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61. 发明授权

US09226969B2 Salt form of a multi-arm polymer-drug conjugate 有权
标题翻译：盐形式的多臂聚合物 - 药物缀合物
公开(公告)号：US09226969B2
公开(公告)日：2016-01-05
申请号：US13510587
申请日：2010-11-18
申请人： Anthony O. Chong , Seoju Lee , Bhalchandra V. Joshi , Brian Bray , Shaoyong Nie , Patrick L. Spence , Antoni Kozlowski , Samuel P. McManus , Sachin Tipnis , David Swallow , John R. Handley , Anthony G. Schaefer
发明人： Anthony O. Chong , Seoju Lee , Bhalchandra V. Joshi , Brian Bray , Shaoyong Nie , Patrick L. Spence , Antoni Kozlowski , Samuel P. McManus , Sachin Tipnis , Greg Lavaty , David Swallow , John R. Handley , Anthony G. Schaefer
IPC分类号： A61K31/4745 , C07D491/22 , A61K47/48 , C08G65/329 , C08G65/333 , C07C51/41 , C07C53/18 , C08G65/48
CPC分类号： C08G65/331 , A61K31/4745 , A61K47/60 , C07C51/412 , C07C53/18 , C07D491/22 , C08G65/329 , C08G65/33396 , C08G65/48 , C08L2203/02
摘要： Among other aspects, provided herein is a hydrohalide salt of a multi-arm water-soluble polyethylene glycol-drug conjugate, along with related methods of making and using the same. The hydrohalide salt is stably formed, and appears to be more resistant to hydrolytic degradation than the corresponding free base form of the conjugate.
摘要翻译：在其它方面，本文提供了多臂水溶性聚乙二醇 - 药物偶联物的氢卤酸盐，以及制备和使用它们的相关方法。氢卤酸盐稳定地形成，似乎比结合物的相应游离碱形式更耐水解降解。

62. 发明申请

US20150376106A1 PROCESS TO PREPARE TREPROSTINIL, THE ACTIVE INGREDIENT IN REMODULIN® 审中-公开
公开(公告)号：US20150376106A1
公开(公告)日：2015-12-31
申请号：US14849981
申请日：2015-09-10
申请人： United Therapeutics Corporation
发明人： Hitesh BATRA , Sudersan M. TULADHAR , Raju PENMASTA , David A. WALSH
IPC分类号： C07C59/72 , C07C51/41
CPC分类号： A61K31/192 , A01N37/10 , C07C39/12 , C07C39/17 , C07C51/08 , C07C51/41 , C07C51/412 , C07C59/60 , C07C59/72 , C07C213/08 , C07C253/00 , C07C405/0075 , C07C2103/12
摘要： This present invention relates to an improved process to prepare prostacyclin derivatives. One embodiment provides for an improved process to convert benzindene triol to treprostinil via salts of treprostinil and to purify treprostinil.

63. 发明授权

US09222035B2 Process for stabilizing an oil-in-water or water-in-oil emulsion 有权
标题翻译：用于稳定水包油或油包水乳液的方法
公开(公告)号：US09222035B2
公开(公告)日：2015-12-29
申请号：US12743358
申请日：2008-11-17
申请人： Jens Emil Vindstad , Heidi Mediaas , Knut Vebjørn Grande
发明人： Jens Emil Vindstad , Heidi Mediaas , Knut Vebjørn Grande
IPC分类号： B01F3/08 , C10G31/08 , C10G19/02 , C10G29/06 , C10M129/56 , C10M129/58 , B01F17/00
CPC分类号： C10G31/08 , A23L33/10 , A23V2002/00 , B01F3/0807 , B01F17/0021 , C07C51/347 , C07C51/412 , C07C51/46 , C10G19/02 , C10G29/06 , C10M129/56 , C10M129/58 , C10M129/93
摘要： A process for the preparation of at least one ARN acid or salt thereof comprising: (I) allowing at least one ARN acid salt to form during the production of crude oil in the presence of water; (II) removing at least 5 wt % of the formed at least one ARN acid salt, e.g. from the oil water interface; and optionally (III) converting said salt into an acid.
摘要翻译：一种制备至少一种ARN酸或其盐的方法，包括：（I）在水存在下在原油生产期间允许形成至少一种ARN酸盐; （II）除去至少5重量％的形成的至少一种ARN酸盐，例如，从油水界面; 和任选地（III）将所述盐转化成酸。

