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公开(公告)号：US11180463B2
公开(公告)日：2021-11-23
申请号：US16382539
申请日：2019-04-12
发明人： Song Li , Wu Zhong , Shuang Cao , Lili Wang , Zhibing Zheng , Junhai Xiao , Xinbo Zhou
IPC分类号： C07D277/22 , A61K31/426 , C07D277/30 , A61K8/49 , A61K31/4422 , A61Q11/00 , A61Q19/08
摘要： The present invention pertains to field of pharmaceutical chemicals, and relates to thiazole inner salt compounds, preparation methods and uses thereof. Specifically, the present invention relates to a compound of Formula I, hydrates or pharmaceutically acceptable salts thereof. The compound of Formula I of the present invention is a potent cross-linking protein cleavage agent, has a stable structure, good physical and chemical properties, and good pharmacological activities, and is suitable for large scale production to obtain samples with stable, controllable and reliable quality, thereby being suitable for pharmaceutical development.
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公开(公告)号：US10314794B2
公开(公告)日：2019-06-11
申请号：US15320200
申请日：2015-06-23
发明人： Chunsheng Gao , Yuli Wang , Meiyan Yang , Li Shan , Jingjing Dai , Yong Qian , Yan Qiu
IPC分类号： A61K31/138 , A61K9/48 , A61K9/50 , A61K31/549 , A61K9/16
摘要： The invention relates to a drug sustained-release composition, particularly a sustained-release composition comprising metoprolol and preparation method thereof. The invention also relates to a combination product comprising a sustained-release composition comprising metoprolol and a pharmaceutical composition comprising hydrochlorothiazide. The sustained-release composition comprising metoprolol according to the invention eliminates the phenomena of delayed release of such sustained-release compositions in the prior art, has a better drug release curve, and also have the advantages such as simple formula, easy operation, stable quality, strong controllability, and good reproducibility, and therefore have good application prospects.
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公开(公告)号：US10301279B2
公开(公告)日：2019-05-28
申请号：US15794666
申请日：2017-10-26
发明人： Wu Zhong , Song Li , Yanqun Zeng , Junhai Xiao , Xinbo Zhou , Zhibing Zheng , Xingzhou Li , Xiaokui Wang
IPC分类号： A61K31/506 , C07D401/04 , C07D401/14 , C07D409/14 , A61K45/06 , A61K31/404 , A61K31/454 , A61K31/4545 , A61K31/517 , A61K31/5377
摘要： The present invention provides a compound of a general formula I, a stereomeride, pharmaceutically acceptable salt or a solvate thereof, a preparation method thereof, and usages in preparing medicines for preventing and/or treating diseases or symptoms caused by drug-resistant tumors or drug-resistant bacteria and in preparing medicines for preventing and/or treating diseases or symptoms related to tumors, neurodegenerative diseases, allogeneic transplantation rejection, and infection. Preferably, the diseases or symptoms related to tumors, neurodegenerative diseases, allogeneic transplantation rejection, and infection are diseases or symptoms caused by a heat shock protein 70 (Hsp70). The compound in the present invention is used for overcoming a difficult problem of drug resistance of tumors, improves the effect of tumor treatment, and provides a new medical strategy for clinical tumor treatment.
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4.发明申请公开(公告)号：US20190077821A1
公开(公告)日：2019-03-14
申请号：US16093754
申请日：2017-04-11
发明人： Song LI , Xinbo ZHOU , Dian XIAO , Wu ZHONG , Junhai XIAO , Zhibing ZHENG , Xingzhou LI , Yunde XIE , Xiaokui WANG
IPC分类号： C07H13/04 , C07D413/12 , C07D271/12 , A61P11/00 , A61P25/28
摘要： Disclosed in the present invention is a compound of Formula (I), a geometric or optical isomer, a pharmaceutically acceptable salt, a solvate or a polymorph thereof. Also disclosed in the present invention is a composition comprising the compound of Formula (I), the geometric or optical isomer, the pharmaceutically acceptable salt, the solvate or the polymorph thereof. Also disclosed in the present invention is a use of the compound of Formula (I), the geometric or optical isomer, the pharmaceutically acceptable salt, the solvate or the polymorph thereof in the treatment of a disease or disorder such as a hypoglutamatergic condition, a neurodegenerative disease or respiratory depression, particularly in the treatment of a disease or disorder associated with AMPA receptor.
