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51. 发明授权

US4057551A Indolo[2,3-a]quinolizines 失效
标题翻译：吲哚并[8-2,3-a {9 quinolizines
公开(公告)号：US4057551A
公开(公告)日：1977-11-08
申请号：US614240
申请日：1975-09-17
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： C07D471/04 , A61K31/437 , C07D471/14 , C07D471/02 , C07D455/02
CPC分类号： C07D471/14 , Y10S514/929
摘要： New compounds of the general formula (I) ##STR1## wherein R stands for an alkyl group, have been prepared by reducing a compound of the general formula (II) ##STR2## wherein R stands for alkyl, B stands for H.sub.2 O or an X.sup.- anion derived from an acid, and if B is an X.sup.- anion, A represents hydrogen, whereas if B is H.sub.2 O, A represents an electron pair. If desired, the racemic compounds of the general formula (I) can be resolved to yield the corresponding optically active isomers. The free bases of the general formula (I) can be converted into their pharmaceutically acceptable salts, or the salts can be treated with an alkaline agent to yield the free bases.The compounds of the general formula (I) can be used in the therapy primarily as vasodilatating agents.
摘要翻译：通式（I）的新化合物其中R代表烷基的化合物是通过还原通式（II）的化合物（II）制备的，其中R代表烷基，B 代表H 2 O或衍生自酸的X阴离子，如果B是X-阴离子，则A表示氢，而如果B是H 2 O，则A表示电子对。如果需要，可以拆分通式（I）的外消旋化合物，得到相应的旋光异构体。通式（I）的游离碱可以转化为其药学上可接受的盐，或者盐可以用碱剂处理以产生游离碱。

52. 发明授权

US4057550A Nitrogen-containing polycyclic compounds 失效
标题翻译：含氮多环化合物
公开(公告)号：US4057550A
公开(公告)日：1977-11-08
申请号：US614239
申请日：1975-09-17
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： C07D471/06 , A61K31/435 , A61K31/4375 , A61K31/439 , A61P9/08 , C07D461/00 , C07D471/02 , C07D455/02
CPC分类号： C07D461/00 , Y10S514/929
摘要： New compounds of the general formula (I) ##STR1## wherein R.sub.1 stands for alkyl and R.sub.2 stands for carboxy, a functional carboxy derivative or a group convertible into carboxy group or a functional derivative thereof, have been prepared by reducing a compound of the general formula ##STR2## wherein R.sub.1 and R.sub.2 each have the same meanings as defined above and X.sup.- represents an anion derived from an acid, and optionally subjecting the obtained compound to hydrolysis. If desired, the racemic compounds of the general formula (I) can be resolved to yield the corresponding optically active isomers. The free bases of the general formula (I) can be converted into their pharmaceutically acceptable salts, or the salts can be treated with an alkaline agent to yield the free bases.The compounds of the general formula (I) can be used in the therapy primarily as vasodilatating agents.
摘要翻译：通式（I）的新化合物其中R1代表烷基，R2代表羧基，官能羧基衍生物或可转化成羧基的基团或其官能衍生物，通过还原化合物通式（II）其中R 1和R 2各自具有与上述相同的含义，并且X代表由酸衍生的阴离子，并且任选地使得到的化合物进行水解。如果需要，可以拆分通式（I）的外消旋化合物，得到相应的旋光异构体。通式（I）的游离碱可以转化为其药学上可接受的盐，或者盐可以用碱剂处理以产生游离碱。

53. 发明授权

US4044012A Indolo-quinolizidine derivatives 失效
标题翻译：吲哚 - 喹嗪啶衍生物
公开(公告)号：US4044012A
公开(公告)日：1977-08-23
申请号：US670243
申请日：1976-03-25
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： C07D471/14 , C07D459/00
CPC分类号： C07D471/14 , Y10S514/929
摘要： New compounds of the formula ##STR1## are provided wherein R.sub.1 is hydrogen, and R.sub.2 stands for an alkyl group and optically active enanthiomers and pharmaceutically acceptable salts thereof.
摘要翻译：提供新的式“IMAGE”化合物，其中R 1是氢，R 2代表烷基和光学活性的对映异构体及其药学上可接受的盐。

