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公开(公告)号：US20180099930A1
公开(公告)日：2018-04-12
申请号：US15835649
申请日：2017-12-08
发明人： Hua Bai , Xuyang Zhao , Yuncai Zhang , Xufei Li , Yong Zhang , Dezhou Xu , Li Zhang , Xiaojie Xu , Qifeng Zhu , Xiaoming Wang , Zhiqing Yang , Zehua Zhong , Jian Zhang
IPC分类号： C07D205/08 , C07C59/56 , C07C51/367 , C07C67/327 , C07C69/65 , C07C67/343 , C07C67/30 , C07C69/732
CPC分类号： C07D205/08 , C07C51/367 , C07C59/56 , C07C67/30 , C07C67/327 , C07C67/343 , C07C69/65 , C07C69/732
摘要： Disclosed is a new method for preparing an azetidinone compound represented by formula (I). The carboxylic ketoester represented by formula (II) serves as the raw material and is subjected to Grignard addition, stereoselective dehydration, ester group reduction, hydroxyl group protection, addition with imine after condensation with a chiral auxiliary, cyclization and deprotection to obtain the compound represented by formula (I). The present invention has advantages of easily available raw material, a few synthetic steps, simple operation, high yield, good stereoselectivity and low cost, and can be used for industrial production.
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公开(公告)号：US09926268B2
公开(公告)日：2018-03-27
申请号：US15317297
申请日：2015-06-05
发明人： Hua Bai , Xuyang Zhao , Yuncai Zhang , Xufei Li , Yong Zhang , Dezhou Xu , Li Zhang , Xiaojie Xu , Qifeng Zhu , Xiaoming Wang , Zhiqing Yang , Zehua Zhong , Jian Zhang
IPC分类号： C07C51/367 , C07C67/327 , C07D205/08 , C07C67/30 , C07C67/343 , C07C69/65 , C07C69/732 , C07C59/56
CPC分类号： C07D205/08 , C07C51/367 , C07C59/56 , C07C67/30 , C07C67/327 , C07C67/343 , C07C69/65 , C07C69/732
摘要： Disclosed is a new method for preparing an azetidinone compound represented by formula (I). The carboxylic ketoester represented by formula (II) serves as the raw material and is subjected to Grignard addition, stereoselective dehydration, ester group reduction, hydroxyl group protection, addition with imine after condensation with a chiral auxiliary, cyclization and deprotection to obtain the compound represented by formula (I). The present invention has advantages of easily available raw material, a few synthetic steps, simple operation, high yield, good stereoselectivity and low cost, and can be used for industrial production.
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公开(公告)号：US09802891B2
公开(公告)日：2017-10-31
申请号：US15386349
申请日：2016-12-21
发明人： Hongyuan Wei , Chongjun Liu , Xuyang Zhao , Xiaojie Xu , Hua Bai , Yuncai Zhang
IPC分类号： C07D205/08 , A61K31/397
CPC分类号： C07D205/08 , A61K31/397 , C07B2200/13
摘要： The present invention provides crystal forms of the compound of (3R,4S)-4-(4-hydroxyphenyl)-3-[3-(4-fluorophenyl)-4-hydroxybut-2(Z)-enyl]-1-(4-fluorophenyl)-2-azetidinone (formula A). The crystal forms can be characterized by X-ray powder diffraction (XRPD) spectra, differential scanning calorimetry (DSC) spectra, infrared absorption spectra and so on. Meanwhile, the present invention also provides methods for preparing the crystal forms of the compound of formula A, pharmaceutical compositions and uses thereof.
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公开(公告)号：US09776959B2
公开(公告)日：2017-10-03
申请号：US15386147
申请日：2016-12-21
发明人： Hongyuan Wei , Chongjun Liu , Xuyang Zhao , Xiaojie Xu , Hua Bai , Yuncai Zhang
IPC分类号： C07D205/08 , A61K31/397
CPC分类号： C07D205/08 , A61K31/397 , C07B2200/13
摘要： The present invention provides crystal forms of the compound of (3R,4S)-4-(4-hydroxyphenyl)-3-[3-(4-fluorophenyl)-4-hydroxybut-2(Z)-enyl]-1-(4-fluorophenyl)-2-azetidinone (formula A). The crystal forms can be characterized by X-ray powder diffraction (XRPD) spectra, differential scanning calorimetry (DSC) spectra, infrared absorption spectra and so on. Meanwhile, the present invention also provides methods for preparing the crystal forms of the compound of formula A, pharmaceutical compositions and uses thereof.
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公开(公告)号：US20160264609A1
公开(公告)日：2016-09-15
申请号：US15036390
申请日：2014-04-28
发明人： Yanghui Guo , Junhui Zhou , Qingfeng Cai , Hegeng Wei , Hua Bai , Fei Long , Yue Zhang , Yingqiu Wu
摘要： The present invention relates to a disaccharide intermediate and a synthesis method thereof, relates to the chemical pharmaceutical field, and more specifically relates to a method for preparing a disaccharide segment of a key intermediate for chemically synthesizing heparin and heparinoid compounds. Disclosed are a new disaccharide intermediate and three methods for synthesizing the disaccharide intermediate, that is, compounds of a formula (4) and glucopyranose protected by different anomeric carbon are made to react in the presence of an active agent, to obtain the disaccharide intermediate. According to the technical solutions of the present invention, synthetic raw materials are easy to obtain, have a mild reaction condition, and are suitable for industrialized production.
