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21. 发明授权

US10759822B2 Brain-targeting prodrug for AMPA receptor synergist, and pharmaceutical applications thereof 有权
公开(公告)号：US10759822B2
公开(公告)日：2020-09-01
申请号：US16093754
申请日：2017-04-11
申请人： Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
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 , C07H1/00 , A61K31/7056 , A61K31/4245
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.

22. 发明授权

US10335417B2 Thiazideamide derivative and use thereof 有权
公开(公告)号：US10335417B2
公开(公告)日：2019-07-02
申请号：US15739872
申请日：2016-06-28
申请人： Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
发明人： Song Li , Junhai Xiao , Boqun Lyu , Hongqiang Wang , Wu Zhong , Lili Wang , Zhibing Zheng , Yunde Xie , Xinbo Zhou , Xingzhou Li , Xiaokui Wang
IPC分类号： C07D279/12 , A61K31/54 , A61P25/28 , A61P25/16
摘要： The invention belongs to the technical field of medicines. In particular, the invention relates to a thiazideamide derivative compound or a pharmaceutically acceptable salt or solvate thereof, a pharmaceutical composition comprising the compound or a pharmaceutically acceptable salt or solvate thereof, a method for preparing the compound or a pharmaceutically acceptable salt or solvate thereof, and a use of the compound or a pharmaceutically acceptable salt or solvate thereof. For example, the compound or a pharmaceutically acceptable salt or solvate thereof according to the invention can be used to prevent and/or treat a neurodegenerative disease or a neuropathic disease caused by a physical trauma or a related disease.

23. 发明授权

US10071994B2 N-sulfonyl homoserine lactone derivatives, preparation method and use thereof 有权
公开(公告)号：US10071994B2
公开(公告)日：2018-09-11
申请号：US15314888
申请日：2015-05-25
申请人： Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
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： C07D307/33 , A61K31/341 , C07D409/12 , A61K31/381 , A61K45/06 , C07D407/12 , C12Q1/02 , C07D405/12 , A61K31/4025 , A61K31/365
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

24. 发明授权

US09522891B2 Pyridazine derivatives and use thereof as medicaments for treating microRNA viral infection 有权
标题翻译：哒嗪衍生物及其用作治疗微小RNA病毒感染的药物
公开(公告)号：US09522891B2
公开(公告)日：2016-12-20
申请号：US14494285
申请日：2014-09-23
申请人： INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY ACADEMY OF MILITARY MEDICAL SCIENCES P.L.A. China
发明人： Song Li , Hongliang Wang , Junhai Xiao , Xian Zhang , Lili Wang , Zhibing Zheng , Wu Zhong , Yunde Xie , Xingzhou Li , Xinbo Zhou , Guoming Zhao , Xiaokui Wang
IPC分类号： C07D237/20
CPC分类号： C07D237/20
摘要： Disclosed are pyridazine derivatives represented by Formula I or pharmaceutically acceptable salts or hydrates thereof, pharmaceutical compositions comprising the compounds, methods of treating and/or preventing diseases or disorders associated with viral infections in patients using the compounds, and the use of the compounds in preparing the medicaments for treating and/or preventing diseases or disorders associated with viral infections. The compounds represented by Formula I have antiviral activity, especially anti-microRNA viral activity. Symbols in the compounds represented are described in the specification.

25. 发明授权

US09139543B2 Thiazole compounds and uses thereof 有权
标题翻译：噻唑化合物及其用途
公开(公告)号：US09139543B2
公开(公告)日：2015-09-22
申请号：US14399680
申请日：2013-05-10
申请人： Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
发明人： Song Li , Wu Zhong , Juan Liu , Kunlun He , Junhai Xiao , Xinbo Zhou
IPC分类号： C07D277/42
CPC分类号： C07D277/42
摘要： The present invention relates to a compound of Formula (I), or an isomer, pharmaceutically acceptable salt and solvate thereof; the present invention further relates to a pharmaceutical composition, which comprises the compound of Formula (I), or isomer, pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents; the present invention further relates to the use of the compound of Formula (I), or isomer, pharmaceutically acceptable salt or solvate thereof, for anti-apoptosis, prophylaxis or treatment of a disease or symptom associated with apoptosis, especially for protecting myocardial cells, and prophylaxis or treatment of a disease or symptom associated with cardiomyocyte apoptosis.
摘要翻译：本发明涉及式（I）化合物或其异构体，药学上可接受的盐和溶剂合物; 本发明还涉及药物组合物，其包含式（I）的化合物或其异构体，药学上可接受的盐或溶剂合物，以及药学上可接受的载体，赋形剂或稀释剂; 本发明还涉及式（I）化合物或其异构体，药学上可接受的盐或溶剂合物用于抗凋亡，预防或治疗与凋亡相关的疾病或症状的用途，特别是用于保护心肌细胞，并预防或治疗与心肌细胞凋亡相关的疾病或症状。

