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1. 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。

2. 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。

3. 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。

4. 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。

5. 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。

6. 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。

7. 发明授权

US07683073B2 Isoquinoline-1,3,4-trione compounds, the synthetic method and the use thereof 失效
标题翻译：异喹啉-1,3,4-三酮化合物，其合成方法及其应用
公开(公告)号：US07683073B2
公开(公告)日：2010-03-23
申请号：US11301638
申请日：2005-12-13
申请人： Fajun Nan , Jia Li , Yihua Chen , Yahui Zhang , Min Gu , Huajie Zhang
发明人： Fajun Nan , Jia Li , Yihua Chen , Yahui Zhang , Min Gu , Huajie Zhang
IPC分类号： C07D217/22 , A61K31/47
CPC分类号： C07D417/04 , C07D217/24
摘要： The invention relates to various substituted isoquinoline-1,3,4-trione, the synthetic method thereof and the use for treating neurodegenerative diseases, especially as the medicine for Alzheimer's disease, apoplexy and brain ischemic injuries.
摘要翻译：本发明涉及各种取代的异喹啉-1,3,4-三酮，其合成方法和治疗神经变性疾病的用途，特别是作为阿尔茨海默氏病，中风和脑缺血性损伤的药物。

8. 发明申请

US20060135557A1 Isoquinoline-1,3,4-trione compounds, the synthetic method and the use thereof 失效
标题翻译：异喹啉-1,3,4-三酮化合物，其合成方法及其应用
公开(公告)号：US20060135557A1
公开(公告)日：2006-06-22
申请号：US11301638
申请日：2005-12-13
申请人： Fajun Nan , Jia Li , Yihua Chen , Yahui Zhang , Min Gu , Huajie Zhang
发明人： Fajun Nan , Jia Li , Yihua Chen , Yahui Zhang , Min Gu , Huajie Zhang
IPC分类号： A61K31/47 , C07D217/22
CPC分类号： C07D417/04 , C07D217/24
摘要： The invention relates to various substituted isoquinoline-1,3,4-trione, the synthetic method thereof and the use for treating neurodegenerative diseases, especially as the medicine for Alzheimer's disease, apoplexy and brain ischemic injuries.
摘要翻译：本发明涉及各种取代的异喹啉-1,3,4-三酮，其合成方法和治疗神经变性疾病的用途，特别是作为阿尔茨海默氏病，中风和脑缺血性损伤的药物。

9. 发明授权

US07715673B2 Imaging system 失效
标题翻译：成像系统
公开(公告)号：US07715673B2
公开(公告)日：2010-05-11
申请号：US11917553
申请日：2006-06-16
申请人： Ling Fu , Min Gu , Xiaosong Gan
发明人： Ling Fu , Min Gu , Xiaosong Gan
IPC分类号： G02B6/02
CPC分类号： A61B1/043 , A61B1/00096 , A61B1/0017 , A61B1/00172 , A61B1/07 , A61B5/0062 , A61B5/0068 , A61B5/0071 , A61B5/0086 , A61B5/4523 , G02B6/32 , G02B23/24 , G02B26/0833
摘要： An imaging system including a multi-mode fiber and a gradient index (GRIN) lens. The invention also relates to a system including a multi-mode fiber, such as a double-clad photonic crystal fiber, for transmitting an excitation signal to a sample for the purpose of imaging, and a scanning mechanism, which preferably includes a microelectromechanical system (MEMS) mirror, for reflecting the excitation signal in varying directions in order to scan the sample.
摘要翻译：一种包括多模光纤和梯度折射率（GRIN）透镜的成像系统。本发明还涉及一种包括诸如双包层光子晶体光纤的多模光纤用于将激发信号传输到用于成像的样品的系统，以及扫描机构，其优选地包括微机电系统（ MEMS）反射镜，用于在变化的方向上反射激励信号，以扫描样品。

10. 发明授权

US07019309B2 Tripartite fiber-coupled fluorescence instrument 失效
标题翻译：三光纤耦合荧光仪器
公开(公告)号：US07019309B2
公开(公告)日：2006-03-28
申请号：US10460188
申请日：2003-06-13
申请人： Min Gu , Damian Bird
发明人： Min Gu , Damian Bird
IPC分类号： G01N21/64
CPC分类号： G02B21/082 , G01N21/6458 , G02B23/2469 , G02B23/26
摘要： A non-linear fluorescence microscope or endoscope includes: (a) a source of coherent light suitable to initiate non-linear fluorescence in a sample of interest located at a sample region; (b) a first light conductor positioned to receive at its terminal light from the light source and direct the light to a coupler; (c) a second light conductor located to receive light introduced to the coupler from the first conductor and direct the light to the sample via a sample end of the second conductor, the sample end also located to receive fluoresced light from the sample such that the second conductor may direct the fluoresced light to the coupler; and (d) a third light conductor located to direct fluoresced light from the coupler to a light detection device via a terminal of the third light conductor.
摘要翻译：非线性荧光显微镜或内窥镜包括：（a）适合于在位于样品区域的感兴趣样品中引发非线性荧光的相干光源; （b）第一光导体，定位成在其端子处接收来自光源的光并将光引导到耦合器; （c）第二光导体，其被定位成接收从第一导体引入耦合器的光，并经由第二导体的样品端将光引导到样品，样品端还定位成接收来自样品的荧光，使得第二导体可以将荧光的光引导到耦合器; 以及（d）第三光导体，其被定位成经由所述第三光导体的端子将来自所述耦合器的荧光的光引导到光检测装置。

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