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1. 发明申请

US20060063914A1 Peptides having protected amines of untargeted sites, methods for production thereof and of specifically conjugated peg peptides using the same 有权
标题翻译：具有非靶向位点的保护胺的肽，其制备方法和使用其的特异性共轭栓肽
公开(公告)号：US20060063914A1
公开(公告)日：2006-03-23
申请号：US10542230
申请日：2003-01-18
申请人： Sang Lee , Kang Choon Lee , Dong Hee Na , Yu Seok Youn
发明人： Sang Lee , Kang Choon Lee , Dong Hee Na , Yu Seok Youn
IPC分类号： C07K14/585 , C07K14/475
CPC分类号： C07K1/1077 , C07K1/063 , C07K1/064
摘要： The present invention relates to synthetic peptides having selectively protected amines of untargeted sites and to methods for production thereof and for specifically conjugating PEG to targeted sites of the synthetic peptides using the same. The present invention provides a much higher yield of PEG conjugated peptides in which PEG is specifically combined to amines at targeted sites.
摘要翻译：本发明涉及具有非靶向位点的选择性保护的胺的合成肽及其生产方法，并且特异性地将PEG与其合成肽的靶位点缀合。本发明提供了高得多的PEG缀合肽的产量，其中PEG在靶位点特异性地结合到胺上。

2. 发明授权

US09321825B2 N-terminal modified PEG-TRAIL 有权
标题翻译： N-末端修饰的PEG-TRAIL
公开(公告)号：US09321825B2
公开(公告)日：2016-04-26
申请号：US12304121
申请日：2007-06-12
申请人： Kang Choon Lee , Su Young Chae , Yu Seok Youn , Won Bae Kim , Sung Kwon Lee
发明人： Kang Choon Lee , Su Young Chae , Yu Seok Youn , Won Bae Kim , Sung Kwon Lee
IPC分类号： C07K14/52 , C07K14/525 , A61K38/19 , A61K47/48 , C07K14/705
CPC分类号： A61K47/60 , A61K38/19 , A61K38/191 , B01D15/361 , C07K14/52 , C07K14/525 , C07K14/70575 , C07K2319/73 , G01N30/96
摘要： Disclosed herein are an N-terminal modified PEG-TRAIL conjugate and a preparation method and use thereof. The PEG-TAIL conjugate has pharmaceutical activity identical or similar to that of native TRAIL (TNF-related apoptosis-inducing ligand) with extended in vivo half-life and enhanced stability. Compared to native TRAIL, the PEG-TAIL conjugate exhibits high solubility and solution stability, with highly improved pharmacokinetic profiles. Thus, the PEG-TAIL conjugate may be very useful for preventing and treating proliferative diseases and autoimmune diseases.
摘要翻译：本文公开了N-末端修饰的PEG-TRAIL缀合物及其制备方法和用途。 PEG-TAIL缀合物具有与具有延长的体内半衰期和增强的稳定性的天然TRAIL（TNF-相关凋亡诱导配体）相同或相似的药物活性。与天然TRAIL相比，PEG-TAIL缀合物显示高溶解度和溶液稳定性，具有高度改善的药代动力学特征。因此，PEG-TAIL缀合物可能非常有用于预防和治疗增殖性疾病和自身免疫性疾病。

3. 发明申请

US20090060955A1 Drug delivery vehicle that mimics viral properties 有权
标题翻译：模仿病毒性质的药物递送载体
公开(公告)号：US20090060955A1
公开(公告)日：2009-03-05
申请号：US11897979
申请日：2007-08-31
申请人： You Han Bae , Eun Seong Lee , Dongin Kim , Yu Seok Youn , Kyung Taek Oh
发明人： You Han Bae , Eun Seong Lee , Dongin Kim , Yu Seok Youn , Kyung Taek Oh
IPC分类号： A61K9/00
CPC分类号： A61K9/1658 , A61K9/1641 , A61K9/167
摘要： A drug delivery vehicle for targeted delivery of a drug mimics viral properties of size, capsid-like protein capsule, cell-specific entry, toxin release, destruction of infected cells, and migration to neighboring cells. This vehicle, termed a virogel, contains a hydrophobic polymeric core, a hydrophilic inner shell, a hydrophilic outer shell, and a ligand. An illustrative drug-loaded virogel includes poly(L-histidine-co-phenylalanine) as the core, doxorubicin loaded in the core, polyethylene glycol as the inner shell, bovine serum albumin as the outer shell, and folic acid as the ligand.
摘要翻译：用于靶向递送药物的药物递送载体模拟大小的病毒性质，衣壳样蛋白质胶囊，细胞特异性进入，毒素释放，感染细胞的破坏以及迁移至相邻细胞。这种载体，称为virogel，含有疏水聚合物芯，亲水内壳，亲水外壳和配体。一种说明性的药物载体的virogel包括聚（L-组氨酸 - 共 - 苯基丙氨酸）为核心，负责核心的多柔比星，作为内壳的聚乙二醇，作为外壳的牛血清白蛋白，以及叶酸作为配体。

