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11. 发明申请

US20080306121A1 Bisheterocycle Tandem Compounds Useful as Antiviral Agents, the Uses Thereof and the Compositions Comprising Such Compounds 失效
标题翻译：用作抗病毒剂的Bisheterocycle Tandem Compounds，其用途和包含这些化合物的组合物
公开(公告)号：US20080306121A1
公开(公告)日：2008-12-11
申请号：US11886593
申请日：2006-01-24
申请人： Fajun Nan , Jianping Zuo , Wenlong Wang , Haijun Chen , Peilan He
发明人： Fajun Nan , Jianping Zuo , Wenlong Wang , Haijun Chen , Peilan He
IPC分类号： A61K31/4439 , A61K31/427 , C07D417/04 , C07D409/04 , A61K31/4178 , A61P31/22 , A61P31/18 , A61P31/12 , C07D413/04 , A61K31/422 , C07D417/14
CPC分类号： C07D277/56 , C07D277/68 , C07D403/04 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14
摘要： The present invention provides small molecule compounds of bisheterocycle in tandem having the structural formula of P1-P2, and the use thereof as well as a composition containing the compounds, each of P1 and P2 is an unsaturated 5-member heterocyclic ring having one or two heteroatoms. This compound may effectively inhibit the replication of influenza virus, the DNA replication of hepatitis B virus (HBV), and the formation of HBsAg and HBeAg. These compounds can be used for the preparation of a medicament for viral diseases, and may overcome the limitations of the known nucleosides drugs, including cytotoxicity, the requirement of other drugs having different structures for against the drug-resistant virus variants induced by long-term therapy. The structure of the compounds according to the invention is relatively simple and easy to be prepared.
摘要翻译：本发明提供具有P1-P2结构式的串联双杂环的小分子化合物及其用途以及含有该化合物的组合物，P1和P2各自为不饱和的5元杂环，具有一个或两个杂原子。该化合物可有效抑制流感病毒的复制，乙型肝炎病毒（HBV）的DNA复制，以及HBsAg和HBeAg的形成。这些化合物可用于制备用于病毒性疾病的药物，并且可以克服已知的核苷类药物的限制，包括细胞毒性，对于长期诱导的抗药性病毒变体具有不同结构的其它药物的要求治疗。根据本发明的化合物的结构相对简单且易于制备。

12. 发明申请

US20130261139A1 USE OF A QUINAZOLINE COMPOUND IN PREPARING A MEDICAMENT AGAINST FLAVIVIRIDAE VIRUS 有权
标题翻译：喹诺酮类化合物在制备药物中的应用
公开(公告)号：US20130261139A1
公开(公告)日：2013-10-03
申请号：US13992870
申请日：2011-12-02
申请人： Jianping Zuo , Youhong Hu , Wei Tang , Bo Chao , Xiankun Tong , Dewen Li , Feihong Ji , Peilan He
发明人： Jianping Zuo , Youhong Hu , Wei Tang , Bo Chao , Xiankun Tong , Dewen Li , Feihong Ji , Peilan He
IPC分类号： C07D239/95 , C07D401/12 , C07D403/12
CPC分类号： C07D239/95 , A61K31/517 , C07D401/12 , C07D403/12 , Y02A50/385
摘要： Disclosed is a use of a quinazoline compound of Formula I having 2,4-diaminoquinazoline as a parent nucleus in preparation of a medicament for treating diseases caused by flaviviridae infection, especially a use in combating Hepatitis C virus infection and Dengue fever virus infection.
摘要翻译：公开了具有2,4-二氨基喹唑啉作为母核的喹唑啉化合物在制备用于治疗由黄病毒感染引起的疾病的药物中的用途，特别是用于对抗丙型肝炎病毒感染和登革热病毒感染的用途。

