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公开(公告)号：US11357861B2
公开(公告)日：2022-06-14
申请号：US16647115
申请日：2018-10-01
发明人： Su Yeon Park , Ji Young Song , Eun Jung Kim , Jong Min Lee , Jong-Soo Lee , Dae Jin Kim
IPC分类号： A61K47/56 , A61K47/54 , C07K14/62 , C08G65/325
摘要： Provided are a protein conjugate in which a physiologically active polypeptide is linked to a biocompatible material via a non-peptidyl polymer-coupled fatty acid derivative compound serving as a linker, exhibiting an increased duration of physiological activity compared to natural forms and a preparation method therefor. Since an increase in serum half-life of the physiologically active polypeptide of the protein conjugate, in which the biocompatible material, the non-peptidyl polymer-coupled fatty acid derivative compound, and the physiologically active polypeptide are linked, is proved, the protein conjugate may be widely used in the field of protein drugs.
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公开(公告)号：US10894089B2
公开(公告)日：2021-01-19
申请号：US15551489
申请日：2016-02-17
发明人： Yong Ho Heo , Jong Soo Lee , Sung Hee Park , Dae Jin Kim , Sung Youb Jung , Se Chang Kwon
IPC分类号： A61K38/28 , A61K47/68 , C07K14/62 , A61K47/50 , A61K47/60 , A61P3/10 , C12N15/67 , A61K38/00
摘要： The present invention relates to insulin and/or an insulin analogue conjugate, and a use thereof, wherein the insulin and/or insulin analogue have improved in vivo durability and stability by linking the same with an Fc region of immunoglobulin. The insulin and/or an insulin analogue conjugate of the present invention show an in vivo activity similar to that of insulin. In addition, the insulin and/or insulin analogue conjugate of the present invention are long-acting formulations of insulin and/or the analogue thereof, in which serum half-life is remarkably increased, and therefore, the present invention provides remarkable insulin and/or an insulin analogue conjugate, which do not induce hypoglycemia, a drawback of insulin treatment.
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公开(公告)号：US10550168B2
公开(公告)日：2020-02-04
申请号：US15960205
申请日：2018-04-23
发明人： Jin Sun Kim , Dae Jin Kim , Sang Hyun Lee , Sung Youb Jung , Se Chang Kwon
IPC分类号： A61K38/22 , A61K38/26 , C07K14/575 , C07K14/605 , C07K16/00 , C07K16/30 , A61K47/64
摘要： Disclosed are a composition for preventing or treating diabetes, disbesity or diabetic complications, containing an oxyntomodulin analog as an active ingredient and a method for treating diabetes, diabesity or diabetic complications, including administering a pharmaceutically effective amount of an oxyntomodulin analog to a subject. The oxyntomodulin analog shows a greater activity to activate a GLP-1 receptor and a glucagon receptor, than native oxyntomodulin. The oxyntomodulin analog induces an expansion of beta-cells and increases insulin secretion, thereby reducing blood glucose levels that were increased due to a high-calorie and high-fat diet. The oxyntomodulin analog induces decreases in a body weight and appetite to improve insulin sensitivity and is useful in maintaining normal blood glucose levels.
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公开(公告)号：US10441665B2
公开(公告)日：2019-10-15
申请号：US15714556
申请日：2017-09-25
发明人： Hyun Uk Kim , Hyung Kyu Lim , Sung Hee Hong , Dae Jin Kim , Sung Min Bae , Se Chang Kwon
IPC分类号： A61K39/00 , A61K38/26 , C07K16/00 , C12P21/08 , A61K47/68 , C07K16/42 , C07K16/28 , C07K16/06 , A61K9/08 , C07K14/575 , C07K14/605 , A61K47/26 , A61K39/395 , C07K19/00 , G01N33/50
摘要： Provided are a liquid formulation of long-acting insulinotropic peptide conjugate, containing a pharmaceutically effective amount of long-acting insulinotropic peptide conjugate consisting of a physiologically active peptide, insulinotropic peptide, and an immunoglobulin Fc region; and an albumin-free stabilizer, wherein the stabilizer comprises a buffer, a sugar alcohol, and a non-ionic surfactant, and a method for preparing the formulation. For the purpose of preventing microbial contamination, a preservative may be added. The liquid formulation of the present invention is free of human serum albumin and other potentially hazardous factors to body, having no risk of viral contamination, and thus can provide excellent storage stability for insulinotropic peptide conjugates at high concentration.
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公开(公告)号：US20180256731A1
公开(公告)日：2018-09-13
申请号：US15983923
申请日：2018-05-18
发明人： Sang Youn Hwang , Yong Ho Huh , Jin Young Kim , Sung Hee Hong , In Young Choi , Sung Youb Jung , Se Chang Kwon , Dae Jin Kim , Hyun Uk Kim , Myung Hyun Jang , Seung Su Kim
摘要： An insulin analog has a reduced insulin titer and a reduced insulin receptor binding affinity compared to the native form for the purpose of increasing the blood half-life of insulin. A conjugate is prepared by linking the insulin analog and a carrier. A long-acting formulation includes the conjugate.
