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61. 发明授权

US4481204A E-Homo-eburnane derivatives, process for their preparation, and pharmaceutical compositions containing these compounds 失效
标题翻译： E-Homo-eburnane衍生物，其制备方法和含有这些化合物的药物组合物
公开(公告)号：US4481204A
公开(公告)日：1984-11-06
申请号：US509150
申请日：1983-06-29
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Sapi , Eva Palosi , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Sapi , Eva Palosi , Egon Karpati , Laszlo Szporny
IPC分类号： C07D471/22 , A61K31/395 , C07D459/00 , C07D461/00
CPC分类号： C07D471/22
摘要： The invention relates to racemic or optically active E-homo-eburnane derivatives of the formula /I/, ##STR1## wherein R.sup.1 and R.sup.2 independently represent an alkyl group having 1 to 6 carbon atoms,and acid addition salts thereof.The new compounds are pharmaceutically active, for example their certain representatives, in particular from the cis-series, show antidepressive activity, while others, especially the compounds of the trans-series, are potent anthypoxial agents. The compounds of the formula /I/ and pharmaceutically acceptable acid addition salts thereof can therefore be employed as active ingredients of pharmaceutical compositions.
摘要翻译：本发明涉及式/ I /，其中R 1和R 2独立地表示具有1至6个碳原子的烷基的式/ I /，/ IMAGE / I / C的外消旋或光学活性的E-均 - burn烷衍生物及其酸加成盐。新化合物是药学上活性的，例如它们的特定代表，特别是顺式的化合物显示出抗抑郁活性，而其它代表，特别是反式系列的化合物是有效的抗氧化剂。因此，式/ I /的化合物及其药学上可接受的酸加成盐可用作药物组合物的活性成分。

62. 发明授权

US4464535A Process for the preparation of eburnamonine derivatives 失效
标题翻译：制备苯丙胺衍生物的方法
公开(公告)号：US4464535A
公开(公告)日：1984-08-07
申请号：US438288
申请日：1982-11-01
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Kreidl , Gyorgy Visky , Andras Nemes , Laszlo Czibula , Maria Farkas nee Kirjak
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Kreidl , Gyorgy Visky , Andras Nemes , Laszlo Czibula , Maria Farkas nee Kirjak
IPC分类号： C07D461/00 , C07D471/14 , C07D455/00
CPC分类号： C07D471/14 , C07D461/00
摘要： The invention relates to a new process for the preparation of eburnamonine derivatives of the general Formula I ##STR1## (wherein R.sup.1 is an alkyl group having 1-6 carbon atoms) and optical and geometrical isomers thereof which comprises reacting a hydroxyimino-octahydro-indolo[2,3-a]quinolizine derivative of the general Formula II ##STR2## (wherein R.sup.1 is as stated above and R.sup.2 stands for an alkyl group having 1-6 carbon atoms being identical with or different from R.sup.1, or a hydrogen atom) or an acid addition salt thereof in an organic protic solvent or solvent mixture with an inorganic base, optionally under the addition of water or an aqueous mineral acid, at a temperature between 60.degree. C. and 200.degree. C.The compounds of the present invention are known drugs having blood pressure decreasing and cerebral vasodilatatory effect. The advantage of the process of the present invention is that it is readily feasible on industrial scale too, provides isomer-free pure products with high yield and requires the use of readily available simple starting materials.
摘要翻译：本发明涉及一种制备通式Ⅰ（I）（Ⅰ）（其中R1是具有1-6个碳原子的烷基）及其光学和几何异构体的本发明化合物的新方法，其包括使羟基亚氨基 - 通式II的八氢 - 吲哚并[2,3-a]喹嗪衍生物（II）（其中R 1如上所述，R 2表示具有1-6个碳原子的烷基，与R 1相同或不同），或氢原子）或其酸加成盐在无机碱的有机质子溶剂或溶剂混合物中，任选在水或无机酸水溶液中，在60℃至200℃的温度下进行。本发明的化合物是具有降血压和脑血管扩张作用的已知药物。本发明方法的优点是在工业规模上也容易实现，提供高产率的无异构体纯产品，并且需要使用容易获得的简单起始原料。

63. 发明授权

US4446139A Hexahydroindoloquinolizinium and octahydroindoloquinolizine esters, and method of increasing blood flow in an animal with hydroxyamino-eburnane derivatives 失效
标题翻译：六氢吲哚喹啉鎓和八氢二吲哚喹啉酯，以及用羟基氨基 - 伊本恩衍生物增加动物血流量的方法
公开(公告)号：US4446139A
公开(公告)日：1984-05-01
申请号：US351506
申请日：1982-02-23
申请人： Csaba Szantay , Lajos Szbao , Gyorgy Kalaus , Janos Sapi , Lajos Dancsi , Tibor Keve
发明人： Csaba Szantay , Lajos Szbao , Gyorgy Kalaus , Janos Sapi , Lajos Dancsi , Tibor Keve
IPC分类号： C07D461/00 , C07D471/14 , A61K31/435 , C07D455/00
CPC分类号： C07D471/14 , C07D461/00
摘要： The invention relates to new hydroxyamino-eburnane derivatives of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each stand for a C.sub.1-6 alkyl group, as well as to pharmaceutically acceptable acid addition salts and optically active isomers of these compounds.These new compounds can be applied as peripheral vasodilatating agents or can be converted into other compounds, e.g. vincamine and apovincamine derivatives, of valuable therapeutical effects.The compounds of the general formula (I) are prepared according to the invention by reacting a hexahydro-indoloquinolisinium derivative of the general formula (II), ##STR2## wherein R.sup.2 is as defined above and X stands for an acid residue, with a methylenemalonic acid diester derivative of the general formula (III), ##STR3## wherein R.sup.1 is as defined above, subjecting the resulting product to catalytic hydrogenation, treating the resulting product with an alkali, and reacting the resulting octahydroindoloquinolisine monoester derivative with a nitrosating agent in an acidic medium.
摘要翻译：本发明涉及通式（I）的新型羟基氨基 - 伊本烷衍生物，其中R1和R2各自表示C1-6烷基，以及药学上可接受的酸加成盐和旋光异构体的这些化合物。这些新化合物可以作为外周血管舒张剂使用，也可以转化为其它化合物，例如长春胺和氨肽素衍生物，具有宝贵的疗效。通式（I）的化合物根据本发明通过使通式（II）的六氢 - 吲哚并喹啉鎓衍生物，其中R 2如上定义，X代表酸残基，与通式（III）的亚甲基丙二酸二酯衍生物，其中R1如上所定义，使所得产物进行催化氢化，用碱处理所得产物，并使所得八氢二吲哚并喹啉酮单酯衍生物在酸性介质中使用亚硝化剂。

