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1. 发明授权

US4829076A Novel dihydropyridines having calcium antagonistic and antihypertensive activity 失效
标题翻译：具有钙拮抗作用和抗高血压活性的新型二氢吡啶类
公开(公告)号：US4829076A
公开(公告)日：1989-05-09
申请号：US97111
申请日：1987-09-16
申请人： Geza Szilagyi , Eva Bozo , Laszlo Czollner , Laszlo Jaszlits , Gyorgy Rabloczky , Jozsef Borsi , Istvan Elekes , Gyongyi Nagy nee Csokas , Andras Varro , ZSuzanne Lang nee Rihmer , Gyorgy Cseh , Gyula Horvath , Ilona Bodi
发明人： Geza Szilagyi , Eva Bozo , Laszlo Czollner , Laszlo Jaszlits , Gyorgy Rabloczky , Jozsef Borsi , Istvan Elekes , Gyongyi Nagy nee Csokas , Andras Varro , ZSuzanne Lang nee Rihmer , Gyorgy Cseh , Gyula Horvath , Ilona Bodi
IPC分类号： A61K31/445 , A61K31/451 , A61K31/455 , A61P3/00 , A61P9/10 , A61P9/12 , C07D211/90 , C07D401/12 , C07D405/12
CPC分类号： C07D401/12 , C07D211/90 , C07D405/12
摘要： The invention relates to new substituted dihydropyridine derivatives of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.6 are as defined herein after, the racemic and optically active variants as well as mixtures thereof, furthermore the acid addition salts of these compounds, pharmaceutical compositions containing the same and a process for the preparation thereof.The compounds of the general formula (I) can be advantageously applied for the treatment of pathologically severe hypertensions, their toxicity is low and they possess an advantageous therapeutic index.
摘要翻译：本发明涉及通式（I）的新的取代二氢吡啶衍生物，其中R 1和R 6如本文所定义，外消旋和光学活性变体及其混合物，此外，这些化合物的酸加成盐，含有该组合物的药物组合物及其制备方法。通式（I）的化合物可以有利地用于治疗病态严重的高血压，其毒性低，并且具有有利的治疗指标。

2. 发明授权

US4835152A 1-(4-Aminophenyl)-4-methyl-7,8-methylenedioxy-3,4-dihydro-5H-2,3-b enzodiazepine and acid addition salts thereof same 失效
标题翻译： 1-（4-氨基苯基）-4-甲基-7,8-亚甲二氧基-3,4-二氢-5H-2,3-苯并二氮杂及其酸加成盐
公开(公告)号：US4835152A
公开(公告)日：1989-05-30
申请号：US87341
申请日：1987-08-20
申请人： Jeno Korosi , Tibor Lang , Ferenc Andrasi , Pal Berzsenyi , Peter Botka , Tamas Hamori , Katalin G. Horvath , Jozsef Borsi , Istvan Elekes , Zsuzsanna L. Rihmer
发明人： Jeno Korosi , Tibor Lang , Ferenc Andrasi , Pal Berzsenyi , Peter Botka , Tamas Hamori , Katalin G. Horvath , Jozsef Borsi , Istvan Elekes , Zsuzsanna L. Rihmer
IPC分类号： C07D405/10 , A61K31/55 , A61K31/551 , A61P25/26 , C07D491/04 , C07D491/056
CPC分类号： C07D491/04
摘要： The invention relates to new 1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-3,4-dihydro-5H-2,3-benzodiazepi ne of formula (1), optically active isomers and acid addition salts thereof as well as to pharmaceutical compositions containing these compounds. ##STR1## The new compounds of formula (I) can be prepared by reducing 1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine of formula (II) with an inorganic or organic-inorganic and/or complex metal hydride and, if desired, separating the optically active forms of the compound of formula (I) thus-obtained and, if desired, converting the base or bases into acid addition salts or converting the salts into the free bases(s). ##STR2## The new compound of formula (I) possesses significant central nervous effects and can advantageously be used in the therapy.
摘要翻译：本发明涉及式（1）的新的1-（4-氨基苯基）-4-甲基-7,8-亚甲二氧基-3,4-二氢-5H-2,3-苯并二氮杂，旋光异构体和酸加成其盐以及含有这些化合物的药物组合物。（I）式（I）的新化合物可以通过将式（II）的1-（4-氨基苯基）-4-甲基-7,8-亚甲二氧基-5H-2,3-苯并二氮杂与无机或有机 - 无机和/或络合金属氢化物，如果需要，分离由此获得的式（I）化合物的光学活性形式，如果需要，将碱或碱转化为酸加成盐或将盐进入游离碱。（II）式（I）的新化合物具有显着的中枢神经作用，可有利地用于治疗。