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公开(公告)号：US20150238629A1
公开(公告)日：2015-08-27
申请号：US14416223
申请日：2013-07-25
发明人： Hyun Uk Kim , Hyung Kyu Lim , Sung Hee Hong , Dae Jin Kim , Sung Min Bae , Se Chang Kwon
IPC分类号： A61K47/48
摘要： The present invention relates to a liquid formulation of long-acting insulinotropic peptide conjugate, comprising a pharmaceutically effective amount of long-acting insulinotropic peptide conjugate consisting of a physiologically active peptide, insulinotropic peptide, and an immunoglobulin Fc region; and an albumin-free stabilizer, wherein the stabilizer comprises a buffer, a sugar alcohol, a non-ionic surfactant, and an isotonic agent, and a method for preparing the formulation. For the purpose of preventing microbial contamination, a preservative may be added. The liquid formulation of the present invention is free of human serum albumin and other potentially hazardous factors to body, having no risk of viral contamination, and thus can provide excellent storage stability for insulinotropic peptide conjugates at high concentration.
摘要翻译： 本发明涉及长效促胰岛素肽缀合物的液体制剂，其包含药学有效量的由生理活性肽，促胰岛素肽和免疫球蛋白Fc区组成的长效促胰岛素肽缀合物; 和无白蛋白的稳定剂，其中稳定剂包括缓冲液，糖醇，非离子表面活性剂和等渗剂，以及制备该制剂的方法。 为了防止微生物污染，可以加入防腐剂。 本发明的液体制剂不含人体血清白蛋白和其他对身体有潜在危害的因素，没有病毒污染的风险，因此可以为高浓度的促胰岛素肽缀合物提供优异的储存稳定性。
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公开(公告)号：US10159715B2
公开(公告)日：2018-12-25
申请号：US15313501
申请日：2015-05-29
发明人： Jung Kuk Kim , Dae Jin Kim , Yong Ho Heo , In Young Choi , Sung Youb Jung , Se Chang Kwon
摘要： The present invention relates to a composition for the prevention or treatment of diabetes including a long-acting insulin conjugate and a long-acting insulinotropic peptide conjugate, and a method for treating diabetes. More specifically, combination administration of the long-acting analog conjugate and the long-acting insulinotropic peptide conjugate inhibits weight gain due to administration of insulin, and vomiting and nausea due to administration of the insulinotropic peptide, and also reduces the required doses of insulin, thereby remarkably improving drug compliance. In addition, the present invention relates to administering a pharmaceutical composition for reducing side effects of pancreatic beta cells in diabetic patients, including a long-acting insulin analog conjugate and a long-acting insulinotropic peptide analog conjugate, and to a method for reducing side effects of pancreatic beta cells in diabetic patients, including the step of administering the composition. Specifically, the present invention is characterized in reducing side effects such as abnormality in the function of pancreatic beta cells associated with the development of diabetes, reduction in the pancreatic beta cell mass, lipotoxicity, or glucotoxicity.
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公开(公告)号：US11925691B2
公开(公告)日：2024-03-12
申请号：US16484290
申请日：2018-02-07
发明人： Su Yeon Park , Dae Jin Kim , Sung Youb Jung , Yong Gyu Jung , Hyun Sik Yun
IPC分类号： A61K47/68 , A61K47/54 , A61K47/60 , C07D225/08
CPC分类号： A61K47/6889 , A61K47/545 , A61K47/60 , A61K47/6803 , C07D225/08
摘要： One aspect of the present invention provides a compound in which a functional group capable of binding to a globulin Fc region or a physiologically active polypeptide is introduced at one end of a non-peptidic polymer and a functional group capable of a click reaction is introduced at the other end; a polypeptide conjugate in which a physiologically active polypeptide binds to one end of the compound; a physiologically active polypeptide conjugate in which a physiologically active polypeptide and an immunoglobulin Fc region bind to both ends thereof by using the compound as a linker; and methods for preparing the same compound, polypeptide conjugate, and physiologically active polypeptide conjugate.
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公开(公告)号：US11603346B2
公开(公告)日：2023-03-14
申请号：US16082737
申请日：2017-03-07
发明人： Dae Jin Kim , Jong Soo Lee , Sung Min Bae , Se Chang Kwon
IPC分类号： C07C47/198 , A61K39/395 , C07C323/22 , C07C323/39 , C07C233/05 , A61K47/50 , C07C237/04 , A61K38/18 , A61K47/60 , C07C233/18 , C07C323/12 , C07D213/71
摘要： The present invention relates to polyethylene glycol derivatives and use thereof.
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公开(公告)号：US11207383B2
公开(公告)日：2021-12-28
申请号：US16665457
申请日：2019-10-28
发明人： Dae Jin Kim , Jong Soo Lee , Young Jin Park , Sung Hee Hong , Sung Min Bae , Se Chang Kwon
IPC分类号： A61K38/21 , A61K47/68 , A61K47/60 , B01D15/36 , B01D15/38 , B01D15/32 , B01D15/34 , C07K14/535 , A61K38/19
摘要： Provided is a complex composition, of which positional isomers are minimized by using a N-terminus of an immunoglobulin Fc region as a binding site when the immunoglobulin Fc region is used as a carrier. Also provided are a protein complex which is prepared by N-terminal-specific binding of immunoglobulin Fc region, thereby prolonging blood half-life of the physiologically active polypeptide, maintaining in vivo potency at a high level, and having no risk of immune responses, a preparation method thereof, and a pharmaceutical composition including the same for improving in vivo duration and stability of the physiologically active polypeptide. The protein complex may be usefully applied to the development of long-acting formulations of various physiologically active polypeptide drugs.
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