54. 发明授权

US5510345A Biologically active eburnamenine derivatives, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译：生物活性白蛋白衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：US5510345A
公开(公告)日：1996-04-23
申请号：US351447
申请日：1994-12-08
申请人： Zoltan Tuba , Sandor Maho , Aniko Gere , Pal Vittay , Bela Kiss , Eva Palosi , Laszlo Szporny , Csaba Szantay , Ferenc Soti , Zsuzsa Baloghne Kardos , Maria Incze , Gabor Balogh , Maria Gazdag
发明人： Zoltan Tuba , Sandor Maho , Aniko Gere , Pal Vittay , Bela Kiss , Eva Palosi , Laszlo Szporny , Csaba Szantay , Ferenc Soti , Zsuzsa Baloghne Kardos , Maria Incze , Gabor Balogh , Maria Gazdag
IPC分类号： C07D471/00 , A61K31/495 , A61K31/505 , A61K31/55 , A61P9/08 , A61P9/10 , A61P13/02 , A61P15/00 , A61P25/28 , C07D239/00 , C07D295/00 , C07D461/00 , C07D401/14 , C07D403/14
CPC分类号： C07D461/00
摘要： The invention relates to novel eburnamenine derivatives of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 as well as R.sup.3 and R.sup.4, independently from each other, stand for hydrogen, C.sub.2-6 alkyl group, C.sub.2-6 alkenyl group; or a C.sub.3-10 alicyclic group involving 1 to 3 rings, and this latter group may be substituted by a C.sub.1-6 alkyl or C.sub.2-6 alkenyl group; or R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4, together with the adjacent nitrogen atom and optionally with an additional oxygen or nitrogen atom, form a 4- to 6-membered, saturated or unsaturated cyclic group which may be substituted by a C.sub.1-6 alkyl or C.sub.2-6 alkenyl group; two of X, Y and Z are nitrogen whereas the third of them means a methine group; n is 1 or 2; W means oxygen or two hydrogen atoms; and the wavy line means .alpha.-/.alpha.-, .alpha.-/.beta.- or .beta.-/.alpha.- steric position, as well as their acid addition salts and solvates. The invention further relates to pharmaceutical compositions containing the above compounds as well as a process for preparing the compounds of formula (I). The compounds of formula (I) possess antioxidant effect and therefore, they are useful for inhibiting the peroxidation of lipids occurring in mammals (including human).
摘要翻译： PCT No.PCT / Hu93 / 00036 Sec。 371日期1994年12月8日第 102（e）日期1994年12月8日PCT提交1993年6月8日PCT公布。出版物WO93 / 25550 本发明涉及式（I）的新颖白蛋白衍生物：其中R 1和R 2以及R 3和R 4彼此独立地代表氢，C 2-6烷基，C 2-6烯基; 或含有1〜3个环的C 3〜10环亚烷基，后者可以被C 1-6烷基或C 2-6烯基取代; 或R 1和R 2和/或R 3和R 4与相邻的氮原子以及任选的另外的氧或氮原子一起形成可被C 1-6烷基取代的4-至6-元饱和或不饱和的环状基团或C 2-6烯基; X，Y和Z中的两个是氮，而第三个是次甲基; n为1或2; W表示氧或两个氢原子; 波浪线表示α - /α - ，α - /β - 或β - / - - - 立体位置，以及它们的酸加成盐和溶剂合物。本发明还涉及含有上述化合物的药物组合物以及制备式（I）化合物的方法。式（I）化合物具有抗氧化作用，因此它们可用于抑制哺乳动物（包括人）中发生的脂质的过氧化反应。

