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1. 发明授权

US5455264A RS-thioctic acid with novel morphology 失效
标题翻译： RS-硫辛酸具有新颖的形态
公开(公告)号：US5455264A
公开(公告)日：1995-10-03
申请号：US134695
申请日：1993-10-12
申请人： Thomas Beisswenger , Horst Bethge , Joachim Goede , Frank Hubner , Klaus Huthmacher , Herbert Klenk , Roland Moller
发明人： Thomas Beisswenger , Horst Bethge , Joachim Goede , Frank Hubner , Klaus Huthmacher , Herbert Klenk , Roland Moller
IPC分类号： C07D339/04 , A61K31/385
CPC分类号： C07D339/04
摘要： RS-thioctic acid with a novel morphology which is obtained by a recrystallization process.
摘要翻译：具有通过重结晶过程获得的新型形态的RS-硫辛酸。

2. 发明授权

US6013815A Production and use of salts of 6,8-bis (amidiniumthio)-octanoic acid 失效
标题翻译： 6,8-双（脒硫代） - 辛酸盐的生产和使用
公开(公告)号：US6013815A
公开(公告)日：2000-01-11
申请号：US40440
申请日：1998-03-18
申请人： Thomas Beisswenger , Rainer Gewald , Alfred Olbrich , Horst Bethge , Frank Hubner , Klaus Huthmacher , Herbert Klenk , Roland Moller , Stephan Rautenberg , Gerhard Sator
发明人： Thomas Beisswenger , Rainer Gewald , Alfred Olbrich , Horst Bethge , Frank Hubner , Klaus Huthmacher , Herbert Klenk , Roland Moller , Stephan Rautenberg , Gerhard Sator
IPC分类号： C07C319/02 , C07C323/52 , C07C335/32 , C07D339/04 , C07B45/00
CPC分类号： C07D339/04 , C07C319/02 , C07C335/32
摘要： The invention relates to the production and purification of salts of 6,8-bis (amidiniumthio)octanoic acid, its enantiomers (+)-6,8-bis(amidiniumthio)octanoic acid and (-)-6,8-bis (amidiniumthio)octanoic acid and of the esters of these compounds as well as to their use to produce dihydrolipoic acid and .alpha.-lipoic acid.
摘要翻译：本发明涉及6,8-双（脒硫）辛酸及其对映体（+） - 6,8-双（脒硫）辛酸和（ - ） - 6,8-双（脒硫））辛酸和这些化合物的酯，以及它们用于产生二氢硫辛酸和α-硫辛酸的用途。

3. 发明授权

US5760268A Production and use of salts of 6, 8-bis (amidiniumthio) -octanoic acid 失效
标题翻译：制备和使用6,8-双（脒硫代） - 辛酸的盐
公开(公告)号：US5760268A
公开(公告)日：1998-06-02
申请号：US786053
申请日：1997-01-21
申请人： Thomas Beisswenger , Rainer Gewald , Alfred Olbrich , Horst Bethge , Frank Hubner , Klaus Huthmacher , Herbert Klenk , Roland Moller , Stephan Rautenberg , Gerhard Sator
发明人： Thomas Beisswenger , Rainer Gewald , Alfred Olbrich , Horst Bethge , Frank Hubner , Klaus Huthmacher , Herbert Klenk , Roland Moller , Stephan Rautenberg , Gerhard Sator
IPC分类号： C07C319/02 , C07C323/52 , C07C335/32 , C07D339/04
CPC分类号： C07D339/04 , C07C319/02 , C07C335/32
摘要： The invention relates to the production and purification of salts of 6,8-bis(amidiniumthio) octanoic acid, its enantiomers (+)-6,8-bis(amidiniumthio)octanoic acid and (-)-6,8-bis (amidiniumthio)octanoic acid and of the esters of these compounds as well as to their use to produce dihydrolipoic acid and .alpha.-lipoic acid.
摘要翻译：本发明涉及6,8-双（脒硫）辛酸及其对映体（+） - 6,8-双（脒硫）辛酸和（ - ） - 6,8-双（脒硫））辛酸和这些化合物的酯，以及它们用于产生二氢硫辛酸和α-硫辛酸的用途。

