公开(公告)号：US20120107236A1

公开(公告)日：2012-05-03

申请号：US13243225

申请日：2011-09-23

申请人： MEI-HUI WANG ,  Wuu-Jyh Lin ,  Hung-Man Yu ,  Chuan-Yi Chien ,  Ping-Yen Wang

发明人： MEI-HUI WANG ,  Wuu-Jyh Lin ,  Hung-Man Yu ,  Chuan-Yi Chien ,  Ping-Yen Wang

IPC分类号： A61K103/20 ,  C07F5/00 ,  A61P43/00

CPC分类号： A61K51/0491 ,  A61K51/0406 ,  A61K51/0497 ,  A61K51/065

摘要： The present invention is related to a pharmaceutical composition for a liver-receptor imaging injection, the pharmaceutical composition including a bi-functional compound which has a ASGPR specificity, wherein the bi-functional compound includes a backbone of alpha-amino acid (or the derivatives thereof) and a poly-galactosamine chain (or a poly-lactose chain) connected to the alpha-amino acid. Thereby, the pharmaceutical composition can quantify potential of liver storage ability and evaluate severity of the course of liver disease. A liver-receptor imaging injection using the same and the one-step dispensing method thereof are also provided to improve defects of iodine-labeled and overcome disadvantages of the reduced labeling-yield and the instability after autoclave sterilization.

摘要翻译： 本发明涉及一种肝 - 受体成像注射用药物组合物，该药物组合物包含具有ASGPR特异性的双功能化合物，其中双官能化合物包括α-氨基酸（或其衍生物 ）和与α-氨基酸连接的聚半乳糖胺链（或聚乳糖链）。 因此，药物组合物可以量化肝脏储存能力的潜力并评估肝脏疾病过程的严重程度。 还提供使用其的肝受体成像注射器及其一步式分配方法，以改善碘标记的缺陷，克服降压标记产率和高压灭菌后的不稳定性的缺点。

公开(公告)号：US09040017B2

公开(公告)日：2015-05-26

申请号：US13243225

申请日：2011-09-23

申请人： Mei-Hui Wang ,  Wuu-Jyh Lin ,  Hung-Man Yu ,  Chuan-Yi Chien ,  Ping-Yen Wang

发明人： Mei-Hui Wang ,  Wuu-Jyh Lin ,  Hung-Man Yu ,  Chuan-Yi Chien ,  Ping-Yen Wang

IPC分类号： A61K51/04 ,  A61K51/06

CPC分类号： A61K51/0491 ,  A61K51/0406 ,  A61K51/0497 ,  A61K51/065

摘要： The present invention is related to a pharmaceutical composition for a liver-receptor imaging injection, the pharmaceutical composition including a bi-functional compound which has a ASGPR specificity, wherein the bi-functional compound includes a backbone of alpha-amino acid (or the derivatives thereof) and a poly-galactosamine chain (or a poly-lactose chain) connected to the alpha-amino acid. Thereby, the pharmaceutical composition can quantify potential of liver storage ability and evaluate severity of the course of liver disease. A liver-receptor imaging injection using the same and the one-step dispensing method thereof are also provided to improve defects of iodine-labeled and overcome disadvantages of the reduced labeling-yield and the instability after autoclave sterilization.

摘要翻译： 本发明涉及一种肝 - 受体成像注射用药物组合物，该药物组合物包含具有ASGPR特异性的双功能化合物，其中双官能化合物包括α-氨基酸（或其衍生物 ）和与α-氨基酸连接的聚半乳糖胺链（或聚乳糖链）。 因此，药物组合物可以量化肝脏储存能力的潜力并评估肝脏疾病过程的严重程度。 还提供使用其的肝受体成像注射器及其一步式分配方法，以改善碘标记的缺陷，克服降压标记产率和高压灭菌后的不稳定性的缺点。

公开(公告)号：US20110097264A1

公开(公告)日：2011-04-28

申请号：US12779328

申请日：2010-05-13

申请人： Mei-Hui Wang ,  Wuu-Jyh Lin ,  Chuan-Yi Chien ,  Hung-Man Yu ,  Reiko Takasaka Lee ,  Yuan-Chuan Lee

发明人： Mei-Hui Wang ,  Wuu-Jyh Lin ,  Chuan-Yi Chien ,  Hung-Man Yu ,  Reiko Takasaka Lee ,  Yuan-Chuan Lee

IPC分类号： A61K51/08 ,  C07K5/083 ,  C07F5/00 ,  A61K51/04

CPC分类号： A61K51/0491 ,  A61K51/0497 ,  C07F13/005 ,  C07K1/13

摘要： A radiolabeling method using a multivalent glycoligand as hepatic receptor imaging agent is provided. The multivalent glycoligand-DTPA derivatives (In-111-DTPA-hexa lactoside and In-111-DTPA-tri-galactosamine glycoside) labeled with In-111 are used as hepatic receptor imaging agent. The effects of imaging of a hepatic receptor in different species are evaluated, the lowest specific radioactivity values of hepatic receptor imaging required in different species are discovered. Since the specificity of the human ASGPR closely resembles that of the mouse. This kind of radiolabelling method, agent and related study about specific radioactivity could be used in clinical trial in the future.