3. 发明授权

US4101552A Novel lysergic acid amides and process for preparing same 失效
标题翻译：新的麦角酸酰胺及其制备方法
公开(公告)号：US4101552A
公开(公告)日：1978-07-18
申请号：US679866
申请日：1976-04-23
申请人： Erzsebet Mago nee Karacsony , Jozsef Borsi , Laszlo Tardos , Ildiko Kiraly , Sandor Elek , Istvan Elekes
发明人： Erzsebet Mago nee Karacsony , Jozsef Borsi , Laszlo Tardos , Ildiko Kiraly , Sandor Elek , Istvan Elekes
IPC分类号： A61K31/48 , A61P43/00 , C07D457/06 , C07D457/08
CPC分类号： C07D457/06 , Y10S514/823
摘要： 9,10-Dihydrolysergic acid-(3'-/pyrrolid-2"-on-1'-yl/-propyl)-amide, 1-methyl-9,10-dihydrolysergic acid-(thiazoline-2'-yl)-amide and lysergic acid-(3'-allyloxy-2'-oxy-propyl)-amide and their pharmaceutically acceptable acid addition salts possess antihypertensive and antiserotonin effect and exert an action on the central nervous system.
摘要翻译： 9,10-二氢肉豆蔻酸 - （3' - /吡咯烷-2“ - 在1'-基 - 丙基） - 酰胺，1-甲基-9,10-二氢麦芽糖酸 - （噻唑啉-2'-基） - 酰胺和麦角酸 - （3'-烯丙氧基-2'-氧 - 丙基） - 酰胺及其药学上可接受的酸加成盐具有抗高血压和抗血清素作用并对中枢神经系统发挥作用。

4. 发明授权

US3963735A Acylated 2-aminothiazole derivatives 失效
标题翻译：酰化2-氨基噻唑衍生物
公开(公告)号：US3963735A
公开(公告)日：1976-06-15
申请号：US518732
申请日：1974-10-29
申请人： Lajos Farkas , Endre Kasztreiner , Ferenc Andrasi , Jozsef Borsi , Istvan Elekes , Istvan Polgari
发明人： Lajos Farkas , Endre Kasztreiner , Ferenc Andrasi , Jozsef Borsi , Istvan Elekes , Istvan Polgari
IPC分类号： C07D277/20 , C07D277/46 , C07D295/14 , C07D417/04 , C07D417/14 , C07D213/56
CPC分类号： C07D417/04 , C07D277/46 , C07D417/14 , Y10S514/927
摘要： New acylated 2-aminothiazole derivatives of the general formula (I), ##SPC1##whereinR.sup.1 stands for phenyl group or a pyridyl group,R.sup.2 stands for hydrogen or lower alkyl,R.sup.3 stands for hydrogen, a lower alkyl group or benzyl group, andR.sup.4 and R.sup.5 each represent hydrogen, a C.sub.1-8 alkyl group, allyl group, a hydroxyalkyl group, a C.sub.3-6 cycloalkyl group, .beta.-dimethylaminoethyl group, .beta.-diethylaminoethyl group, benzyl group, 2-furylmethyl group, or a phenyl group having optionally a halogen, methyl, methoxy or trifluoromethyl substituent, orR.sup.4 and R.sup.5 may form, together with the adjacent nitrogen atom, a 5 to 8 membered polymethyleneimino group, morpholino group, piperazino group, N-methylpiperazino group or N-phenylpiperazino group, the compounds of formula I are anticholinergics.
摘要翻译：新的通式（I）的酰化2-氨基噻唑衍生物，其中R1代表苯基或吡啶基，R2代表氢或低级烷基，R3代表氢，低级烷基或苄基，R4和R5 各自表示氢，C1-8烷基，烯丙基，羟基烷基，C3-6环烷基，β-二甲基氨基乙基，β-二乙基氨基乙基，苄基，2-呋喃基甲基或任选具有卤素，甲基，甲氧基或三氟甲基取代基，或者R4和R5可以与相邻的氮原子一起形成5至8元多亚甲基亚氨基，吗啉代基，哌嗪基，N-甲基哌嗪基或N-苯基哌嗪基，配方I是抗胆碱能药。