13. 发明授权

US08129426B2 Water-soluble artemisinin derivatives, their preparation methods, the pharmaceutical compositions and the use thereof 有权
标题翻译：水溶性青蒿素衍生物，其制备方法，药物组合物及其用途
公开(公告)号：US08129426B2
公开(公告)日：2012-03-06
申请号：US11989135
申请日：2006-07-20
申请人： Ying Li , Jianping Zuo , Zhongshun Yang , Junxia Wang , Yu Zhang , Wei Tang , Jianxin Zhang
发明人： Ying Li , Jianping Zuo , Zhongshun Yang , Junxia Wang , Yu Zhang , Wei Tang , Jianxin Zhang
IPC分类号： A61K31/35
CPC分类号： C07D493/18
摘要： Water-soluble artemisinin derivatives, their preparation methods, the pharmaceutical compositions containing the same derivatives and the use thereof are disclosed. The artemisinin derivatives have following formula I. It has been proved by pharmacological tests that these compounds and compositions have evident immuno-suppressive activities, and may be used in the preparation of novel immuno-suppressants for treating the diseases caused by hyperfunction of human immunity (e.g. the auto-immune diseases such as lupus erythematosus, rheumatoid arthritis, multiple sclerosis and the like), and for inhibiting the graft rejection after cell or organ transplantation.
摘要翻译：公开了水溶性青蒿素衍生物及其制备方法，含有相同衍生物的药物组合物及其用途。青蒿素衍生物具有以下式I：通过药理学实验证明，这些化合物和组合物具有明显的免疫抑制活性，可用于制备用于治疗由人免疫功能障碍引起的疾病的新型免疫抑制剂（例如自身免疫疾病如红斑狼疮，类风湿性关节炎，多发性硬化症等），以及用于抑制细胞或器官移植后的移植排斥反应。

14. 发明授权

US09133138B2 Use of a quinazoline compound in preparing a medicament against flaviviridae virus 有权
标题翻译：喹唑啉化合物在制备抗黄病毒病毒的药物中的应用
公开(公告)号：US09133138B2
公开(公告)日：2015-09-15
申请号：US13992870
申请日：2011-12-02
申请人： Jianping Zuo , Youhong Hu , Wei Tang , Bo Chao , Xiankun Tong , Dewen Li , Feihong Ji , Peilan He
发明人： Jianping Zuo , Youhong Hu , Wei Tang , Bo Chao , Xiankun Tong , Dewen Li , Feihong Ji , Peilan He
IPC分类号： A61K31/517 , C07D239/95 , C07D401/12 , C07D403/12
CPC分类号： C07D239/95 , A61K31/517 , C07D401/12 , C07D403/12 , Y02A50/385
摘要： Disclosed is a use of a quinazoline compound of Formula I having 2,4-diaminoquinazoline as a parent nucleus in preparation of a medicament for treating diseases caused by flaviviridae infection, especially a use in combating Hepatitis C virus infection and Dengue fever virus infection.
摘要翻译：公开了具有2,4-二氨基喹唑啉作为母核的喹唑啉化合物在制备用于治疗由黄病毒感染引起的疾病的药物中的用途，特别是用于对抗丙型肝炎病毒感染和登革热病毒感染的用途。

