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1. 发明申请

US20100216715A1 FGF21 Derivatives With Albumin Binder A-B-C-D-E- And Their Use 有权
标题翻译： FGF21衍生物与白蛋白粘合剂A-B-C-D-E-及其用途
公开(公告)号：US20100216715A1
公开(公告)日：2010-08-26
申请号：US12692227
申请日：2010-01-22
申请人： Tina Møller Tagmose , Patrick William Garibay , Bírgítte Andersen , Jishu Wang , Kílían Waldemar Conde-Frieboes , Kristían Sass Bak-Jensen , Henning Thøgersen , Helle Wöldike , Peter Kresten Nielsen , Rita Slaaby , Xujia Zhang , Birgit Wieczorek
发明人： Tina Møller Tagmose , Patrick William Garibay , Bírgítte Andersen , Jishu Wang , Kílían Waldemar Conde-Frieboes , Kristían Sass Bak-Jensen , Henning Thøgersen , Helle Wöldike , Peter Kresten Nielsen , Rita Slaaby , Xujia Zhang , Birgit Wieczorek
IPC分类号： A61K38/18 , C07K14/50 , A61P3/00 , A61P3/04 , A61P9/00
CPC分类号： A61K47/48046 , A61K38/00 , A61K47/543 , A61K47/60 , A61K47/643 , C07K14/50
摘要： The present invention relates to Fibroblast Growth Factor 21 (FGF21), more in particular to derivatives of FGF21 compounds having an albumin binder of the formula A-B-C-D-E- covalently attached. The invention also relates to novel FGF21 analogues, as well as to the pharmaceutical use of these FGF21 derivatives and analogues, in particular for the treatment of diabetes, dyslipidemia, obesity, cardiovascular diseases, metabolic syndrome, and/or Non Alcoholic Fatty Liver Disease (NAFLD). The derivatives of the invention are protracted, e.g. capable of maintaining a low blood glucose level for a longer period of time, capable of increasing the in vivo half-life of FGF21, and/or result in a lower clearance of FGF21. The derivatives of the invention are preferably furthermore of an improved oxidative stability.
摘要翻译：本发明涉及成纤维细胞生长因子21（FGF21），更具体地涉及具有共价连接的式A-B-C-D-E-的白蛋白结合物的FGF21化合物的衍生物。本发明还涉及新型FGF21类似物，以及这些FGF21衍生物和类似物的药物用途，特别是用于治疗糖尿病，血脂异常，肥胖症，心血管疾病，代谢综合征和/或非酒精性脂肪肝病（ NAFLD）。本发明的衍生物是延长的，例如。能够维持较长时间的低血糖水平，能够增加FGF21的体内半衰期，和/或导致FGF21的较低清除率。本发明的衍生物优选还具有改善的氧化稳定性。

2. 发明授权

US09266940B2 Double-acylated GLP-1 derivatives 有权
标题翻译：双酰化GLP-1衍生物
公开(公告)号：US09266940B2
公开(公告)日：2016-02-23
申请号：US14009902
申请日：2012-04-12
申请人： Birgit Wieczorek , Lars Linderoth
发明人： Birgit Wieczorek , Lars Linderoth
IPC分类号： A61K38/26 , C07K14/605 , A61K47/48
CPC分类号： C07K14/605 , A61K38/00 , A61K38/26 , A61K47/542 , A61K47/60
摘要： The invention relates to a derivative of a GLP-1 analog, which analog comprises a first K residue at a position corresponding to position 27 of GLP-1(7-37) (SEQ ID NO: 1); a second K residue at a position corresponding to position T of GLP-1(7-37), where T is an integer in the range of 7-37 except 18 and 27; and a maximum of ten amino acid changes as compared to GLP-1(7-37); wherein the first K residue is designated K27, and the second K residue is designated KT; which derivative comprises two albumin binding moieties attached to K27 and KT, respectively, via a linker, wherein the albumin binding moiety comprises a protracting moiety selected from HOOC—(CH2)x—CO— and HOOC—C6H4—O—(CH2)y—CO—; in which x is an integer in the range of 6-16, and y is an integer in the range of 3-17; wherein the linker comprises an element of the formula —NH—(CH2)2—(O—(CH2)2)k—O—(CH2)n—CO—, wherein k is an integer in the range of 1-5, and n is an integer in the range of 1-5; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to the pharmaceutical use thereof, for example in the treatment and/or prevention of all forms of diabetes and related diseases, as well as to corresponding novel GLP-1 analogs. The derivatives are suitable for oral administration.
摘要翻译：本发明涉及GLP-1类似物的衍生物，其类似物包含在对应于GLP-1（7-37）（SEQ ID NO：1）的位置27的位置处的第一个K残基; 在对应于GLP-1（7-37）的位置T的位置处的第二个K残基，其中T是除了18和27之外的7-37范围内的整数; 与GLP-1（7-37）相比最多10个氨基酸变化。其中第一K残基指定为K27，第二K残基指定为KT; 该衍生物通过接头分别包含与K27和KT连接的两个白蛋白结合部分，其中白蛋白结合部分包含选自HOOC-（CH 2）x -CO-和HOOC-C 6 H 4 -O-（CH 2）y -CO-; 其中x是6-16的整数，y是3-17的整数; 其中所述连接体包含式-NH-（CH 2）2 - （O-（CH 2）2）k -O-（CH 2）n -CO-的元素，其中k是1-5的整数， n为1-5的整数; 或其药学上可接受的盐，酰胺或酯。本发明还涉及其药物用途，例如用于治疗和/或预防所有形式的糖尿病和相关疾病，以及相应的新型GLP-1类似物。该衍生物适用于口服给药。