5. 发明授权

US4235912A Biologically active new 8.beta.-hydrazinomethyl-ergoline derivatives and a process for the preparation thereof 失效
标题翻译：生物活性的新的8β-肼基甲基 - 麦角灵衍生物及其制备方法
公开(公告)号：US4235912A
公开(公告)日：1980-11-25
申请号：US21947
申请日：1979-03-19
申请人： Tivadar Rettegi , Erzsebet Mago nee Karacsony , Lajos Toldy , Jozsef Borsi , Laszlo Tardos
发明人： Tivadar Rettegi , Erzsebet Mago nee Karacsony , Lajos Toldy , Jozsef Borsi , Laszlo Tardos
IPC分类号： A61K31/48 , A61P9/12 , A61P25/24 , A61P25/26 , A61P43/00 , C07D457/02
CPC分类号： C07D457/02
摘要： The invention relates to new 8.beta.-hydrazinomethyl-ergoline derivatives of the general formula (I), ##STR1## wherein x y stands for a ##STR2## or ##STR3## group, R stands for hydrogen or methyl group, andR.sub.1 stands for hydrogen, a lower acyl group, a di-(lower-alkylaminocarbonyl group, a group of the general formula (VI), ##STR4## wherein Z.sub.1, Z.sub.2 and Z.sub.3 each represent hydrogen, halogen or a trifluoromethyl group, or a group of the general formula (VII), ##STR5## wherein Y represents a lower alkyl group, allyl group or phenyl group, and acid addition salts thereof. These compounds possess valuable antiserotonine, antidepressant and hypotensive effects, furthermore they can be applied as starting substances in the preparation of other biologically active ergoline derivatives.The new compounds of the general formula (I) are prepared according to the invention by reacting the respective 6-methyl-8.beta.-mesyloxymethyl or -tosyloxymethyl-ergoline derivatives with dry hydrazine. In order to obtain the N-substituted hydrazinomethyl compounds, the N-unsubstituted derivatives are reacted with an acylating agent or with an isothiocyanate.
摘要翻译：本发明涉及通式（I）的新的8β-肼基甲基 - 麦角灵衍生物，其中xy代表或基团，R代表氢或甲基，R1表示代表氢，低级酰基，二 - （低级烷基氨基羰基，通式（VI）的基团，其中Z 1，Z 2和Z 3各自表示氢，卤素或三氟甲基，或者通式（VII）的基团，其中Y代表低级烷基，烯丙基或苯基，及其酸加成盐，这些化合物具有有价值的抗塞冬糖，抗抑郁药和降压作用，而且它们可以将其用作制备其它生物活性麦角灵衍生物的起始物质，通式（I）的新化合物根据本发明通过使各自的6-甲基-8β-甲氧基甲基或 - 苯甲氧基甲基 - 麦角灵衍生物用干肼。为了得到N-取代的肼基甲基化合物，N-未取代的衍生物与酰化剂或异硫氰酸酯反应。

