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11. 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。

12. 发明授权

US4490378A N-Desmethyl-N-(allyloxymethyl)-vinblastine and antileukemic and antilymphomic compositions and method of treatment 失效
标题翻译： N-去甲基-N-（烯丙氧基甲基） - 长春花碱和抗白血病和抗病毒组合物和治疗方法
公开(公告)号：US4490378A
公开(公告)日：1984-12-25
申请号：US503791
申请日：1983-06-13
申请人： Lajos Dancsi , Tibor Keve , Gyorgy Fekete , Eszter Dezseri , Sandor Gorog , Tibor cs , Csaba Szantay , Lajos Szabo , Katalin Honty , Sandor Eckhardt , Ivan Hindi , Sandor Kerpel-Fronius , Zsuzsanna Relle nee Somfa , Janos Sugar
发明人： Lajos Dancsi , Tibor Keve , Gyorgy Fekete , Eszter Dezseri , Sandor Gorog , Tibor cs , Csaba Szantay , Lajos Szabo , Katalin Honty , Sandor Eckhardt , Ivan Hindi , Sandor Kerpel-Fronius , Zsuzsanna Relle nee Somfa , Janos Sugar
IPC分类号： A61K31/475 , A61P35/00 , C07D519/04
CPC分类号： C07D519/04 , Y10S514/908
摘要： The invention relates to new cytostatic compound, process for their preparation and pharmaceutical compositions containing them. More particularly, there are provided new compounds of the general formula ##STR1## in which R.sup.4 is .beta.-hydroxyl andR.sup.3 is .alpha.-ethyl; orR.sup.4 is hydrogen andR.sup.3 is .beta.-ethyl;R" is a straight chained alkyl having from 1 to 10 carbon atoms, or a branched chained alkyl having from 3 to 10 carbon atoms, in which groups the carbon atom attached to the >N.sub.a --CH.sub.2 --O-- group has a primary or secondary configuration or an alkenyl or alkinyl having from 3 to 6 carbon atoms, or an aralkyl having from 1 to 3 carbon atoms in the alkyl moiety;R.sup.1 is methoxy andR.sup.2 is acetyl, provided that if R.sup.3 is .alpha.-ethyl and R.sup.4 .beta.-hydroxyl,R.sup.4 is other than ethyl.These compounds and N-desmethyl-N-(ethoxymethyl)-vinblastine can be prepared according to the invention by transetherification of compounds of the compounds of the general formula ##STR2## with a large excess of alcohols of the general formulaR"--OH [III]Pharmaceutical compositions containing compounds of the general formula [I] as active ingredients are also within the scope of invention.
摘要翻译：本发明涉及新的细胞生长抑制化合物，其制备方法和含有它们的药物组合物。更具体地，提供了通式为“IMAGE”/ I /的新化合物，其中R 4是β-羟基和R 3是α-乙基; 或R4是氢，R3是β-乙基; R“是具有1至10个碳原子的直链烷基或具有3至10个碳原子的支链烷基，其中与> Na-CH 2 -O-基团连接的碳原子具有伯或二级构型或具有3至6个碳原子的烯基或炔基，或在烷基部分具有1至3个碳原子的芳烷基; R1是甲氧基，R2是乙酰基，条件是如果R3是α-乙基和R4β-羟基，R4不是乙基。这些化合物和N-去甲基-N-（乙氧基甲基） - 长春花碱可以根据本发明通过将通式为“IMAGE”/ II /的化合物的化合物与大量过量的通式R' '-OH [III]含有通式[I]化合物作为活性成分的药物组合物也在本发明的范围内。

13. 发明授权

US4315011A 1-Alkyl-9-bromohexahydroindolo quinolizium salts and use thereof to increase blood flow 失效
标题翻译： 1-烷基-9-溴六氢吲哚喹啉盐及其用于增加血流量的用途
公开(公告)号：US4315011A
公开(公告)日：1982-02-09
申请号：US56395
申请日：1979-07-10
申请人： Csaba Szantay , Lajos Szabo , Gyoorgy Kalaus , Lajos Dancsi , Tibor Keve , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyoorgy 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： The invention is directed to 1-alkyl-9-bromohexagydro indoloquinolizium salts and a method for their use to increase blood circulation and decrease in blood vessel resistance.
摘要翻译：本发明涉及1-烷基-9-溴六氢吲哚喹啉鎓盐及其用于增加血液循环和降低血管阻力的方法。

