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1. 发明授权

US4474960A Apovincaminic acid esters 失效
标题翻译：氨基丁酸酯
公开(公告)号：US4474960A
公开(公告)日：1984-10-02
申请号：US387676
申请日：1982-06-11
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Kreidl , Laszlo Czibula , Gyorgy Visky , Andras Nemes , Maria Farkas nee Kirlyak
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Kreidl , Laszlo Czibula , Gyorgy Visky , Andras Nemes , Maria Farkas nee Kirlyak
IPC分类号： C07B57/00 , C07D461/00 , C07D471/14 , A61K31/475
CPC分类号： C07D471/14 , C07D461/00
摘要： A process is disclosed for the preparation of racemic cis or trans apovincaminic acid esters of the formula (I) ##STR1## and the corresponding optically active derivatives of the formulae (Ia) ##STR2## wherein R.sup.1 and R.sup.2 are identical or different alkyl groups having 1 to 6 carbon atoms. Apovincaminic acid alkyl esters are well-known vasodilating compounds.
摘要翻译：公开了一种制备式（I）的外消旋顺式或反式亚氨基酸酯和式（Ia）和/或（Ib）的相应的光学活性衍生物的方法。（Ⅰb）和/或（Ⅰc）（Ⅰc）和（ⅰ）其中R1和R2是具有1-6个碳原子的相同或不同的烷基。氨基丁酸烷基酯是众所周知的血管扩张化合物。

2. 发明授权

US4464534A Process for the preparation of vincaminic acid esters 失效
标题翻译：用于制备长春酸酯的方法
公开(公告)号：US4464534A
公开(公告)日：1984-08-07
申请号：US425866
申请日：1982-09-28
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Kreidl , Andras Nemes , Maria Farkas nee Kirjak , Gyorgy Visky , Laszlo Czibula
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Kreidl , Andras Nemes , Maria Farkas nee Kirjak , Gyorgy Visky , Laszlo Czibula
IPC分类号： C07D461/00 , C07D455/00
CPC分类号： C07D461/00
摘要： The invention relates to a new process for the preparation of apovincaminic acid esters. More particularly, the invention concerns a process for preparing racemic and optionally active vincaminic acid esters of the formula (I) ##STR1## in which R.sup.1 and R.sup.2 independently stand for alkyl having from one to 6 carbon atoms, and 14-epimers thereof.According to the invention an octahydroindolo[2,3-a]quinolizine-oxime ester of the formula (II) ##STR2## in which R.sup.1 and R.sup.2 have the same meaning as defined above, is reacted with an aqueous solution of sulfurous acid or a salt thereof at a temperature of 80.degree. to 110.degree. C. and the 14-epimeric mixture obtained is epimerized or separated in a known manner and if desired, the racemic vincaminic acid esters are resolved.The valuable, pharmaceutically active compounds of the formula (I) can be prepared according to the invention in a considerably improved yield and the undesired side reactions can be suppressed and/or the by-products can easily be converted into other pharmaceutically active materials.
摘要翻译：本发明涉及一种用于制备氨磷酸酯的新方法。更具体地说，本发明涉及一种制备式（I）的外消旋和任选活性的长春胺酸酯的方法，其中R 1和R 2独立代表具有1至6个碳原子的烷基，和14-差向异构体其中。根据本发明，其中R 1和R 2具有与上述相同的含义的式（II）的二氢吲哚并[2,3-a]喹嗪肟酯与其中的亚硫酸酯水溶液酸或其盐，并且所得的14-差向异构体混合物以已知方式进行差向异构化或分离，如果需要，外消旋的长春碱酯被分解。式（I）的有价值的药物活性化合物可以按照本发明以显着提高的产量制备，并且可以抑制不期望的副反应和/或副产物可以容易地转化成其它药物活性物质。

