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1. 发明申请

US20120277448A1 PREPARATION METHOD FOR 3BETA-ARACHIDYLAMIDO-7ALPHA, 12ALPHA, 5BETA-CHOLAN-24-CARBOXYLIC ACID 审中-公开
标题翻译： 3BETA-ARACHIDYLAMIDO-7ALPHA，12ALPHA，5BETA-CHOLAN-24-羧酸的制备方法
公开(公告)号：US20120277448A1
公开(公告)日：2012-11-01
申请号：US13520117
申请日：2010-11-25
申请人： Xiangrui Jiang , Lijun Guo , Yiru Dai , Jianfeng Li , Jin Suo , Rongxia Zhang , Zheng Liu
发明人： Xiangrui Jiang , Lijun Guo , Yiru Dai , Jianfeng Li , Jin Suo , Rongxia Zhang , Zheng Liu
IPC分类号： C07J41/00 , C07J9/00
CPC分类号： C07J41/0011 , C07J9/005 , C07J31/006 , C07J41/0005 , C07J41/0027 , Y02P20/55
摘要： A method for preparing 3β-arachidylamido-7α,12α,5β-cholan-24-carboxylic acid represented by the following formula V is disclosed, which includes the following steps: converting cholic acid to the compound of formula III by acylation reaction and azidation reaction, reducing the compound of formula III to the compound of formula IV and in the end acylating the compound of formula IV with arachidoyl chloride to get the compound of formula V. The method avoids the use of protection groups.
摘要翻译：公开了一种制备由下式V表示的3'- bgr-酰胺基酰胺基-7α，12α，5'- b-胆碱-24-羧酸的方法，其包括以下步骤：通过酰化反应将胆酸转化为式III化合物，叠氮化反应，将式III化合物还原成式Ⅳ化合物，最后用芳ido酰氯酰化式Ⅳ化合物，得到式Ⅴ化合物。该方法避免使用保护基团。

2. 发明授权

US09527849B2 Salt and polymorph of pyrazolopyrimidinone compound, and pharmaceutical composition containing the same, preparation method and use thereof 有权
标题翻译：吡唑并嘧啶酮化合物的盐和多晶型物，以及含有它们的药物组合物，其制备方法和用途
公开(公告)号：US09527849B2
公开(公告)日：2016-12-27
申请号：US14238790
申请日：2012-08-14
申请人： Jianfeng Li , Guanghui Tian , Zhen Wang , Jin Suo , Xiangrui Jiang , Zheng Liu , Xiaojun Yang , Zhu Xie , Xianguo Zhao , Weiliang Zhu , Hualiang Jiang , Jingshan Shen
发明人： Jianfeng Li , Guanghui Tian , Zhen Wang , Jin Suo , Xiangrui Jiang , Zheng Liu , Xiaojun Yang , Zhu Xie , Xianguo Zhao , Weiliang Zhu , Hualiang Jiang , Jingshan Shen
IPC分类号： C07D487/04 , A61K31/519 , A61P15/10 , A61P13/10 , A61P9/10 , A61P9/04 , A61P13/12 , A61P11/06 , A61P29/00 , A61P27/06 , A61P9/12
CPC分类号： C07D487/04 , C07B2200/13
摘要： The present invention relates to new salts of pyrazolopyrimidinone represented by formula (I), and pharmaceutically acceptable polymorph, solvate, hydrate, dehydrate, co-crystallization, anhydrous, or amorphous form thereof, the pharmaceutical compositions, and a pharmaceutical unit dosage form containing the same, wherein x represents organic or inorganic acids, preferable maleic acid, succinic acid, methanesulfonic acid, hydrochloric acid, etc. The invention further relates to co-crystals or complexes of compounds of pyrazolopyrimidinone and pharmaceutical compositions containing the same. The present invention also relates to a process for the preparation, use thereof and pharmaceutical preparation containing the salts or crystalline forms.
摘要翻译：本发明涉及由式（I）表示的吡唑并嘧啶酮的新盐及其药学上可接受的多晶型物，溶剂化物，水合物，脱水，共结晶，无水或无定形形式，药物组合物和含有相同的，其中x表示有机或无机酸，优选的马来酸，琥珀酸，甲磺酸，盐酸等。本发明还涉及吡唑并嘧啶酮化合物的共晶或络合物和含有它们的药物组合物。本发明还涉及其制备方法，使用方法和含有盐或结晶形式的药物制剂。

3. 发明申请

US20140309241A1 SALT AND POLYMORPH OF PYRAZOLOPYRIMIDINONE COMPOUND, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME, PREPARATION METHOD AND USE THEREOF 有权
标题翻译：吡唑并嘧啶酮化合物的盐和多元醇以及含有它们的药物组合物，其制备方法和用途
公开(公告)号：US20140309241A1
公开(公告)日：2014-10-16
申请号：US14238790
申请日：2012-08-14
申请人： Jianfeng Li , Guanghui Tian , Zhen Wang , Jin Suo , Xiangrul Jiang , Zheng Liu , Xiaojun Yang , Zhu Xix , Xianguo Zhao , Weilang Zhu , Hualiang Jiang , Jingshan Shen
发明人： Jianfeng Li , Guanghui Tian , Zhen Wang , Jin Suo , Xiangrul Jiang , Zheng Liu , Xiaojun Yang , Zhu Xix , Xianguo Zhao , Weilang Zhu , Hualiang Jiang , Jingshan Shen
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07B2200/13
摘要： The present invention relates to new salts of pyrazolopyrimidinone represented by formula (I), and pharmaceutically acceptable polymorph, solvate, hydrate, dehydrate, co-crystallization, anhydrous, or amorphous form thereof, the pharmaceutical compositions, and a pharmaceutical unit dosage form containing the same, wherein x represents organic or inorganic acids, preferable maleic acid, succinic acid, methanesulfonic acid, hydrochloric acid, etc. The invention further relates to co-crystals or complexes of compounds of pyrazolopyrimidinone and pharmaceutical compositions containing the same. The present invention also relates to a process for the preparation, use thereof and pharmaceutical preparation containing the salts or crystalline forms.
摘要翻译：本发明涉及由式（I）表示的吡唑并嘧啶酮的新盐及其药学上可接受的多晶型物，溶剂化物，水合物，脱水，共结晶，无水或无定形形式，药物组合物和含有相同的，其中x表示有机或无机酸，优选的马来酸，琥珀酸，甲磺酸，盐酸等。本发明还涉及吡唑并嘧啶酮化合物的共晶或络合物和含有它们的药物组合物。本发明还涉及其制备方法，使用方法和含有盐或结晶形式的药物制剂。