55. 发明授权

US4806545A (-)-1.beta.-ethyl-1.alpha.-hydroxymethyl-1,2,3,4,6,7,12, 12B.alpha.-octahydroindolo(2,3-A)quinolizine, process for its preparation and pharmaceutical compositions containing same 失效
标题翻译：（ - ） - 1β-乙基-1α-羟甲基-1,2,3,4,6,7,12,12aαα-八氢吲哚（2,3-A）喹嗪，其制备方法和含有它们的药物组合物
公开(公告)号：US4806545A
公开(公告)日：1989-02-21
申请号：US851327
申请日：1986-04-14
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Zsolt Szombathelyi , Egon Karpati , Bela Kiss , Katalin Csomor , Istvan Laszlovszky , Erzsebet Lapis , Laszlo Szporny , Lilla Forgacs , Csaba Kuthi , Aniko Gere
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Zsolt Szombathelyi , Egon Karpati , Bela Kiss , Katalin Csomor , Istvan Laszlovszky , Erzsebet Lapis , Laszlo Szporny , Lilla Forgacs , Csaba Kuthi , Aniko Gere
IPC分类号： A61K31/435 , A61P9/00 , A61P9/08 , C07D471/14 , C07D455/00
CPC分类号： C07D471/14
摘要： The invention relates to the new (-)-1.beta.-ethyl-1.alpha.-hydroxymethyl-1,2, 3,4,6,7,12,12b.alpha.-octa-hydroindolo[2,3-a] quinolizine of the formula (I) ##STR1## and acid addition salts thereof. According to another aspect of the invention there is provided a process for the preparation of the compound of formula (I) and acid addition salts thereof by resolution of the corresponding racemic compound and optionally by subsequent hydrolysis and/or salt formation.The compound of formula (I) shows a remarkable peripheral vasodilating and antihypoxial activity. Pharmaceutical compositions comprising it as active ingredient are also within the scope of the invention.
摘要翻译：本发明涉及新的（ - ） - 1β-乙基-1α-羟基甲基-1,2,3,4,6,7,12,12bα-正 - 氢吲哚并[2,3-a]喹嗪式（I）化合物（I）及其酸加成盐。根据本发明的另一方面，提供了通过拆分相应的外消旋化合物和任选地随后的水解和/或盐形成来制备式（I）化合物及其酸加成盐的方法。式（I）化合物显示出显着的外周血管扩张和抗低氧活性。包含其作为活性成分的药物组合物也在本发明的范围内。

