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1. 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。

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

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。

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

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。

7. 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。

8. 发明授权

US5261620A Pope roll winder having direct drive 失效
标题翻译：教练辊卷绕机直接驱动
公开(公告)号：US5261620A
公开(公告)日：1993-11-16
申请号：US837734
申请日：1992-02-19
申请人： Dieter Holzinger , Roland Moller , Karl Ruck
发明人： Dieter Holzinger , Roland Moller , Karl Ruck
IPC分类号： B65H19/22 , B65H18/16
CPC分类号： B65H19/2261 , B65H2408/236 , B65H2515/12
摘要： A winder for winding a running web of paper, foil or similar. A support drum of web width is provided, and a winding drum on which the web is wound to a roll. A pair of primary swivel levers each feature on one end a fork for receiving a winding drum bearing and is mounted with its other end in the region of the support roll axis in such a way that the winding drum, in swiveling from a first position above the support roll, will in the running direction of the web approach the support roll while moving around it, passing in the process a primary section until reaching a second position. The winding drum with the still unfinished paper roll is taken over by a pair of secondary swivel levers with an essentially horizontal guideway extending from the second position across a secondary section up to a third position. A contact device forces the winding drum onto the support roll, and a drive is coordinated with the winding drum. A slide features guideways for guidance of the drive as it passes through the primary section, and is connected with the primary levers in such a way that it also will perform their swivel movement. A connecting link guide adjusts the radial position of the slide according to the current paper roll diameter, and ensures the slide tracking according to the increase in paper roll diameter. A guide rod clutch is arranged between the drive and the winding drum.
摘要翻译：用于卷绕纸张，箔片或类似物的运行网络的卷绕机。提供腹板宽度的支撑鼓，以及卷筒，卷筒卷绕在卷筒上。一对主旋转杆各自在一端具有用于接收卷绕鼓轴承的叉，并且其另一端安装在支撑辊轴线的区域中，使得卷绕滚筒从上方的第一位置旋转支撑辊将沿着卷筒的运动方向接近支撑辊，同时在其周围移动，在该过程中通过主要部分直到达到第二位置。具有仍未完成的卷筒纸的卷绕筒被一对辅助旋转杆带走，该第二旋转杆具有从第二位置穿过次级部分延伸到第三位置的基本上水平的导轨。接触装置将卷绕鼓施加到支撑辊上，并且驱动器与卷绕鼓配合。滑块具有用于在驱动器穿过主要部分时引导的导轨，并且与主杆连接，使得其也将执行其旋转运动。连接导轨根据当前纸卷直径调整滑块的径向位置，并根据纸卷直径的增加确保滑块跟踪。导杆离合器布置在驱动器和卷绕鼓之间。

9. 发明申请

US20070265462A1 Method for Producing Amino- or Hydroxybenzonitriles 有权
标题翻译：生产氨基或羟基苯腈的方法
公开(公告)号：US20070265462A1
公开(公告)日：2007-11-15
申请号：US11791579
申请日：2005-11-29
申请人： Roland Moller , Mario Gomez , Klaus Einmayr , Jens Hildebrad , Hans-Georg Erben , Hans-Peter Krimmer
发明人： Roland Moller , Mario Gomez , Klaus Einmayr , Jens Hildebrad , Hans-Georg Erben , Hans-Peter Krimmer
IPC分类号： C07C253/00
CPC分类号： C07C253/22 , C07C253/34 , Y02P20/127 , C07C255/53
摘要： What is claimed is a process for preparing amino- or hydroxybenzonitriles, in which, in the course of an ammonolysis, the corresponding amino- or hydroxybenzoic acid compounds are reacted with ammonia in the presence of a supported catalyst comprising phosphate at temperatures between 250° C. and 500° C. The actual preparation step is performed in a reaction gas (mixture) and without involvement of an organic solvent, and is followed by an at least 2-stage purification step. In this purification step, the gaseous mixture obtained from the preparation step is first converted to an aqueous basic suspension and then the product present in the solid is released from this suspension. The main advantage of this combination process is that the starting materials are not esters, which is why the resulting products, in contrast to the processes which are otherwise customary, are free of the by-products which are otherwise customary, which leads to a high product purity. The process claimed can additionally be performed in an extremely economically viable manner, since the end product and the by-products are present in different states of matter in the suspension used and can therefore be separated easily from one another. In this way, solvent-free amino- or hydroxyl-containing benzonitriles are obtained in high yield and significantly improved product quality.
摘要翻译：所要求的是制备氨基或羟基苯腈的方法，其中在氨解过程中，相应的氨基或羟基苯甲酸化合物在含有磷酸盐的负载型催化剂存在下，与氨反应，温度在250℃ 和500℃。实际的制备步骤在反应气体（混合物）中进行，而不涉及有机溶剂，然后进行至少2阶段的纯化步骤。在该纯化步骤中，将从制备步骤获得的气体混合物首先转化为碱性悬浮液，然后将固体中存在的产物从该悬浮液中释放。这种组合方法的主要优点是起始原料不是酯类，这就是为什么所产生的产品与其他习惯方法相反的方法不同于其他习惯的副产物，这导致高产品纯度所要求的方法可另外以非常经济可行的方式进行，因为最终产物和副产物以所使用的悬浮液中物质的不同状态存在，因此可以彼此容易地分离。以这种方式，可以高产率获得无溶剂的含氨基或羟基的苯腈，并显着提高产品质量。

10. 发明授权

US5760221A Method for the preparation of hexahydroazepinones and hexahydroazepinoles 失效
标题翻译：六氢吖嗪酮和六氢吖庚因的制备方法
公开(公告)号：US5760221A
公开(公告)日：1998-06-02
申请号：US359457
申请日：1994-12-19
申请人： Alfred Olbrich , Jurgen Engel , Bernhard Kutscher , Roland Moller
发明人： Alfred Olbrich , Jurgen Engel , Bernhard Kutscher , Roland Moller
IPC分类号： C07D243/02 , B01J19/18 , B01J19/26 , C07D223/08 , C07D267/04 , C07D281/02 , C07D403/04 , C07D267/02 , C07D243/00
CPC分类号： C07D403/04 , B01J19/1881 , B01J19/26 , B01J2208/00247
摘要： This disclosure describes two technical procedures for the high-yield synthesis of heterocyclic seven-membered ring-systems by Dieckmann-condensation avoiding usual dilution techniques and long reaction times. Thus, it significantly increases the overall yields of the pharmaceutically active ingredients azelastine and flezelastine, whose synthesis, starting from these seven-membered heterocyclic rings, is reported elsewhere. Yields range from 80-89%, avoiding waste and increasing economics of the synthesis.
摘要翻译：本公开描述了通过Dieckmann缩合避免常规稀释技术和长反应时间高收率合成杂环七元环体系的两个技术程序。因此，它显着增加了药物活性成分阿斯巴斯丁和哌拉斯他汀的总产率，其合成从这些七元杂环开始在其他地方报道。产量在80-89％之间，避免了浪费和增加合成的经济性。

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