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1. 发明授权

US5047396A Intravenous pharmaceutical composition and process for preparing the same 失效
标题翻译：静脉内药物组合物及其制备方法
公开(公告)号：US5047396A
公开(公告)日：1991-09-10
申请号：US383024
申请日：1989-07-21
申请人： Erno Orban , Tibor Balogh , Lajos Ila , Gabor Ambrus , Antonia Jekkel , Sandor Elek , Eva Tomori , Istvan Elekes , Eva T. Sarudy , Imre Moravcsik , Lajos Siklosi
发明人： Erno Orban , Tibor Balogh , Lajos Ila , Gabor Ambrus , Antonia Jekkel , Sandor Elek , Eva Tomori , Istvan Elekes , Eva T. Sarudy , Imre Moravcsik , Lajos Siklosi
IPC分类号： A61K9/08 , A61K9/00 , A61K38/00 , A61K38/13 , A61K47/10 , A61K47/14 , A61K47/34 , A61P37/06 , C07K7/64 , C07K14/195 , C07K14/41
CPC分类号： A61K9/0019 , A61K38/13 , A61K47/10 , A61K47/14 , Y10S514/885 , Y10S514/922 , Y10S514/943 , Y10S514/97
摘要： The present invention relates to an intravenous pharmaceutical composition comprising cyclosporin as active ingredient. The composition is composed ofa) 1 part by mass of one or more cyclosporins,b) 8 to 13 parts by mass of a monoester of a saturated hydroxylated fatty acid formed with polyethylene glycol or the mixture of said monoesters,c) 4 to 10 parts by mass of one or more intravenously administerable mono- or polivalent alcohols.The invention further relates to a process for preparing such composition.
摘要翻译：本发明涉及包含环孢菌素作为活性成分的静脉内药物组合物。该组合物由以下组成：a）1质量份的一种或多种环孢菌素，b）8〜13质量份由聚乙二醇形成的饱和羟基化脂肪酸的单酯或所述单酯的混合物，c）4〜10 质量份的一种或多种可静脉给药的单价或多价醇。本发明还涉及制备这种组合物的方法。

2. 发明授权

US4423044A 3,4-Dihydro-5H-2,3-benzodiazepine derivatives and pharmaceutical use thereof 失效
标题翻译： 3,4-二氢-5H-2,3-苯并二氮杂衍生物及其药物用途
公开(公告)号：US4423044A
公开(公告)日：1983-12-27
申请号：US352346
申请日：1982-02-25
申请人： Jeno Korosi , Tibor Lang , Ferene Andrasi , Jozsef Szekely , Tamas Hamori , Tibor Balogh , Lajos Ila , Katalin Goldschmidt , Eleonora Sineger , Imre Moravcsik
发明人： Jeno Korosi , Tibor Lang , Ferene Andrasi , Jozsef Szekely , Tamas Hamori , Tibor Balogh , Lajos Ila , Katalin Goldschmidt , Eleonora Sineger , Imre Moravcsik
IPC分类号： A61K31/55 , A61K31/551 , A61P23/00 , A61P25/04 , A61P25/20 , C07D243/02 , C07D243/04 , C07D405/04 , C07D409/04 , C07D243/00
CPC分类号： C07D243/02
摘要： The invention relates to new 3,4-dihydro-5H-2,3-benzodiazepine derivatives of general formula (I) and pharmaceutically acceptable acid addition salts thereof, ##STR1## wherein R represents a phenyl group optionally carrying one or two substituents selected from the group consisting of halogen, hydroxy, C.sub.1-4 alkoxy and benzyloxy; a furyl or a thienyl group,R.sup.1 stands for a hydrogen atom or a C.sub.1-4 alkyl group,R.sup.2 and R.sup.3 each represent hydrogen atom, C.sub.1-4 alkoxy, C.sub.4-7 cycloalkoxy or benzyloxy group.The new compounds of the general formula (I) can be prepared by reducing a 5H-2,3-benzodiazepine derivative of the general formula (II) ##STR2## wherein R, R.sup.1, R.sup.2 and R.sup.3 have the above-defined meanings, with an inorganic or organic hydride and/or complex metal hydride.The new compounds of the general formula (I) possess significant central nervous effects and can advantageously be used in the therapy.
摘要翻译：本发明涉及通式（I）的新的3,4-二氢-5H-2,3-苯并二氮杂衍生物及其药学上可接受的酸加成盐，其中R表示任选携带一个或两个选自卤素，羟基，C 1-4烷氧基和苄氧基的取代基; 呋喃基或噻吩基，R1表示氢原子或C1-4烷基，R2和R3各自表示氢原子，C1-4烷氧基，C4-7环烷氧基或苄氧基。通式（I）的新化合物可以通过还原通式（II）的式（II）的5H-2,3-苯并二氮杂衍生物制备：其中R，R 1，R 2和R 3具有上述定义含有无机或有机氢化物和/或络合金属氢化物。通式（I）的新化合物具有显着的中枢神经效应，并且可以有利地用于治疗。

3. 发明授权

US4329457A Process for the preparation of 6-(substituted amino)-3-pyridazinylhydrazines and their salts 失效
公开(公告)号：US4329457A
公开(公告)日：1982-05-11
申请号：US147224
申请日：1980-05-06
申请人： Geza Szilagyi , Peter Matyus , Endre Kasztreiner , Tibor Balogh , Lajos Ila
发明人： Geza Szilagyi , Peter Matyus , Endre Kasztreiner , Tibor Balogh , Lajos Ila
IPC分类号： A61K31/50 , A61P9/12 , C07D237/20 , C07D413/02
CPC分类号： C07D237/20
摘要： The invention relates to a novel process for the preparation of 6-(substituted amino)-3-pyridazinylhydrazines having the general formula I ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R.sup.1 stands for hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms;R.sup.2 and R.sup.3 may be the same or different and stand for alkyl groups containing from 1 to 6 carbon atoms, alkenyl groups containing from 2 to 6 carbon atoms, hydroxyalkyl groups containing from 2 to 4 carbon atoms, cycloalkyl groups containing from 3 to 8 carbon atoms, phenyl or benzyl groups or phenyl, benzyl or phenylethyl groups containing one or two halogen atoms, nitro, methoxy or hydroxyl groups, and one of R.sup.2 and R.sup.3 may stand also for a hydrogen atom, or R.sup.2 and R.sup.3 together with the neighboring nitrogen atom may build up also a morpholino, pyrrolidino, piperidino, heptamethyleneimino or N-methylpiperazino group.The process consists in that a compound having the general formula II ##STR2## wherein R.sup.1 is as defined above, R.sup.4 stands for a chlorine or bromine atom or methylthio group, while A stands for a 1,7,7-trimethyl-2-bicyclo(2,2,1)heptylidene or a benzylidene group substituted by an R.sup.5 group, wherein R.sup.5 stands for hydrogen, chlorine or bromine atom, or a methoxy, nitro or methylsulphonyl group - is reacted with an amine having the general formula IIIR.sup.2 R.sup.3 NH (III)wherein R.sup.2 and R.sup.3 are as defined above - and the compound thus obtained having the general formula IV ##STR3## wherein R.sup.1, R.sup.2, R.sup.3 and A are as defined above - is subjected to acidic hydrolysis.The 6-(substituted amino)-3-pyridazinylhydrazines having the general formula I and prepared by the novel process of invention, possess a significant hypotensive effect as well as they are used as starting materials for the preparation of 6-(substituted amino)-3-pyridazinylhydrazines having a very significant hypotensive action.

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