4. 发明申请

US20120123118A1 Process For The Preparation Of Nitroorotic Acid 有权
标题翻译：硝基乙酸的制备方法
公开(公告)号：US20120123118A1
公开(公告)日：2012-05-17
申请号：US13201486
申请日：2010-02-22
申请人： Rolf Dach , Xiangrui Jiang , Jingshan Shen , Jin Suo , Yi Zhu
发明人： Rolf Dach , Xiangrui Jiang , Jingshan Shen , Jin Suo , Yi Zhu
IPC分类号： C07D487/04 , C07D239/557
CPC分类号： C07D487/04 , C07D239/557
摘要： Subject of the present invention is a new improved process for the preparation of nitroorotic acid via nitration of orotic acid.
摘要翻译：本发明的主题是通过乳清酸硝化制备硝酸根酸的新的改进方法。

5. 发明授权

US08513413B2 Process for the preparation of nitroorotic acid 有权
标题翻译：制备硝基酸的方法
公开(公告)号：US08513413B2
公开(公告)日：2013-08-20
申请号：US13201486
申请日：2010-02-22
申请人： Rolf Dach , Xiangrui Jiang , Jingshan Shen , Jin Suo , Yi Zhu
发明人： Rolf Dach , Xiangrui Jiang , Jingshan Shen , Jin Suo , Yi Zhu
IPC分类号： C07D239/02
CPC分类号： C07D487/04 , C07D239/557
摘要： Subject of the present invention is a new improved process for the preparation of nitroorotic acid via nitration of orotic acid.
摘要翻译：本发明的主题是通过乳清酸硝化制备硝酸根酸的新的改进方法。

6. 发明申请

US20060148866A1 Novel process for preparing pramipexole and its optical isomeric mixture by reduction with sodium triacetoxyborohydride 审中-公开
标题翻译：用三乙酰氧基硼氢化钠还原制备普拉克索及其光学异构体混合物的新方法
公开(公告)号：US20060148866A1
公开(公告)日：2006-07-06
申请号：US11299752
申请日：2005-12-13
申请人： Guangxin Xia , Yifeng Nian , Tiema Yan , Jin Suo , Michael Brand , Oded Arad
发明人： Guangxin Xia , Yifeng Nian , Tiema Yan , Jin Suo , Michael Brand , Oded Arad
IPC分类号： C07D277/82 , A61K31/428
CPC分类号： C07D277/82
摘要： A novel process is provided for producing pramipexole base or its optical isomeric mixture as defined hereinabove i.e. (R,S)-2-amino-6-propyl-4,5,6,7-tetrahydrobenzothiazole avoiding the use of borane tetrahydrofuran complex and using a more convenient reducing agent like sodium triacetoxyborohydride instead. The provided process comprises reacting the starting material (S)-2,6-diamino-4,5,6,7-tetrahydrobenzothiazole or its optical isomeric mixture as defined hereinabove i.e. (R,S)-2,6-diamino-4,5,6,7-tetrahydrobenzothiazole with propionaldehyde in an organic solvent to obtain the respective enamine, which is subsequently reduced in situ, optionally without isolation, to obtain pramipexole or its optical isomeric mixture as defined hereinabove i.e. (R,S)-2-amino-6-propyl-4,5,6,7-tetrahydrobenzothiazole, and the acid addition salts thereof. The present invention also provides a process for purifying pramipexole dihydrochloride or the dihydrochloride salt of its optical isomeric mixture as defined hereinabove i.e. (R,S)-2-amino-6-propyl-4,5,6,7-tetrahydrobenzothiazole dihydrochloride by re-crystallization from a suitable solvent.
摘要翻译：提供了一种制备普拉克索碱或其如上所述的光学异构体混合物的新方法，即（R，S）-2-氨基-6-丙基-4,5,6,7-四氢苯并噻唑，避免使用硼烷四氢呋喃络合物并使用一种更方便的还原剂，如三乙酰氧基硼氢化钠。所提供的方法包括使起始原料（S）-2,6-二氨基-4,5,6,7-四氢苯并噻唑或其如上文所定义的光学异构体混合物即（R，S）-2,6-二氨基-4， 5,6,7-四氢苯并噻唑与丙醛在有机溶剂中反应，得到各自的烯胺，其随后可原位还原，任选不分离，得到如上所述的普拉克索或其旋光异构体混合物，即（R，S）-2- 氨基-6-丙基-4,5,6,7-四氢苯并噻唑及其酸加成盐。本发明还提供了纯化普拉克索二盐酸盐或其如上所述的光学异构体混合物的二盐酸盐的方法，即（R，S）-2-氨基-6-丙基-4,5,6,7-四氢苯并噻唑二盐酸盐， - 从合适的溶剂中结晶。

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