26. 发明申请

US20150056292A1 Joint Product Comprising Synephrine and Topiramate 有权
标题翻译：联合产品包括昔萘福林和托吡酯
公开(公告)号：US20150056292A1
公开(公告)日：2015-02-26
申请号：US14386478
申请日：2013-03-22
申请人： Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A.China
发明人： Song Li , Chunsheng Gao , Wu Zhong , Yuli Wang , Meiyan Yang , Li Shan , Xinbo Zhou , Zhibing Zheng , Xiaokui Wang
IPC分类号： A61K31/357 , A61K9/50 , A61K31/137
CPC分类号： A61K31/357 , A61K9/1635 , A61K9/1652 , A61K9/1676 , A61K9/5026 , A61K9/5047 , A61K9/5078 , A61K9/5084 , A61K9/5089 , A61K31/137 , A61K31/7048 , A61K45/06 , A61K2300/00
摘要： The present invention provides a joint product comprising synephrine and topiramate, in which the synephrine or salt thereof is administered in form of rapid-release preparation, preferably rapid-release pellet, having daily dose of 2 mg to 25 mg, preferably 5 mg to 20 mg; the topiramate is administered in form of sustained-release or controlled-release preparation, preferably sustained-release pellet, having daily dose of 20 mg to 100 mg, preferably 23 mg to 92 mg. The composition is used for treatment of obesity or other diseases associated with obesity.
摘要翻译：本发明提供了包含昔萘福芬和托吡酯的联合产品，其中昔萘福林或其盐以快速释放制剂，优选快速释放丸剂的形式施用，每日剂量为2mg至25mg，优选5mg至20mg 毫克托吡酯以持续释放或控释制剂的形式施用，优选缓释丸剂，每日剂量为20mg至100mg，优选为23mg至92mg。该组合物用于治疗与肥胖相关的肥胖或其它疾病。

27. 发明授权

US12115226B2 Linker containing arylnitro, antibody-drug conjugate containing linker and use of linker 有权
公开(公告)号：US12115226B2
公开(公告)日：2024-10-15
申请号：US17271882
申请日：2019-08-28
申请人： Academy of Military Medical Sciences
发明人： Xinbo Zhou , Yanming Wang , Song Li , Wu Zhong , Shiyong Fan , Dian Xiao , Junhai Xiao , Zhibing Zheng , Xingzhou Li , Yunde Xie , Ruiyuan Cao , Xiaokui Wang
IPC分类号： A61K47/68 , A61K31/337 , A61K31/4745 , A61K31/537 , A61K31/5517 , A61K31/704 , A61K38/07 , A61K47/54 , A61P35/00 , C07C237/04 , C07D207/452 , C07D233/94 , C07D307/71 , C07D333/44 , C07D403/04 , C07D405/12 , C07D409/12
CPC分类号： A61K47/6811 , A61K31/337 , A61K31/4745 , A61K31/537 , A61K31/5517 , A61K31/704 , A61K38/07 , A61K47/545 , A61K47/6803 , A61K47/6809 , A61P35/00 , C07C237/04 , C07D207/452 , C07D233/94 , C07D307/71 , C07D333/44 , C07D403/04 , C07D405/12 , C07D409/12
摘要： The present application relates to a linker containing arylnitro, an antibody-drug conjugate the linker and use of the linker, as well as a pharmaceutical composition comprising the antibody-drug conjugate and use of the antibody-drug conjugate for treatment and/or prevention of a disease

28. 发明授权

US11318115B2 Oral pharmaceutical composition of Tecovirimat and preparation method thereof 有权
公开(公告)号：US11318115B2
公开(公告)日：2022-05-03
申请号：US16317942
申请日：2017-07-04
申请人： Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
发明人： Wu Zhong , Meiyan Yang , Wei Gong , Yuli Wang , Chunsheng Gao , Xinbo Zhou , Song Li
IPC分类号： A61K31/4035 , A61K47/18 , A61K47/40
摘要： The present invention relates to a pharmaceutical composition, comprising Tecovirimat, cyclodextrin and an additive, and optionally a pharmaceutically acceptable excipient. The present invention also relates to a method for preparing the pharmaceutical composition. The composition improves the solubility of Tecovirimat in water by using cyclodextrin and meglumine in combination, as compared with the solubility of Tecovirimat in water by using cyclodextrin or meglumine alone.

29. 发明授权

US10647690B2 2,3-epoxy succinyl derivative, preparation method and use thereof 有权
公开(公告)号：US10647690B2
公开(公告)日：2020-05-12
申请号：US16081204
申请日：2017-03-02
申请人： Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
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 , C07D405/12 , A61K31/5377 , A61K31/541 , A61K31/336 , A61K31/4025 , A61K31/4523 , A61K31/427 , C07D417/12 , A61P19/00 , A61P37/02 , A61P35/00 , C07D301/27
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.

30. 发明申请

US20190336479A1 Injectable Pharmaceutical Composition of Tecovirimat and Preparation Method Thereof 审中-公开
公开(公告)号：US20190336479A1
公开(公告)日：2019-11-07
申请号：US16318044
申请日：2017-07-04
申请人： Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
发明人： Wu Zhong , Meiyan Yang , Wei Gong , Yuli Wang , Chunsheng Gao , Xinbo Zhou , Song Li
IPC分类号： A61K31/403 , A61K47/40 , A61K9/19 , A61K47/26
摘要： The present invention relates to a pharmaceutical composition of Tecovirimat for injection, comprising Tecovirimat as an active ingredient, cyclodextrin and an additive. The present invention also relates to a method for preparing the pharmaceutical composition. The composition improves the solubility of Tecovirimat in water by using cyclodextrin and meglumine in combination, as compared with the solubility of Tecovirimat in water by using cyclodextrin or meglumine alone.

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