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公开(公告)号：US20150191480A1
公开(公告)日：2015-07-09
申请号：US14411783
申请日：2013-07-03
发明人： Hua Bai , Xuyang Zhao , Jinqing Zhong , Yongxiang Gong , Qifeng Zhu , Xiaoyu Liu , Xiaohe Zheng , Lifei Liu
IPC分类号： C07D491/056 , C07D491/113
CPC分类号： C07D491/056 , A61K31/435 , A61K31/4523 , C07D401/06 , C07D491/04 , C07D491/113
摘要： Provided in the present invention are novel benzodioxole derivatives and preparation methods thereof. These compounds represented by formula (I) or pharmaceutically acceptable salts thereof have acetylcholinesterase inhibitory activity, so can be used in the treatment or prevention of Alzheimer's disease. The definitions of R1, R2 and A of formula (I) can be seen in the description.
摘要翻译： 本发明提供新的苯并间二氧杂环戊烯衍生物及其制备方法。 由式（I）表示的这些化合物或其药学上可接受的盐具有乙酰胆碱酯酶抑制活性，因此可用于治疗或预防阿尔茨海默氏病。 在描述中可以看出式（I）的R1，R2和A的定义。
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公开(公告)号：US11622939B2
公开(公告)日：2023-04-11
申请号：US16766292
申请日：2018-11-23
发明人： Li Ding , Jun Dai , Chunrong Feng , Changliang Dai
IPC分类号： A61K9/20 , A61K9/00 , A61K31/397
摘要： An HS-25 tablet, an HS-25 solid dispersion composition, a preparation method therefor and usage thereof. The HS-25 tablet is made by using HS-25 and excipients for wet granulation, drying, granulating and tablet pressing.
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公开(公告)号：US20220220107A1
公开(公告)日：2022-07-14
申请号：US17610167
申请日：2020-05-21
发明人： Jianfeng ZHENG , Liang ZHANG , Min ZHAO , Zhenjuan SHI , Xufei LI , Zhiqing YANG
IPC分类号： C07D471/04
摘要： Crystal forms A, B, C, D, E, F, G and H of a compound represented by formula I and a preparation method therefor, as well as medical uses for the various crystal forms and advantages thereof in various aspects.
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公开(公告)号：US20210032606A1
公开(公告)日：2021-02-04
申请号：US16301377
申请日：2017-05-08
发明人： Min Zhou , Xing Jiang , Shuang Han , Yingying He , Linghui Zheng
摘要： The present invention relates to a DoxA protein mutant having an amino acid sequence set forth in SEQ ID No. 16, and coding gene thereof. The protein mutant or the coding gene thereof can be used for producing epirubicin. The present invention further relates to a Streptomyces capable of efficiently expressing epirubicin, which is constructed by replacing the dnmV gene of a starting Streptomyces in situ with the avrE gene and mutating the doxA gene of the starting Streptomyces into a gene encoding the protein set forth in SEQ ID No. 16. The fermentation broth of this Streptomyces has an epirubicin potency of up to 102.0 μg/ml.
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公开(公告)号：US10526668B2
公开(公告)日：2020-01-07
申请号：US15562187
申请日：2016-03-25
发明人： Yun Teng , Meidong Xu , Meiyi Mo , Zhihui He , Zhengjie Chen , Lianiqing Jiang , Hua Bai
摘要： Provided are a Streptomyces (Streptomyces hygroscopicus) HS7522 and a method for preparing milbemycin A4 by culturing the Streptomyces. The Streptomyces (Streptomyces hygroscopicus) HS7522 of the present invention is deposited in “China General Microbiological Culture Collection Center” with an accession number of CGMCC No. 9671 on Sep. 16, 2014.
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公开(公告)号：US10508112B2
公开(公告)日：2019-12-17
申请号：US16014678
申请日：2018-06-21
发明人： Fuli Zhang , Zhezhou Yang , Rusheng Bao , Weiwei Xu , Hua Bai
IPC分类号： C07C237/22 , C07D471/04 , A61K31/4985 , C07C231/02 , C07C231/14
摘要： Intermediate compounds for the preparation of Praziquantel are provided. In particular, the intermediate compounds provided include a compound of formula (IV) and a compound of formula (V). Also provided are processes for preparing the intermediate compounds. Additionally, the raw materials are inexpensive and easy to obtain, the key intermediates are easy to prepare, and the total reaction yield and purity of the obtained target compound Praziquantel is high, so that industrialized mass production of Praziquantel using the intermediate compounds is easy to achieve.
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公开(公告)号：US10442835B2
公开(公告)日：2019-10-15
申请号：US15553088
申请日：2016-11-09
发明人： Haibo Wang , Hongfu Kuang , Wei Zhang , Zhengjiang Cai , Tianmin Zhu , Xiaohe Zheng , Zhongwei Wu , Zhiqing Yang
摘要： The present invention relates to technical fields of organic chemistry and pharmaceutical chemistry, specifically to water-soluble rapamycin derivatives modified with glutathione. More specifically, the present invention discloses a compound of formula I and the preparation method thereof, wherein R1 and R2 are as defined in the description. The compound of formula I can be used in inducing immunosuppression and in the treatment of diseases such as transplant rejection and solid tumor, etc.
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公开(公告)号：US10399992B2
公开(公告)日：2019-09-03
申请号：US16087308
申请日：2017-03-28
发明人： Jinqing Zhong , Xuyang Zhao , Hua Bai , Yongxiang Gong , Xinlong Zhang , Qifeng Zhu , Weiwei Liu , Ya Zhou
IPC分类号： C07D491/056 , C07D491/113 , A61P25/28
摘要： Disclosed are a method for preparing a benzodioxole derivative (AD-35) shown by Formula (I) and an intermediate thereof. The method of the present invention involves: using piperic acid as a raw material; and performing bromination, esterification, cyanidation, cyclopropane lactamization, amide nitrogen alkylation, deprotection, piperidine nitrogen alkylation and salification to obtain the compound of Formula (I). The method has cheap and easily available start raw materials, short synthesis routes and simple operation, and is suitable for industrial production.
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公开(公告)号：US10316052B2
公开(公告)日：2019-06-11
申请号：US15324555
申请日：2015-07-07
发明人： Huijun Ren , Daochao Li , Xuexiao Ying , Feng Chen , Linghui Zheng , Lingping Wang , Hua Bai
摘要： A fidaxomicin purification method, comprising: fermenting Actinoplanes sp. HS-16-20 to generate fermented liquid; conducting solid/liquid separation on the fermented liquid, soaking mycelium in an organic solvent, and filtering to obtain a solution containing fidaxomicin; treating the solution with nanofiltration concentrate, and separating to obtain fidaxomicin crude product; conducting preparative column chromatography on the fidaxomicin crude product, eluting with an acid aqueous solution containing an organic solvent, and separating to obtain the refined fidaxomicin product.
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公开(公告)号：US20190161476A1
公开(公告)日：2019-05-30
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 , A61P35/00 , C07D403/04 , C07D403/12
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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