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1. 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。

2. 发明授权

US4614740A 5H-2,3-benzodiazepine derivatives and pharmaceutical compositions containing the same 失效
标题翻译： 5H-2,3-苯并二氮杂衍生物和含有它们的药物组合物
公开(公告)号：US4614740A
公开(公告)日：1986-09-30
申请号：US759169
申请日：1985-07-26
申请人： Tibor Lang , Jeno Korosi , Ferenc Andrasi , Peter Botka , Tamas Hamori , Pal Berzsenyi , Katalin Goldschmidt , Gabor Zolyomi , Istvan Elekes , Zsuzsanna Lang nee Rihmer
发明人： Tibor Lang , Jeno Korosi , Ferenc Andrasi , Peter Botka , Tamas Hamori , Pal Berzsenyi , Katalin Goldschmidt , Gabor Zolyomi , Istvan Elekes , Zsuzsanna Lang nee Rihmer
IPC分类号： A61K31/55 , A61P21/02 , A61P25/20 , C07D243/02 , C07D243/04 , C07D243/10 , C07D491/04 , C07D491/056 , A61K31/35 , C07D243/00
CPC分类号： C07D491/04 , C07D243/02
摘要： The invention relates to new 5H-2,3-benzodiazepine derivatives and a process for the preparation thereof, furthermore to pharmaceutical compositions containing the same.The new 5H-2,3-benzodiazepine derivatives of the invention possess valuable central nervous effect and in particular exert antiaggressive, anxiolytic, narcosis potentiating and soporific properties.
摘要翻译：本发明涉及新的5H-2,3-苯并二氮杂衍生物及其制备方法，此外涉及含有它们的药物组合物。本发明的新的5H-2,3-苯并二氮杂衍生物具有有价值的中枢神经效应，特别是具有抗刺激，抗焦虑，麻醉增效和口服特性。

3. 发明授权

US4785104A 3-(hydroxymethyl)-isoquinoline derivatives 失效
标题翻译： 3-（羟甲基） - 异喹啉衍生物
公开(公告)号：US4785104A
公开(公告)日：1988-11-15
申请号：US51767
申请日：1987-05-20
申请人： Gyorgy Rabloczky , Jeno Korosi , Tibor Lang , Istvan Ling , Tamas Hamori , Maria Kuhar nee Kurthy , Istvan Elekes , Peter Botka , Andras Varro , Sandor Elek , Judit Sarossy nee Kincsessy , Gabor Zolyomi , Zsuzsanna Lang nee Rihmer , Imre Moravcsik
发明人： Gyorgy Rabloczky , Jeno Korosi , Tibor Lang , Istvan Ling , Tamas Hamori , Maria Kuhar nee Kurthy , Istvan Elekes , Peter Botka , Andras Varro , Sandor Elek , Judit Sarossy nee Kincsessy , Gabor Zolyomi , Zsuzsanna Lang nee Rihmer , Imre Moravcsik
IPC分类号： C07D217/08 , A61K31/47 , A61K31/472 , A61P9/04 , A61P9/08 , A61P9/10 , A61P43/00 , C07D217/16 , C07D491/04 , C07D491/056
CPC分类号： C07D491/04 , C07D217/16
摘要： This invention relates to new 3-(hydroxymethyl)-isoquinoline derivatives of the general formula (I), their acid addition salts, and to a process for the preparation thereof, furthermore to pharmaceutical compositions containing the same, ##STR1## wherein R and R.sup.1 are identical or different and stand for a hydrogen or halogen atom, a nitro or a C.sub.1-4 alkoxy group,R.sup.2 stands for a hydrogen atom or a C.sub.1-4 alkyl group,R.sup.3 and R.sup.4 are identical or different and stand for a hydrogen atom or a C.sub.1-4 alkyl group, or R.sup.3 and R.sup.4 combined denote a methylene group,with the proviso that when R stands for 3-methoxy, R.sup.1 for 4-methoxy, R.sup.3 and R.sup.4 are identical and represent methyl or ethyl groups, R.sup.2 is other than hydrogen atom.The compounds of the general formula (I) exert valuable positive inotropic (cardiotonic) potency, they are capable to increase the myocardiac contractile force (heart performance in cardiac insufficiency), thus they can be applied in the therapy of chronic heart failure and coronary ailments.
摘要翻译：本发明涉及通式（I）的新的3-（羟甲基） - 异喹啉衍生物及其酸加成盐，以及其制备方法，此外还涉及含有它们的药物组合物，其中 R和R1相同或不同，代表氢或卤素原子，硝基或C1-4烷氧基，R2代表氢原子或C1-4烷基，R3和R4相同或不同，代表氢原子或C1-4烷基，或R3和R4组合表示亚甲基，条件是当R代表3-甲氧基时，R1代表4-甲氧基，R3和R4相同，代表甲基或乙基 R2不是氢原子。通式（I）的化合物发挥有价值的正性肌力（强心）效能，它们能够增加心肌收缩力（心脏功能不全的心脏性能），因此可用于治疗慢性心力衰竭和冠状动脉疾病。