4. 发明授权

US5281722A Preparation and use of salts of the pure enantiomers of alpha-lipoic acid 失效
标题翻译： α-硫辛酸纯对映异构体的盐的制备和使用
公开(公告)号：US5281722A
公开(公告)日：1994-01-25
申请号：US975075
申请日：1992-11-12
申请人： Gottfried Blaschke , Ursula Scheidemantel , Horst Bethge , Roland Moller , Thomas Beisswenger , Klaus Huthmacher
发明人： Gottfried Blaschke , Ursula Scheidemantel , Horst Bethge , Roland Moller , Thomas Beisswenger , Klaus Huthmacher
IPC分类号： A61K31/385 , A61P25/04 , A61P29/00 , C07B57/00 , C07C319/06 , C07C323/52 , C07D339/04 , C11C3/00
CPC分类号： C07C319/06 , C07D339/04
摘要： The pure enantiomers of alpha-lipoic acid are obtained by formation of the diastereomeric salt pairs with the optical antipodes of alpha-methylbenzylamine in solution.
摘要翻译：通过与溶液中的α-甲基苄胺的光学对映体形成非对映体盐对获得α-硫辛酸的纯对映体。

5. 发明授权

US5981767A Method of producing dry thioctic acid 失效
标题翻译：干硫辛酸生产方法
公开(公告)号：US5981767A
公开(公告)日：1999-11-09
申请号：US102758
申请日：1998-06-23
申请人： Herbert Tanner , Karlheinz Drauz , Gerhard Sator , Horst Bethge , Roland Moller , Frank Hubner , Thomas Tacke , Claus Rehren
发明人： Herbert Tanner , Karlheinz Drauz , Gerhard Sator , Horst Bethge , Roland Moller , Frank Hubner , Thomas Tacke , Claus Rehren
IPC分类号： A61K31/385 , A61P25/00 , A61P25/04 , A61P29/00 , C07D339/04 , C07D333/24
CPC分类号： C07D339/04 , Y02P20/544
摘要： The present invention is relative to a method of producing dry thioctic acid in which a raw material in which concentrated thioctic acid is present is treated with liquid or supercritical CO.sub.2, thus yielding thioctic acid with low residual solvent contents in a simple industrial method.
摘要翻译：本发明涉及一种生产干硫辛酸的方法，其中存在浓硫硫酸的原料用液体或超临界CO 2处理，从而以简单的工业方法产生具有低残留溶剂含量的硫辛酸。

6. 发明授权

US5041655A Method of preparing 1,6-di(N.sup.3 -cyano-N.sup.1 -guanidino) hexane 失效
标题翻译：制备1,6-二（N 3 - 氰基-N 1胍基）己烷的方法
公开(公告)号：US5041655A
公开(公告)日：1991-08-20
申请号：US241116
申请日：1988-09-06
申请人： Klaus Huthmacher , Axel Kleemann , Horst Bethge , Rolf Braun
发明人： Klaus Huthmacher , Axel Kleemann , Horst Bethge , Rolf Braun
IPC分类号： C07C67/00 , C07C239/00 , C07C277/08 , C07C279/28
CPC分类号： C07C279/28
摘要： An improved method of preparing 1,6-di(N.sup.3 -cyano-N.sup.1 -guanidino) hexane from alkali dicyanamide and a hexamethylene diammonium salt in alcoholic solution or suspension. The reaction is carried out in the presence of a limited amount of water and of a catalytic amount of a base, preferably a tertiary amine. The pH of the reaction mixture at the start of the reaction is 8 to 10. After the reaction is over, the reaction mixture is compounded with water at a temperature above 80.degree. C. and the coarse product which crystallizes out is separated from the liquid phase.Preferably, sodium dicyanamide and hexamethylene diamine dihydrochloride, preferably formed in situ from aqueous 1,6-diaminohexane and aqueous hydrochloric acid, are reacted at pH 9-9.5 in n-butanol in the presence of 0.1 to 20% by wt. water in relation to the solvent including water.1,6-di(N.sup.3 -cyano-N.sup.1 -guanidino) hexane is obtained in a high yield (85-86%) and with great purity (95-97%) and with a considerably improved space-time yield.
摘要翻译：一种在醇溶液或悬浮液中由碱二氰胺和六亚甲基二铵盐制备1,6-二（N 3 - 氰基-N 1胍基）己烷的改进方法。反应在有限量的水和催化量的碱，优选叔胺的存在下进行。反应开始时反应混合物的pH值为8〜10。反应结束后，将反应混合物在高于80℃的温度下与水混合，将结晶出来的粗产物与液体分离相。优选地，优选在1,6-二氨基己烷水溶液和盐酸水溶液中原位形成的二氰胺钠和六亚甲基二胺盐酸盐在pH为9-9.5的正丁醇中，在0.1-20重量％的存在下反应。相对于包括水在内的溶剂的水。以高产率（85-86％）和高纯度（95-97％）获得1,6-二（N 3 - 氰基-N 1胍基）己烷，并具有显着提高的时空产率。

