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1. 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。

2. 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。

3. 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。

4. 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。

5. 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。

6. 发明授权

US4419522A Hexitols containing free carboxy groups and a process for the preparation thereof 失效
标题翻译：含有游离羧基的己糖醇及其制备方法
公开(公告)号：US4419522A
公开(公告)日：1983-12-06
申请号：US315182
申请日：1981-10-26
申请人： Ilona Elekes , Laszlo Institoris , Kalman Medzihradsz , Laszlo tvos , Hedvig Medzihradszky-Schweiger , Katalin De Gleria , Janos Sugar , Somfai Relle , Sandor Eckhardt , Ivan Hidy , Sandor Kerpel-Fronius
发明人： Ilona Elekes , Laszlo Institoris , Kalman Medzihradsz , Laszlo tvos , Hedvig Medzihradszky-Schweiger , Katalin De Gleria , Janos Sugar , Somfai Relle , Sandor Eckhardt , Ivan Hidy , Sandor Kerpel-Fronius
IPC分类号： C07C69/003 , A61K31/22 , A61K31/225 , A61K31/335 , A61K31/336 , A61P35/00 , A61P35/02 , C07D303/16 , C07D407/12 , C07C69/63 , C07C69/635 , C07C69/65 , C07C69/653 , C07C69/657
CPC分类号： C07D303/16
摘要： The invention relates to new hexitols having the general formula (I) and (II), ##STR1## wherein the hexitol skeleton is dulcitol, mannitol or iditol,X represents halogen, preferably bromine,R is a saturated or unsaturated C.sub.4-10 alkylcarbonyl group which also contains a free carboxy group, andR.sup.1 is hydrogen, a saturated or unsaturated C.sub.4-10 alkylcarbonyl group which also contains a free carboxy group, a saturated or unsaturated C.sub.2-10 alkylcarbonyl group, a saturated or unsaturated C.sub.4-10 alkylcarbonyl group which also contains an alkoxycarbonyl group, or a saturated or unsaturated C.sub.8-10 aralkylcarbonyl group,and salts of these compounds. The new compounds according to the invention have tumor-inhibiting affects.The above compounds are prepared according to the invention so that(a) a compound of the general formula (IX), whereinthe hexitol skeleton is dulcitol, mannitol or iditol,Q is a saturated or unsaturated C.sub.11-17 alkylcarbonyl group which also contains a benzyloxycarbonyl group, andQ.sup.1 is hydrogen, a saturated or unsaturated C.sub.2-10 alkylcarbonyl group, a saturated or unsaturated C.sub.4-10 alkylcarbonyl group which also contains an alkoxycarbonyl group, a saturated or unsaturated C.sub.11-17 alkylcarbonyl group which also contains a benzyloxycarbonyl group, or a saturated or unsaturated C.sub.8-10 aralkylcarbonyl group, is hydrogenated in an anhydrous solvent in the presence of a weakly active catalyst which does not affect the epoxide ring, or(b) a 1,2-5,6-dianhydrohexitol of the general formula (X), wherein the hexitol skeleton is dulcitol, mannitol or iditol, is reacted with a dicarboxylic acid anhydride of the general formula (XI), wherein A is a C.sub.2-10 alkyl, aralkyl or aryl group, or(c) a compound of the general formula (I) is reacted with an alkali halide and/or hydrogen halide. ##STR2##
摘要翻译：本发明涉及具有通式（I）和（II）的新己二醇，其中己糖醇骨架是杜尔醇醇，甘露糖醇或甘油，X代表卤素，优选溴，R是饱和或不饱和的C 4-10烷基羰基其还含有游离的羧基，并且R 1是氢，也含有游离羧基，饱和或不饱和的C 2-10烷基羰基的饱和或不饱和C 4-10烷基羰基，饱和或不饱和的C 4-10烷基羰基，还含有烷氧基羰基，或饱和或不饱和的C 8-10芳烷基羰基，以及这些化合物的盐。根据本发明的新化合物具有肿瘤抑制作用。根据本发明制备上述化合物，使得（a）通式（Ⅸ）的化合物，其中己糖醇骨架是二糖醇，甘露糖醇或甘露糖醇，Q是饱和或不饱和的C 11-17烷基羰基，其还含有苄氧基羰基，Q 1为氢，饱和或不饱和的C 2-10烷基羰基，饱和或不饱和的还含有烷氧基羰基的C 4-10烷基羰基，也含有苄氧基羰基的饱和或不饱和C 11-17烷基羰基，或饱和或不饱和的C 8-10芳烷基羰基在无影响环氧化物环的弱活性催化剂的存在下，在无水溶剂中氢化，或（b）一般的1,2-5,6-二脱水己糖醇式（X）其中己糖醇骨架是杜尔醇醇，甘露糖醇或甘油，与通式（XI）的二羧酸酐反应，其中A是C 2-10烷基，芳烷基或芳基，或（c）组合和通式（I）的化合物与碱金属卤化物和/或卤化氢反应。

7. 发明授权

US4209443A Process for separating pharmaceutically active diindole alkaloids 失效
标题翻译：用于分离药物活性二吲哚生物碱的方法
公开(公告)号：US4209443A
公开(公告)日：1980-06-24
申请号：US882418
申请日：1978-03-01
申请人： Karola Jovanovics , Lajos Dancsi , Sandor Eckhardt , Csaba Lorincz , Janos Sugar , Zsuzsa Relle nee Somfai , Kalman Szasz , Jozsef Tamas , Aron Szollosy
发明人： Karola Jovanovics , Lajos Dancsi , Sandor Eckhardt , Csaba Lorincz , Janos Sugar , Zsuzsa Relle nee Somfai , Kalman Szasz , Jozsef Tamas , Aron Szollosy
IPC分类号： C07D519/04
CPC分类号： C07D519/04 , Y10S514/851
摘要： A mixture of minor diindole alkaloids from Vinca-containing vinblastine and 4-deacetoxy-vinblastine vines, are separated by subjecting the mixture to a deacetylation to correct the vinblastine to deacetyl-vinblastine prior to chromatographic separation of said mixture in a single stage.
摘要翻译：在将单一阶段色谱分离之前，将来自长春花碱的长春花碱和4-脱乙酰氧基 - 长春花碱葡萄藤的小二萜生物碱混合物分离，使混合物脱乙酰化以将长春花碱修饰成脱乙酰基长春花碱。

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