号：US865428
申请日：1977-12-29
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： C07D455/02 , A61K31/435 , A61K31/439 , A61P9/08 , C07D471/14 , C07D471/04 , A61K31/445
CPC分类号： C07D471/14 , Y10S514/929
摘要： New pharmacologically active octahydro-indolo[2,3-a]quinolizine derivatives of the formula ##STR1## wherein Q is hydrogen or an A--CH.sub.2 --CH.sub.2 -- group and A is cyano or -COOR, wherein R is C.sub.1-6 alkyl are prepared by reacting 2,3,4,6,7,12-hexahydro-indolo[2,3-a]quinolizine with a compound of the formula CH.sub.2 .dbd.CH--A, and reducing the obtained hexahydroindolo[2,3-a] quinolizine derivative of the formula ##STR2##
摘要翻译：其中Q是氢或A-CH 2 -CH 2 - 基，A是氰基或-COOR的新的药理活性的八氢 - 吲哚并[2,3-a]喹嗪衍生物，其中R是C 1-6烷基是通过使2,3,4,6,7,12-六氢 - 吲哚并[2,3-a]喹嗪与式CH 2 = CH-A的化合物反应制得，并将所得六氢吲哚并[2,3-a] 喹诺酮衍生物

7. 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。

8. 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。

9. 发明授权

US4432982A Polycyclic compounds substituted on the A-ring, pharmaceutical compositions containing them, and methods of treating psoriasis with them 失效
标题翻译：在A环上取代的多环化合物，含有它们的药物组合物，以及用它们治疗牛皮癣的方法
公开(公告)号：US4432982A
公开(公告)日：1984-02-21
申请号：US345633
申请日：1982-02-04
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Mari Zajer nee Balazs , Lilla Forgach , Egon Karpati , Arpad Kiraly , Gyongyver Kiraly nee Soos , Laszlo Szporny , Bela Rosdy
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Mari Zajer nee Balazs , Lilla Forgach , Egon Karpati , Arpad Kiraly , Gyongyver Kiraly nee Soos , Laszlo Szporny , Bela Rosdy
IPC分类号： A61K31/435 , A61K31/4375 , A61K31/475 , A61K31/585 , A61P17/00 , A61P35/00 , A61P43/00 , C07D461/00 , C12N9/99
CPC分类号： C07D461/00 , A61K31/585 , Y10S514/863
摘要： The invention relates to new polycyclic compounds substituted on the A-ring. More particularly, the invention concerns new polycyclic compounds of the formula (I) ##STR1## wherein R.sup.1 is methoxy or halogen andR.sup.2 is hydrogen; orR.sup.1 is hydrogen andR.sup.2 is halogen and acid addition salts thereof.
摘要翻译：本发明涉及在A环上取代的新的多环化合物。更具体地说，本发明涉及新的式（I）的多环化合物，其中R1是甲氧基或卤素，R2是氢; 或R 1为氢，R 2为卤素及其酸加成盐。

10. 发明授权

US4424224A Apovincaminol derivative and compositions and methods utilizing it for treating psoriasis 失效
标题翻译：氨基氨基酚衍生物及其用于治疗牛皮癣的组合物和方法
公开(公告)号：US4424224A
公开(公告)日：1984-01-03
申请号：US345632
申请日：1982-02-04
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Zsuzsanna Gyulai , Maria Zajer nee Balazs , Lilla Forgach , Egon Karpati , Arpad Kiraly , Gyongyver Kiraly nee Soos , Laszlo Szporny , Bela Rosdy
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Zsuzsanna Gyulai , Maria Zajer nee Balazs , Lilla Forgach , Egon Karpati , Arpad Kiraly , Gyongyver Kiraly nee Soos , Laszlo Szporny , Bela Rosdy
IPC分类号： A61K31/435 , A61P17/00 , A61P35/00 , A61P43/00 , C07D461/00 , C12N9/99
CPC分类号： C07D461/00 , Y10S514/863
摘要： The invention relates to the new apovincaminol-3',4',5'-trimethoxy-benzoate and acid addition salts thereof. The new compound may be prepared by reacting apovincaminol or an acid addition salt thereof with 3,4,5-trimethoxy benzoic acid or a reactive derivative thereof capable of acylation and if desired converting the compound thus obtained into an acid addition salt. The new compound of the present invention can be used in therapy in the treatment of skin diseases attached to pathological cell proliferation and in the propylaxis of such diseases.
摘要翻译：本发明涉及新的氨基嘌呤-3'，4'，5'-三甲氧基苯甲酸酯及其酸加成盐。新化合物可以通过将亚氨基胺醇或其酸加成盐与能够酰化的3,4,5-三甲氧基苯甲酸或其反应性衍生物反应并且如果需要将所得化合物转化为酸加成盐来制备。本发明的新化合物可用于治疗与病理性细胞增殖和这种疾病的丙型病症相关的皮肤病的治疗。

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