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1. 发明授权

US11098007B2 Crystal of amino acid salt of 3-hydroxyisovaleric acid and production method thereof 有权
公开(公告)号：US11098007B2
公开(公告)日：2021-08-24
申请号：US16311061
申请日：2017-06-23
申请人： KYOWA HAKKO BIO CO., LTD. , OTSUKA PHARMACEUTICAL FACTORY, INC.
发明人： Tomoya Yokoi , Hiroshi Nagano , Takayuki Shimizu
IPC分类号： C07C227/42 , C07C229/26 , C07C51/41 , C07C59/01 , C07C51/43 , C07C277/06 , C07C279/14
摘要： An object of the present invention is to provide a crystal of an amino acid salt of HMB which is easy to handle and has high solubility, and to provide a method for producing the same. According to the present invention, the crystal of an amino acid salt of HMB can be precipitated by dissolving an amorphous amino acid salt of HMB in a solvent containing alcohol and stirring or allowing the solvent to left stand. In addition, the crystal of an amino acid salt of HMB can be precipitated by concentrating an aqueous HMB solution of an amino acid salt which has a pH of 2.5 to 11.0.

2. 发明申请

US20070161821A1 METHOD FOR REMOVAL OF GUANIDINE COMPOUND FROM AQUEOUS MEDIA 失效
标题翻译：从水性介质中去除胍基化合物的方法
公开(公告)号：US20070161821A1
公开(公告)日：2007-07-12
申请号：US11684882
申请日：2007-03-12
申请人： David Hall , Thomas Guggenheim , James Silva , Farid Khouri , Matthew Littlejohn , Balakrishnan Ganesan , Ashok Shyadligeri , Pradeep Nadkarni
发明人： David Hall , Thomas Guggenheim , James Silva , Farid Khouri , Matthew Littlejohn , Balakrishnan Ganesan , Ashok Shyadligeri , Pradeep Nadkarni
IPC分类号： C07C277/06
CPC分类号： C02F9/00 , B01D61/027 , C02F1/281 , C02F1/283 , C02F1/44 , C02F2101/38 , C07C277/06 , C07C279/04
摘要： Disclosed is a method for removing a neutral or an ionic guanidine compound from aqueous media optionally comprising an alkali metal halide, wherein the method is selected from the group consisting of (a) adsorption onto a carbonaceous adsorbent, (b) adsorption onto a clay adsorbent, (c) filtration through a nanofiltration membrane, and (d) removal of water and calcination.
摘要翻译：公开了一种从任选地包含碱金属卤化物的水性介质中除去中性或离子胍化合物的方法，其中所述方法选自（a）吸附到含碳吸附剂上，（b）吸附到粘土吸附剂上，（c）通过纳滤膜过滤，和（d）去除水和煅烧。

3. 发明申请

US20220251034A1 Preparation Method for Metformin Hydrochloride 有权
公开(公告)号：US20220251034A1
公开(公告)日：2022-08-11
申请号：US17629840
申请日：2019-07-25
申请人： ASYMCHEM LIFE SCIENCE (TIANJIN) CO., LTD
发明人： Hao HONG , Jiangping LU , Jian TAO , Yan ZHANG , Fan WANG , Gonzalez MIGUEL
IPC分类号： C07C277/06
摘要： The present disclosure provides a preparation method for metformin hydrochloride. The preparation method includes: microwave heating raw materials containing dicyandiamide and dimethylamine hydrochloride, and reacting the two at 100° C. to 160° C. to obtain a product system containing metformin hydrochloride. Microwave heating is adopted to heat the dicyandiamide and the dimethylamine hydrochloride. Compared with a conventional heating mode that requires heat to be gradually transferred from the outside to the inside, microwave heating can directly heat each part inside the reactant, which can make the internal temperature of the reactant more uniform, thereby reducing the generation of impurities.

4. 发明申请

US20130331604A1 (1S,2S,3S,4R)-3-[(1S)-1-acetylamino-2-ethyl-butyl)-4-guanidino-2-hydroxy-cyclopentyl-1-carboxylic acid hydrates pharmaceutical uses thereof 有权
标题翻译：（1S，2S，3S，4R）-3 - [（1S）-1-乙酰氨基-2-乙基 - 丁基）-4-胍基-2-羟基 - 环戊基-1-羧酸水合物
公开(公告)号：US20130331604A1
公开(公告)日：2013-12-12
申请号：US13968645
申请日：2013-08-16
申请人： Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A., China
发明人： Song Li , Wu Zhong , Zhibing Zheng , Xinbo Zhou , Junhai Xiao , Yunde Xie , Lili Wang , Xingzhou Ll , Guoming Zhao , Xiaokui Wang , Hongying Liu
IPC分类号： C07C277/06
CPC分类号： C07C279/16 , C07B2200/07 , C07C277/06 , C07C277/08 , C07C2601/08
摘要： The present invention relates to (1S,2S,3S,4R)-3-[(1S)-1-acetylamino-2-ethyl-butyl]-4-guanidino-2-hydroxy-cyclopentyl-1-carboxylic acid hydrates compounds, preparing methods thereof, pharmaceutical compositions containing said compounds and preparing methods thereof, and the clinical uses of said compounds as neuramidinase inhibitors for anti-influenza.
摘要翻译：本发明涉及（1S，2S，3S，4R）-3 - [（1S）-1-乙酰氨基-2-乙基 - 丁基] -4-胍基-2-羟基 - 环戊基-1-羧酸水合物，其制备方法，含有所述化合物的药物组合物及其制备方法，以及所述化合物作为抗流感病毒的神经脒酶抑制剂的临床应用。