4. 发明授权

US4840948A 1-(hydroxystyrl)-5H-2,3-benzodiazepine derivatives, and pharmaceutical compositions containing the same 失效
标题翻译： 1-（羟基苯乙烯）-5H-2,3-苯并二氮杂衍生物和含有它们的药物组合物
公开(公告)号：US4840948A
公开(公告)日：1989-06-20
申请号：US51777
申请日：1987-05-20
申请人： Tibor Lang , Jeno Korosi , Gyorgy Rabloczky , Tamas Hamori , Maria Kuhar nee Kurthy , Istvan Polgari , Istvan Elekes , Gabor Zolyomi , Krisztina Heltai , Judit Sarossy nee Kincsesy , Zsuzsanna Lang nee Rihmer , Imre Moravcsik
发明人： Tibor Lang , Jeno Korosi , Gyorgy Rabloczky , Tamas Hamori , Maria Kuhar nee Kurthy , Istvan Polgari , Istvan Elekes , Gabor Zolyomi , Krisztina Heltai , Judit Sarossy nee Kincsesy , Zsuzsanna Lang nee Rihmer , Imre Moravcsik
IPC分类号： A61K31/55 , A61K31/551 , A61P9/04 , C07D243/02 , C07D243/04 , C07D491/056
CPC分类号： C07D243/02
摘要： This invention relates to new 1-(hydroxystyryl)-5H-2,3-benzodiazepine derivatives of the general formula (I) and to a process for the preparation thereof, furthermore to pharmaceutical compositions containing the same, ##STR1## wherein R stands for a hydrogen or halogen atom, or a C.sub.1-4 alkoxy group,R.sup.1 represents a hydrogen atom or a C.sub.1-4 alkyl group,R.sup.2 and R.sup.3 are identical and denote a C.sub.1-4 alkyl group, or combined they denote a methylene group.The compounds of the general formula (I) possess valuable positive inotropic (cardiotonic) potency, are capable to increase the myocardiac contractile force (heart performance in cardiac insufficiency), thus they can be applied in the therapy of chronic heart failure and coronary ailments.
摘要翻译：本发明涉及通式（I）的新的1-（羟基苯乙烯基）-5H-2,3-苯并二氮杂衍生物及其制备方法，此外还涉及含有它们的药物组合物，其中 R代表氢或卤素原子，或C1-4烷氧基，R1代表氢原子或C1-4烷基，R2和R3相同并表示C1-4烷基，或组合它们表示亚甲基组。通式（I）的化合物具有有价值的正性肌力（强心）效能，能够增加心肌收缩力（心脏功能不全的心脏性能），因此可用于慢性心力衰竭和冠状动脉疾病的治疗。