3. 发明授权

US09480753B2 FGF21 derivatives with albumin binder A-B-C-D-E- and their use 有权
标题翻译：具有白蛋白结合剂A-B-C-D-E-的FGF21衍生物及其用途
公开(公告)号：US09480753B2
公开(公告)日：2016-11-01
申请号：US12692227
申请日：2010-01-22
申请人： Tina Møller Tagmose , Patrick William Garibay , Bírgítte Andersen , Henning Thøgersen , Birgit Wieczorek
发明人： Tina Møller Tagmose , Patrick William Garibay , Bírgítte Andersen , Henning Thøgersen , Birgit Wieczorek
IPC分类号： A01N43/64 , A61K31/41 , A01N43/36 , A61K31/40 , A01N37/00 , A61K31/19 , A61K47/48 , C07K14/50 , A61K38/00
CPC分类号： A61K47/48046 , A61K38/00 , A61K47/543 , A61K47/60 , A61K47/643 , C07K14/50
摘要： The present invention relates to Fibroblast Growth Factor 21 (FGF21), more in particular to derivatives of FGF21 compounds having an albumin binder of the formula A-B-C-D-E- covalently attached. The invention also relates to novel FGF21 analogues, as well as to the pharmaceutical use of these FGF21 derivatives and analogues, in particular for the treatment of diabetes, dyslipidemia, obesity, cardiovascular diseases, metabolic syndrome, and/or Non Alcoholic Fatty Liver Disease (NAFLD). The derivatives of the invention are protracted, e.g. capable of maintaining a low blood glucose level for a longer period of time, capable of increasing the in vivo half-life of FGF21, and/or result in a lower clearance of FGF21. The derivatives of the invention are preferably furthermore of an improved oxidative stability.
摘要翻译：本发明涉及成纤维细胞生长因子21（FGF21），更具体地涉及具有共价连接的式A-B-C-D-E-的白蛋白结合物的FGF21化合物的衍生物。本发明还涉及新型FGF21类似物，以及这些FGF21衍生物和类似物的药物用途，特别是用于治疗糖尿病，血脂异常，肥胖症，心血管疾病，代谢综合征和/或非酒精性脂肪肝病（ NAFLD）。本发明的衍生物是延长的，例如。能够维持较长时间的低血糖水平，能够增加FGF21的体内半衰期，和/或导致FGF21的较低清除率。本发明的衍生物优选还具有改善的氧化稳定性。

