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1. 发明专利

IL215792D0 PRODRUGS BASED ON GEMCITABINE STRUCTURE AS WELL AS SYNTHETIC METHODS AND APPLICATIONS THEREOF 未知
公开(公告)号：IL215792D0
公开(公告)日：2012-01-31
申请号：IL21579211
申请日：2011-10-23
申请人： SANLUGEN PHARMATECH LTD
IPC分类号： C07H20060101
摘要： Prodrugs based on gemcitabine structure shown in formula (I) as well as their synthetic method and application are disclosed in the present invention, wherein the definitions for the groups of a, b, c, d, E, Z and V are described in the specification. By modifying the N 4 group, the solubility, the bioavailability and the organ specificity of the prodrugs are improved. Therefore, the fast metabolism problem is overcome for the produced prodrugs compounds. Intestinal toxicity induced by gemcitabine is decreased. Thereby, the prodrugs can be delivered by oral administration in clinics and further improve their anti-tumor, anti-cancer, anti-infection and diffusion preventing capability, and can also specifically act on liver or colon. The synthetic method is simple and adapted to industrial production.

2. 发明专利

CA2759474A1 PRODRUGS BASED ON GEMCITABINE STRUCTURE AND SYNTHETIC METHODS AND APPLICATIONS THEREOF 未知
公开(公告)号：CA2759474A1
公开(公告)日：2010-10-28
申请号：CA2759474
申请日：2010-03-25
申请人： SANLUGEN PHARMATECH LTD
发明人： XUE XIAOXIA , LI GANG , SUN CHANGJUN , LI WENBAO
IPC分类号： C07H19/073 , A61K31/7068 , A61P35/00
摘要： Prodrugs based on gemcitabine structure shown as formula (I) as well as their synthetic method and application are disclosed, wherein the definitions for the groups of a, b, c, d, E, Z and V are described in the specification. By modifying the N4 group, the solubility, the bioavailability and the organ specificity of the prodrugs are improved. Therefore, the fast metabolism problem is solved and intestinal toxicity induced by gemcitabine is decreased. As a result, the prodrugs can be delivered by oral administration and further improve their antagonistic capacity in respect of tumors, cancer, infection and diffusion, and can also specifically act on liver or colon. The synthetic method is simple and adapted to industrial production.

3. 发明申请

US20120088908A1 Prodrugs Based on Gemcitabine Structure and Synthetic Methods and Applications Thereof 失效
标题翻译：基于吉西他滨结构的前体药物及其合成方法及应用
公开(公告)号：US20120088908A1
公开(公告)日：2012-04-12
申请号：US13265335
申请日：2010-03-25
申请人： Xiaoxia Xue , Gang Li , Changjun Sun , Wenbao Li
发明人： Xiaoxia Xue , Gang Li , Changjun Sun , Wenbao Li
IPC分类号： C07H19/00
CPC分类号： C07H19/06 , A61K31/7068
摘要： Prodrugs based on gemcitabine structure shown in formula (I) as well as their synthetic method and application are disclosed in the present invention, wherein the definitions for the groups of a, b, c, d, E, Z and V are described in the specification. By modifying the N4 group, the solubility, the bioavailability and the organ specificity of the prodrugs are improved. Therefore, the fast metabolism problem is overcome for the produced prodrugs compounds. Intestinal toxicity induced by gemcitabine is decreased. Thereby, the prodrugs can be delivered by oral administration in clinics and further improve their anti-tumor, anti-cancer, anti-infection and diffusion preventing capability, and can also specifically act on liver or colon. The synthetic method is simple and adapted to industrial production.
摘要翻译：基于式（I）所示的吉西他滨结构的前药以及它们的合成方法和应用在本发明中公开，其中a，b，c，d，E，Z和V组的定义描述于规范。通过改变N4基团，前药的溶解度，生物利用度和器官特异性得到改善。因此，所制备的前药化合物克服了快速代谢问题。吉西他滨引起的肠毒性降低。因此，前药可以通过口服给药在临床中进一步提高其抗肿瘤，抗癌，抗感染和扩散防止能力，并且还可以特异性地作用于肝脏或结肠。合成方法简单，适应工业生产。