5. 发明授权

US5696407A Process for the production of spherulitic particles 失效
标题翻译：生产球晶颗粒的方法
公开(公告)号：US5696407A
公开(公告)日：1997-12-09
申请号：US731174
申请日：1996-10-07
申请人： Klaus-Dieter Thiel , Herbert Heinisch
发明人： Klaus-Dieter Thiel , Herbert Heinisch
IPC分类号： C07C277/06 , C06B21/00 , C06B25/00 , C06B25/34 , C07C277/08 , C07C279/06 , C07C279/34
CPC分类号： C07C277/08 , C06B21/0091 , C06B25/34 , C07C279/34 , Y10S149/111
摘要： In the production of spherulitic nitroguanidine having a high bulk and tap ensity nitroguanidine is dissolved in dipolar, aprotic solvents, e.g. DMF, DMSO, NMP, etc., by heating to above the saturation temperature t.sub.s and the supersaturated solution is cooled with a controlled temperature gradient (.degree.C./min), crystallization being assisted by the addition of particulate, spherulitic material. In order to obtain spherical nitroguanidine with high yield in a continuous process and with mother liquor reuse, during the heating to above the saturation temperature t.sub.s, spherical control particles with a diameter of 5 to 500 .mu.m are regularly added to the solution in a quantity of 0.05 to 5.00 mass %. The particle size is chosen in such a way that, as a function of the solution behaviour of the nitroguanidine used and its concentration, on dropping below the saturation temperature spherical control particles are still present in the indicated quantity in the supersaturated solution.
摘要翻译：在生产具有高体积和振实密度的球形硝基胍的情况下，将硝基胍溶解于偶极，非质子溶剂，例如， DMF，DMSO，NMP等，通过加热到饱和温度ts以上，过饱和溶液用受控的温度梯度（℃/ min）冷却，通过加入颗粒状球晶材料来辅助结晶。为了在连续的方法中获得高产率的球形硝基胍，并且在母液再利用中，在加热到高于饱和温度ts之前，将一定直径为5至500μm的球形控制颗粒定量地添加到溶液中为0.05〜5.00质量％。选择粒径是这样一种方式：使用的硝基胍的溶液行为及其浓度随着饱和温度的降低而降低，球形控制颗粒在过饱和溶液中仍以指定量存在。

6. 发明授权

US09518008B2 (1S,2S,3S,4R)-3-[(1S)-1-acetylamino-2-ethyl-butyl]-4-uanidino-2-hydroxyl-cyclopentyl-1-carboxylic acid hydrates pharmaceutical uses thereof 有权
标题翻译：（1S，2S，3S，4R）-3 - [（1S）-1-乙酰氨基-2-乙基 - 丁基] -4- uan基-2-羟基 - 环戊基-1-羧酸水合物
公开(公告)号：US09518008B2
公开(公告)日：2016-12-13
申请号：US14511783
申请日：2014-10-10
申请人： Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A., China
发明人： Song Li , Wu Zhong , Zhibing Zheng , Xinbo Zhou , Junhai Xiao , Yunde Xie , Lili Wang , Xingzhou Li , Guoming Zhao , Xiaokui Wang , Hongying Liu
IPC分类号： A61K31/196 , C07C279/16 , C07C277/08 , A61P31/16 , C07C277/06
CPC分类号： C07C279/16 , C07B2200/07 , C07C277/06 , C07C277/08 , C07C2601/08
摘要： The present invention relates to (1S,2S,3S,4R)-3-[(1S)-1-acetylamino-2-ethyl-butyl]-4-guanidino-2-hydroxy-cyclopentyl-1-carboxylic acid hydrates compounds, preparing methods thereof, pharmaceutical compositions containing said compounds and preparing methods thereof, and the clinical uses of said compounds as neuramidinase inhibitors for anti-influenza.
摘要翻译：本发明涉及（1S，2S，3S，4R）-3 - [（1S）-1-乙酰氨基-2-乙基 - 丁基] -4-胍基-2-羟基 - 环戊基-1-羧酸水合物，其制备方法，含有所述化合物的药物组合物及其制备方法，以及所述化合物作为抗流感病毒的神经脒酶抑制剂的临床应用。