摘要翻译： 提供了一种使用多价糖配位体作为肝脏受体成像剂的放射性标记方法。 用In-111标记的多价甘油配体-DTPA衍生物（In-111-DTPA-hexa lactoside和In-111-DTPA-tri-galactosamine glycoside）用作肝脏受体显像剂。 对不同物种肝受体成像的影响进行了评估，发现了不同物种所需肝脏受体成像的最低比放射性值。 由于人类ASGPR的特异性与小鼠的特异性非常相似。 这种放射性标记方法，药剂和相关研究有关的放射性可以在今后的临床试验中使用。

公开(公告)号：US08435491B2

公开(公告)日：2013-05-07

申请号：US12779374

申请日：2010-05-13

申请人： Mei-Hui Wang ,  Wuu-Jyh Lin ,  Chuan-Yi Chien ,  Hung-Man Yu ,  Reiko Takasaka Lee ,  Yuan-Chuan Lee

发明人： Mei-Hui Wang ,  Wuu-Jyh Lin ,  Chuan-Yi Chien ,  Hung-Man Yu ,  Reiko Takasaka Lee ,  Yuan-Chuan Lee

IPC分类号： A61K51/00 ,  A61K38/14 ,  A61M36/14 ,  C07K9/00

CPC分类号： C07H15/04 ,  A61K51/0491 ,  A61K51/0497

摘要： A test indicator for quantifying remaining liver function is provided. A novel liver receptor imaging agent with liver targeting property is utilized to develop a method for quantifying remaining liver function to serve as test indicator for judging the liver failure outcome in clinic, particularly for judging the necessity of liver transplantation for patients with liver failure or liver disease. The radioactivity uptake of the test indicator was negatively correlated with the extent of liver reserve. The cutoff value of liver reserve for liver transplantation is also disclosed.

摘要翻译： 提供了用于量化剩余肝功能的测试指标。 利用具有肝靶向特性的新型肝脏受体显像剂，开发了一种量化剩余肝功能的方法，作为判断临床肝功能衰竭结果的检测指标，特别是用于判断肝衰竭或肝脏肝移植的必要性 疾病。 测试指标的放射性摄取与肝脏储备的程度呈负相关。 肝移植肝储备的临界值也被披露。

公开(公告)号：US20110097265A1

公开(公告)日：2011-04-28

申请号：US12779374

申请日：2010-05-13

申请人： Mei-Hui Wang ,  Wuu-Jyh Lin ,  Chuan-Yi Chien ,  Hung-Man Yu ,  Reiko Takasaka Lee ,  Yuan-Chuan Lee

发明人： Mei-Hui Wang ,  Wuu-Jyh Lin ,  Chuan-Yi Chien ,  Hung-Man Yu ,  Reiko Takasaka Lee ,  Yuan-Chuan Lee

IPC分类号： A61K49/14 ,  A61K49/10 ,  C07F5/00 ,  C07K9/00 ,  C07F13/00

CPC分类号： C07H15/04 ,  A61K51/0491 ,  A61K51/0497

摘要： A test indicator for quantifying remaining liver function is provided. A novel liver receptor imaging agent with liver targeting property is utilized to develop a method for quantifying remaining liver function to serve as test indicator for judging the liver failure outcome in clinic, particularly for judging the necessity of liver transplantation for patients with liver failure or liver disease. The radioactivity uptake of the test indicator was negatively correlated with the extent of liver reserve. The cutoff value of liver reserve for liver transplantation is also disclosed.

摘要翻译： 提供了用于量化剩余肝功能的测试指标。 利用具有肝靶向特性的新型肝脏受体显像剂，开发了一种量化剩余肝功能的方法，作为判断临床肝功能衰竭结果的检测指标，特别是用于判断肝衰竭或肝脏肝移植的必要性 疾病。 测试指标的放射性摄取与肝脏储备的程度呈负相关。 肝移植肝储备的临界值也被公开。