15. 发明申请

US20090298881A1 Water-Soluble Artemisinin Derivatives, Their Preparation Methods, the Pharmaceutical Compositions and the Use Thereof 有权
标题翻译：水溶性青蒿素衍生物及其制备方法，药物组合物及其用途
公开(公告)号：US20090298881A1
公开(公告)日：2009-12-03
申请号：US11989135
申请日：2006-07-20
申请人： Ying Li , Jianping Zuo , Zhongshun Yang , Junxia Wang , Yu Zhang , Wei Tang , Jianxin Zhang
发明人： Ying Li , Jianping Zuo , Zhongshun Yang , Junxia Wang , Yu Zhang , Wei Tang , Jianxin Zhang
IPC分类号： A61K31/357 , C07D493/14 , A61K31/4025 , A61K31/453
CPC分类号： C07D493/18
摘要： Water-soluble artemisinin derivatives, their preparation methods, the pharmaceutical compositions containing the same derivatives and the use thereof are disclosed. The artemisinin derivatives have following formula I. It has been proved by pharmacological tests that these compounds and compositions have evident immuno-suppressive activities, and may be used in the preparation of novel immuno-suppressants for treating the diseases caused by hyperfunction of human immunity (e.g. the auto-immune diseases such as lupus erythematosus, rheumatoid arthritis, multiple sclerosis and the like), and for inhibiting the graft rejection after cell or organ transplantation.
摘要翻译：公开了水溶性青蒿素衍生物及其制备方法，含有相同衍生物的药物组合物及其用途。青蒿素衍生物具有以下式I：通过药理学实验证明，这些化合物和组合物具有明显的免疫抑制活性，可用于制备用于治疗由人免疫功能障碍引起的疾病的新型免疫抑制剂（例如自身免疫疾病如红斑狼疮，类风湿性关节炎，多发性硬化症等），以及用于抑制细胞或器官移植后的移植排斥反应。

16. 发明申请

US20080139642A1 Artemisinin (Qinghaosu) Derivatives, Their Preparation Methods And Their Use, And Pharmaceutical Compositions Containing The Same 有权
标题翻译：青蒿素（Qinghaosu）衍生物及其制备方法及其用途及含有它们的药物组合物
公开(公告)号：US20080139642A1
公开(公告)日：2008-06-12
申请号：US11883652
申请日：2006-01-27
申请人： Ying Li , Jianping Zuo , Zhongshun Yang , Wenliang Zhou , Yi Sui , Junxia Wang , Yu Zhang , Yu Zhou , Jinming Wu
发明人： Ying Li , Jianping Zuo , Zhongshun Yang , Wenliang Zhou , Yi Sui , Junxia Wang , Yu Zhang , Yu Zhou , Jinming Wu
IPC分类号： A61K31/357 , C07D313/06 , A61P37/00
CPC分类号： C07D493/18
摘要： The invention provides a type of artemisinin derivatives having following structure I, its preparation method and use, as well as a pharmaceutical composition containing such artemisinin derivatives and its use. The artemisinin derivatives of the present invention and their pharmaceutical composition containing the artemisinin derivatives. have immunosuppressive activities and can be used more safely. The composition which comprises the artemisinin derivatives can be formulated into long-term dosage forms such as tablet, pellet and the like, and have wider productive and use value.
摘要翻译：本发明提供一种具有以下结构I的青蒿素衍生物及其制备方法和用途，以及含有这种青蒿素衍生物的药物组合物及其用途。本发明的青蒿素衍生物及其含有青蒿素衍生物的药物组合物。具有免疫抑制活性，可以更安全地使用。包含青蒿素衍生物的组合物可以配制成长期剂型，如片剂，丸剂等，具有更广泛的生产和使用价值。