5. 发明授权

US4308278A Anorexigenic 4-[(3,4-dialkoxyphenyl)alkyl]-2-imidazolidinone derivatives 失效
标题翻译：厌氧性4 - [（3,4-二烷氧基苯基）烷基] -2-咪唑烷酮衍生物
公开(公告)号：US4308278A
公开(公告)日：1981-12-29
申请号：US90450
申请日：1979-11-01
申请人： Geza Schneider , Ferenc Andrasi , Pal Berzsenyi , Arpad Lazar , Sandor Elek , Istvan Elekes , Istvan Polgari
发明人： Geza Schneider , Ferenc Andrasi , Pal Berzsenyi , Arpad Lazar , Sandor Elek , Istvan Elekes , Istvan Polgari
IPC分类号： A61K31/415 , A61K31/4166 , A61P1/00 , A61P3/04 , C07C45/71 , C07D233/32 , C07D233/34 , C07D233/38 , C07D233/78
CPC分类号： C07C255/00 , C07C45/71 , C07D233/32 , C07D233/38 , C07D233/78 , Y10S514/91
摘要： 4-[(3,4-Dialkoxyphenyl)alkyl]-2-imidazolidinone derivatives having the formula I ##STR1## wherein R.sup.1 stands for a cycloalkyl group containing from 3 to 6 carbon atoms or benzyl group;R.sup.2 stands for hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms;R.sup.3 stands for hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms;R.sup.4 stands for hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms or an alkoxycarbonyl group containing from 1 to 4 carbon atoms; andR.sup.5 stands for hydrogen atom or an alkoxycarbonyl group containing from 1 to 4 carbon atoms,are prepared by(a) reducing a hydantoin derivative having the general formula II, wherein R.sup.1 and R.sup.2 are as defined above, with lithium aluminum hydride in a neutral organic solvent, or(b) hydrogenating catalytically an 1,3-dihydro-2H-imidazol-2-one derivative having the general formula III, wherein R.sup.1 and R.sup.3 are as defined above, while the meaning of R.sup.4 is hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms, or(c) reacting a carbamate derivative having the general formula IV, wherein R.sup.1 is as defined above, while R.sup.6 stands for an alkyl group containing from 1 to 4 carbon atoms, with an organic or inorganic base.The compounds having the formula I possess valuable therapeutical properties, mainly anorexigenic activity.
摘要翻译： 4 - [（3,4-二烷氧基苯基）烷基] -2-咪唑啉酮衍生物，其具有式I其中R1代表含有3至6个碳原子的环烷基或苄基; R2代表氢原子或含有1至4个碳原子的烷基; R3代表氢原子或含有1至4个碳原子的烷基; R4表示氢原子或含有1至4个碳原子的烷基或含有1至4个碳原子的烷氧基羰基; 并且R5代表氢原子或含有1至4个碳原子的烷氧基羰基，是通过以下步骤制备的：（a）将具有通式II的乙内酰脲衍生物（其中R 1和R 2如上定义）与中性的氢化铝锂有机溶剂，或（b）催化氢化具有通式III的1,3-二氢-2H-咪唑-2-酮衍生物，其中R 1和R 3如上所定义，而R 4的含义是氢原子或烷基含有1至4个碳原子的基团，或（c）使具有通式IV的氨基甲酸酯衍生物与其中R 1如上定义，而R6代表含有1至4个碳原子的烷基，与有机或无机基础。具有式I的化合物具有有价值的治疗性质，主要是厌食症活性。

