公开(公告)号：US20120003712A1

公开(公告)日：2012-01-05

申请号：US13255199

申请日：2010-03-18

申请人： Dae Hae Song ,  Jae Hee Shin ,  Jae Min Lee ,  Young Kyung Park ,  Se Chang Kwon ,  Gwan Sun Lee

发明人： Dae Hae Song ,  Jae Hee Shin ,  Jae Min Lee ,  Young Kyung Park ,  Se Chang Kwon ,  Gwan Sun Lee

IPC分类号： C12N9/00 ,  C07K14/505 ,  C07K14/52 ,  C07K14/53 ,  C07K14/575 ,  C07K14/585 ,  C07K14/59 ,  C07K14/595 ,  C07K14/605 ,  C07K14/61 ,  C07K14/62 ,  C07K14/655 ,  C07K7/16 ,  C07K7/04 ,  C07K9/00 ,  C07K14/475

CPC分类号： C07K1/1077 ,  A61K47/60 ,  C07K14/575 ,  C07K14/605 ,  C07K14/62

摘要： The present invention provides a method for preparing a site-specific physiologically active polypeptide conjugate in a high yield by treating a physiologically active polypeptide with a non-peptidyl polymer in the presence of an alcohol at a specific pH, which can be desirably employed in the development of long acting formulations of various peptide drugs having high in-vivo activity and markedly prolonged in-blood half-life.

摘要翻译： 本发明提供了一种通过在特定pH下在醇的存在下用非肽基聚合物处理生理活性多肽而以高产率制备位点特异性生理活性多肽缀合物的方法，其可以理想地用于 开发具有高体内活性和明显延长的血液半衰期的各种肽药物的长效制剂。

公开(公告)号：US08895281B2

公开(公告)日：2014-11-25

申请号：US13255199

申请日：2010-03-18

申请人： Dae Hae Song ,  Jae Hee Shin ,  Jae Min Lee ,  Young Kyung Park ,  Se Chang Kwon ,  Gwan Sun Lee

发明人： Dae Hae Song ,  Jae Hee Shin ,  Jae Min Lee ,  Young Kyung Park ,  Se Chang Kwon ,  Gwan Sun Lee

IPC分类号： C12N9/00 ,  C07K7/04 ,  C07K14/00 ,  C07K1/107 ,  A61K47/48 ,  C07K14/575 ,  C07K14/605 ,  C07K14/62

CPC分类号： C07K1/1077 ,  A61K47/60 ,  C07K14/575 ,  C07K14/605 ,  C07K14/62

摘要： The present invention provides a method for preparing a site-specific physiologically active polypeptide conjugate in a high yield by treating a physiologically active polypeptide with a non-peptidyl polymer in the presence of an alcohol at a specific pH, which can be desirably employed in the development of long acting formulations of various peptide drugs having high in-vivo activity and markedly prolonged in-blood half-life.

摘要翻译： 本发明提供了一种通过在特定pH下在醇的存在下用非肽基聚合物处理生理活性多肽而以高产率制备位点特异性生理活性多肽缀合物的方法，其可以理想地用于 开发具有高体内活性和明显延长的血液半衰期的各种肽药物的长效制剂。

公开(公告)号：US20110200623A1

公开(公告)日：2011-08-18

申请号：US13055406

申请日：2009-07-23

申请人： Dae Hae Song ,  Jae Hee Shin ,  Mi Ji Lee ,  Sung Hee Hong ,  Se Chang Kwon ,  Gwan Sun Lee

发明人： Dae Hae Song ,  Jae Hee Shin ,  Mi Ji Lee ,  Sung Hee Hong ,  Se Chang Kwon ,  Gwan Sun Lee

IPC分类号： A61K39/395 ,  C07K17/00 ,  C12N9/96 ,  A61K39/00 ,  A61P31/00 ,  A61P5/00 ,  A61P5/50

CPC分类号： A61K47/48715 ,  A61K47/60 ,  A61K47/6811 ,  A61K47/6889 ,  C07K14/59 ,  C07K19/00 ,  C07K2319/31

摘要： Disclosed is a protein complex, comprising a physiologically active polypeptide, a dimeric protein and a non-peptidyl polymer having three functional ends (3-arm), with the linkage of both the physiologically active polypeptide and the dimeric protein to the 3-arm non-peptidyl polymer via respective covalent bonds. The protein complex guarantees the long acting activity and biostability of a physiologically active polypeptide. Having the ability to maintain the bioactivity of physiologically active polypeptides or peptides highly and to significantly improve the serum half life of the polypeptides or peptides, the protein complex can be applied to the development of sustained release formulations of various physiologically active polypeptide drugs. Also, it utilizes raw materials including the physiologically active polypeptides without significant loss, thereby increasing the production yield. Further, it can be easily purified.

