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    Process for the preparation of benzo(a)quinolizidine derivatives
    2.
    发明授权
    Process for the preparation of benzo(a)quinolizidine derivatives 失效
    苯并（a）喹嗪衍生物的制备方法

    公开(公告)号：US4102886A

    公开(公告)日：1978-07-25

    申请号：US624470

    申请日：1975-10-21

    申请人： Csaba Szantay ,  Lajos Szabo ,  Laszlo Toke ,  Istvan Toth ,  Sandor Virag ,  Erzsebet Kanyo ,  Agoston David

    发明人： Csaba Szantay ,  Lajos Szabo ,  Laszlo Toke ,  Istvan Toth ,  Sandor Virag ,  Erzsebet Kanyo ,  Agoston David

    IPC分类号： C07D455/06 ,  C07D491/056 ,  C07D491/14

    CPC分类号： C07D491/14 ,  C07D455/06

    摘要： A process for the preparation of a compound of the formula I or a salt thereof ##STR1## wherein R.sup.1 and R.sup.2 each represent hydrogen or a C.sub.1-4 alkoxy group, or together form a methylenedioxy group;R.sup.3, r.sup.4, r.sup.5 and R.sup.6 are the same or different and are hydrogen or a group of the formula --CH.sub.2 --(CH.sub.2).sub.n --R.sup.7 with the proviso that at least one of the members R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is other than hydrogen; R.sup.7 is carboxyl or a carboxylic acid derivative group;N = 0.1 or 2 which comprises reacting a compound of the formula II ##STR2## with an organic secondary amine and reacting the N-amine of the formula III ##STR3## thus obtained wherein R.sup.8 and R.sup.9 each represent a C.sub.1-5 alkyl group, or together with the adjacent nitrogen atom form a 5- or 6-membered heterocyclic ring which can contain a further heteroatom, with a compound of the formula IVch.sub.2 .dbd. ch -- (ch.sub.2).sub.n -- R.sup.10 (IV)wherein R.sup.10 is a cyano or alkoxycarbonyl group.

    摘要翻译： 一种制备式I化合物或其盐的方法，其中R 1和R 2各自代表氢或C 1-4烷氧基，或一起形成亚甲二氧基; R 3，R 4，R 5和R 6相同或不同，为氢或式-CH 2 - （CH 2）n -R 7的基团，条件是至少有一个R 3，R 4，R 5和R 6不是 氢; R7是羧基或羧酸衍生物基团; N = 0.1或2，其包含用有机仲胺反应式II化合物，并使由此得到的式III的N-胺反应，其中R 8和R 9各自表示C 1-5烷基， 或者与相邻的氮原子一起形成可以含有另外的杂原子的5或6元杂环与式IV的化合物CH2 = CH-（CH2）n-R10（IV），其中R10是氰基或 烷氧基羰基。

    Benzo(a)quinolizidine derivatives
    3.
    发明授权
    Benzo(a)quinolizidine derivatives 失效
    苯并（a）喹嗪啶衍生物

    公开(公告)号：US4342871A

    公开(公告)日：1982-08-03

    申请号：US744608

    申请日：1976-11-24

    申请人： Csaba Szantay ,  Lajos Szabo ,  Laszlo Toke ,  Istvan Toth ,  Sandor Virag ,  Erzsebet Kanyo ,  Agoston David

    发明人： Csaba Szantay ,  Lajos Szabo ,  Laszlo Toke ,  Istvan Toth ,  Sandor Virag ,  Erzsebet Kanyo ,  Agoston David