3. 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。

4. 发明授权

US4735946A Eburnane derivatives, process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：伊本恩衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US4735946A
公开(公告)日：1988-04-05
申请号：US718917
申请日：1985-04-02
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Kreidl , Maria Farkas nee Kirjak , Laszlo Czibula , Bela Stefko , Gyorgy Visky , Judit Meszaros nee Brill
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Kreidl , Maria Farkas nee Kirjak , Laszlo Czibula , Bela Stefko , Gyorgy Visky , Judit Meszaros nee Brill
IPC分类号： A61K31/435 , A61P25/00 , A61P25/08 , B01J31/00 , B01J31/04 , C07B61/00 , C07D461/00 , C07D471/14 , A61K31/44
CPC分类号： C07D461/00
摘要： The invention relates to new eburnane derivatives of the formula (I) ##STR1## wherein R.sup.1 is alkyl having from 1 to 6 carbon atoms, and acid addition salts thereof.The invention further relates to a process for the preparation of these compounds and pharmaceutical compositions containing them.Compounds of formula (I) show remarkable CNS-activity and are useful intermediates in the preparation of other, pharmaceutically active compounds.
摘要翻译：本发明涉及式（I）的新的伊本恩衍生物，其中R1是具有1至6个碳原子的烷基，及其酸加成盐。本发明还涉及制备这些化合物的方法和含有它们的药物组合物。式（I）化合物显示出显着的CNS活性，并且是制备其它药学活性化合物的有用中间体。

5. 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。

6. 发明授权

US5122607A Racemic and optically active octahydro-indolo(2,3-a) tetrahydropyranyl (2,3-c) quinolizine diester derivatives and process for preparing the same 失效
标题翻译：（2,3-A）四氢呋喃（2,3-C）喹啉衍生物及其制备方法
公开(公告)号：US5122607A
公开(公告)日：1992-06-16
申请号：US542485
申请日：1990-06-21
申请人： Janos Kreidl , Csaba Szantay , Lajos Szaho , Maria Farkas nee Kirjak , Gyorgy Kalaus , Katalin Nogradi , Andras Nemes , Judit Meszaros nee Brill , Zsuzsanna Aracs nee Tischler , Bela Stefko , Janos Sapi , Ida Deutsch nee Juhasz , Istvan Hegedus , Bela Benke , Kalman Graf , Kalmam Gaf , Katalin Horvath nee Berki
发明人： Janos Kreidl , Csaba Szantay , Lajos Szaho , Maria Farkas nee Kirjak , Gyorgy Kalaus , Katalin Nogradi , Andras Nemes , Judit Meszaros nee Brill , Zsuzsanna Aracs nee Tischler , Bela Stefko , Janos Sapi , Ida Deutsch nee Juhasz , Istvan Hegedus , Bela Benke , Kalman Graf , Kalmam Gaf , Katalin Horvath nee Berki
IPC分类号： C07D461/00 , C07D471/14 , C07D491/22
CPC分类号： C07D471/14 , C07D461/00
摘要： New intermediate compounds are disclosed of the formula I, ##STR1## wherein R.sub.1 and R.sub.2 are independently alkyl having 1 to 4 carbon atoms,or acid-addition salts thereof of formula Ib, ##STR2## wherein X represents an acid residue, and a process for the preparation of the intermediate compounds.
摘要翻译：公开了新的中间体化合物，其中R 1和R 2独立地为具有1至4个碳原子的烷基，或其酸式加成盐，其中X代表酸残基，中间体化合物的制备方法。