14. 发明授权

US4410459A Process for preparation of cytostatic compounds 失效
标题翻译：细胞生长抑制化合物的制备方法
公开(公告)号：US4410459A
公开(公告)日：1983-10-18
申请号：US293611
申请日：1981-08-17
申请人： Lajos Dancsi , Tibor Keve , Lajos Szabo , Katalin Honty , Sandor Eckhardt , Ivan Hindi , Sandor Kerpel-Fronius , Gyorgy Fekete , Eszter Dezseri , Sandor Gorog , Tibor Acs , Csaba Szantay , Zsuzsanna Relle nee Somfai , Janos Sugar
发明人： Lajos Dancsi , Tibor Keve , Lajos Szabo , Katalin Honty , Sandor Eckhardt , Ivan Hindi , Sandor Kerpel-Fronius , Gyorgy Fekete , Eszter Dezseri , Sandor Gorog , Tibor Acs , Csaba Szantay , Zsuzsanna Relle nee Somfai , Janos Sugar
IPC分类号： A61K31/475 , A61P35/00 , C07D519/04
CPC分类号： C07D519/04 , Y10S514/908
摘要： The invention relates to new cytostatic compound, process for their preparation and pharmaceutical compositions containing them. More particularly, there are provided new compounds of the general formula ##STR1## in which R.sup.4 is .beta.-hydroxyl andR.sup.3 is .alpha.-ethyl; orR.sup.4 is hydrogen andR.sup.3 is .beta.-ethyl;R" is a straight chained alkyl having from 1 to 10 carbon atoms, or a branched chained alkyl having from 3 to 10 carbon atoms, in which groups the carbon atom attached to the >N.sub.a -CH.sub.2 -O-- group has a primary or secondary configuration or an alkenyl or alkinyl having from 3 to 6 carbon atoms, or an aralkyl having from 1 to 3 carbon atoms in the alkyl moiety;R.sup.1 is methoxy andR.sup.2 is acetyl,provided that if R.sup.3 is .alpha.-ethyl and R.sup.4 .beta.-hydroxyl, R.sup.4 is other than ethyl.These compounds and N-desmethyl-N- ethoxy- methyl -vinblastine can be prepared according to the invention by transetherification of compounds of the compounds of the general formula ##STR2## with a large excess of alcohols of the general formulaR"--OH (III)Pharmaceutical compositions containing compounds of the general formula /I/ as active ingredients are also within the scope of invention.
摘要翻译：本发明涉及新的细胞生长抑制化合物，其制备方法和含有它们的药物组合物。更具体地，提供了通式为（I）的新化合物，其中R 4是β-羟基并且R 3是α-乙基; 或R4是氢，R3是β-乙基; R“是具有1至10个碳原子的直链烷基或具有3至10个碳原子的支链烷基，其中与> Na-CH 2 -O-基团连接的碳原子具有伯或二级构型或具有3至6个碳原子的烯基或炔基，或在烷基部分具有1至3个碳原子的芳烷基; R1是甲氧基，R2是乙酰基，条件是如果R3是α-乙基和R4β-羟基，R4不是乙基。这些化合物和N-去甲基-N-乙氧基 - 甲基 - 长春花碱可以根据本发明通过将通式为“IMAGE”（II）的化合物的化合物与大量过量的通式R' '-OH（III）含有通式I I化合物作为活性成分的药物组合物也在本发明的范围内。

15. 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。

16. 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.

17. 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。

18. 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

19. 发明授权

US4199505A Process for the preparation of alkaloids of the leurosine type 失效
标题翻译：制备柠檬酸类生物碱的方法
公开(公告)号：US4199505A
公开(公告)日：1980-04-22
申请号：US907626
申请日：1978-05-19
申请人： Csaba Szantay , Lajos Szabo , Katalin Honty , Katalin Nogradi , Karola Jovanovics , Eszter Dezseri , Lajos Dancsi , Csaba Lorincz , Bela Szarvady , Lajos Kovacs
发明人： Csaba Szantay , Lajos Szabo , Katalin Honty , Katalin Nogradi , Karola Jovanovics , Eszter Dezseri , Lajos Dancsi , Csaba Lorincz , Bela Szarvady , Lajos Kovacs
IPC分类号： A61K31/407 , A61K31/475 , A61P35/00 , C07D471/20 , C07D519/04
CPC分类号： C07D519/04
摘要： A process for the preparation of alkaloids of the leurosine type having the formula I ##STR1## and the acid addition salts thereof. In the formula I R is hydrogen or methyl. The compounds prepared according to the invention are known compounds showing cytostatic activity.
摘要翻译：一种制备具有式I（I）的黎明酪型生物碱及其酸加成盐的方法。在式I中R 1是氢或甲基。根据本发明制备的化合物是显示出细胞抑制活性的已知化合物。

20. 发明授权

US4659816A Process for the preparation of dimeric alkaloids 失效
标题翻译：二聚生物碱的制备方法
公开(公告)号：US4659816A
公开(公告)日：1987-04-21
申请号：US688932
申请日：1985-01-04
申请人： Csaba Szantay , Katalin Honty , Lajos Szabo , Tibor Keve , Tibor cs
发明人： Csaba Szantay , Katalin Honty , Lajos Szabo , Tibor Keve , Tibor cs
IPC分类号： A61K31/475 , A61P35/00 , C07D519/04
CPC分类号： C07D519/04
摘要： A process is disclosed for the preparation of dimeric alkaloids of formula (II) ##STR1## wherein R stands for methyl or formyl, as well as acid addition salts thereof which comprises oxidizing the vinblastine of formula (III) ##STR2## with chromium (VI) oxide or bichromate or chromic acid alcohol ester in an inert solvent, converting the compound of formula (II), wherein R stands for methyl, so obtained to the acid addition salt and optionally further oxidizing the acid addition salt obtained with an oxidizing agent as defined above and optionally converting the compound of formula (II), wherein R stands for formyl, so obtained to the acid addition salt.
摘要翻译：公开了用于制备式（II）的二聚生物碱的方法，其中R代表甲基或甲酰基，以及其酸加成盐，其包括氧化式（III）的长春花碱（IMA） III）与惰性溶剂中的重铬酸铬（VI）或重铬酸盐或铬酸醇酯反应，将得到的式（II）化合物（其中R代表甲基）转化成酸加成盐，并任选地进一步氧化酸加成盐用如上定义的氧化剂获得，并任选地将所得到的式（II）化合物（其中R代表甲酰基）转化成酸加成盐。

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