专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 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。

3. 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。

4. 发明授权

US4172077A Process for the isolation of alkaloid components from the plant Vinca Rosea L. 失效
标题翻译：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。

5. 发明授权

US4070358A Process for the preparation of diindole alkaloids or of the acid addition salts thereof 失效
标题翻译：二吲哚生物碱或其酸加成盐的制备方法
公开(公告)号：US4070358A
公开(公告)日：1978-01-24
申请号：US735004
申请日：1976-10-22
申请人： Karola Jovanovics , Kalman Szasz , Csaba Lorincz , Laszlo Hermann , Eszter Dezseri
发明人： Karola Jovanovics , Kalman Szasz , Csaba Lorincz , Laszlo Hermann , Eszter Dezseri
IPC分类号： A61K31/404 , A61K31/475 , A61K36/24 , C07D519/04
CPC分类号： C07D519/04
摘要： A process is disclosed for the separation and recovery of vinblastine and leurosine from a mixture of diindole alkaloids obtained by extraction of the plant, Vinca rosea L.
摘要翻译：公开了从通过提取植物获得的二吲哚生物碱的混合物中分离和回收长春花碱和亮氨酸的方法，即长春花

6. 发明授权

US4189432A N-formyl and N-desmethyl leurosine derivatives 失效
标题翻译： N-甲酰基和N-去甲基柠檬酸衍生物
公开(公告)号：US4189432A
公开(公告)日：1980-02-19
申请号：US422100
申请日：1973-12-05
申请人： Karola Jovanovics , Kalman Szasz , Bela Kellner , Laszlo Nemeth , Zsuzsa Relle , Emil Bittner , Eszter Dezseri , Janos Eles
发明人： Karola Jovanovics , Kalman Szasz , Bela Kellner , Laszlo Nemeth , Zsuzsa Relle , Emil Bittner , Eszter Dezseri , Janos Eles
IPC分类号： A61K31/475 , A61P35/00 , C07D519/00 , C07D519/04
CPC分类号： C07D519/04 , Y10S514/883
摘要： Leurosine derivatives of the formula (I), ##STR1## wherein R is hydrogen or formyl, or pharmaceutically acceptable acid addition salts thereof were prepared by oxidizing leurosine or an acid addition salt thereof, optionally formylating the thus-obtained product and then separating, and, if desired, converting any of the free bases into its acid addition salt. The new compounds of the invention possess strong cytostatic activity, and can be used in the human therapy with great advantage.
摘要翻译：通过氧化酪氨酸或其酸加成盐制备其中R为氢或甲酰基的式（I），其中R为氢或甲酰基的式（I）的Leurosine衍生物或其药学上可接受的酸加成盐，任选地将如此获得的产物甲酰化，然后如果需要，将任何游离碱转化成其酸加成盐。本发明的新化合物具有强的细胞生长抑制活性，可用于人类治疗中，具有很大的优势。

7. 发明授权

US4279816A N-Formyl leurosine derivatives in a dosage form effective for treating lymphoid leukemia 失效
标题翻译：可以有效治疗淋巴样白血病的剂型中的N-甲酰基赖氨酸衍生物
公开(公告)号：US4279816A
公开(公告)日：1981-07-21
申请号：US547374
申请日：1975-02-05
申请人： Karola Jovanovics , Kalman Szasz , Bela Kellner , Laszlo Nemeth , Zsuzsa Relle , Emil Bittner , Eszter Dezseri , Janos Eles
发明人： Karola Jovanovics , Kalman Szasz , Bela Kellner , Laszlo Nemeth , Zsuzsa Relle , Emil Bittner , Eszter Dezseri , Janos Eles
IPC分类号： C07D519/04 , A61K31/475
CPC分类号： C07D519/04
摘要： New leurosine derivatives of the general formula (1), ##STR1## wherein R stands for hydrogen or formyl, or pharmaceutically acceptable acid addition salts thereof were prepared by oxidizing leurosine or an acid addition salt thereof, optionally formylating the thus-obtained product and then separating, and, if desired, converting any of the free bases into its acid addition salt.
摘要翻译：通过氧化酪氨酸或其酸加成盐来制备通式（1）的新的赖氨酸衍生物，其中R代表氢或甲酰基，或其药学上可接受的酸加成盐，任选地将由此得到的然后分离，并且如果需要，将任何游离碱转化成其酸加成盐。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式