7. 发明授权

US5705192A Method of producing flowable R,S-thioctic acid, R,S-thioctic acid and its use 失效
标题翻译：生产可流动的R，S-硫辛酸，R，S-硫辛酸及其用途的方法
公开(公告)号：US5705192A
公开(公告)日：1998-01-06
申请号：US618790
申请日：1996-03-20
申请人： Horst Bethge , Kurt Klostermann , Roland Moller , Gerhard Sator
发明人： Horst Bethge , Kurt Klostermann , Roland Moller , Gerhard Sator
IPC分类号： C07D339/04 , A61K9/16 , A61K9/20 , A61K31/385 , A61K9/14
CPC分类号： A61K9/1688 , A61K31/385
摘要： 1. A method of producing flowable R,S-thioctic acid, R,S-thioctic acid and its use. 2.1. Known methods of preparing flowable thioctic acid which can be galenically further processed by pressing to highly-concentrated, solid presentations with active-substance contents of more than 200 mg pure substance require the mixing of the thioctic-acid forms of different origins and/or a spraying on of galenic adjuvants from aqueous solution and a subsequent grinding process in order to arrive at a pressable granulate. 2.2. As a result of the fact that thioctic acid of any origin is placed in the fluid bed of a device suited for producing a fluid bed and that a built-up granulate consisting of thioctic acid is obtained by spraying a solution of thioctic acid of any origin onto the matter placed in the fluid bed under simultaneous removal of the solvent, it is possible to make a thioctic-acid form available which does not adhere to the pressing tool or exhibit a tendency to form fissures on the tablet even when tablets with 600 mg or more active-substance content are prepared. The novel R,S-thioctic acid has a specific surface of >0.7 m.sup.2 /g and a number of mesopores with a diameter between 2 and 30 nm.
摘要翻译： 1.生产可流动的R，S-硫辛酸，R，S-硫辛酸及其用途的方法。 2.1。制备可流动的硫辛酸的已知方法，其可以通过压制具有超过200mg纯物质的活性物质含量的高浓度固体表现物进一步加工而进一步加工，需要混合不同来源的硫辛酸形式和/或从水溶液中喷洒盖仑佐剂并随后进行研磨处理以得到可挤压颗粒。 2.2。由于任何来源的硫辛酸被放置在适于生产流化床的装置的流化床中，并且由硫辛酸组成的积层颗粒通过喷洒任何起源的硫辛酸溶液而获得在同时除去溶剂的情况下放置在流化床中的物质上，可以制备硫辛酸形式，其不粘附到压制工具上，或者表现出在片剂上形成裂缝的趋势，即使具有600mg 或更多的活性物质含量。新型R，S-硫辛酸具有> 0.7m 2 / g的比表面积和直径在2和30nm之间的多个中孔。

8. 发明授权

US5621117A Method for the racemization of enantiomers of .alpha.-lipoic acid 失效
标题翻译： α-硫辛酸对映异构体外消旋化的方法
公开(公告)号：US5621117A
公开(公告)日：1997-04-15
申请号：US504557
申请日：1995-07-20
申请人： Horst Bethge , Roland Moeller , Gerhard Sator , Stefan Merget , Thomas Beisswenger
发明人： Horst Bethge , Roland Moeller , Gerhard Sator , Stefan Merget , Thomas Beisswenger
IPC分类号： A61K31/385 , A61P29/00 , A61P43/00 , C07D339/04
CPC分类号： C07D339/04
摘要： Method for the conversion of the enantiomers of .alpha.-lipoic acid into the corresponding racemic mixture by racemizing the .alpha.-lipoic acid (pure optical isomers of .alpha.-lipoic acid or mixtures of optical isomers of .alpha.-lipoic acid wherein one of the optical isomers is present in excess) at temperatures of between 110.degree. C. and 200.degree. C. at pressures of from normal pressure up to 50 bar for a reaction time of 10 to 48 hours.
摘要翻译：将α-硫辛酸的对映异构体转化成相应的外消旋混合物的方法，其中将α-硫辛酸（α-硫辛酸的纯光学异构体或α-硫辛酸的光学异构体的混合物，其中一种光学异构体是存在于过量的温度下，在110℃至200℃的温度下，在常压至50巴的压力下反应10至48小时。