摘要翻译： 公开了一种蛋白质复合物，其包含生理活性多肽，二聚体蛋白质和具有三个功能性末端（3-臂）的非肽基聚合物，其具有生理活性多肽和二聚体蛋白质与3-臂非 - - 肽基聚合物。 蛋白质复合物保证生理活性多肽的长效和生物稳定性。 具有维持生理活性多肽或肽的生物活性以及显着改善多肽或肽的血清半衰期的能力，蛋白质复合物可用于开发各种生理活性多肽药物的持续释放制剂。 此外，它利用包括生理活性多肽的原料，而不会显着损失，从而提高产量。 此外，它可以容易地纯化。

公开(公告)号：US09636420B2

公开(公告)日：2017-05-02

申请号：US13055406

申请日：2009-07-23

申请人： Dae Hae Song ,  Jae Hee Shin ,  Mi Ji Lee ,  Sung Hee Hong ,  Se Chang Kwon ,  Gwan Sun Lee

发明人： Dae Hae Song ,  Jae Hee Shin ,  Mi Ji Lee ,  Sung Hee Hong ,  Se Chang Kwon ,  Gwan Sun Lee

IPC分类号： A61K47/48 ,  C07K14/62 ,  C07K14/505 ,  C07K14/52 ,  C07K14/56 ,  C07K14/61 ,  C07K14/475 ,  C07K19/00 ,  A61K38/28 ,  C07K14/59

CPC分类号： A61K47/48715 ,  A61K47/60 ,  A61K47/6811 ,  A61K47/6889 ,  C07K14/59 ,  C07K19/00 ,  C07K2319/31

摘要： Disclosed is a protein complex, comprising a physiologically active polypeptide, a dimeric protein and a non-peptidyl polymer having three functional ends (3-arm), with the linkage of both the physiologically active polypeptide and the dimeric protein to the 3-arm non-peptidyl polymer via respective covalent bonds. The protein complex guarantees the long acting activity and biostability of a physiologically active polypeptide. Having the ability to maintain the bioactivity of physiologically active polypeptides or peptides highly and to significantly improve the serum half life of the polypeptides or peptides, the protein complex can be applied to the development of sustained release formulations of various physiologically active polypeptide drugs. Also, it utilizes raw materials including the physiologically active polypeptides without significant loss, thereby increasing the production yield. Further, it can be easily purified.

公开(公告)号：US09422349B2

公开(公告)日：2016-08-23

申请号：US12669372

申请日：2008-07-16

申请人： Sung Youb Jung ,  Chang Ki Lim ,  Dae Hae Song ,  Sung Min Bae ,  Young Hoon Kim ,  Se Chang Kwon ,  Gwan Sun Lee

发明人： Sung Youb Jung ,  Chang Ki Lim ,  Dae Hae Song ,  Sung Min Bae ,  Young Hoon Kim ,  Se Chang Kwon ,  Gwan Sun Lee

IPC分类号： C07K14/605 ,  A61K38/26 ,  C07K14/46 ,  C07K14/575

CPC分类号： C07K14/46 ,  A61K38/26 ,  C07K14/57563 ,  C07K14/605

摘要： The present invention relates to an N-terminal amino acid-modified insulinotropic peptide having a high activity, and to a pharmaceutical composition comprising the same. The insulinotropic peptide derivatives according to the present invention exhibit therapeutic effects, which are not observed in native and other insulinotropic peptide analogs. Therefore, the insulinotropic peptide derivatives and the pharmaceutical composition comprising the same according to the present invention can be effectively provided for the treatment of the diseases.