17. 发明申请

US20070197476A1 Triptolide Derivatives And Their Uses 有权
标题翻译：雷公藤内酯衍生物及其用途
公开(公告)号：US20070197476A1
公开(公告)日：2007-08-23
申请号：US10540908
申请日：2003-01-28
申请人： Yuanchao Li , Jianping Zuo , Fan Zhang , Ru Zhou , Jian Ding
发明人： Yuanchao Li , Jianping Zuo , Fan Zhang , Ru Zhou , Jian Ding
IPC分类号： A61K31/675 , A61K31/365 , C07D493/22
CPC分类号： C07D493/22 , A61K31/34
摘要： The invention relates to triptolide derivatives of Formula (I), their pharmaceutically acceptable salts and optical isomers, Formula (I): wherein, C5 and C6 connect with each other by a C—C single bond or double bond; when C5 and C6 are connected with C—C single bond, X and Y represents independently hydrogen, oxygen, hydroxyl, halogen, lower alkyl-oxy, lower alkyl-amino, mercapto, lower alkyl-thio, the group of formula —OCOR, —OSO2R or —OPO(OH)2, each of which is attached to C5 and C6, R represents —(CH2)nCO2Na, —(CO2)nCO2K, or —(CH2)nCH3, wherein n=1-6; Z represents hydrogen, oxygen, hydroxyl, halogen, lower alkyl-oxy, lower alkyl-amino, mercapto, lower alkyl-thio, the group of formula —OCOR, —OSO2R or —OPO(OH)2, each of which is linked at C14-position, R represents —(CH2)nCO2Na, —(CO2)nCO2K, or —(CH2)nCH2, wherein n=1-6; wherein, the “_” linked with X, Y, and Z represents “” or “”, but X and Y cannot both be hydrogen atom at the same time, the methods for preparing them and their use as antiphlogistic agent, immunosuppressive agent or therapeutic agent for other related diseases.
摘要翻译：本发明涉及式（I）的雷公藤内酯衍生物，其药学上可接受的盐和旋光异构体，式（I）：其中C5和C6通过C-C单键或双键相互连接; 当C5和C6与CC单键连接时，X和Y独立地表示氢，氧，羟基，卤素，低级烷基氧基，低级烷基 - 氨基，巯基，低级烷基 - 硫基，式-OCOR基团，-OSO （OH）2 N，其各自与C5和C6连接，R表示 - （CH 2）nCO 2， Na 2， - （CO 2）n CO 2 K，或 - （CH 2 2）n CH 3 其中n = 1-6; Z代表氢，氧，羟基，卤素，低级烷基 - 氧基，低级烷基 - 氨基，巯基，低级烷基 - 硫基，式-OCOR，-OSO 2 R或-OPO（OH ）2，其各自在C14位连接，R表示 - （CH 2）n CO 2 Na， - （CO 2 N 2）n CO 2 K，或 - （CH _{“或”“，但X和Y不能同时为氢原子，制备它们及其用作消炎剂，免疫抑制剂或其他相关疾病的治疗剂。}

18. 发明申请

US20060142383A1 3D-Structure model of SARS coronavirus 3CL protease and anti-SARS drugs 失效
标题翻译： SARS冠状病毒3CL蛋白酶和抗SARS药物的3D结构模型
公开(公告)号：US20060142383A1
公开(公告)日：2006-06-29
申请号：US11293847
申请日：2005-12-02
申请人： Jianhua Shen , Hualiang Jiang , Xu Shen , Jianping Zuo , Xiaomin Luo , Donglu Bai , Jingkang Shen , Kaixian Chen , Chunshan Gui , Lili Chen , Jing Chen , Yifu Yang , Xianhan Zhuang , Yiming Yang , Xuchang He , Hong Liu , Bing Xiong , Haibin Luo , Tao Sun , Fei Ye
发明人： Jianhua Shen , Hualiang Jiang , Xu Shen , Jianping Zuo , Xiaomin Luo , Donglu Bai , Jingkang Shen , Kaixian Chen , Chunshan Gui , Lili Chen , Jing Chen , Yifu Yang , Xianhan Zhuang , Yiming Yang , Xuchang He , Hong Liu , Bing Xiong , Haibin Luo , Tao Sun , Fei Ye
IPC分类号： C12Q1/70 , G06F19/00 , C12N9/48 , A61K31/21 , A61K31/235 , A61K31/165
CPC分类号： C12N9/506 , A61K31/167
摘要： The present invention discloses 3D-structure of SARS-CoV Viral 3CL Protease obtained through molecular simulation. The 3D-structure is used as a drug target for screening the existing medical database CMC (Comprehensive Medicinal Chemistry, MDL Information System, Inc.), and a group of compounds which have the activity of inhibiting SARS-CoV virus 3CL Protease are found. Cinanserin was tested at molecular and viral levels, and it was found to be able to inhibit the SARS-CoV viral 3CL protease and SARS-CoV viruses. Cinanserin analogs were synthesized and tested at molecular and viral levels, they were found to be able to inhibit the SARS-CoV virus 3CL Protease and SARS-CoV viruses, and may be used for treating and/or preventing SARS-CoV virus infection.
摘要翻译：本发明公开了通过分子模拟获得的SARS-CoV病毒3CL蛋白酶的三维结构。使用3D结构作为筛选现有医学数据库CMC（Comprehensive Medicinal Chemistry，MDL Information System，Inc。）的药物靶点，并发现一组具有抑制SARS-CoV病毒3CL蛋白酶活性的化合物。在分子和病毒水平测试了Cinanserin，发现能够抑制SARS-CoV病毒3CL蛋白酶和SARS-CoV病毒。合成Cinanserin类似物并在分子和病毒水平进行测试，发现它们能够抑制SARS-CoV病毒3CL蛋白酶和SARS-CoV病毒，可用于治疗和/或预防SARS-CoV病毒感染。