64. 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。

65. 发明授权

US4399069A Process for an enantioselective synthesis of optically active 14-oxo-E-homo-eburnane derivatives 失效
标题翻译：光学活性的14-氧代 - 均 - 伊本恩衍生物的对映选择性合成方法
公开(公告)号：US4399069A
公开(公告)日：1983-08-16
申请号：US312128
申请日：1981-10-16
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Sapi , Janos Kreidl , Maria Farkas nee Kirjak , Andras Nemes , Laszlo Cibula
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Sapi , Janos Kreidl , Maria Farkas nee Kirjak , Andras Nemes , Laszlo Cibula
IPC分类号： C07D461/00 , C07D471/14 , C07D471/22
CPC分类号： C07D471/14
摘要： The invention relates to a new enantioselective synthesis for the preparation of optically active 14-oxo-E-homo-eburnane derivatives of the formula (Ia) ##STR1## wherein R.sup.1 is alkyl having from 1 to 4 carbon atom. In the synthesis optically active 6-alkoxycarbonylhexahydroindoloquinolizinium salts are employed as starting materials, which contain a center of chirality at the site of attachment of the carboxyl group. This center of chirality preserves the optical activity of the optically active tryptophan ester from which this compound has been prepared until a new center of chirality is formed in the molecule in a configuration corresponding to the desired end product. The carboxyl group, which is not needed in the end product and only serves to preserving the optical activity can then be eliminated.Compounds of the formula (Ia) are known in the art and may be used in the synthesis of (+)-vincamine and (+)-apovincaminic acid ethylester.
摘要翻译：本发明涉及用于制备式（Ia）的光学活性的14-氧代-E-高 - 同型异烟酸衍生物的新的对映选择性合成。其中R 1是具有1至4个碳原子的烷基。在合成光学活性中，使用6-烷氧基羰基六氢吲哚喹啉鎓盐作为起始原料，其在羧基连接位点含有手性中心。该手性中心保留了光学活性色氨酸酯的光学活性，从该化合物已经制备出光学活性，直至在分子中形成对应于所需最终产物的构型的新的手性中心。然后可以消除最终产物中不需要的仅用于保持光学活性的羧基。式（Ia）的化合物是本领域已知的，可用于合成（+） - 长春胺和（+） - 氨基丁酸乙酯。

66. 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）

67. 发明授权

US4210650A Antiphlogistic method of treatment 失效
标题翻译：消炎治疗方法
公开(公告)号：US4210650A
公开(公告)日：1980-07-01
申请号：US13271
申请日：1979-02-21
申请人： Csaba Szantay , Lajos Szabo , Laszlo Toke , Istvan Toth , Sandor Virag , Erzsebet Kanyo , Agoston David
发明人： Csaba Szantay , Lajos Szabo , Laszlo Toke , Istvan Toth , Sandor Virag , Erzsebet Kanyo , Agoston David
IPC分类号： C07D455/06 , A61K31/47
CPC分类号： C07D455/06
摘要： 2-oxo-3-(.beta.-cyanoethyl)-9,10-methylenedioxy-1,2,3,4,6,7-hexahydro-11bH-benzo(a)quinolizidine (SC-118) especially and the corresponding 9,10-diethoxy compound are superior antiphlogistics which are used in effective amounts in antiphlogistic therapy.
摘要翻译：特别是2-氧代-3-（β-氰基乙基）-9,10-亚甲二氧基-1,2,3,4,6,7-六氢-11H-苯并（a）喹唑啶（SC-118）和相应的9 ，10-二乙氧基化合物是有效量用于消炎治疗的优良消炎药。

68. 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。

69. 发明授权

US4036841A Indolo[2,3.alpha.]quinolizine derivatives 失效
标题翻译：吲哚洛尔{8 2,3 {60 {9喹嗪衍生物
公开(公告)号：US4036841A
公开(公告)日：1977-07-19
申请号：US575038
申请日：1975-05-06
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
IPC分类号： C07D459/00 , C07D471/14
CPC分类号： C07D471/14 , Y10S514/929
摘要： Compounds of the formula ##STR1## wherein R.sub.1 stands for hydrogen or an acyl group, andR.sub.2 stands for an alkyl group are disclosed.A process for making the above compounds is also disclosed. The compounds are useful as vasodilatating agents for example.
摘要翻译：公开了其中R1代表氢或酰基，R2代表烷基的式“IMAGE”的化合物。

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