6. 发明授权

US4005089A Compounds with ergoline skeleton 失效
标题翻译：麦角骨骨架化合物
公开(公告)号：US4005089A
公开(公告)日：1977-01-25
申请号：US579979
申请日：1975-05-22
申请人： Erzsebet Mago nee Karacsony , Jozsef Borsi , Endre Csanyi , Katalin Pik , Lajos Wolf
发明人： Erzsebet Mago nee Karacsony , Jozsef Borsi , Endre Csanyi , Katalin Pik , Lajos Wolf
IPC分类号： A61K31/48 , A61P25/24 , A61P25/26 , A61P43/00 , C07D457/02 , C07D457/06
CPC分类号： C07D457/06 , C07D457/02 , Y10S514/823
摘要： New compounds of the general formula (I) ##STR1## wherein R stands for hydrogen or methyl group,x y stands for a group of the formula ##STR2## and R.sub.1 stands for a group of the formula (III), (IV) or (V) ##STR3## wherein n is an integer from 4 to 10, ARE PREPARED BY ACYLATING A COMPOUND OF THE GENERAL FORMULA (II), ##STR4## wherein R and x y each have the same meanings as defined above, and R.sub.2 stands for a group of the formula (VI), (VII) or (VIII), ##STR5## with a C.sub.6-12 carboxylic acid or a C.sub.6-12 carboxylic acid halide. The new compounds of the general formula (I) and their acid addition salts can be used as antidepressants and antiserotonine agents with prolonged effects.
摘要翻译：通式（I）的新化合物其中R表示氢或甲基，XY表示式的化合物，R1表示式（III），（IV ）或（V）其中n为4至10的整数，（IV）其中n为4至10的整数，ARE为通用化合物（II）制备的ARE，（II）其中R和xy各自具有与上述相同的含义，并且R 2表示式（VI），（VII）或（VIII），（VI），（VII）（VIII）与C6-12羧酸或C6-12羧酸卤化物反应。

7. 发明授权

US4322346A 5H-2,3-Benzodiazepine derivatives 失效
标题翻译： 5H-2,3-苯并二氮杂衍生物
公开(公告)号：US4322346A
公开(公告)日：1982-03-30
申请号：US191811
申请日：1980-09-26
申请人： Jeno Korosi , Tibor Lang , Jozsef Szekely , Ferenc Andrasi , Gabor Zolyomi , Jozsef Borsi , Katalin Goldschmidt nee Horvath , Tamas Hamori , Gabriella Szabo nee Czibula , Zsuzsanna Meszaros nee Dunai-Kovacs , Erzsebet Miglecz
发明人： Jeno Korosi , Tibor Lang , Jozsef Szekely , Ferenc Andrasi , Gabor Zolyomi , Jozsef Borsi , Katalin Goldschmidt nee Horvath , Tamas Hamori , Gabriella Szabo nee Czibula , Zsuzsanna Meszaros nee Dunai-Kovacs , Erzsebet Miglecz
IPC分类号： C07D253/02 , A61K31/55 , A61P25/00 , A61P25/20 , C07D243/02 , C07D243/04 , C07D311/76 , C07D405/04 , C07D409/04 , C07D491/056 , C07D243/00 , C07D407/04
CPC分类号： C07D243/02 , C07D311/76
摘要： New 5H-2,3-benzodiazepine derivatives of the formula ##STR1## wherein R is phenyl having a trifluoromethyl or halogen substituent,R.sup.1 is methyl,R.sup.2 is hydrogen,R.sup.3 is methoxy and R.sup.4 is methoxy, and the pharmaceutically acceptable acid addition salts thereof, are potent tranquilizers.
摘要翻译：式（I）的新的5H-2,3-苯并二氮杂衍生物，其中R是具有三氟甲基或卤素取代基的苯基，R 1是甲基，R 2是氢，R 3是甲氧基，R 4是甲氧基，其药学上可接受的酸加成盐它们是有力的镇定剂。

