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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

US4746665A Nitro derivatives of vinblastine-type bisindoles, and pharmaceutical compositions containing them 失效
标题翻译：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。

4. 发明授权

US4753948A Furfuryl derivatives of vinblastine-type bis-indoles, and pharmaceutical compositions containing them 失效
标题翻译：长春花碱型双吲哚的糠基衍生物和含有它们的药物组合物
公开(公告)号：US4753948A
公开(公告)日：1988-06-28
申请号：US873525
申请日：1986-06-12
申请人： Csaba Szantay , Lajos Szabo , Katalin Honty , Tibor Keve , Tibor Acs , Sandor Eckhardt , Janos Sugar , Zsuzsa Somjai , Eva Ivan , Zsuzsa Kneffel
发明人： Csaba Szantay , Lajos Szabo , Katalin Honty , Tibor Keve , Tibor Acs , Sandor Eckhardt , Janos Sugar , Zsuzsa Somjai , 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 furfuryl 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 hydroxyl 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; andB stands for a hydroxyl of an O-acyl group, 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 commerically available known vinblastine-type bis-indole alkaloid drugs.
摘要翻译：本发明涉及通式（I）的新颖糠基衍生物，其中R1代表氢原子或乙酰基，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R4一起代表氧桥; B表示O-酰基的羟基，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）的化合物显示出比商业上可获得的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。

5. 发明授权

US4757077A Bis-indole derivatives and pharmaceutical compositions containing them 失效
标题翻译：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。

6. 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。

7. 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。

8. 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。

9. 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）

10. 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。

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