摘要翻译： 本发明涉及具有高活性的N-末端氨基酸修饰的促胰岛素肽以及包含其的药物组合物。 根据本发明的促胰岛素肽衍生物显示出在天然和其他促胰岛素肽类似物中未观察到的治疗效果。 因此，可以有效地提供促胰岛素肽衍生物和包含其的本发明的药物组合物用于治疗疾病。

公开(公告)号：US08124094B2

公开(公告)日：2012-02-28

申请号：US11910962

申请日：2005-04-28

申请人： Young Min Kim ,  Sung Min Bae ,  Dae Jin Kim ,  Dae Hae Song ,  Chang Ki Lim ,  Se Chang Kwon ,  Gwan Sun Lee

发明人： Young Min Kim ,  Sung Min Bae ,  Dae Jin Kim ,  Dae Hae Song ,  Chang Ki Lim ,  Se Chang Kwon ,  Gwan Sun Lee

IPC分类号： A61K39/00

CPC分类号： A61K47/6835 ,  A61K47/6811 ,  A61K47/6813 ,  C07K2317/52 ,  C07K2319/30

摘要： Disclosed are an Fc fragment modified by a non-peptide polymer, a pharmaceutical composition comprising the Fc fragment modified by the non-peptide polymer as a carrier, a complex of the Fc fragment and a drug via a linker and a pharmaceutical composition comprising such a complex. The Fc fragment modified by a non-peptide peptide according to the present invention lacks immunogenicity and effector functions. Due to these properties, the Fc fragment maintains the in vivo activity of a drug conjugated thereto in high levels, remarkably increases the serum half-life of the drug, and remarkably reduces the risk of inducing immune responses.

摘要翻译： 公开了由非肽聚合物修饰的Fc片段，包含由作为载体的非肽聚合物修饰的Fc片段的药物组合物，Fc片段的复合物和通过接头的药物和包含这样的 复杂。 由本发明的非肽肽修饰的Fc片段缺乏免疫原性和效应子功能。 由于这些性质，Fc片段以高水平维持与其结合的药物的体内活性，显着增加了药物的血清半衰期，并显着降低了诱导免疫应答的风险。

公开(公告)号：US20100330108A1

公开(公告)日：2010-12-30

申请号：US12744660

申请日：2008-11-28

申请人： Dae Hae Song ,  Min Young Kim ,  Young Jin Park ,  Eun Hee Kang ,  Sung Youb Jung ,  Se Chang Kwon ,  Gwan Sun Lee

发明人： Dae Hae Song ,  Min Young Kim ,  Young Jin Park ,  Eun Hee Kang ,  Sung Youb Jung ,  Se Chang Kwon ,  Gwan Sun Lee

IPC分类号： A61K39/00 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  C07K16/00

CPC分类号： C07K19/00 ,  A61K47/6811 ,  A61K47/6813 ,  A61K47/6835 ,  C07K2319/30

摘要： The present invention relates to a composition for treating obesity-related diseases comprising an insulinotropic peptide conjugate, more particularly, to a composition for treating obesity-related diseases comprising a conjugate prepared by covalently linking the insulinotropic peptide with a carrier substance via a non-peptidyl linker, and a method for treating obesity-related diseases by using the same. In particular, the composition for treating obesity-related diseases according to the present invention remarkably improves the efficacy of suppressing food intake and its duration to reduce body weight and body fat, thereby being useful for the treatment of obesity-related diseases.

摘要翻译： 本发明涉及一种用于治疗肥胖相关疾病的组合物，其包括促胰岛素肽缀合物，更具体地，涉及用于治疗肥胖相关疾病的组合物，其包含通过非肽基共价连接促胰岛素肽与载体物质而制备的缀合物 接头，以及通过使用它们来治疗肥胖相关疾病的方法。 特别地，本发明的治疗肥胖相关疾病的组合物显着地提高了抑制食物摄取的效果及其减轻体重和体脂的持续时间，从而可用于治疗肥胖相关疾病。

公开(公告)号：US20100204451A1

公开(公告)日：2010-08-12

申请号：US12669372

申请日：2008-07-16

申请人： Sung Youb Jung ,  Chang Ki Lim ,  Dae Hae Song ,  Sung Min Bae ,  Young Hoon Kim ,  Se Chang Kwon ,  Gwan Sun Lee

发明人： Sung Youb Jung ,  Chang Ki Lim ,  Dae Hae Song ,  Sung Min Bae ,  Young Hoon Kim ,  Se Chang Kwon ,  Gwan Sun Lee

IPC分类号： C07K14/00

CPC分类号： C07K14/46 ,  A61K38/26 ,  C07K14/57563 ,  C07K14/605

摘要： The present invention relates to an N-terminal amino acid-modified insulinotropic peptide having a high activity, and to a pharmaceutical composition comprising the same. The insulinotropic peptide derivatives according to the present invention exhibit therapeutic effects, which are not observed in native and other insulinotropic peptide analogs. Therefore, the insulinotropic peptide derivatives and the pharmaceutical composition comprising the same according to the present invention can be effectively provided for the treatment of the diseases.

