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51. 发明授权

US4140790A 3-(4-Substituted piperazino)-1-xanthene-9-carbonyloxy-propanes 失效
标题翻译： 3-（4-取代的哌嗪子基）-1-呫吨-9-羰基氧基 - 丙烷
公开(公告)号：US4140790A
公开(公告)日：1979-02-20
申请号：US859928
申请日：1977-12-12
申请人： Karoly Felfoldi , Jozsef Apjok , Mihaly Bartok , Jozsef Czombos , Arpad Molnar , Ferenc Noteisz , Egon Karpati , Laszlo Szporny
发明人： Karoly Felfoldi , Jozsef Apjok , Mihaly Bartok , Jozsef Czombos , Arpad Molnar , Ferenc Noteisz , Egon Karpati , Laszlo Szporny
IPC分类号： C07D243/26 , A61K31/495 , A61K31/55 , A61K31/551 , A61P3/00 , A61P9/06 , A61P9/08 , A61P25/20 , C07D241/04 , C07D243/16 , C07D243/18 , C07D243/24 , C07D295/08 , C07D295/088 , C07D295/096 , C07D307/68 , C07D311/82 , C07D311/84 , C07D405/12 , C07D295/14 , C07D241/06 , C07D241/10
CPC分类号： C07D295/088 , C07D307/68 , C07D311/84 , Y10S514/821
摘要： The invention relates to novel piperazine derivatives having the formula (I), ##STR1## wherein R.sub.1 represents a C.sub.1-5 alkyl group having optionally a phenyl, trimethoxyphenyl, phenoxy, methoxy-cyclohexyl or heptamethyleneimino substituent on the terminal carbon atom, allyl group, a phenyl group having optionally one or more halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trihalomethyl or allyl substituent(s), or a C.sub.2-5 alkoxycarbonyl group,R.sub.2 represents hydrogen or a C.sub.1-4 alkyl group, andR.sub.3 represents furyl group, 9-xanthenyl group or a C.sub.5-6 cycloalkyl group having a C.sub.1-4 alkoxy substituent,Or acid addition salts or quaternary salts thereof.The invention also relates to pharmaceutical compositions containing the above compounds, furthermore to a process for the preparation of the novel compounds and pharmaceutical compositions.The novel compounds according to the invention possess anti-arrhythmic and coronary dilatating effects.The novel compounds can be prepared by reacting a compound of the formula (II) ##STR2## with a compound of the formula (III),R.sup.3 --COOH (III)or a reactive derivative thereof.
摘要翻译：本发明涉及具有式（I）的新型哌嗪衍生物，其中R 1表示在末端碳原子上具有任选的苯基，三甲氧基苯基，苯氧基，甲氧基 - 环己基或七亚甲基亚氨基取代基的C 1-5烷基，烯丙基，任选具有一个或多个卤素的苯基，C 1-4烷基，C 1-4烷氧基，三卤代甲基或烯丙基取代基，或C 2-5烷氧基羰基，R 2表示氢或C 1-4烷基， R3表示呋喃基，9-呫吨基或具有C1-4烷氧基取代基的C5-6环烷基，或其酸加成盐或季铵盐。

52. 发明授权

US4054571A Nitrogen-containing polycyclic compounds and a process for the preparation thereof 失效
标题翻译：含氮多环化合物及其制备方法
公开(公告)号：US4054571A
公开(公告)日：1977-10-18
申请号：US614151
申请日：1975-09-17
申请人： Csaba Szantay , Lajor Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajor Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
IPC分类号： C07D471/06 , A61K31/4375 , A61K31/4745 , C07D461/00 , C07D471/04
CPC分类号： C07D461/00
摘要： The invention relates to new eburnamenine derivatives of the general formula (I), ##STR1## wherein R.sub.1 stands for an alkyl group,R.sub.2 stands for a carboxy group, a functional carboxy derivative (preferably an ester group) or a group convertable into carboxy group or a functional derivative thereof (preferably cyano group), andX.sup.- is an anion derived from an acid,And the corresponding free bases.These compounds are valuable intermediates of the preparation of eburnamenine derivatives with advantageous therapeutical effects.The above compounds are prepared as follows: a compound of the general formula (II), ##STR2## wherein R.sub.1 has the same meanings as defined above, is reacted with a compound of the general formula (III), ##STR3## wherein R.sub.2 has the same meanings as defined above and Y is halogen, and, if desired, a thus-obtained compound of the general formula (I), wherein R.sub.1 and R.sub.2 each have the same meanings as defined above and X.sup.- is a halide ion, is reacted with an acid, and/or, if desired, a compound of the general formula (I), wherein R.sub.1 and X.sup.- each have the same meanings as defined above and R.sub.2 is cyano or an ester group, is subjected to hydrolysis, and/or, if desired, a compound of the general formula (I), wherein R.sub.1, R.sub.2 and X.sup.- each have the same meanings as defined above, is treated with a base.
摘要翻译：本发明涉及通式（I），其中R1代表烷基，R2代表羧基，官能羧基衍生物（优选酯基）或可转化基团的新颖的本本母胺衍生物羧基或其功能性衍生物（优选氰基），X是衍生自酸的阴离子，和相应的无碱基。