    IPC分类号： C07D455/06 ,  C07D491/056 ,  C07D491/14 ,  C07D455/03 ,  A61K31/47

    CPC分类号： C07D491/14 ,  C07D455/06

    摘要： An antiphlogistic compound of the formula (I) ##STR1## or a pharmaceutically effective salt thereof wherein R.sup.1 and R.sup.2 are hydrogen or C.sub.1-4 alkoxy or together form a methylenedioxy group;R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are hydrogen or a group of the formula --CH.sub.2 --(CH.sub.2).sub.n -R.sup.7 with the proviso that at least one of R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is other than hydrogen;R.sup.7 is a carboxylic group or a carboxylic acid derivative group; n=0, 1 or 2, provided that if R.sup.3, R.sup.4 and R.sup.5 are hydrogen and R.sup.7 in the group R.sup.6 is cyano or alkoxycarbonyl, and n=1, then R.sup.1 and R.sup.2 are hydrogen, C.sub.2-4 alkoxy, or together form a methylenedioxy group.

    摘要翻译： 式（I）的消炎化合物（I）或其药学上有效的盐，其中R 1和R 2是氢或C 1-4烷氧基或一起形成亚甲二氧基; R3，R4，R5和R6是氢或式-CH2-（CH2）n-R7的基团，条件是R3，R4，R5和R6中的至少一个不是氢; R7是羧基或羧酸衍生物基团; n = 0,1或2，条件是如果R3，R4和R5是氢，R6中的R7是氰基或烷氧基羰基，n = 1，则R1和R2是氢，C2-4烷氧基或一起形成 亚甲二氧基。

    13-Thia-prostacycline derivatives
    5.
    发明授权
    13-Thia-prostacycline derivatives 失效
    13-前列环素衍生物

    公开(公告)号：US4425358A

    公开(公告)日：1984-01-10

    申请号：US370503

    申请日：1982-04-21

    申请人： Csaba Szantay ,  Lajos Novak ,  Jozsef Aszodi ,  Vilmos Simonidesz ,  Geza Galambos ,  Gabor Kovacs ,  Sandor Virag ,  Istvan Stadler ,  Peter Kormoczy

    发明人： Csaba Szantay ,  Lajos Novak ,  Jozsef Aszodi ,  Vilmos Simonidesz ,  Geza Galambos ,  Gabor Kovacs ,  Sandor Virag ,  Istvan Stadler ,  Peter Kormoczy

    IPC分类号： C07D307/935 ,  A61K31/557 ,  A61P7/02 ,  A61P9/12 ,  C07C405/00 ,  C07D307/937 ,  C07D407/12

    CPC分类号： C07D307/937 ,  C07C405/0033 ,  C07D407/12 ,  Y10S514/822

    摘要： The invention relates to new optically active or racemic 13-thia-prostacycline derivatives of the Formula I ##STR1## wherein R.sup.1 is hydrogen, a pharmaceutically acceptable cation or a straight or branched chain alkyl group having 1-5 carbon atoms;R.sup.2 is straight or branched chain alkyl having 4-9 carbon atoms or monosubstituted phenoxymethyl;--A--B-- is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- of Z-- or E-- configuration or --C.tbd.C--;one of the symbols X and Y is hydrogen, methyl or ethyl and the other is hydroxy, tetrahydropyranyoxy, 1-ethoxy-ethoxy or trialkylsilyloxy; orX and Y together form a --O--CH.sub.2 --CH.sub.2 --O-- group;Z is a sulfur atom or a --SO-- group.The compounds of the Formula I can be prepared by reacting a 13-thia-prostaglandine of the Formula III ##STR2## if desired after oxidation into the corresponding 13-oxide derivative--with a halogenating agent; and treating the 5-halogeno-13-thia-prostacycline of the Formula II ##STR3## thus obtained wherein E is halogen with an organic or inorganic base; and thereafter if desired removing the protecting groups X and/or Y and if desired converting a compound of the Formula I obtained into a salt or setting free the same from a salt. The new compounds of the Formula I possess anti-coagulant and hypotensive properties and can be used in therapy.