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公开(公告)号：US20190062290A1
公开(公告)日：2019-02-28
申请号：US16081204
申请日：2017-03-02
发明人： Song LI , Junhai XIAO , Xiaoye ZHANG , Hongliang WANG , Wu ZHONG , Zhibing ZHENG , Yunde XIE , Xingzhou LI , Xinbo ZHOU , Xiaokui WANG
IPC分类号： C07D303/48 , C07D301/27 , C07D405/12
摘要： The present invention relates to a 2,3-epoxy succinyl derivative, a preparation method and a use thereof, in particular, the present invention relates to a compound represented by Formula (1), a racemate or an optical isomer thereof, a solvate thereof, or a pharmaceutically acceptable salt thereof. The compound according to the present invention has good inhibitory activity and/or selectivity against cathepsin, especially Cathepsin B, can be used in the treatment of multiple diseases associated with cathepsin, for example, osteoporosis, rheumatoid arthritis and osteoarthritis that are associated with Cathepsin K, Ebola virus infection, a degenerative disease and an autoimmune disease that are associated with Cathepsin L, S, especially Cathepsin B-related tumor diseases, such as gastric cancer, cervical cancer, lung cancer, breast cancer, prostate cancer, bladder cancer, colon cancer, neuroglioma, and melanoma.
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公开(公告)号：US10196411B2
公开(公告)日：2019-02-05
申请号：US15539266
申请日：2015-12-11
发明人： Song Li , Xingzhou Li , Wu Zhong , Zhibing Zheng , Junhai Xiao , Xinbo Zhou , Yunde Xie , Xiaokui Wang , Lili Wang , Wei Chen , Fei Xie
IPC分类号： C07D277/58 , C07F9/6539 , A61K31/426 , A61K31/675 , A61P31/20 , A61P31/14 , A61P31/16 , A61P31/06 , A61P33/02 , A61P33/04 , A61P33/10 , A61P1/00
摘要： The invention relates to tizoxanide phosphate or alkane sulfonate compounds represented by Formula I, and pharmaceutically acceptable salts thereof, isomers thereof, hydrates thereof or solvates thereof, and pharmaceutical applications of the compounds.
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公开(公告)号：US20180370928A1
公开(公告)日：2018-12-27
申请号：US15777774
申请日：2016-11-24
发明人： Song LI , Junhai XIAO , Libao XU , Ruiyuan CAO , Fangyuan CAO , Hongliang WANG , Wu ZHONG , Zhibing ZHENG , Yunde XIE , Xingzhou LI , Xinbo ZHOU , Xiaokui WANG
IPC分类号： C07D277/54 , A61P31/14
摘要： The present invention relates to a compound represented by Formula I, a racemate or optical isomer thereof, or a pharmaceutically acceptable salt, a solvate or a hydrate thereof, a pharmaceutical composition comprising the compound, and a use thereof in the manufacture of a medicament for preventing and/or treating a disease or disorder associated with a viral infection.
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公开(公告)号：US20180179193A1
公开(公告)日：2018-06-28
申请号：US15314888
申请日：2015-05-25
发明人： Song LI , Junhai XIAO , Qi SUN , Wu ZHONG , Lili WANG , Zhibing ZHENG , Yunde XIE , Xingzhou Li , Xinbo ZHOU , Xiaokui WANG , Ruiyuan CAO
IPC分类号： C07D409/12 , A61K31/381 , A61K45/06 , C07D407/12 , A61K31/365 , C07D405/12 , A61K31/4025 , C07D307/33 , C12Q1/02
CPC分类号： C07D409/12 , A61K31/34 , A61K31/365 , A61K31/381 , A61K31/4025 , A61K45/06 , C07D307/33 , C07D405/00 , C07D405/12 , C07D407/12 , C12Q1/025 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/478
摘要： The invention relates to a homoserine lactone derivative of Formula I, preparation method and use thereof. The compound has an effect of regulatory of bacterial quorum sensing, and is useful for preventing and/or treating a disease caused by infection of a bacterium.
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公开(公告)号：US09630957B2
公开(公告)日：2017-04-25
申请号：US14893391
申请日：2014-05-28
发明人： Song Li , Junhai Xiao , Xian Zhang , Wu Zhong , Zhibing Zheng , Lili Wang , Yunde Xie , Xingzhou Li , Xinbo Zhou , Xiaokui Wang
IPC分类号： C07D417/12 , C07D303/48 , C07D417/14
CPC分类号： C07D417/12 , C07D303/48 , C07D417/14
摘要： Provided are a compound of formula I which can be used as a drug against small RNA virus infections, and optical isomers, pharmaceutically acceptable salts, solvates or hydrates thereof. Also provided are the preparation method of the compound, the method for using the compound for treating bacterial infections and the use of the compound in the preparation of a drug for preventing and/or treating viral diseases caused by small RNA viruses.
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![(1S,2S,3S,4R)-3-[(1S)-1-acetylamino-2-ethyl-butyl]-4-uanidino-2-hydroxyl-cyclopentyl-1-carboxylic acid hydrates pharmaceutical uses thereof](/abs-image/US/2016/12/13/US09518008B2/abs.jpg.150x150.jpg)
10.发明授权(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（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
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。
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