53. 发明授权

US4810709A Nintrovincaminic acid derivatives having pharmaceutical utility 失效
标题翻译：具有药用效用的新一代氨基酸衍生物
公开(公告)号：US4810709A
公开(公告)日：1989-03-07
申请号：US105959
申请日：1987-10-07
申请人： Andras Vedres , Csaba Szantay , Istvan Moldvai , Bela Stefko , Dora Groo , Egon Karpati , Bela Kiss , Eva Palosi , Miklos Riesz , Zsolt Szombathelyi , Laszlo Szporny , Maria Zajer nee Balazs
发明人： Andras Vedres , Csaba Szantay , Istvan Moldvai , Bela Stefko , Dora Groo , Egon Karpati , Bela Kiss , Eva Palosi , Miklos Riesz , Zsolt Szombathelyi , Laszlo Szporny , Maria Zajer nee Balazs
IPC分类号： A61K31/435 , A61P9/00 , A61P9/08 , A61P25/08 , C07D461/00 , A61K31/475
CPC分类号： C07D461/00
摘要： The invention relates to a new process for preparing novel racemic and optically active 9- or 11-nitroapovincaminic acid derivatives of the general formula (I) ##STR1## wherein R stands for a --CO--X group, wherein X means a halogen atom; orfor a --CO--OR.sup.1 group, wherein R.sup.1 means an optionally mono- or polysubstituted C.sub.1-10 aliphatic group, a C.sub.3-8 alicyclic group or an aromatic C.sub.6-14 hydrocarbyl group; orfor a --CO--NR.sup.2 R.sup.3 group, wherein R.sup.2 and R.sup.3 are the same or different and stand for a hydrogen atom or a C.sub.1-8 alkyl group optionally forming a saturated heterocycle together with the adjacent nitrogen atom and optionally with one or more further nitrogen atoms or other heteroatoms, and R.sup.3 may also represent an amino group when R.sup.2 stands for a hydrogen atom; orfor a cyano group,as well as their salts and pharmaceutical preparations containing these compounds. Furthermore the invention relates to a process for preparing these compounds and preparations.The racemic and optically active substances of the general formula (I) as well as their pharmaceutically acceptable acid addition and quaternary salts have valuable therapeutic properties, namely vasodilating, spasmolytic, antihypoxic and anticonvulsive effects.
摘要翻译：本发明涉及制备通式（I）的新型外消旋和光学活性的9-或11-硝基
氨基嘌呤酸衍生物的新方法，其中R代表-CO-X基团，其中X表示卤素原子; 或-CO-OR 1基团，其中R 1表示任选的单取代或多取代的C 1-10脂族基团，C 3-8脂环族基团或芳族C 6-14烃基; 或-CO-NR 2 R 3基团，其中R 2和R 3相同或不同，代表氢原子或任选地与相邻的氮原子一起形成饱和杂环的C 1-8烷基，并且任选地与一个或多个另外的氮原子或其它杂原子，当R 2代表氢原子时，R 3也可以表示氨基; 或氰基，以及它们的含有这些化合物的盐和药物制剂。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）的外消旋和光学活性物质及其药学上可接受的酸加成盐和季盐具有有价值的治疗性质，即血管舒张，解痉，抗缺氧和抗惊厥作用。