56. 发明授权

US4782052A Octahydroindolo[2,3-a]quinolizin-1-yl-alkanecarboxylic acid amines and their therapeutically useful acid addition salts, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译：八氢吲哚并[2,3-a]喹嗪酮-1-基 - 链烷羧酸胺及其治疗上有用的酸加成盐，含有它们的药物组合物及其制备方法
公开(公告)号：US4782052A
公开(公告)日：1988-11-01
申请号：US783911
申请日：1985-10-03
申请人： Ferenc Soti , Csaba Szantay , Maria Incze , Zsuzsanna Balogh nee Kardos , Elemer Ezer , Judit Matuz , Laszlo Szporny , Gyorgy Hajos , Csaba Kuthi
发明人： Ferenc Soti , Csaba Szantay , Maria Incze , Zsuzsanna Balogh nee Kardos , Elemer Ezer , Judit Matuz , Laszlo Szporny , Gyorgy Hajos , Csaba Kuthi
IPC分类号： C07D487/14 , A61K31/404 , A61K31/435 , A61K31/4375 , A61K31/454 , A61K31/475 , A61P1/04 , A61P9/06 , A61P9/08 , A61P21/02 , C07D209/04 , C07D221/00 , C07D471/14 , C07D471/22 , A61K31/55 , A61K31/535 , C07D471/04
CPC分类号： C07D471/14
摘要： The invention relates to new 1,2,3,4,6,7,12,12b-octahydroindolo[2,3,-a]quinolizin-1-yl-alkanecarboxylic acid amides of the formula (I), ##STR1## wherein R.sub.1 and R.sub.2 stand independently for a hydrogen or halogen atom, or a hydroxyl, nitro or C.sub.1-4 alkoxy group;R.sub.3 and R.sub.4 stand independently for a hydrogen atom or a C.sub.1-4 alkyl group;R.sub.5 and R.sub.6 stand independently for a hydrogen atom, C.sub.1-8 alkyl group, C.sub.3-8 alkenyl or cycloalkyl group, aryl or aralkyl group, heteroaryl or heteroaralkyl group containing oxygen, nitrogen or sulphur atom, all these groups being optionally substituted; orR.sub.5 and R.sub.6 together form an optionally substituted C.sub.2-8 .alpha.,.omega.-alkylene group, wherein one carbon atom may optionally be replaced by an oxygen or nitrogen atom; andG means a C.sub.1-4 straight chained alkylene group, as well as to their therapeutically suitable acid addition salts and pharmaceutical compositions containing these compounds. The compounds of the formula (I) have valuable therapeutic properties, namely vasodilatory, spasmolytic, antiarrhythmic and gastrocytoprotective effects. The gastrocytoprotective effect is particularly important.
摘要翻译：本发明涉及式（I）的新的1,2,3,4,6,7,12,12b-八氢吲哚并[2,3-a]喹嗪-1-基 - 烷脒酰胺，（I）其中R1和R2独立地代表氢或卤素原子，或羟基，硝基或C1-4烷氧基; R3和R4独立地表示氢原子或C1-4烷基; R5和R6独立地表示氢原子，C1-8烷基，C3-8烯基或环烷基，芳基或芳烷基，含氧，氮或硫原子的杂芳基或杂芳烷基，所有这些基团都可以被取代; 或R 5和R 6共同形成任选取代的C 2-8α，ω-亚烷基，其中一个碳原子可任选地被氧或氮原子代替; 和G表示C 1-4直链亚烷基，以及它们的治疗上合适的酸加成盐和含有这些化合物的药物组合物。式（I）化合物具有有价值的治疗特性，即血管舒张，解痉，抗心律失常和胃肠保护作用。胃肠保护作用尤其重要。

57. 发明授权

US4780537A Pyrimidine derivatives and process preparing the same 失效
标题翻译：嘧啶衍生物及其制备方法
公开(公告)号：US4780537A
公开(公告)日：1988-10-25
申请号：US72010
申请日：1987-07-10
申请人： Andras Vedres , Csaba Szantay , Bela Stefko , Janos Kreidl , Andras Nemes , Gabor Blasko , Erik Bogsch , Denes Mathe , Istvan Hegedus , Adrien Szuchovszky nee Gergely , Tamas Mester
发明人： Andras Vedres , Csaba Szantay , Bela Stefko , Janos Kreidl , Andras Nemes , Gabor Blasko , Erik Bogsch , Denes Mathe , Istvan Hegedus , Adrien Szuchovszky nee Gergely , Tamas Mester
IPC分类号： C07D239/48 , C07D239/50 , C07D239/02
CPC分类号： C07D239/48 , C07D239/50
摘要： A pyrimidine derivative of the formulae (Ia), (Ib) and (Ic), ##STR1## wherein R stands for an alkyl group group with 1 to 6 carbon atoms or an aryl group optionally substituted by halogen atom; andX stands for chlorine or bromine atom or an arylsulfonyloxy group optionally substituted by 1 to 3 lower alkyl groups.The subject pyrimidine derivatives are intermediates for preparing 6-amino-1,2-dihydro-1-hydroxy-2-imino-4-piperidinopyrimidine.
摘要翻译：（Ia），（Ib）和（Ic）的嘧啶衍生物，其中R代表具有1至6个碳原子的烷基基团或任选被卤素原子取代的芳基; X代表氯或溴原子或任选被1至3个低级烷基取代的芳基磺酰氧基。本发明的嘧啶衍生物是制备6-氨基-1,2-二氢-1-羟基-2-亚氨基-4-哌啶并嘧啶的中间体。

58. 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。

59. 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。

60. 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。

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