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    Process for the isolation of alkaloid components from the plant Vinca Rosea L.
    2.
    发明授权
    Process for the isolation of alkaloid components from the plant Vinca Rosea L. 失效
    从植物中分离生物碱成分的方法长春花

    公开(公告)号：US4172077A

    公开(公告)日：1979-10-23

    申请号：US908584

    申请日：1978-05-22

    申请人： Karola Jovanovics ,  Gyorgy Fekete ,  Eszter Dezseri ,  Lajos Dancsi ,  Csaba Lorincz ,  Bela Szarvady ,  Gyorgy Dobo ,  Csaba Szantay ,  Lajos Szabo

    发明人： Karola Jovanovics ,  Gyorgy Fekete ,  Eszter Dezseri ,  Lajos Dancsi ,  Csaba Lorincz ,  Bela Szarvady ,  Gyorgy Dobo ,  Csaba Szantay ,  Lajos Szabo

    IPC分类号： C07D471/18 ,  C07D471/20 ,  C07D471/22 ,  C07D519/04 ,  C07D215/00 ,  C07G5/00

    CPC分类号： C07D519/04

    摘要： Tumor inhibiting alkaloids are recovered from Vinca Rosea L. by a method which comprises extracting the dried leaves with a solvent selected from the group consisting of an alkanol having 1 to 5 carbon atoms, a mixture of an alkanol having 1 to 5 carbon atoms and a dilute, aqueous solution, benzene and benzene homologs; subsequently purifying the alkaloid extract obtained by a phase-change method between immiscible solvents, precipitating the main amount of dimeric alkaloids in form of their sulphuric acid addition salts, isolating leurosine, vincistine, vinblastine, desacetoxy-vinblastine, N-desmethyl-vinblastine and desacetyl-vinblastine from the salt mixture obtained, and then completing the separation and isolation of the remaining alkaloids by separation and isolation by adjusting the pH-value of the mother liquor, after precipitation and removal of the salt mixture, to 5.5 to 10, extracting the solution with a water-immiscible organic solvent and separating vindoline, catharantine, 3',4' -anhydrovinblastine and leurosine from the extract by chromatography, extracting vindoline in the pH-range of 2.5 to 3.5 and catharantine 3',4'-anhydrovinblastine and leurosine in the pH-range of 5 to 6 with benzene or a benzene homologue, from the mother liquor obtained when isolating the salt mixture, and separating a mixture of leurosine and 3',4'-anhydrovinblastine by crystallization, epoxidizing this mixture with an oxygen source, or separating the mixture into its components by chromatography, and subsequently epoxidizing the 3',4'-anhydrovinblastine component to leurosine, and isolating catharantine remaining from the mother liquor obtained when separating the crystalline mixture, or separating the extract containing catharantine, 3',4'-anhydrovinblastine and leurosine into its components by chromatography.

    摘要翻译： 通过包括用选自具有1至5个碳原子的链烷醇，具有1至5个碳原子的链烷醇和1至5个碳原子的链烷醇的溶剂萃取干燥叶子的方法从长春花（Vinca Rosea L.）回收肿瘤抑制生物碱 稀释水溶液，苯和苯同系物; 随后将不相溶溶剂之间的相变法获得的生物碱提取物纯化，以其硫酸加成盐的形式沉淀出主要量的二聚生物碱，分离出白蛋白，长春新碱，长春花碱，去乙酰氧基 - 长春花碱，N-去甲基长春花碱和去乙酰基 从所得的盐混合物中分离并分离残留的生物碱，然后通过调节沉淀和除去盐混合物后的pH值，分离和分离，得到5.5〜10 溶液与水不混溶的有机溶剂混合，并通过色谱法从提取物中分离出vindoline，catharantine，3'，4'-脱氢长春花碱和leurosine，在2.5至3.5的pH范围内提取vindoline，并检测3'，4'-脱氢长春花碱和 柠檬酸在5〜6的pH范围内用苯或苯同系物，从分离盐混合物时得到的母液，和sepa 通过结晶评估白蛋白和3'，4'-脱氢长春花碱的混合物，用氧源将该混合物环氧化，或通过色谱法将该混合物分离成其组分，随后将3'，4'-脱氢长春花碱组分环氧化成亮氨酸，以及 隔离离开结晶混合物时获得的母液中残留的检疫物，或通过色谱法将含有检疫胺，3'，4'-脱氢长春花碱和酪氨酸的提取物分离成其组分。

    Process for preparation of cytostatic compounds
    3.
    发明授权
    Process for preparation of cytostatic compounds 失效
    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。

    N-Desmethyl-N-(allyloxymethyl)-vinblastine and antileukemic and antilymphomic compositions and method of treatment
    4.
    发明授权
    N-Desmethyl-N-(allyloxymethyl)-vinblastine and antileukemic and antilymphomic compositions and method of treatment 失效
    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。

    Process for the preparation of dimeric alkaloids
    5.
    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。

    Bis-indole derivatives and pharmaceutical compositions containing them
    6.
    发明授权
    Bis-indole derivatives and pharmaceutical compositions containing them 失效
    双吲哚衍生物和含有它们的药物组合物

    公开(公告)号：US4757077A

    公开(公告)日：1988-07-12

    申请号：US873540

    申请日：1986-06-12

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

    发明人： Csaba Szantay ,  Lajos Szabo ,  Katalin Honty ,  Tibor Keve ,  Tibor Acs ,  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 bis-indole derivatives of the general formula (I) ##STR1## wherein R.sub.1 stands for a hydrogen atom or an acetyl group;R.sub.2 stands for a hydrogen atom;R.sub.3 means an ethyl group of .alpha.-position; orR.sub.2 and R.sub.3 together represent an oxygen bridge;R.sub.4 represents an ethyl or hydroxyl group of .beta.-position; andR.sub.5 stands for a hydrogen atom or a hydroxyl group;A represents a C.sub.1-10 straight-chain or C.sub.3-10 branched-chain alkyl group, hydroxy-alkyl, acetyl-alkyl, benzyl, C.sub.3-6 alkenyl or alkynyl or C.sub.5-7 cycloalkyl group or an aromatic group or a heteroaromatic group containing one nitrogen or one oxygen atom, andX stands for oxygen or sulphur atom,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）的新的双吲哚衍生物：其中R1代表氢原子或乙酰基; R2代表氢原子; R3表示α-位的乙基; 或R2和R3一起表示氧桥; R4表示β-位的乙基或羟基; R5代表氢原子或羟基; A表示C 1-10直链或C 3-10支链烷基，羟基 - 烷基，乙酰基 - 烷基，苄基，C 3-6烯基或炔基或C 5-7环烷​​基或芳族基团或含杂芳基 一个氮原子或一个氧原子，X代表氧或硫原子，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。

    Process for the preparation of halovincamone derivatives
    7.
    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
    9.
    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。