64. 发明申请

US20150361216A1 PROCESS FOR THE PREPARATION OF A POLYAMIDE 有权
标题翻译：制备聚酰胺的方法
公开(公告)号：US20150361216A1
公开(公告)日：2015-12-17
申请号：US14763642
申请日：2014-01-30
申请人： DSM IP ASSETS B.V.
发明人： Eric GROLMAN , Rudy RULKENS , Konraad Albert Louise Hector DULLAERT , Renier Henricus Maria KIERKELS , Geert Adelina Rudolf VANDEN POEL
IPC分类号： C08G69/32
CPC分类号： C08G69/32 , C07C51/412 , C07C209/68 , C08G69/26 , C08G69/265 , C08G69/30 , C08L77/06 , C08L77/10 , C07C63/333 , C07C63/38 , C07C63/28 , C07C211/12 , C07C211/09
摘要： The invention relates to a process for preparing a semi-aromatic polyamide from diamine and dicarboxylic acid, comprising steps of •(i) dosing a liquid diamine to an agitated powder comprising an aromatic dicarboxylic acid thereby forming a powder comprising a diamine/dicarboxylic acid salt (DD-salt), and •(ii) solid-state polymerizing the DD-salt to obtain the polyamide.
摘要翻译：本发明涉及一种由二胺和二羧酸制备半芳族聚酰胺的方法，包括以下步骤：（i）将液体二胺加入到包含芳族二羧酸的搅拌粉末中，从而形成包含二胺/二羧酸盐的粉末（DD-盐），和（ii）固态聚合DD盐以获得聚酰胺。

65. 发明申请

US20150361028A1 PROCESS FOR PREPARING A DIAMINE/DICARBOXYLIC ACID SALT 有权
标题翻译：制备二胺/二羧酸盐的方法
公开(公告)号：US20150361028A1
公开(公告)日：2015-12-17
申请号：US14234248
申请日：2012-07-26
申请人： Eric Grolman , Rudy Rulkens
发明人： Eric Grolman , Rudy Rulkens
IPC分类号： C07C209/68 , C07C51/41 , C07C211/12 , C07C55/20 , C07C211/09 , C07C63/28 , C07C55/14
CPC分类号： C07C209/68 , C07B2200/13 , C07C51/412 , C07C55/14 , C07C55/20 , C07C63/28 , C07C211/09 , C07C211/12 , C08G69/04 , C08G69/265 , C07C63/24 , C07C63/26 , C07C63/36
摘要： The present invention also relates to a process for preparing a diamine/dicarboxylic acid salt wherein the dicarboxylic acid comprises an aromatic dicarboxylic acid and is provided in a powder form; the diamine is provided in a liquid form gradually dosed to the dicarboxylic acid powder, while keeping the dicarboxylic acid powder in constant movement; the processing temperature is above 0° C. and below the boiling temperature of the diamine and the melting temperature of the acid and the salt, and the reaction mixture comprises at most 5 wt. % of water. The present invention also relates to an anhydrous diamine/dicarboxylic acid salt obtainable by the process according to invention, or any embodiment thereof as described above.
摘要翻译：本发明还涉及一种制备二胺/二羧酸盐的方法，其中二羧酸包括芳族二羧酸并以粉末形式提供; 二胺以逐渐递送到二羧酸粉末的液体形式提供，同时保持二羧酸粉末恒定运动; 处理温度高于0℃，低于二胺的沸点温度和酸和盐的熔融温度，反应混合物至多为5重量％。％的水。本发明还涉及通过本发明的方法获得的无水二胺/二羧酸盐或其如上所述的任何实施方案。