4. 发明授权

US08653048B2 Prodrugs based on gemcitabine structure and synthetic methods and applications thereof 失效
标题翻译：基于吉西他滨结构的前体药物及其合成方法及应用
公开(公告)号：US08653048B2
公开(公告)日：2014-02-18
申请号：US13265335
申请日：2010-03-25
申请人： Xiaoxia Xue , Gang Li , Changjun Sun , Wenbao Li
发明人： Xiaoxia Xue , Gang Li , Changjun Sun , Wenbao Li
IPC分类号： A61K31/70 , C07H19/00
CPC分类号： C07H19/06 , A61K31/7068
摘要： Prodrugs based on gemcitabine structure shown in formula (I) as well as their synthetic method and application are disclosed in the present invention, wherein the definitions for the groups of a, b, c, d, E, Z and V are described in the specification. By modifying the N4 group, the solubility, the bioavailability and the organ specificity of the prodrugs are improved. Therefore, the fast metabolism problem is overcome for the produced prodrugs compounds. Intestinal toxicity induced by gemcitabine is decreased. Thereby, the prodrugs can be delivered by oral administration in clinics and further improve their anti-tumor, anti-cancer, anti-infection and diffusion preventing capability, and can also specifically act on liver or colon. The synthetic method is simple and adapted to industrial production.
摘要翻译：基于式（I）所示的吉西他滨结构的前药以及它们的合成方法和应用在本发明中公开，其中a，b，c，d，E，Z和V组的定义描述于规范。通过改变N4基团，前药的溶解度，生物利用度和器官特异性得到改善。因此，所制备的前药化合物克服了快速代谢问题。吉西他滨引起的肠毒性降低。因此，前药可以通过口服给药在临床中进一步提高其抗肿瘤，抗癌，抗感染和扩散防止能力，并且还可以特异性地作用于肝脏或结肠。合成方法简单，适应工业生产。

5. 发明公开

EP2423215A4 PRODRUGS BASED ON GEMCITABINE STRUCTURE AS WELL AS SYNTHETIC METHOD AND APPLICATION THEREOF 审中-公开
标题翻译： ON GEMCITABINSTRUKTUR基于前体药物和合成工艺及其应用
公开(公告)号：EP2423215A4
公开(公告)日：2013-05-22
申请号：EP10766577
申请日：2010-03-25
申请人： SANLUGEN PHARMATECH LTD
发明人： XUE XIAOXIA , LI GANG , SUN CHANGJUN , LI WENBAO
IPC分类号： C07H19/073 , A61K31/7068 , A61P35/00
CPC分类号： C07H19/06 , A61K31/7068

6. 发明公开

EP2423215A1 PRODRUGS BASED ON GEMCITABINE STRUCTURE AS WELL AS SYNTHETIC METHOD AND APPLICATION THEREOF 审中-公开
标题翻译： AUF GEMCITABINSTRUKTUR BASIERENDE PRODRUGS SOWIE SYNTHETISCHES VERFAHREN UND ANWENDUNG
公开(公告)号：EP2423215A1
公开(公告)日：2012-02-29
申请号：EP10766577.0
申请日：2010-03-25
申请人： Sanlugen Pharmatech Ltd.
发明人： XUE, Xiaoxia , LI, Gang , SUN, Changjun , LI, Wenbao
IPC分类号： C07H19/073 , A61K31/7068 , A61P35/00
CPC分类号： C07H19/06 , A61K31/7068
摘要： Prodrugs based on gemcitabine structure shown in formula (I) as well as their synthetic method and application are disclosed in the present invention, wherein the definitions for the groups of a, b, c, d, E, Z and V are described in the specification. By modifying the N 4 group, the solubility, the bioavailability and the organ specificity of the prodrugs are improved. Therefore, the fast metabolism problem is overcome for the produced prodrugs compounds. Intestinal toxicity induced by gemcitabine is decreased. Thereby, the prodrugs can be delivered by oral administration in clinics and further improve their anti-tumor, anti-cancer, anti-infection and diffusion preventing capability, and can also specifically act on liver or colon. The synthetic method is simple and adapted to industrial production.
摘要翻译：在本发明中公开了基于吉西他滨结构的前药，以及它们的合成方法和应用，其中a，b，c，d，E，Z和V的基团的定义描述于规范。通过改变N 4基团，前药的溶解度，生物利用度和器官特异性得到改善。因此，所制备的前药化合物克服了快速代谢问题。吉西他滨引起的肠毒性降低。因此，前药可以通过口服给药在临床中进一步提高其抗肿瘤，抗癌，抗感染和扩散防止能力，并且还可以特异性地作用于肝脏或结肠。合成方法简单，适应工业生产。

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