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1. 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。

2. 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。

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

US4356305A Process for the preparation of halovincamone derivatives 失效
标题翻译：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。

6. 发明授权

US4428877A Cis-10-bromo-E-homoeburnanes 失效
标题翻译：顺式-10-溴-E-高乙炔二醇
公开(公告)号：US4428877A
公开(公告)日：1984-01-31
申请号：US234577
申请日：1981-02-13
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 , C07D459/00
CPC分类号： C07D471/14 , C07D209/16 , C07D209/42 , C07D461/00
摘要： A novel process for preparing 10-bromo-vincaminic acid esters and homologous compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each stand for a C.sub.1-6 alkyl group is disclosed.All the intermediate products are new and exhibit valuable therapeutical effect on the blood circulation.
摘要翻译：公开了一种制备10-溴 - 长春胺酸酯和通式为“IMAGE”的同系化合物的新方法，其中R1和R2各自代表C1-6烷基。所有的中间产品都是新的，对血液循环具有宝贵的治疗作用。

7. 发明授权

US4285865A Process for the preparation of halogenated 15-hydroxy-E-homoeburnane compounds 失效
标题翻译：制备卤代的15-羟基-E-高硼烷化合物的方法
公开(公告)号：US4285865A
公开(公告)日：1981-08-25
申请号：US175385
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： C07D461/00 , A61K31/4375 , A61P9/08 , C07D471/22 , C07D487/14 , C07D487/16
CPC分类号： C07D471/22
摘要： The invention relates to new, racemic or optically active, halogenated 15-hydroxy-E-homoeburnane derivatives of the general formula (Ia) and/or (Ib), ##STR1## wherin R is a C.sub.1-6 alkyl group and X is halogen, and acid addition salts thereof. These compounds are biologically active, furthermore they can be applied as intermediates in the synthesis of other pharmaceutically active substances.The compounds of the general formulae (Ia) and (Ib) are prepared by halogenating the respective racemic or optically active 15-hydroxy-E-homoeburnane derivative of the general formula (II), wherein R is as defined above. ##STR2##
摘要翻译：本发明涉及通式（Ia）和/或（Ib）的新的外消旋或光学活性的卤代的羟基 - 均聚乙二醇衍生物，其中R是 C 1-6烷基，X为卤素，及其酸加成盐。这些化合物是生物活性的，此外它们可以作为其它药物活性物质合成中的中间体使用。通式（Ia）和（Ib）的化合物通过卤化通式（II）的各自的外消旋或光学活性的15-羟基-E-高硼烷衍生物而制备，其中R定义如上。（二）

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

US4429129A 1.alpha.-Ethyl-1.beta.-(2'-alkoxy carbonyl-2'-hydroxyiminoethyl)-10-methoxy 1,2,3,4,6,7,12,12.beta.-octahydroindolo(2,3A)quinolizines 失效
标题翻译： 1α-乙基-1β-（2'-烷氧基羰基-2'-羟基亚氨基乙基）-10-甲氧基1,2,3,4,6,7,12,12β-八氢吲哚（2,3A）喹嗪
公开(公告)号：US4429129A
公开(公告)日：1984-01-31
申请号：US410052
申请日：1982-08-20
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Tibor Keve , Lajos Dancsi , Janos Galambos , Ferenc Vezekenyi , Tibor Acs
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Tibor Keve , Lajos Dancsi , Janos Galambos , Ferenc Vezekenyi , Tibor Acs
IPC分类号： C07D461/00 , C07D471/14 , C07D471/22 , C07D459/00
CPC分类号： C07D471/14 , C07D461/00
摘要： The invention relates to a new process for the preparation of alkoxyvincaminic acid esters of the formula (I) ##STR1## and/or alkoxyapovincaminic acid esters of the formula (II) ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 independently stand for alkyl groups having from one to 6 carbon atoms.The compounds of the formulae (I) and (II) are pharmaceutically active, thus some of them show psychostimulant activity.
摘要翻译：本发明涉及一种制备式（I）的烷氧基氨基酸酯和式（II）的烷氧基氨基酸酯的新方法，其中R1，R2和R3 独立地代表具有1至6个碳原子的烷基。式（I）和（II）的化合物是药学活性的，因此它们中的一些显示出精神兴奋作用。

10. 发明授权

US4400514A Process for the preparation of apovincaminic acid ester derivatives 失效
标题翻译：氨基丁酸酯衍生物的制备方法
公开(公告)号：US4400514A
公开(公告)日：1983-08-23
申请号：US209265
申请日：1980-11-21
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Lajos Dancsi , Tibor Keve , Ferenc Drexler , Krisztina Mihalyfi
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Lajos Dancsi , Tibor Keve , Ferenc Drexler , Krisztina Mihalyfi
IPC分类号： B01J23/00 , C07B61/00 , C07D461/00 , C07D471/22
CPC分类号： C07D461/00
摘要： The invention concerns a new process for the preparation of apovincaminic acid ester derivatives of the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 independently represent an alkyl group having 1 to 6 carbon atoms,and pharmaceutically acceptable salts thereof.According to the invention the apovincaminic acid ester derivatives of the general formula (I) are prepared by reacting the corresponding 9- and/or 10- and/or 11-halo-14-oxo-15-hydroxyimino-E-homo-eburnane derivatives with an alkanol of the general formula R.sup.1 --OH, wherein R.sup.1 is as defined above, and with a dehydrating concentrated acid, and subsequently reducing the 9- and/or 10- and/or 11-halo-apovincaminic acid esters obtained, selectively on the aromatic ring. Alternatively, the 9- and/or 10- and/or 11-halo-apovincaminic acid esters can also be used as starting materials. The invention includes the preparation of racemic and optically active apovincaminic acid ester derivatives and of their pharmaceutically acceptable salts, as well.
摘要翻译：本发明涉及一种制备通式（I）的氨基苯甲酸酯衍生物的新方法，其中R1和R2独立地表示具有1至6个碳原子的烷基，及其药学上可接受的盐。根据本发明，通式（I）的氨基亚氨酸酯衍生物通过相应的9-和/或10-和/或11-卤代-14-氧代-15-羟基亚氨基-E-高 - 伊本恩衍生物与通式R 1 -OH的烷醇，其中R 1如上定义，并与脱水浓酸反应，然后选择性地将所得的9-和/或10-和/或10-卤代 - 氨基丁酸酯还原芳香环。或者，9-和/或10-和/或11-卤代 - 氨基丁酸酯也可以用作原料。本发明还包括外消旋和光学活性氨肽酸酯衍生物及其药学上可接受的盐的制备。

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