54. 发明授权

US4753949A 2-chloronicergoline having antihypoxic activity 失效
标题翻译：具有抗低氧活性的2-氯麦角林
公开(公告)号：US4753949A
公开(公告)日：1988-06-28
申请号：US877294
申请日：1986-06-23
申请人： Gabor Megyeri , Tibor Keve , Bala Stefko , Erik Bogsch , Janos Galambos , Anna Kassi nee Zieger , Ferenc Trischler , Eva Palosi , Dora Groo , Egon Karpati , Zsolt Szombathelyi , Laszlo Szporny , Bela Kiss , Istvan Laszlovszky , Erzsebet Lapis
发明人： Gabor Megyeri , Tibor Keve , Bala Stefko , Erik Bogsch , Janos Galambos , Anna Kassi nee Zieger , Ferenc Trischler , Eva Palosi , Dora Groo , Egon Karpati , Zsolt Szombathelyi , Laszlo Szporny , Bela Kiss , Istvan Laszlovszky , Erzsebet Lapis
IPC分类号： A61K31/48 , A61P3/00 , A61P3/14 , A61P9/00 , A61P25/02 , A61P25/28 , C07D457/02
CPC分类号： C07D457/02
摘要： The invention relates to a novel process for the preparation of partially new 2-halonicergoline derivatives of the formula (I), ##STR1## wherein X stands for chlorine, bromine or iodine atom, as well as their acid addition salts.The process of the invention comprises esterifying a novel 2-halo-1-methyllumilysergol of the formula (II), ##STR2## wherein X is the same as defined above, or an acid addition salt thereof and, if desired, converting the thus-obtained 2-halonicergoline derivative of the formula (I) to an acid addition salt.The compounds of the invention improve the cognitive function of the brain and show an antihypoxic as well as a strong .alpha.-adrenerg blocking and calcium-antagonistic action.
摘要翻译：本发明涉及制备式（I）的部分新的2-卤代麦角灵衍生物的新方法，其中X代表氯，溴或碘原子，以及它们的酸加成盐。本发明的方法包括酯化式（II）的新的2-卤代-1-甲基烯丙基谷维素，其中X与上述定义相同，或其酸加成盐，如果需要，转化将由此获得的式（I）的2-卤代麦角灵衍生物与酸加成盐反应。本发明的化合物改善了脑的认知功能，并且显示出抗低氧以及强的α-肾上腺素能阻断和钙拮抗作用。

55. 发明授权

US4549020A Eburnane oxime ethers 失效
标题翻译：伊本安肟醚
公开(公告)号：US4549020A
公开(公告)日：1985-10-22
申请号：US508437
申请日：1983-06-27
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Sapi , Maria Zajer nee Balazs , Bela Kiss , Elemer Ezer , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Sapi , Maria Zajer nee Balazs , Bela Kiss , Elemer Ezer , Egon Karpati , Laszlo Szporny
IPC分类号： A61K31/435 , A61P25/02 , A61P25/20 , C07D461/00
CPC分类号： C07D461/00
摘要： The invention relates to optically active or racemic eburnane-oxime ethers of the formulae (Ia) and/or ##STR1## wherein R represents an alkyl group having 1 or 2 carbon atoms,R.sup.2 represents an alkyl group having 1 to 6 carbon atoms,and the configuration of the hydrogen in the 3-position and the R.sup.2 group is .alpha.,.alpha. and/or .beta.,.beta. or .alpha.,.beta. and/or .beta.,.alpha. and acid addition salts thereof.The new compounds show valuable pharmaceutical activities, thus are potent CNS-tranquillants, smooth muscle relaxants, sedatives and hypnotic agents, and can therefore be employed as active ingredients of pharmaceutical compositions, which are also within the scope of the present invention.
摘要翻译：本发明涉及式（Ia）和/或其中R表示具有1或2个碳原子的烷基的式（Ia）和/或其中R 1表示烷基的光学活性或外消旋的桦烷 - 肟醚，具有1至6个碳原子的基团，并且3-位和R2基团中的氢的构型是α，α和/或β，β或α，β和/或β，α和其酸加成盐。新化合物显示出有价值的药物活性，因此是有效的CNS-镇定剂，平滑肌松弛剂，镇静剂和催眠剂，因此可用作药物组合物的活性成分，其也在本发明的范围内。