8. 发明授权

US4108855A Compounds of ergolene and ergoline structure and method for the preparation thereof 失效
标题翻译：己二烯和麦角灵结构的化合物及其制备方法
公开(公告)号：US4108855A
公开(公告)日：1978-08-22
申请号：US773792
申请日：1977-03-02
申请人： Erzsebet Mago nee Karacsony , Sandor Bajusz , Jozsef Borsi , Ildiko Kiraly , Endre Csanyi , Istvan Polgari
发明人： Erzsebet Mago nee Karacsony , Sandor Bajusz , Jozsef Borsi , Ildiko Kiraly , Endre Csanyi , Istvan Polgari
IPC分类号： A61K31/48 , A61P9/12 , A61P25/24 , A61P25/26 , A61P43/00 , C07D457/02
CPC分类号： C07D457/02 , Y02P20/55
摘要： The invention relates to a novel compound of the formula ##STR1## and the pharmaceuticlly acceptable acid addition salts thereof, wherein R stands for a hydrogen atom or methyl group, x y designates a ##STR2## Q is a hydrogen atom or a benzyloxycarbonyl- or N-tert.-butyloxycarbonyl protective group, and R.sub.1 is the side chain of a natural .alpha.-amino acid selected from the group consisting of Arg--, Tryp-13 , Phe--, Ser--, Leu--, Val--, Meth--, Tyr--, His-- or Prol---side-chain.The compounds according to the invention possess antiserotonin and hypotensive effects and act upon the central nervous system.
摘要翻译：本发明涉及式（I）的新化合物及其药学上可接受的酸加成盐，其中R代表氢原子或甲基，xy表示Q是氢原子或苄氧基羰基 - 或N-叔丁氧基羰基保护基，R1是天然α-氨基酸的侧链，其选自Arg-，Tryp-13，Phe-，Ser-，Leu-，Val-，Meth - ，Tyr-，His-或Prol - 侧链。

9. 发明授权

US4064249A Compounds with ergoline skeleton 失效
标题翻译：麦角骨骨架化合物
公开(公告)号：US4064249A
公开(公告)日：1977-12-20
申请号：US749398
申请日：1976-12-10
申请人： Erzsebet Mago nee Karacsony , Jozsef Borsi , Endre Csanyi , Katalin Pik , Lajos Wolf
发明人： Erzsebet Mago nee Karacsony , Jozsef Borsi , Endre Csanyi , Katalin Pik , Lajos Wolf
IPC分类号： C07D457/02 , C07D457/06 , A61K31/48
CPC分类号： C07D457/06 , C07D457/02
摘要： New compounds of the formula ##STR1## wherein R is hydrogen or methyl group,X y is a group of the formula ##STR2## and N IS AN INTEGER OF FROM 4 TO 10, ARE PREPARED BY ACYLATING THE APPROPRIATE LYSERGIC ACID-(3'-ALLYLOXY-2'-OXY-PROPYL)-AMIDE COMPOUNDS WITH CARBOXYLIC ACIDS OF 6 TO 12 CARBON ATOMS OR WITH THEIR REACTIVE DERIVATIVES. If desired, the new compounds can be converted into their pharmaceutically acceptable acid addition salts.The above compounds possess prolonged antidepressive activities.
摘要翻译：式（I）的新化合物其中R是氢或甲基，XY是组合式的组合，N是4至10的整数，是通过合成适当的LYSERGIC ACID-（ 3-ALLYLOXY-2'-OXY-PROPYL） - 酰胺化合物与6至12个碳原子或其反应衍生物的羧酸反应。如果需要，新化合物可以转化成其药学上可接受的酸加成盐。

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