4. 发明授权

US09708383B2 Double-acylated GLP-1 derivatives 有权
公开(公告)号：US09708383B2
公开(公告)日：2017-07-18
申请号：US13882947
申请日：2011-11-09
申请人： Alice Ravn Madsen , Birgit Wieczorek , Jacob Kofoed , Jesper Lau , Jane Spetzler , Janos Tibor Kodra , Lars Linderoth , Patrick William Garibay , Per Sauerberg , Thomas Kruse
发明人： Alice Ravn Madsen , Birgit Wieczorek , Jacob Kofoed , Jesper Lau , Jane Spetzler , Janos Tibor Kodra , Lars Linderoth , Patrick William Garibay , Per Sauerberg , Thomas Kruse
IPC分类号： A61K38/00 , C07K14/605 , A61K47/48
CPC分类号： C07K14/605 , A61K47/542
摘要： The invention relates to a derivative of a GLP-1 analog, which analog comprises a first K residue at a position corresponding to position 18 of GLP-1(7-37) (SEQ ID NO: 1), a second K residue at another position, and a maximum of twelve amino acid changes as compared to GLP-1(7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 1, Chem. 2, and Chem. 3: HOOC—(CH2)x—CO—* Chem. 1: HOOC—C6H4—O—(CH2)y—CO—* Chem. 2: R2—C6H4—(CH2)z—CO—*, Chem. 3: in which x is an integer in the range of 6-18, y is an integer in the range of 3-17, z is an integer in the range of 1-5, and R2 is a group having a molar mass not higher than 150 Da; and the linker comprises *—NH—(CH2)2—(O—(CH2)2)k—O—(CH2)n—CO—*. Chem. 4: wherein k is an integer in the range of 1-5, and n is an integer in the range of 1-5; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to the pharmaceutical use thereof, for example in the treatment and/or prevention of all forms of diabetes and related diseases, as well as to corresponding novel peptides and side chain intermediates. The derivatives are suitable for oral administration.

5. 发明申请

US20130288960A1 Double-Acylated GLP-1 Derivatives 有权
标题翻译：双酰化GLP-1衍生物
公开(公告)号：US20130288960A1
公开(公告)日：2013-10-31
申请号：US13882947
申请日：2011-11-09
申请人： Alice Ravn Madsen , Birgit Wieczorek , Jacob Kofoed , Jesper Lau , Jane Spetzler , Janos Tibor Kodra , Lars Linderoth , Patrick William Garibay , Per Sauerberg , Thomas Kruse
发明人： Alice Ravn Madsen , Birgit Wieczorek , Jacob Kofoed , Jesper Lau , Jane Spetzler , Janos Tibor Kodra , Lars Linderoth , Patrick William Garibay , Per Sauerberg , Thomas Kruse
IPC分类号： C07K14/605
CPC分类号： C07K14/605 , A61K47/542
摘要： The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 18 of GLP-1 (7-37) (SEQ ID NO: 1), a second K residue at another position, and a maximum of twelve amino acid changes as compared to GLP-1 (7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 1, Chem. 2, and Chem. 3: Chem.: HOOC—(CH2)x—CO—* Chem. 2: HOOC—C6H4-0-(CH2)y—CO—* Chem. 3: R2—C6H4—(CH2)z—CO—*, in which x is an integer in the range of 6-18, y is an integer in the range of 3-17, z is an integer in the range of 1-5, and R2 is a group having a molar mass not higher than 150 Da; and the linker comprises Chem. 4: *—NH—(CH2)2-(0-(CH2)2)k-0-(CH2)n—CO—*. wherein k is an integer in the range of 1-5, and n is an integer in the range of 1-5; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to the pharmaceutical use thereof, for example in the treatment and/or prevention of all forms of diabetes and related diseases, as well as to corresponding novel peptides and side chain intermediates. The derivatives are suitable for oral administration.
摘要翻译：本发明涉及GLP-1类似物的衍生物，其类似物包含在对应于GLP-1（7-37）（SEQ ID NO：1）的第18位的位置处的第一个K残基，另一个的第二个K残基位置和与GLP-1（7-37）相比最多12个氨基酸变化; 该衍生物分别包含通过接头分别连接到所述第一和第二K残基的两个伸长部分，其中伸长部分选自Chem。 1，Chem。 2和Chem。 3：化学式：HOOC-（CH2）x-CO- * 2：HOOC-C6H4-0-（CH2）y-CO- * Chem。 3：R2-C6H4-（CH2）z-CO- *，其中x是6-18的整数，y是3-17的整数，z是1的整数 -5和R2是摩尔质量不高于150Da的基团; 连接体包括Chem。 4：* -NH-（CH 2）2 - （O-（CH 2）2）k -O-（CH 2）n -CO- *。其中k是1-5的整数，n是1-5的整数; 或其药学上可接受的盐，酰胺或酯。本发明还涉及其药物用途，例如用于治疗和/或预防所有形式的糖尿病和相关疾病，以及相应的新型肽和侧链中间体。该衍生物适用于口服给药。

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