7. 发明授权

US09272992B2 (1S,2S,3S,4R)-3-[(1S)-1-acetylamino-2-ethyl-butyl]-4-guanidino-2-hydroxy-cyclopentyl-l-carboxylic acid hydrates pharmaceutical uses thereof 有权
标题翻译：（1S，2S，3S，4R）-3 - [（1S）-1-乙酰氨基-2-乙基 - 丁基] -4-胍基-2-羟基 - 环戊基-1-羧酸水合物
公开(公告)号：US09272992B2
公开(公告)日：2016-03-01
申请号：US13968645
申请日：2013-08-16
申请人： Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A., China
发明人： Song Li , Wu Zhong , Zhibing Zheng , Xinbo Zhou , Junhai Xiao , Yunde Xie , Lili Wang , Xingzhou Li , Guoming Zhao , Xiaokui Wang , Hongying Liu
IPC分类号： A61K31/24 , A01N37/12 , A01N37/44 , C07C279/16 , C07C277/06 , C07C277/08
CPC分类号： C07C279/16 , C07B2200/07 , C07C277/06 , C07C277/08 , C07C2601/08
摘要： The present invention relates to (1S,2S,3S,4R)-3-[(1S)-1-acetylamino-2-ethyl-butyl]-4-guanidino-2-hydroxy-cyclopentyl-1-carboxylic acid hydrates compounds, preparing methods thereof, pharmaceutical compositions containing said compounds and preparing methods thereof, and the clinical uses of said compounds as neuramidinase inhibitors for anti-influenza.
摘要翻译：本发明涉及（1S，2S，3S，4R）-3 - [（1S）-1-乙酰氨基-2-乙基 - 丁基] -4-胍基-2-羟基 - 环戊基-1-羧酸水合物，其制备方法，含有所述化合物的药物组合物及其制备方法，以及所述化合物作为抗流感病毒的神经脒酶抑制剂的临床应用。

8. 发明申请

US20110263901A1 Process of Preparation of Proguanil 审中-公开
标题翻译：氯胍的制备方法
公开(公告)号：US20110263901A1
公开(公告)日：2011-10-27
申请号：US12525587
申请日：2009-01-13
申请人： Dhananjay Govind Sathe , Harish Kashinath Mondkar , Tanaji Shamrao Jadhav , Nitin Nivrutti Hagavane
发明人： Dhananjay Govind Sathe , Harish Kashinath Mondkar , Tanaji Shamrao Jadhav , Nitin Nivrutti Hagavane
IPC分类号： C07C279/26 , C07C277/06 , C07C277/08
CPC分类号： C07C279/26
摘要： Disclosed herein is the process for the preparation of 1-(4-chlorophenyl)-5-isopropyl-biguanide hydrochloride (Proguanil hydrochloride), Formula-I, an antimalarial agent.
摘要翻译：本文公开了制备1-（4-氯苯基）-5-异丙基 - 双胍盐酸盐（盐酸氯胍），式I，抗疟药剂的方法。

9. 发明申请

US20030166959A1 Process for the separation of reaction mixtures and the recirculation of quaternary salts 失效
标题翻译：分离反应混合物的方法和季盐的再循环
公开(公告)号：US20030166959A1
公开(公告)日：2003-09-04
申请号：US10320009
申请日：2002-12-16
发明人： Claus-Peter Reisinger , Sven Michael Hansen , Peter Fischer , Michael Traving
IPC分类号： C07F005/04 , C07F009/02 , C07C277/06
CPC分类号： B01J31/4053 , B01J31/0214 , B01J31/0215 , B01J31/0235 , B01J31/0239 , B01J31/0255 , B01J31/0268 , B01J31/26 , B01J31/28 , B01J38/48 , B01J2231/34 , C07C37/72 , C07C68/08 , Y02P20/52 , Y02P20/584 , C07C69/96 , C07C39/04
摘要： A process for the separation and recycling of catalyst components from a chemical reaction mixture is disclosed. The process entails at least one extraction step.
摘要翻译：公开了一种从化学反应混合物中分离和再循环催化剂组分的方法。该过程需要至少一个提取步骤。

10. 发明授权

US4914235A Process for obtaining guanidine hydrohalides from by-product mixtures obtained in the production of mercaptoalkylsilanes 失效
标题翻译：在生产巯基烷基硅烷中获得的副产物混合物中获得卤代氢胍的方法
公开(公告)号：US4914235A
公开(公告)日：1990-04-03
申请号：US320154
申请日：1989-03-07
申请人： Clemens Grambow , Ferdinand Beck
发明人： Clemens Grambow , Ferdinand Beck
IPC分类号： C07C277/06 , C07C277/08 , C07C279/02
CPC分类号： C07C277/08
摘要： The present invention provides a process for obtaining guanidine hydrohalides from the by-product mixture obtained in the production of mercaptoalkylsilanes and consisting essentially of guanidine hydrohalide, ammonium halide, thiourea and silane compounds, wherein the by-product mixture is extracted with an aliphatic ketone containing up to 7 carbon atoms and the extract is separated from the residue containing the guanidine hydrohalide.
摘要翻译：本发明提供了一种从巯基烷基硅烷生产中得到的副产物混合物获得胍氢卤化物的方法，其基本上由氢卤酸胍，卤化铵，硫脲和硅烷化合物组成，其中副产物混合物用含有最多7个碳原子，并将提取物与含有氢卤酸胍的残余物分离。

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