9. 发明授权

US5962696A Process for the preparation of 1-(N 2-(S)-ethoxycarbonyl)--3 phenylpropyl-N6-trifluoracetyl))-L-lysyl-L-prolin (Lisinopril(Tfa) ethylester, LPE)) 失效
标题翻译：制备1-（N 2 - （S） - 乙氧基羰基）-3-苯基丙基-N6-三氟乙酰基））-L-赖氨酰-L-脯氨酸（赖诺普利（Tfa）乙酯，LPE））的方法）
公开(公告)号：US5962696A
公开(公告)日：1999-10-05
申请号：US94319
申请日：1998-06-09
申请人： Herbert Tanner , Karlheinz Drauz , Klaus Stingl , Gerhard Sator , Horst Bethge , Roland Moller , Thomas Tacke , Claus Rehren
发明人： Herbert Tanner , Karlheinz Drauz , Klaus Stingl , Gerhard Sator , Horst Bethge , Roland Moller , Thomas Tacke , Claus Rehren
IPC分类号： C07K1/36 , C07K5/02 , C07K5/068 , C07D207/08
CPC分类号： C07K5/0222 , Y02P20/544
摘要： There is provided a process for the work-up of this material having the formula ##STR1## because of its poor crystallizability has heretofore been available only with large yield losses. The yield losses are due to the fact that the crystals of this compound are associated with large amounts of residual solvent material which gives rise to complex and expensive drying procedures. In accordance with the present invention the crude LPE is dried by means of fluid or supercritical carbon dioxide which maces it possible to reduce drying times from the previous range of about 124 hours to about 10 hours for the same amount of product and thus produce a dry LPE which has smaller amounts of residual solvent, as well as smaller by-products than that obtained by conventional drying.
摘要翻译：提供了具有该配方的这种材料的处理方法，因为其结晶性差，迄今为止只有大的产率损失才可用。产率损失是由于这种化合物的晶体与大量的残留溶剂材料相关联，导致复杂且昂贵的干燥程序。根据本发明，粗液LPE通过流体或超临界二氧化碳进行干燥，可以使干燥时间从相同量产物的约124小时至约10小时的干燥时间减少，从而产生干燥 LPE具有较少量的残留溶剂，以及比通过常规干燥获得的副产物更小的副产物。

10. 发明授权

US4415738A Process for the production thiazolines-(3) 失效
标题翻译：生产噻唑啉的方法 - （3）
公开(公告)号：US4415738A
公开(公告)日：1983-11-15
申请号：US281858
申请日：1981-07-09
申请人： Jurgen Martens , Paul Scherberich , Horst Bethge , Axel Kleemann
发明人： Jurgen Martens , Paul Scherberich , Horst Bethge , Axel Kleemann
IPC分类号： C07D277/10 , C07D277/60 , C07D277/08
CPC分类号： C07D277/60 , C07D277/10
摘要： There are produced thiazoline-(3) compounds which optionally are substituted or unsubstituted in the 2 and/or 5 positions by reaction of oxo compounds with a metal sulfides, ammonia and oxo compounds which are substituted by halogen in the position adjacent to the oxo group. In this process a mixture of oxo compounds, metal sulfides and ammonia is present and the halogen substituted oxo compound is introduced into the mixture. By using in this manner of mixing, high yields are obtained in a relatively short period of time.
摘要翻译：产生噻唑啉 - （3）化合物，其任选在2和/或5位上被取代或未取代，其中氧代化合物与金属硫化物，氨和氧代化合物的反应，所述卤代化合物在与氧代基相邻的位置被卤素取代。在该方法中，存在氧化合物，金属硫化物和氨的混合物，并将卤素取代的氧代化合物引入混合物中。通过以这种混合方式使用，在相对短的时间内获得高产率。

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