4. 发明授权

US08420598B2 Mono modified exendin with polyethylene glycol or its derivatives and uses thereof 有权
标题翻译：用聚乙二醇或其衍生物和单体修饰的毒蜥外泌肽及其用途
公开(公告)号：US08420598B2
公开(公告)日：2013-04-16
申请号：US12596010
申请日：2007-04-20
申请人： Kang Choon Lee , Chan Woong Park , Yu Seok Youn , Su Young Chae
发明人： Kang Choon Lee , Chan Woong Park , Yu Seok Youn , Su Young Chae
IPC分类号： A61K38/00 , C07K14/605
CPC分类号： C07K14/57563 , A61K38/00 , A61K47/60
摘要： Disclosed herein are exendin singly modified with polyethylene glycole or a derivative thereof, a method for the preparation of the same, and uses thereof. Exendin modified at lysine (27) with polyethylene glycol shows biological activity similar to that of natural exendin, but is improved in half life. In addition, the modification position and the number of PEG or its derivative are restricted so as to minimize the side effects caused by a variety of combinations of such factors. The exendin is useful in the prevention and treatment of diseases caused by the over-secretion of insulin, or diseases caused due to a decrease in plasma glucose level, the inhibition of gastric or intestinal motility, the promotion of satiety, or the inhibition of food intake, especially diabetes, obesity and irritable colon syndrome.
摘要翻译：本文公开了用聚乙二醇单体改性的聚乙二醇或其衍生物，其制备方法及其用途。在赖氨酸（27）与聚乙二醇修饰的毒蜥外泌物显示出与天然毒蜥外泌肽相似的生物活性，但半衰期有所改善。此外，PEG或其衍生物的修饰位置和数目受到限制，以使由这些因素的各种组合引起的副作用最小化。毒蜥外泌肽可用于预防和治疗由胰岛素过分分泌引起的疾病，或由于血浆葡萄糖水平降低引起的疾病，胃或肠蠕动的抑制，促进饱腹感或抑制食物摄入，特别是糖尿病，肥胖和肠易激综合征。

5. 发明授权

US08394391B2 Drug delivery vehicle that mimics viral properties 有权
公开(公告)号：US08394391B2
公开(公告)日：2013-03-12
申请号：US11897979
申请日：2007-08-31
申请人： You Han Bae , Eun Seong Lee , Dongin Kim , Yu Seok Youn , Kyung Taek Oh
发明人： You Han Bae , Eun Seong Lee , Dongin Kim , Yu Seok Youn , Kyung Taek Oh
IPC分类号： A61K9/00
CPC分类号： A61K9/1658 , A61K9/1641 , A61K9/167
摘要： A drug delivery vehicle for targeted delivery of a drug mimics viral properties of size, capsid-like protein capsule, cell-specific entry, toxin release, destruction of infected cells, and migration to neighboring cells. This vehicle, termed a virogel, contains a hydrophobic polymeric core, a hydrophilic inner shell, a hydrophilic outer shell, and a ligand. An illustrative drug-loaded virogel includes poly(L-histidine-co-phenylalanine) as the core, doxorubicin loaded in the core, polyethylene glycol as the inner shell, bovine serum albumin as the outer shell, and folic acid as the ligand.