66. 发明授权

US09162961B2 Process for manufacturing succinic acid 有权
标题翻译：制备琥珀酸的方法
公开(公告)号：US09162961B2
公开(公告)日：2015-10-20
申请号：US13578350
申请日：2011-02-14
申请人： Willem Jacob Groot , Jan Van Breugel
发明人： Willem Jacob Groot , Jan Van Breugel
IPC分类号： C25B7/00 , C07C27/06 , C07C51/41 , C07C29/149 , C07C51/02 , C07C51/43 , C12P7/46
CPC分类号： C12P7/18 , C07C29/149 , C07C51/02 , C07C51/412 , C07C51/43 , C12P7/46 , C07C31/207 , C07C55/10
摘要： A process for the preparation of succinic acid comprising the steps of: a) providing an aqueous medium comprising magnesium succinate by fermentation of a carbohydrate source, in the presence of a magnesium base; b) processing the aqueous medium wherein the magnesium succinate is treated with a monovalent base, prior to or after a crystallization step, to provide a magnesium base and an aqueous solution comprising a monovalent succinate salt; c) adjusting the concentration of the monovalent succinate salt to between 10 and 35 wt. %; d) subjecting the aqueous solution to water-splitting electrodialysis, to produce a first solution comprising monovalent base and a second solution comprising succinic acid and monovalent succinate salt, the electrodialysis causing conversion of 40 to 95 mole %; e) separating the second solution into succinic acid and the monovalent succinate salt by crystallization; f) recycling the monovalent succinate salt solution of step e) to step d).
摘要翻译：一种制备琥珀酸的方法，包括以下步骤：a）在镁碱存在下，通过发酵碳水化合物源提供包含琥珀酸镁的水性介质; b）在结晶步骤之前或之后，用单价碱处理其中琥珀酸镁的水性介质，以提供镁碱和包含一价琥珀酸盐的水溶液; c）将单价琥珀酸盐的浓度调节至10至35wt。％; d）使水溶液进行水分解电渗析，以产生包含一价碱和包含琥珀酸和一价琥珀酸盐的第二溶液的第一溶液，该电渗析导致40至95摩尔％的转化率; e）通过结晶将第二溶液分离成琥珀酸和单价琥珀酸盐; f）将步骤e）的单价琥珀酸盐溶液再循环到步骤d）。

67. 发明授权

US09162960B2 Process for the preparation of a benzene derivative 有权
标题翻译：制备苯衍生物的方法
公开(公告)号：US09162960B2
公开(公告)日：2015-10-20
申请号：US14346380
申请日：2012-09-28
申请人： Furanix Technologies B.V. , Stichting Dienst Landbouwkunding Onderzoek
发明人： Matheus Adrianus Dam , Edserd de Jong , Jacco van Haveren , Aliaksei Pukin
IPC分类号： C07C51/16 , C07C51/41 , C07C51/285 , C07D493/18 , C07C51/275 , C07D307/42
CPC分类号： C07C51/41 , C07C51/16 , C07C51/275 , C07C51/285 , C07C51/412 , C07D307/42 , C07D493/18 , C07C65/21 , C07C63/307
摘要： A substituted benzene derivative is prepared in a process, which includes reacting a furan derivative of formula (I): wherein R is an alkyl group, with an olefin of formula (II): R1—CH═CH—R2 (II) wherein R1 and R2 are the same or different and independently are selected from the group consisting of hydrogen, —CN, —CHO and —COOR3, wherein R3 is selected from hydrogen or an alkyl group, or R1 and R2 together form a —C(O)—O—(O)C— group, with the proviso that R1 and R2 are not both hydrogen, to produce a bicyclic ether; and dehydrating the bicyclic ether to obtain a benzene derivative. The benzene derivative thus obtained can suitably be converted to a benzene carboxylic acid compound by oxidation.
摘要翻译：在一种方法中制备取代的苯衍生物，其包括使式（I）的呋喃衍生物（其中R是烷基）与式（II）的烯烃反应：其中R 1为-CH 和R 2相同或不同且独立地选自氢，-CN，-CHO和-COOR 3，其中R 3选自氢或烷基，或者R 1和R 2一起形成-C（O） -O-（O）C-基团，条件是R1和R2不同时为氢，以产生双环醚; 并使双环醚脱水得到苯衍生物。由此获得的苯衍生物可以通过氧化适当地转化成苯羧酸化合物。