7. 发明授权

US5707976A Substituted propane-2-OL derivatives 失效
标题翻译：取代的丙烷-2-OL衍生物
公开(公告)号：US5707976A
公开(公告)日：1998-01-13
申请号：US605052
申请日：1996-03-04
申请人： Janos Kreidl , Csaba Szantay , Laszlo Czibula , Maria nee Kirjak Farkas , Ida nee Juhasz Deutsch , Mihaly Szegedi , Istvan Hegedus
发明人： Janos Kreidl , Csaba Szantay , Laszlo Czibula , Maria nee Kirjak Farkas , Ida nee Juhasz Deutsch , Mihaly Szegedi , Istvan Hegedus
IPC分类号： A61K31/695 , A61P31/04 , A61P31/10 , C07F7/18
CPC分类号： C07F7/1856
摘要： Anti-Fungal compounds are disclosed of the Formula (I) ##STR1## wherein R.sup.1 is C.sub.1 to C.sub.10 alkyl, phenyl, or phenyl-C.sub.1 to C.sub.6 alkyl, and the phenyl moiety of the two latter groups may carry at least one substituent selected from the group consisting of a halogen atom, C.sub.1 to C.sub.6 alkoxy group, phenyl group, phenoxy group, and trifluorome thyl group; R.sup.2 is a hydrogen atom, a C.sub.1 to C.sub.10 alkyl group or a phenyl group; R.sup.3 and R.sup.4 are independently from each other a C.sub.1 to C.sub.10 alkyl group or a phenyl group; X is a hydrogen atom, halogen atom or a group of the formula (A) ##STR2## and in this formula Y.sup.1 and Y.sup.2 are independently from each other, a --N.dbd. atom or a group of the formula --CH.dbd., or an optical antipode thereof.
摘要翻译： PCT No.PCT / HU94 / 00040 Sec。 371日期：1996年3月4日 102（e）1996年3月4日PCT PCT 1994年9月22日PCT公布。出版物WO95 / 08552 日期：1995年3月30日公开了式（I）的化合物：其中R 1为C 1至C 10烷基，苯基或苯基-C 1至C 6烷基，并且后两个基团的苯基部分可以携带至少一个选自卤素原子，C1-C6烷氧基，苯基，苯氧基和三氟甲基三基的取代基; R2是氢原子，C1〜C10烷基或苯基; R 3和R 4彼此独立地为C 1至C 10烷基或苯基; X是氢原子，卤素原子或式（A）基团（A），在该式中Y1和Y2彼此独立地是-N =原子或式-CH = ，或其光学对映体。

8. 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。

9. 发明授权

US4052404A Indolo (2,3-.alpha.)quinolizines 失效
标题翻译：吲哚（2,3'）喹啉
公开(公告)号：US4052404A
公开(公告)日：1977-10-04
申请号：US635092
申请日：1975-11-25
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 , A61K31/404 , A61K31/435 , A61K31/4375 , A61P9/08 , C07D471/02 , C07D471/14 , C07D455/02
CPC分类号： C07D471/14 , Y10S514/929
摘要： The invention relates to new indolo-quinolizidine derivatives of the general formula (I) or salts or optically active isomers thereof, ##STR1## wherein R stands for an alkyl group, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME, AS WELL AS TO A PROCESS FOR THE PREPARATION THEREOF.The new compounds according to the invention possess vasodilatating and hypotensive effects and can be used in the therapy as medicines. The new compounds according to the invention are completely devoid of harmful side-effects.

10. 发明授权

US4345082A Process for the preparation of hydroxyamino-eburnane derivatives and octahydroindoloquinolizine intermediates 失效
标题翻译：羟基氨基 - 伊本烷衍生物和八氢吲哚喹啉中间体的制备方法
公开(公告)号：US4345082A
公开(公告)日：1982-08-17
申请号：US154329
申请日：1980-05-29
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Sapi , Lajos Dancsi , Tibor Keve , Maria Gazdac
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Sapi , Lajos Dancsi , Tibor Keve , Maria Gazdac
IPC分类号： C07D459/00 , A61K31/435 , A61K31/4375 , A61K31/475 , A61P9/08 , C07D461/00 , C07D471/14 , C07D455/00
CPC分类号： C07D471/14 , C07D461/00 , Y10S514/929
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，例如长春胺和氨基丁胺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R 1如上定义，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。

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