6. 发明申请

US20090203599A1 N-TERMINAL MODIFIED PEG-TRAIL, METHOD FOR PREPARING AND USES THEREOF 有权
标题翻译： N-末端修饰的PEG-TRAIL，其制备方法和用途
公开(公告)号：US20090203599A1
公开(公告)日：2009-08-13
申请号：US12304121
申请日：2007-06-12
申请人： Kang Choon Lee , Su Young Chae , Yu Seok Youn , Won Bae Kim , Sung Kwon Lee
发明人： Kang Choon Lee , Su Young Chae , Yu Seok Youn , Won Bae Kim , Sung Kwon Lee
IPC分类号： A61K38/16 , C07K14/00 , C07K1/00
CPC分类号： A61K47/60 , A61K38/19 , A61K38/191 , B01D15/361 , C07K14/52 , C07K14/525 , C07K14/70575 , C07K2319/73 , G01N30/96
摘要： Disclosed herein are an N-terminal modified PEG-TRAIL conjugate and a preparation method and use thereof. The PEG-TAIL conjugate has pharmaceutical activity identical or similar to that of native TRAIL (TNF-related apoptosis-inducing ligand) with extended in vivo half-life and enhanced stability. Compared to native TRAIL, the PEG-TAIL conjugate exhibits high solubility and solution stability, with highly improved pharmacokinetic profiles. Thus, the PEG-TAIL conjugate may be very useful for preventing and treating proliferative diseases and autoimmune diseases.
摘要翻译：本文公开了N-末端修饰的PEG-TRAIL缀合物及其制备方法和用途。 PEG-TAIL缀合物具有与具有延长的体内半衰期和增强的稳定性的天然TRAIL（TNF-相关凋亡诱导配体）相同或相似的药物活性。与天然TRAIL相比，PEG-TAIL缀合物显示高溶解度和溶液稳定性，具有高度改善的药代动力学特征。因此，PEG-TAIL缀合物可能非常有用于预防和治疗增殖性疾病和自身免疫性疾病。

7. 发明申请

US20100137558A1 MONO MODIFIED EXENDIN WITH POLYETHYLENE GLYCOL OR ITS DERIVATIVES AND USES THEREOF 有权
标题翻译：聚乙烯甘油或其衍生物的单体改性维生素及其用途
公开(公告)号：US20100137558A1
公开(公告)日：2010-06-03
申请号：US12596010
申请日：2007-04-20
申请人： Kang Choon Lee , Chan Woong Park , Yu Seok Youn , Su Young Chae
发明人： Kang Choon Lee , Chan Woong Park , Yu Seok Youn , Su Young Chae
IPC分类号： C07K14/605
CPC分类号： C07K14/57563 , A61K38/00 , A61K47/60
摘要： Disclosed herein are exendin singly modified with polyethylene glycole or a derivative thereof, a method for the preparation of the same, and uses thereof. Exendin modified at lysine (27) with polyethylene glycol shows biological activity similar to that of natural exendin, but is improved in half life. In addition, the modification position and the number of PEG or its derivative are restricted so as to minimize the side effects caused by a variety of combinations of such factors. The exendin is useful in the prevention and treatment of diseases caused by the over-secretion of insulin, or diseases caused due to a decrease in plasma glucose level, the inhibition of gastric or intestinal motility, the promotion of satiety, or the inhibition of food intake, especially diabetes, obesity and irritable colon syndrome.
摘要翻译：本文公开了用聚乙二醇单体改性的聚乙二醇或其衍生物，其制备方法及其用途。在赖氨酸（27）与聚乙二醇修饰的毒蜥外泌物显示出与天然毒蜥外泌肽相似的生物活性，但半衰期有所改善。此外，PEG或其衍生物的修饰位置和数目受到限制，以使由这些因素的各种组合引起的副作用最小化。毒蜥外泌肽可用于预防和治疗由胰岛素过分分泌引起的疾病，或由于血浆葡萄糖水平降低引起的疾病，胃或肠蠕动的抑制，促进饱腹感或抑制食物摄入，特别是糖尿病，肥胖和肠易激综合征。

8. 发明授权

US07662915B2 Peptides having protected amines of untargeted sites, methods for production thereof and of specifically conjugated PEG peptides using the same 有权
标题翻译：具有非靶向位点的保护胺的肽，其制备方法和使用其的特异性缀合的PEG肽
公开(公告)号：US07662915B2
公开(公告)日：2010-02-16
申请号：US10542230
申请日：2003-01-18
申请人： Sang Deuk Lee , Kang Choon Lee , Dong Hee Na , Yu Seok Youn
发明人： Sang Deuk Lee , Kang Choon Lee , Dong Hee Na , Yu Seok Youn
IPC分类号： C07K1/06 , C07K1/107 , C07K1/04 , C07K1/00
CPC分类号： C07K1/1077 , C07K1/063 , C07K1/064
摘要： The present invention relates to synthetic peptides having selectively protected amines of untargeted sites and to methods for production thereof and for specifically conjugating PEG to targeted sites of the synthetic peptides using the same. The present invention provides a much higher yield of PEG conjugated peptides in which PEG is specifically combined to amines at targeted sites.
摘要翻译：本发明涉及具有非靶向位点的选择性保护的胺的合成肽及其生产方法，并且特异性地将PEG与其合成肽的靶位点缀合。本发明提供了高得多的PEG缀合肽的产量，其中PEG在靶位点特异性地结合到胺上。

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