68. 发明授权

US09115052B2 Separation of an enantiomer mixture of (R)- and (S)-3-amino-1-butanol 有权
标题翻译：分离（R） - 和（S）-3-氨基-1-丁醇的对映异构体混合物
公开(公告)号：US09115052B2
公开(公告)日：2015-08-25
申请号：US13144726
申请日：2010-01-15
申请人： Klaus Ditrich , Michael Bartsch , Harald Winsel
发明人： Klaus Ditrich , Michael Bartsch , Harald Winsel
IPC分类号： C07C59/00 , C07C213/10 , C07C51/41 , C07C59/50 , C07C215/08 , C07C217/10
CPC分类号： C07C213/10 , C07B2200/07 , C07C51/412 , C07C59/50 , C07C215/08 , C07C217/10 , Y02P20/55
摘要： The present invention relates to a process for separating an enantiomer mixture of (R)- and (S)-3-amino-1-butanol optionally protected on the oxygen atom, and to a process for preparing essentially enantiomerically pure (R)-3-amino-1-butanol which optionally bears a protecting group on the oxygen atom.
摘要翻译：本发明涉及分离任选保护在氧原子上的（R） - 和（S）-3-氨基-1-丁醇的对映异构体混合物的方法，以及制备基本上对映体纯的（R）-3 - 氨基-1-丁醇，其任选地在氧原子上带有保护基。

69. 发明授权

US09051260B2 Elimination of organohalo and oxirane species in carboxylic acid ester streams 有权
标题翻译：在羧酸酯流中消除有机卤代和环氧乙烷物质
公开(公告)号：US09051260B2
公开(公告)日：2015-06-09
申请号：US13816998
申请日：2011-09-02
申请人： Joseph C. Rongione , Jenifer Heydinger Galante
发明人： Joseph C. Rongione , Jenifer Heydinger Galante
IPC分类号： C11B11/00 , C07C67/48 , C07C51/487 , C11B7/00 , C07C51/41 , C11B3/06 , C11B3/00 , C11C1/08
CPC分类号： C07C67/48 , C07C51/412 , C07C51/487 , C11B3/001 , C11B3/06 , C11B7/0083 , C11C1/08
摘要： The present technology provides a process of reducing, removing or eliminating organohalo, glycidol, and oxirane species from carboxylic acid esters streams and crude and refined triglyceride oils to provide a carboxylic acid ester stream or triglyceride oil with reduced levels or essentially free of organohalo, glycidyl or other oxirane species. The process includes adding to the carboxylic acid ester stream or triglyceride oil an amount of a carboxylate anion and a cation counterion sufficient to react with the organohalo, glycidyl and oxirane species present.
摘要翻译：本技术提供了一种从羧酸酯流和粗精制甘油三酯油中还原，除去或除去有机卤代，缩水甘油和环氧乙烷物质的方法，以提供具有降低的水平或基本上没有有机卤代的缩水甘油基的羧酸酯流或甘油三酸酯油或其他环氧乙烷物种。该方法包括向羧酸酯流或甘油三酯油中加入一定量的羧酸根阴离子和足以与存在的有机卤代，缩水甘油基和环氧乙烷物质反应的阳离子抗衡离子。

70. 发明申请

US20150112072A1 PROCESS OF PREPARING SOLIFENACIN OR SALT THEREOF, AND NOVEL INTERMEDIATE USED IN THE PROCESS 有权
标题翻译：制备溶液或其盐的方法和方法中使用的中间体
公开(公告)号：US20150112072A1
公开(公告)日：2015-04-23
申请号：US14382529
申请日：2013-03-21
申请人： KYUNG DONG PHARM. CO., LTD.
发明人： Byoung Suk Lee , Sang Hoon Shin , Ki Young Lee
IPC分类号： C07D453/02
CPC分类号： C07D453/02 , A61K31/439 , C07C51/412 , C07C55/10
摘要： Disclosed herein is a method of preparing solifenacin or a salt thereof, including the steps of: (a) reacting (R)-quinuclidinol with bis(pentafluorophenyl)carbonate in an organic solvent to prepare a solifenacin intermediate, (3R)-1-azabicyclo[2,2,2]oct-3-yl pentafluorophenylcarbonate, and (b) reacting the solifenacin intermediate with (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline in an organic solvent to prepare solifenacin. The method is advantageous in that high-purity solifenacin or a salt thereof can be simply and efficiently prepared with high yield using a novel intermediate.
摘要翻译：本文公开了一种制备索非那新或其盐的方法，包括以下步骤：（a）使（R） - 奎宁环醇与双（五氟苯基）碳酸酯在有机溶剂中反应，制备索申诺辛中间体，（3R）-1-氮杂双环 [2,2,2]辛-3-基五氟苯基碳酸酯，和（b）使索乃克辛中间体与（1S）-1-苯基-1,2,3,4-四氢异喹啉在有机溶剂中反应制备索非那新。该方法的优点在于，可以使用新的中间体以高产率简单有效地制备高纯度索非那新或其盐。

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