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1. 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.

2. 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。

3. 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。

4. 发明申请

US20120264793A1 Pharmaceutical Use of 2',2-Bis-Thiazole Non-Nucleoside Compounds as Hepatitis C Virus Inhibitor 审中-公开
标题翻译： 2'，2-双噻唑非核苷化合物作为丙型肝炎病毒抑制剂的药物用途
公开(公告)号：US20120264793A1
公开(公告)日：2012-10-18
申请号：US13518549
申请日：2010-11-24
申请人： Fajun Nan , Jianping Zuo , Yangming Zhang , Feihong Ji , Haijun Chen , Xiankun Tong
发明人： Fajun Nan , Jianping Zuo , Yangming Zhang , Feihong Ji , Haijun Chen , Xiankun Tong
IPC分类号： A61K31/427 , C07D417/14 , A61P31/14 , C07D417/04
CPC分类号： A61K31/427
摘要： The present invention discloses the pharmaceutical use of a 2′,2-bis-thiazole non-nucleoside compound of formula I as an inhibitor of hepatitis C virus (HCV). The 2′,2-bis-thiazole non-nucleoside compound can inhibit the replication of HCV, and thus has an anti-HCV activity and is useful for treating hepatitis C.
摘要翻译：本发明公开了作为丙型肝炎病毒（HCV）抑制剂的式I的2'，2-双噻唑非核苷化合物的药物用途。 2'，2-双噻唑非核苷化合物可以抑制HCV的复制，因此具有抗HCV活性，可用于治疗丙型肝炎。

5. 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。

6. 发明授权

US08247549B2 Method for preparing 4-(6-amino-purin-9-YL)-2(S)-hydroxy-butyric acid methyl ester 有权
标题翻译：制备4-（6-氨基嘌呤-9-YL）-2（S） - 羟基 - 丁酸甲酯的方法
公开(公告)号：US08247549B2
公开(公告)日：2012-08-21
申请号：US12747312
申请日：2008-11-06
申请人： Fajun Nan , Jianping Zuo , Yangming Zhang , Min Gu , Wei Tang
发明人： Fajun Nan , Jianping Zuo , Yangming Zhang , Min Gu , Wei Tang
IPC分类号： C07D473/34
CPC分类号： C07D473/34 , Y02P20/55
摘要： The present invention discloses a novel method for preparing and purifying 4-(6-Amino-purin-9-yl)-2(S)-hydroxy-butyric acid methyl ester. The preparation started from cheap and easily available L-malic acid, which was transformed to intermediate I after simultaneous protection of the groups of 1-carboxyl and 2-hydroxyl. The intermediate I was selectively reduced to intermediate alcohol II, whose hydroxyl group was further transformed to an easily leaving group to afford intermediate III. The intermediate III was nucleophilically substituted with adenine to afford intermediate IV. The intermediate IV was deprotected and methyl-esterified simultaneously in methanol in the presence of an acid or a base to afford crude 4-(6-Amino-purin-9-yl)-2(S)-hydroxy-butyric acid methyl ester, which was purified by recrystallization to afford the purified product. Comparing with the prior preparation methods, the present method has advantages in low cost, mild conditions, high retention of the chiral center during the reaction, high productivity, great improvement in the quality and yield of the product and great decrease in cost, and thus is suitable for the production on a large scale.
摘要翻译：本发明公开了一种制备和纯化4-（6-氨基嘌呤-9-基）-2（S） - 羟基 - 丁酸甲酯的新方法。该制剂从便宜且易于获得的L-苹果酸开始，其在同时保护1-羧基和2-羟基的基团后转化为中间体I. 将中间体I选择性还原成中间体醇II，其中羟基进一步转化为容易离去的基团，得到中间体III。中间体III被腺嘌呤亲核取代，得到中间体IV。将中间体IV在酸或碱的存在下在甲醇中同时脱甲基酯化，得到粗制的4-（6-氨基 - 嘌呤-9-基）-2（S） - 羟基 - 丁酸甲酯，通过重结晶纯化，得到纯化产物。与现有的制备方法相比，本发明方法具有成本低，条件温和，反应中手性中心保留性高，生产效率高，产品质量和产量大幅提高，成本大幅降低的优点，适合大规模生产。

7. 发明申请

US20110166172A1 Rapamycin Carbonic Ester Analogues, Pharmaceutical Compositions, Preparations and Uses Thereof 失效
标题翻译：雷帕霉素碳酸酯类似物，药物组合物，制剂及其用途
公开(公告)号：US20110166172A1
公开(公告)日：2011-07-07
申请号：US13119700
申请日：2009-09-17
申请人： Fajun Nan , Jian Ding , Jianping Zuo , Linqian Yu , Linghua Meng , Yangming Zhang , Na Yang , Min Gu
发明人： Fajun Nan , Jian Ding , Jianping Zuo , Linqian Yu , Linghua Meng , Yangming Zhang , Na Yang , Min Gu
IPC分类号： A61K31/436 , C07D267/00 , A61P35/00
CPC分类号： A61K31/436 , C07D498/18
摘要： Rapalogs of formula I, pharmaceutically acceptable salts, pharmaceutical compositions, and preparation methods and uses thereof. The rapalogs have the structure of formula I and can be used as an anti-tumor medicament. Comparing with rapamycin, the rapalogs of the present invention exhibit enhanced water solubility, and improved pharmacological and pharmacokinetic properties by introducing a hydrophilic and polar group such as a hydroxyl.
摘要翻译：式I的药学上可接受的盐，药物组合物及其制备方法和用途。 rapalogs具有式I的结构，可用作抗肿瘤药物。与雷帕霉素相比，本发明的rapalogs通过引入亲水性和极性基团如羟基表现出增强的水溶性，以及改善的药理学和药代动力学性质。

8. 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。

9. 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。

10. 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。}

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