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1. 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。

2. 发明申请

US20110201810A1 Method for Preparing 4-[9-(6-Aminopurine)]-2-(S)-Hydroxyl-Butyric Acid Methyl Ester 有权
标题翻译： 4- [9-（6-氨基嘌呤）] - 2-（S） - 羟基 - 丁酸甲酯的制备方法
公开(公告)号：US20110201810A1
公开(公告)日：2011-08-18
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用腺嘌呤亲核取代，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。

3. 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。

4. 发明授权

US08455510B2 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：US08455510B2
公开(公告)日：2013-06-04
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： C07D498/18 , A61K31/436 , 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。

5. 发明授权

US08426606B2 2′,2-bisthiazole non-nucleoside compounds, preparation methods, pharmaceutical compositions and uses as hepatitis virus inhibitors thereof 失效
标题翻译： 2'，2-双噻唑非核苷化合物，制备方法，药物组合物和用途作为其肝炎病毒抑制剂
公开(公告)号：US08426606B2
公开(公告)日：2013-04-23
申请号：US13636488
申请日：2011-03-16
申请人： Fajun Nan , Jianping Zuo , Yangming Zhang , Wei Tang
发明人： Fajun Nan , Jianping Zuo , Yangming Zhang , Wei Tang
IPC分类号： C07D417/04 , A61K31/427
CPC分类号： C07D277/56
摘要： The present disclosure belongs to the field of pharmaceutical chemistry, and relates to a class of 2′,2-bisthiazole non-nucleoside compounds of following formula I, the preparation method and the pharmaceutical composition thereof. The compounds have both the anti-HBV and anti-HCV activities and are useful in treating hepatitides B and C. Pharmacokinetic tests showed the compounds have good bioavailability.
摘要翻译：本公开属于药物化学领域，涉及一类下式I的2'，2-双噻唑非核苷化合物，其制备方法及其药物组合物。该化合物具有抗HBV和抗HCV活性，可用于治疗肝素B和C.药代动力学试验显示，化合物具有良好的生物利用度。

6. 发明申请

US20130059895A1 2',2-DITHIAZOL NON-NUCLEOSIDE COMPOUNDS, PREPARATION METHODS, PHARMACEUTICAL COMPOSITIONS AND USES AS HEPATITIS VIRUS INHIBITORS THEREOF 失效
标题翻译： 2'，2-DITHIAZOL非核苷酸化合物，制备方法，药物组合物和用作其中的HEPATITIS病毒抑制剂
公开(公告)号：US20130059895A1
公开(公告)日：2013-03-07
申请号：US13636488
申请日：2011-03-16
申请人： Fajun Nan , Jianping Zuo , Yangming Zhang , Wei Tang
发明人： Fajun Nan , Jianping Zuo , Yangming Zhang , Wei Tang
IPC分类号： A61K31/427 , A61P31/20 , A61P31/14 , C07D417/04
CPC分类号： C07D277/56
摘要： The present disclosure belongs to the field of pharmaceutical chemistry, and relates to a class of 2′,2-bisthiazole non-nucleoside compounds of following formula I, the preparation method and the pharmaceutical composition thereof. The compounds have both the anti-HBV and anti-HCV activities and are useful in treating hepatitides B and C. Pharmacokinetic tests showed the compounds have good bioavailability.
摘要翻译：本公开属于药物化学领域，涉及一类下式I的2'，2-双噻唑非核苷化合物，其制备方法及其药物组合物。该化合物具有抗HBV和抗HCV活性，可用于治疗肝素B和C.药代动力学试验显示，化合物具有良好的生物利用度。

7. 发明授权

US08653115B2 Heterocyclic non-nucleoside compounds, their preparation, pharmaceutical composition and their use as antiviral agents 失效
标题翻译：杂环非核苷化合物，其制备方法，药物组合物及其作为抗病毒剂的用途
公开(公告)号：US08653115B2
公开(公告)日：2014-02-18
申请号：US12304598
申请日：2007-06-13
申请人： Fajun Nan , Jianping Zuo , Haijun Chen , Guifeng Wang , Min Gu , Fenghua Zhu , Wei Tang
发明人： Fajun Nan , Jianping Zuo , Haijun Chen , Guifeng Wang , Min Gu , Fenghua Zhu , Wei Tang
IPC分类号： A61K31/426 , C07D277/24
CPC分类号： C07D417/04 , C07D263/32 , C07D263/34 , C07D277/24 , C07D277/56 , C07D513/04
摘要： The invention relates a kind of antiviral agents, more concretely, relates to a kind of heterocyclic non-nucleoside compounds with the following structures, their preparation and pharmaceutical compositions including the compounds. The said compounds can be used as antiviral agents and as medicaments for treating diseases such as hepatitis B, influenza, herpes, HIV and so on.
摘要翻译：本发明涉及一种抗病毒剂，更具体地说，涉及一种具有以下结构的杂环非核苷化合物，其制备方法和包括该化合物的药物组合物。所述化合物可用作抗病毒剂和用作治疗诸如乙型肝炎，流感，疱疹，HIV等疾病的药物。

8. 发明申请

US20100056569A1 Heterocyclic Non-Nucleoside Compounds, Their Preparation, Pharmaceutical Composition And Their Use As Antiviral Agents 失效
标题翻译：杂环非核苷化合物，其制备，药物组合物及其作为抗病毒剂的用途
公开(公告)号：US20100056569A1
公开(公告)日：2010-03-04
申请号：US12304598
申请日：2007-06-13
申请人： Fajun Nan , Jianping Zuo , Haijun Chen , Guifeng Wang , Min Gu , Fenghua Zhu , Wei Tang
发明人： Fajun Nan , Jianping Zuo , Haijun Chen , Guifeng Wang , Min Gu , Fenghua Zhu , Wei Tang
IPC分类号： A61K31/4439 , C07D401/04 , A61K31/4709 , A61P31/12
CPC分类号： C07D417/04 , C07D263/32 , C07D263/34 , C07D277/24 , C07D277/56 , C07D513/04
摘要： The invention relates a kind of antiviral agents, more concretely, relates to a kind of heterocyclic non-nucleoside compounds with the following structures, their preparation and pharmaceutical compositions including the compounds. The said compounds can be used as antiviral agents and as medicaments for treating diseases such as hepatitis B, influenza, herpes, HIV and so on.
摘要翻译：本发明涉及一种抗病毒剂，更具体地说，涉及一种具有以下结构的杂环非核苷化合物，其制备方法和包括该化合物的药物组合物。所述化合物可用作抗病毒剂和用作治疗诸如乙型肝炎，流感，疱疹，HIV等疾病的药物。

9. 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。

10. 发明授权

US07741348B2 Bisheterocycle tandem compounds useful as antiviral agents, the uses thereof and the compositions comprising such compounds 失效
标题翻译：可用作抗病毒剂的双组分串联化合物，其用途和包含这些化合物的组合物
公开(公告)号：US07741348B2
公开(公告)日：2010-06-22
申请号：US11886593
申请日：2006-01-24
申请人： Fajun Nan , Jianping Zuo , Wenlong Wang , Guifeng Wang , Haijun Chen , Peilan He
发明人： Fajun Nan , Jianping Zuo , Wenlong Wang , Guifeng Wang , Haijun Chen , Peilan He
IPC分类号： A61K31/427 , C07D277/20
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：本发明提供了具有P1-P2结构式的双杂环的小分子化合物及其用途以及含有这些化合物的组合物，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。

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