摘要翻译： 本发明涉及具有高活性的N-末端氨基酸修饰的促胰岛素肽以及包含其的药物组合物。 根据本发明的促胰岛素肽衍生物显示出在天然和其他促胰岛素肽类似物中未观察到的治疗效果。 因此，可以有效地提供促胰岛素肽衍生物和包含其的本发明的药物组合物用于治疗疾病。

公开(公告)号：US20090238838A1

公开(公告)日：2009-09-24

申请号：US11947697

申请日：2007-11-29

申请人： Dae Jin Kim ,  Sung Min Bae ,  Chang Ki Lim ,  Se Chang Kwon ,  Gwan Sun Lee ,  Dae Hae Song ,  Young Hoon Kim

发明人： Dae Jin Kim ,  Sung Min Bae ,  Chang Ki Lim ,  Se Chang Kwon ,  Gwan Sun Lee ,  Dae Hae Song ,  Young Hoon Kim

IPC分类号： A61K39/00 ,  C07K16/00 ,  A61P3/10 ,  A61P3/04 ,  A61P9/00

CPC分类号： C07K19/00 ,  A61K47/6811 ,  A61K47/6813 ,  A61K47/6835 ,  C07K2319/30

摘要： The present invention relates to an insulinotropic peptide conjugate having improved in-vivo duration of efficacy and stability, comprising an insulinotropic peptide, a non-peptide polymer and a carrier substance, which are covalently linked to each other, and a use of the same. The insulinotropic peptide conjugate of the present invention has the in-vivo activity which is maintained relatively high, and has remarkably increased blood half-life, and thus it can be desirably employed in the development of long acting formulations of various peptide drugs.

摘要翻译： 本发明涉及具有改善的功效和稳定性的体内持续时间的促胰岛素肽缀合物，其包含彼此共价连接的促胰岛素肽，非肽聚合物和载体物质及其用途。 本发明的促胰岛素肽缀合物具有保持较高的体内活性，并且血液半衰期显着增加，因此可以理想地用于开发各种肽药物的长效制剂。

公开(公告)号：US08476230B2

公开(公告)日：2013-07-02

申请号：US12523050

申请日：2008-01-04

申请人： Dae Hae Song ,  Chang Ki Lim ,  Tae Hun Song ,  Young Hoon Kim ,  Se Chang Kwon ,  Gwan Sun Lee ,  Sung Youb Jung ,  In Young Choi

发明人： Dae Hae Song ,  Chang Ki Lim ,  Tae Hun Song ,  Young Hoon Kim ,  Se Chang Kwon ,  Gwan Sun Lee ,  Sung Youb Jung ,  In Young Choi

IPC分类号： A61K38/00 ,  A61K39/395 ,  A61P5/50

CPC分类号： C07K14/57563 ,  A61K38/00 ,  A61K47/6835 ,  C07K14/605

摘要： The present invention relates to an insulinotropic peptide conjugate having improved in-vivo duration of efficacy and stability, comprising an insulinotropic peptide, a non-peptide polymer and an immunoglobulin Fc region, which are covalently linked to each other, and a use of the same. The insulinotropic peptide conjugate of the present invention has the in-vivo activity which is maintained relatively high, and has remarkably increased blood half-life, and thus it can be desirably employed in the development of long acting formulations of various peptide drugs.

摘要翻译： 本发明涉及具有改善的功效和稳定性的体内持续时间的促胰岛素肽缀合物，其包含彼此共价连接的促胰岛素肽，非肽聚合物和免疫球蛋白Fc区，并且使用它们 。 本发明的促胰岛素肽缀合物具有保持较高的体内活性，并且血液半衰期显着增加，因此可以理想地用于开发各种肽药物的长效制剂。