56. 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。

57. 发明授权

US4432982A Polycyclic compounds substituted on the A-ring, pharmaceutical compositions containing them, and methods of treating psoriasis with them 失效
标题翻译：在A环上取代的多环化合物，含有它们的药物组合物，以及用它们治疗牛皮癣的方法
公开(公告)号：US4432982A
公开(公告)日：1984-02-21
申请号：US345633
申请日：1982-02-04
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Mari Zajer nee Balazs , Lilla Forgach , Egon Karpati , Arpad Kiraly , Gyongyver Kiraly nee Soos , Laszlo Szporny , Bela Rosdy
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Mari Zajer nee Balazs , Lilla Forgach , Egon Karpati , Arpad Kiraly , Gyongyver Kiraly nee Soos , Laszlo Szporny , Bela Rosdy
IPC分类号： A61K31/435 , A61K31/4375 , A61K31/475 , A61K31/585 , A61P17/00 , A61P35/00 , A61P43/00 , C07D461/00 , C12N9/99
CPC分类号： C07D461/00 , A61K31/585 , Y10S514/863
摘要： The invention relates to new polycyclic compounds substituted on the A-ring. More particularly, the invention concerns new polycyclic compounds of the formula (I) ##STR1## wherein R.sup.1 is methoxy or halogen andR.sup.2 is hydrogen; orR.sup.1 is hydrogen andR.sup.2 is halogen and acid addition salts thereof.
摘要翻译：本发明涉及在A环上取代的新的多环化合物。更具体地说，本发明涉及新的式（I）的多环化合物，其中R1是甲氧基或卤素，R2是氢; 或R 1为氢，R 2为卤素及其酸加成盐。

58. 发明授权

US4424224A Apovincaminol derivative and compositions and methods utilizing it for treating psoriasis 失效
标题翻译：氨基氨基酚衍生物及其用于治疗牛皮癣的组合物和方法
公开(公告)号：US4424224A
公开(公告)日：1984-01-03
申请号：US345632
申请日：1982-02-04
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Zsuzsanna Gyulai , Maria Zajer nee Balazs , Lilla Forgach , Egon Karpati , Arpad Kiraly , Gyongyver Kiraly nee Soos , Laszlo Szporny , Bela Rosdy
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Zsuzsanna Gyulai , Maria Zajer nee Balazs , Lilla Forgach , Egon Karpati , Arpad Kiraly , Gyongyver Kiraly nee Soos , Laszlo Szporny , Bela Rosdy
IPC分类号： A61K31/435 , A61P17/00 , A61P35/00 , A61P43/00 , C07D461/00 , C12N9/99
CPC分类号： C07D461/00 , Y10S514/863
摘要： The invention relates to the new apovincaminol-3',4',5'-trimethoxy-benzoate and acid addition salts thereof. The new compound may be prepared by reacting apovincaminol or an acid addition salt thereof with 3,4,5-trimethoxy benzoic acid or a reactive derivative thereof capable of acylation and if desired converting the compound thus obtained into an acid addition salt. The new compound of the present invention can be used in therapy in the treatment of skin diseases attached to pathological cell proliferation and in the propylaxis of such diseases.
摘要翻译：本发明涉及新的氨基嘌呤-3'，4'，5'-三甲氧基苯甲酸酯及其酸加成盐。新化合物可以通过将亚氨基胺醇或其酸加成盐与能够酰化的3,4,5-三甲氧基苯甲酸或其反应性衍生物反应并且如果需要将所得化合物转化为酸加成盐来制备。本发明的新化合物可用于治疗与病理性细胞增殖和这种疾病的丙型病症相关的皮肤病的治疗。