19. 发明申请

US20200181109A1 PHTHALAZINONE COMPOUND, METHOD FOR PREPARATION THEREOF, PHARMACEUTICAL COMPOSITION THEREOF, AND USE THEREOF 审中-公开
公开(公告)号：US20200181109A1
公开(公告)日：2020-06-11
申请号：US16786710
申请日：2020-02-10
申请人： Youhong Hu , Jianping Zuo , Dong Lu , Li Yang , Limin Zeng , Feifei Liu , Yunzhe Zhang , Wuhong Chen , Xiankun Tong
发明人： Youhong Hu , Jianping Zuo , Dong Lu , Li Yang , Limin Zeng , Feifei Liu , Yunzhe Zhang , Wuhong Chen , Xiankun Tong
IPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , C07D405/14 , A61P31/20
摘要： Provided are a phthalazinone compound, method for preparation thereof, pharmaceutical composition thereof, and a use thereof; the structure of said phthalazinone compound is as represented by formula I; the compound of said formula I is targeted to a viral nucleocapsid; it can inhibit the replication of a virus by means of interference of the viral nucleocapsid, has a potent activity for inhibiting HBV DNA replication and a good liver targeting, can stably exist and enrich in the liver, and is a new and effective anti-HBV inhibitor.

20. 发明授权

US07910750B2 Artemisinin (qinghaosu) derivatives, their preparation methods and their use, and pharmaceutical compositions containing the same 有权
标题翻译：青蒿素（青蒿素）衍生物及其制备方法及其应用，以及含有它们的药物组合物
公开(公告)号：US07910750B2
公开(公告)日：2011-03-22
申请号：US11883652
申请日：2006-01-27
申请人： Ying Li , Jianping Zuo , Zhongshun Yang , Wenliang Zhou , Yi Sui , Junxia Wang , Yu Zhang , Yu Zhou , Jinming Wu
发明人： Ying Li , Jianping Zuo , Zhongshun Yang , Wenliang Zhou , Yi Sui , Junxia Wang , Yu Zhang , Yu Zhou , Jinming Wu
IPC分类号： C07D323/04 , A61K31/357
CPC分类号： C07D493/18
摘要： The invention provides a type of artemisinin derivatives having following structure I, its preparation method and use, as well as a pharmaceutical composition containing such artemisinin derivatives and its use. The arteminsinin derivatives of the present invention and their pharmaceutical composition containing the artemisinin derivatives. have immunosuppressive activities and can be used more safely. The composition which comprises the artemisinin derivatives can be formulated into long-term dosage forms such as tablet, pellet and the like, and have wider productive and use value.
摘要翻译：本发明提供一种具有以下结构I的青蒿素衍生物及其制备方法和用途，以及含有这种青蒿素衍生物的药物组合物及其用途。本发明的青蒿素衍生物及其含有青蒿素衍生物的药物组合物。具有免疫抑制活性，可以更安全地使用。包含青蒿素衍生物的组合物可以配制成长期剂型，如片剂，丸剂等，具有更广泛的生产和使用价值。

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