摘要翻译： 本发明涉及二糖中间体及其合成方法，涉及化学药物领域，更具体地涉及制备化学合成肝素和类肝素化合物的关键中间体的二糖段的方法。 公开了一种新的二糖中间体和三种合成二糖中间体的方法，即式（4）的化合物和由不同端基异构体碳保护的吡喃葡萄糖在活性剂存在下反应，得到二糖中间体。 根据本发明的技术方案，合成原料易于获得，反应条件温和，适用于工业化生产。
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16.发明申请CRYSTALLINE FORM OF 2-((1'-N-HEXYLOXY) ETHYL)-2-DIVINYL-PYROPHEOPHORBIDE-A AND METHOD FOR PREPARING THEREOF 有权2 - （（1'-N-HEXYLOXY）乙基）-2-二乙基吡咯烷酮A的晶体形式及其制备方法公开(公告)号：US20150099873A1
公开(公告)日：2015-04-09
申请号：US14377375
申请日：2013-02-07
发明人： Zhenliang Chen , Fei Zheng , Yumei Wu , Tianmin Zhu , Hua Bai
IPC分类号： C07D487/22
CPC分类号： C07D487/22 , A61K41/0071
摘要： The present invention provides a crystalline form of HPPH (2-((1′-n-hexyloxy)ethyl)-2-divinyl-pyropheophorbide-a). The crystalline form can be characterized by an X-ray powder diffraction (XRD) pattern and differential scanning calorimeter (DSC) pattern. The present invention also provides a method for preparing the crystalline form of HPPH.
摘要翻译： 本发明提供了HPPH（2 - （（1'-正己氧基）乙基）-2-二乙烯基 - 焦脱镁叶绿酸a）的结晶形式。 结晶形式可以通过X射线粉末衍射（XRD）图案和差示扫描量热仪（DSC）图案来表征。 本发明还提供了制备HPPH结晶形式的方法。
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公开(公告)号：US20150065699A1
公开(公告)日：2015-03-05
申请号：US14389357
申请日：2013-04-01
发明人： Guobin Ren , Changliang Dai , Jinyao Chen , Feng Chen , Minghui Qi , Wenming Zhu , Minghuang Hong , Hua Bai
IPC分类号： C07J17/00
CPC分类号： C07J17/00 , C07B2200/13 , C07J17/005
摘要： Provided are several types of ginsenoside polymorphic substances and a method for preparing same. In particular, new crystal form A, crystal form B, crystal form C, crystal form E, crystal form F, crystal form I, crystal form K, crystal form L, crystal form M, crystal form N, and crystal form O are involved.
摘要翻译： 提供几种类型的人参皂苷多晶型物质及其制备方法。 特别是新的晶型A，晶型B，晶型C，晶型F，晶型F，晶型I，晶型K，晶型L，晶型M，晶型N，晶型O 。
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公开(公告)号：US20200207745A1
公开(公告)日：2020-07-02
申请号：US16800057
申请日：2020-02-25
发明人： Lei Chen , Dongliang Guan , Hua Bai , Jun Gou , Weifeng Zhao , Zhongli Wang , Long Ling , Yutao Ma
IPC分类号： C07D403/14 , C07D403/12 , C07D471/10 , C07D487/10 , A61K31/506 , A61P35/00 , C07D403/04
摘要： The present invention relates to a pyrimidine derivative, a method for preparing same and use thereof in medicine. In particular, the present invention relates to a pyrimidine derivative represented by general formula (I), a method for preparing same and a pharmaceutically acceptable salt thereof as well as use thereof as a therapeutic agent, in particular as a FGFR4 kinase inhibitor, definitions of each substituent in the general formula (I) being the same as those defined in the description.
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公开(公告)号：US10654836B2
公开(公告)日：2020-05-19
申请号：US16302310
申请日：2017-05-19
发明人： Lei Chen , Dongliang Guan , Hua Bai , Jun Gou , Weifeng Zhao , Zhongli Wang , Long Ling , Yutao Ma
IPC分类号： C07D403/14 , C07D403/12 , C07D471/10 , C07D487/10 , A61K31/506 , A61P35/00 , C07D403/04
摘要： The present invention relates to a pyrimidine derivative, a method for preparing same and use thereof in medicine. In particular, the present invention relates to a pyrimidine derivative represented by general formula (I), a method for preparing same and a pharmaceutically acceptable salt thereof as well as use thereof as a therapeutic agent, in particular as a FGFR4 kinase inhibitor, definitions of each substituent in the general formula (I) being the same as those defined in the description.
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公开(公告)号：US10519148B2
公开(公告)日：2019-12-31
申请号：US15766692
申请日：2016-10-11
发明人： Dongliang Guan , Shouyi Sheng , Hua Bai
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
摘要： The present invention relates to an acrylic acid derivative as shown in general formula (I), a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, the preparation method thereof, a pharmaceutical composition containing same, and the use thereof as therapeutic agents, in particular as selective estrogen receptor degraders (SERD), wherein the substituents of general formula (I) are the same as those defined in the description.
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