59. 发明授权

US4419359A Nitro-substituted polycyclic derivatives useful in the treatment of psoriasis 失效
标题翻译：用于治疗牛皮癣的硝基取代多环衍生物
公开(公告)号：US4419359A
公开(公告)日：1983-12-06
申请号：US345631
申请日：1982-02-04
申请人： Tibor Keve , Gyorgy Fekete , Csaba Lorincz , Janos Galambos , Bela Zsadon , Maria Zajer nee Balazs , Lilla Forgach , Egon Karpati , Arpad Kiraly , Gyongyver Kiraly nee Soos , Laszlo Szporny , Bela Rosdy
发明人： Tibor Keve , Gyorgy Fekete , Csaba Lorincz , Janos Galambos , Bela Zsadon , Maria Zajer nee Balazs , Lilla Forgach , Egon Karpati , Arpad Kiraly , Gyongyver Kiraly nee Soos , Laszlo Szporny , Bela Rosdy
IPC分类号： C07D461/00 , A61K31/435
CPC分类号： C07D461/00 , Y10S514/863
摘要： The present invention relates to the compounds of the Formulae 1a and 1b and pharmaceutically acceptable acid addition salts thereof.The new 9-nitro-apovincaminol-3',4',5'-trimethoxybenzoate of the Formula 1a ##STR1## and the 11-nitro-apovincaminol-3',4',5'-trimethoxy-benzoate of the Formula 1b ##STR2## and pharmaceutically acceptable acid addition salts thereof can be prepared by nitrating the apovincaminol-3',4',5'-trimethoxy-benzoate of the Formula 11, ##STR3## if desired separating the mixture of the compounds of the Formulae 1a and 1b thus obtained into its components, if desired converting a compound of the Formula 1a or 1b thus obtained into pharmaceutically acceptable acid addition salts thereof.The new compounds of the present invention can be used in therapy in the treatment of psoriasis.
摘要翻译：本发明涉及式1a和1b的化合物及其药学上可接受的酸加成盐。式1b的新的9-硝基 - 亚氨基胺醇-3'，4'，5'-三甲氧基苯甲酸酯和式1b的11-硝基 - 亚氨基胺醇-3'，4'，5'-三甲氧基 - 苯甲酸酯< IMAGE>及其药学上可接受的酸加成盐可以通过将式11的亚氨基胺醇-3'，4'，5'-三甲氧基 - 苯甲酸酯硝化，如果需要，将式1a的化合物和 1b，如果需要，将由此获得的式1a或1b的化合物转化为其药学上可接受的酸加成盐。本发明的新化合物可用于治疗牛皮癣的治疗。

60. 发明授权

US4179467A Dopamine hydroxylase inhibiting 2-amino-cyclopent-1-ene-1-thiocarboxylic acid-disulfides 失效
标题翻译：多巴胺羟化酶抑制2-氨基 - 环戊-1-烯-1-硫代羧酸二硫化物
公开(公告)号：US4179467A
公开(公告)日：1979-12-18
申请号：US865429
申请日：1977-12-29
申请人： Gyorgy Matolcsy , Piroska Bartok nee Berencsy , Bella Kiss , Eva Palosi , Egon Karpati , Laszlo Szporny
发明人： Gyorgy Matolcsy , Piroska Bartok nee Berencsy , Bella Kiss , Eva Palosi , Egon Karpati , Laszlo Szporny
IPC分类号： A61K31/13 , C07C87/02
CPC分类号： C10M1/08
摘要： New 2-amino-cyclopent-1-ene-thiocarboxylic acid-disulfides of the formula, ##STR1## wherein R is a C.sub.1-6 alkyl group having optionally a C.sub.1-4 alkoxy, hydroxy, carboxy and/or amino substituent, a C.sub.2-4 alkenyl group, or a C.sub.3-8 cycloalkyl group, are prepared by oxidizing the respective 2-amino-cyclopent-1-ene-dithiocarboxylic acids of the formula, ##STR2## wherein R is as defined above. The compounds of the formula (I) exert dopamine-.beta.-hydroxylase inhibiting effects and can be applied in therapy.
摘要翻译：新的2-氨基 - 环戊-1-烯 - 硫代羧酸 - 二硫化物，其中R是具有任选C 1-4烷氧基的C 1-6烷基，羟基，羧基和/或氨基取代基，C 2-4链烯基或C 3-8环烷基，是通过将下式所示的2-氨基环戊-1-烯二硫代羧酸，其中R如上定义。式（I）化合物发挥多巴胺-β-羟化酶抑制作用，可用于治疗。

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