6. 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。

7. 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。

8. 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。

9. 发明授权

US4310549A Treatment of hypertension with 1-tert.-butylamino-3-(2,5-dichlorophenoxy)-2-propanol 失效
标题翻译：用1-叔丁基氨基-3-（2,5-二氯苯氧基）-2-丙醇治疗高血压
公开(公告)号：US4310549A
公开(公告)日：1982-01-12
申请号：US72295
申请日：1979-09-04
申请人： Andor Hajos , Marton Fekete , Marianna Kurti , Tibor Lang , Lajos Toldy , Janos Borvendeg , Laszlo Nagy , Sandor Elek , Istvan Elekes , Istvan Polgari
发明人： Andor Hajos , Marton Fekete , Marianna Kurti , Tibor Lang , Lajos Toldy , Janos Borvendeg , Laszlo Nagy , Sandor Elek , Istvan Elekes , Istvan Polgari
IPC分类号： C07C217/34 , A61K31/055 , A61K31/13 , A61K31/135 , C07C20060101 , C07C57/00 , C07C67/00 , C07C213/00
CPC分类号： C07D303/24
摘要： 1-tert.-butylamino-3-(2,5-dichlorophenoxy)-2-propanol and its pharmaceutically acceptable acid addition salts possess hypotensive and bradycardizing effects. Thus they can be applied in human therapy for the treatment of hypertension and simultaneously also of tachycardia.
摘要翻译： 1-叔丁基氨基-3-（2,5-二氯苯氧基）-2-丙醇及其药学上可接受的酸加成盐具有降血压和减速作用。因此，它们可以应用于人类治疗用于治疗高血压，同时也可用于心动过速。

10. 发明授权

US4251658A 3-(1-Pyrazolyl)-pyridazine derivatives 失效
标题翻译： 3-（1-吡唑基） - 哒嗪衍生物
公开(公告)号：US4251658A
公开(公告)日：1981-02-17
申请号：US914084
申请日：1978-06-09
申请人： Geza Szilagyi , Endre Kasztreiner , Laszlo Tardos , Edit Kosa , Laszlo Jaszlits , Gyorgy Cseh , Andras Divald , Pal Tolnay , Sandor Elek , Istvan Elekes , Istvan Polgari
发明人： Geza Szilagyi , Endre Kasztreiner , Laszlo Tardos , Edit Kosa , Laszlo Jaszlits , Gyorgy Cseh , Andras Divald , Pal Tolnay , Sandor Elek , Istvan Elekes , Istvan Polgari
IPC分类号： C07D401/14 , A61K31/50 , A61K31/501 , A61P9/12 , A61P43/00 , C07D403/04 , C07D403/14 , C07D405/14
CPC分类号： C07D403/04
摘要： 3-(1-Pyrazolyl)-pyridazine derivatives of the formula I, or pharmaceutically acceptable acid addition salts thereof, which decrease high blood pressure and inhibit catabolism or prostaglandins, ##STR1## wherein R.sup.1 is hydrogen or C.sub.1-4 alkyl,R.sup.2 is hydrogen, cyano, carboxyl, carbamoyl, carbaxoyl or C.sub.1-4 alkoxycarbonyl,R.sup.3 is hydrogen or chlorine or --NR.sup.4 NHR.sup.5 or NR.sup.6 R.sup.7, wherein R.sup.4 and R.sup.5 are each hydrogen or C.sub.1-4 alkyl, wherein R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-5 alkyl, C.sub.1-5 hydroxyalkyl, C.sub.3-7 cycloalkyl, phenyl or benzyl, or benzyl or phenylethyl substituted with one or two chlorine atoms or methoxy groups, or a furylmethyl, pyridylmethyl, pyrrolidine or piperazine ring, or when R.sup.7 is hydrogen, R.sup.6 is --(CH.sub.2).sub.n --NR.sup.4 R.sup.5 wherein n is an integer from 1 to 3.
摘要翻译：降低高血压并抑制分解代谢或前列腺素的式I的3-（1-吡唑基） - 哒嗪衍生物或其药学上可接受的酸加成盐，其中R 1是氢或C 1-4烷基， R2是氢，氰基，羧基，氨基甲酰基，碳酰基或C1-4烷氧基羰基，R3是氢或氯或-NR4NHR5或NR6R7，其中R4和R5分别是氢或C1-4烷基，其中R6和R7各自是氢或C1 或烷基，C 1-5羟基烷基，C 3-7环烷基，苯基或苄基，或被一个或两个氯原子或甲氧基取代的苄基或苯乙基，或呋喃基甲基，吡啶基甲基，吡咯烷或哌嗪环，或者当R7为氢时， R 6为 - （CH 2）n -NR 4 R 5，其中n为1至3的整数。

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