    摘要翻译： 本发明涉及式I的新的光学活性或外消旋的13-前列环素衍生物，其中R1是氢，可药用阳离子或具有1-5个碳原子的直链或支链烷基; R2是具有4-9个碳原子的直链或支链烷基或单取代的苯氧基甲基; -A-B-是Z-或E-构型的-CH 2 -CH 2 - ， - CH = CH-或-C 3 D C-; 符号X和Y之一是氢，甲基或乙基，另一个是羟基，四氢吡喃基氧基，1-乙氧基 - 乙氧基或三烷基甲硅烷氧基; 或X和Y一起形成-O-CH 2 -CH 2 -O-基团; Z是硫原子或-SO-基。 式I的化合物可以通过使式III的13-前 - 前列腺素（III）反应来制备。

    Process for the preparation of dimeric alkaloids
    6.
    发明授权
    Process for the preparation of dimeric alkaloids 失效
    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。

    Process for the preparation of vincaminic acid esters
    7.
    发明授权
    Process for the preparation of vincaminic acid esters 失效
    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。

    Process for the preparation of halovincamone derivatives
    8.
    发明授权
    Process for the preparation of halovincamone derivatives 失效
    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。

    Nitro derivatives of vinblastine-type bisindoles, and pharmaceutical compositions containing them
    10.
    发明授权
    Nitro derivatives of vinblastine-type bisindoles, and pharmaceutical compositions containing them 失效
    长春花碱型双吲哚的硝基衍生物和含有它们的药物组合物

    公开(公告)号：US4746665A

    公开(公告)日：1988-05-24

    申请号：US873537

    申请日：1986-06-12

    申请人： Csaba Szantay ,  Lajos Szabo ,  Katalin Honty ,  Tibor Keve ,  Tibor cs ,  Sandor Eckhardt ,  Janos Sugar ,  Zsuzsa Somfai ,  Eva Ivan ,  Zsuzsa Kneffel

    发明人： Csaba Szantay ,  Lajos Szabo ,  Katalin Honty ,  Tibor Keve ,  Tibor cs ,  Sandor Eckhardt ,  Janos Sugar ,  Zsuzsa Somfai ,  Eva Ivan ,  Zsuzsa Kneffel

    IPC分类号： A61K31/475 ,  A61P35/00 ,  C07D519/04

    CPC分类号： C07D519/04

    摘要： The invention relates to novel nitro derivatives of the general formula (I) ##STR1## wherein R.sub.1 stands for a methyl or a formyl group;R.sub.2 stands for a hydroxy or ethyl group of .beta.-position;R.sub.3 means an ethyl group of .alpha.-position;R.sub.4 represents a hydrogen atom; orR.sub.3 and R.sub.4 together represent an oxygen bridge or a double bond;R.sub.5, R.sub.6 and R.sub.7 stand for a nitro group or hydrogen atom, with the proviso that simultaneously only one of them may stand for hydrogen atom; andY stands for --N.dbd. when R.sub.5 stands for a nitro group; whereasY stands for --NH-- when R.sub.5 stands for a hydrogen atom and a valence bond exists between the C.sub.2, and C.sub.7, atoms,as well as their acid addition salts and pharmaceutical preparations containing these compounds.Further on, the invention relates to a process for preparing these compounds and preparations.The compounds of the general formula (I) show a cytostatic activity with less toxicity than that of the known vinblastine-type bis-indole alkaloid drugs which are commercially available.

    摘要翻译： 本发明涉及通式（I）的新型硝基衍生物（Ⅰ），其中R1代表甲基或甲酰基; R2代表β位的羟基或乙基; R3表示α-位的乙基; R4代表氢原子; 或R3和R4一起表示氧桥或双键; R5，R6和R7代表硝基或氢原子，条件是同时只有一个可以代表氢原子; 而Y代表-N =当R5代表硝基时; 而当R5表示氢原子且Y代表-NH-时，C2和C7原子之间存在价键，以及它们的酸加成盐和含有这些化合物的药物制剂。 此外，本发明涉及一种制备这些化合物和制剂的方法。 通式（I）的化合物显示出具有比可商购的已知长春花碱型双吲哚生物碱药物毒性小的细胞生长抑制活性。