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21. 发明申请

WO2015022400A1 GLP-1 DERIVATIVES, AND USES THEREOF 审中-公开
标题翻译： GLP-1衍生物及其用途
公开(公告)号：WO2015022400A1
公开(公告)日：2015-02-19
申请号：PCT/EP2014/067413
申请日：2014-08-14
申请人： NOVO NORDISK A/S
发明人： SAUERBERG, Per , KOFOED, Jacob
IPC分类号： A61K47/48 , C07K14/605
CPC分类号： C07K14/605 , A61K38/00 , A61K47/54 , A61K47/58 , A61K47/60
摘要： The present invention relates to tri-acylated GLP-1 derivatives, acylated at positions corresponding to positions (18, 22, 30), (18, 26, 37), (18, 27, 37), (26, 30, 37), or (27, 30, 37) of the native human glucagon-like peptide 1 (GLP-1 (7-37) (SEQ ID NO: 1); or pharmaceutically acceptable salts, amides, or esters thereof. The acylated side chains comprise a protracting moiety selected from Chem. 1 : HOOC-(CH 2 ) 16 -CO-*, Chem. 1a: HOOC-(CH 2 ) 18 -CO-*, and Chem. 2: HO 3 S-(CH 2 ) 15 -CO-*, and the protracting moieties are connected, via a linker, to a Lys residue of the GLP-1 peptide. The GLP-1 peptide has a maximum of seven amino acid changes as compared to GLP-1 (7-37) (SEQ ID NO: 1). The invention also relates to intermediate products in the form of novel GLP-1 analogues, as well as to pharmaceutical compositions and uses of the derivatives and analogues, in particular for the treatment of type 2 diabetes. The derivatives have very long half-lives while maintaining a satisfactory potency, which makes them potentially suitable for once-monthly administration.
摘要翻译：本发明涉及三酰化GLP-1衍生物，其在对应于位置（18,22,30），（18,26,37），（18,27,37），（26,30,37），，或天然人胰高血糖素样肽1（GLP-1（7-37）（SEQ ID NO：1））的（27,30,37）或其药学上可接受的盐，酰胺或酯。酰化侧链包括选自化学式1：HOOC-（CH 2）16 -CO- *，化学式1a：HOOC-（CH 2）18 -CO- *和化学式2：HO 3 S-（CH 2）15 -CO- *，并且延伸部分通过接头连接到GLP-1肽的Lys残基。与GLP-1（7-37）（SEQ ID NO：1）相比，GLP-1肽具有最多7个氨基酸变化本发明还涉及新型GLP-1类似物形式的中间产物，以及衍生物和类似物的药物组合物和用途，特别是用于治疗2型糖尿病。衍生物具有很长的半生，同时保持令人满意的效力 h使他们潜在地适合每月一次的管理。

22. 发明申请

WO2013167455A1 DOUBLE-ACYLATED GLP-1 DERIVATIVES 审中-公开
标题翻译：双取代的GLP-1衍生物
公开(公告)号：WO2013167455A1
公开(公告)日：2013-11-14
申请号：PCT/EP2013/059113
申请日：2013-05-02
申请人： NOVO NORDISK A/S
发明人： KOFOED, Jacob , GARIBAY, Patrick
IPC分类号： A61K38/26 , C07K14/605
CPC分类号： C07K14/605 , A61K38/00 , A61K38/26
摘要： The invention relates to a derivative of a GLP-1 peptide, which peptide comprises a first K residue and a second K residue, at positions corresponding to position 26, and 34, respectively, of GLP-1(7-37) (SEQ ID NO:1), and a maximum of eight 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 Chem. 2: HOOC-C 6 H 4 -0-(CH 2 ) y -CO-*, in which y is an integer in the range of 6-13; and the linker comprises Chem. 3a: *-NH-(CH 2 ) q -CH[(CH 2 ) w -NR 1 R 2 ]-CO-*, wherein q is an integer in the range of 0-5, R 1 and R 2 independently represent *-H or *-CH 3 , and w is an integer in the range of 0-5; 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 peptide and linker intermediates. The derivatives are potent, stable, protracted, and suitable for oral administration.
摘要翻译：本发明涉及GLP-1肽衍生物，该肽的肽分别包含第一个K残基和第二个K残基，分别位于GLP-1（7-37）的位置26和34（SEQ ID NO： NO：1），与GLP-1（7-37）相比最多8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，其中伸长部分是Chem。 2：HOOC-C6H4-0-（CH2）y-CO- *，其中y是6-13的整数; 连接体包括Chem。 3a：* -NH-（CH2）q-CH [（CH2）w-NR1R2] -CO- *，其中q是0-5的整数，R1和R2独立地表示* -H或* w为0-5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，以及相应的新的肽和连接物中间体。衍生物有效，稳定，延长，适合口服给药。

23. 发明授权

EP3129041B1 DOUBLE-ACYLATED GLP-1 COMPOUNDS 有权
公开(公告)号：EP3129041B1
公开(公告)日：2019-06-12
申请号：EP15713772.0
申请日：2015-04-07
申请人： Novo Nordisk A/S
发明人： LINDEROTH, Lars , KOFOED, Jacob , LAU, Jesper , BLOCH, Paw , GARIBAY, Patrick William , KODRA, János Tibor
IPC分类号： A61K38/26 , C07K14/605

24. 发明授权

EP2753642B8 GLP-1 DERIVATIVES 有权转让
标题翻译： GLP-1衍生物
公开(公告)号：EP2753642B8
公开(公告)日：2017-12-13
申请号：EP12805429.3
申请日：2012-09-06
申请人： Novo Nordisk A/S
发明人： LAU, Jesper , BLOCH, Paw , KOFOED, Jacob , GARIBAY, Patrick
IPC分类号： C07K14/605 , A61K38/26
CPC分类号： C07K14/605 , A61K38/00 , A61K38/26

25. 发明授权

EP3010546B1 GLP-1 DERIVATIVES AND USES THEREOF 有权
标题翻译： GLP-1衍生物及其用途
公开(公告)号：EP3010546B1
公开(公告)日：2017-08-09
申请号：EP14731951.1
申请日：2014-06-19
申请人： Novo Nordisk A/S
发明人： REEDTZ-RUNGE, Steffen , SAUERBERG, Per , KOFOED, Jacob , PETTERSSON, Ingrid , TORNØE, Christian, Wenzel
IPC分类号： A61K47/50
CPC分类号： A61K38/26 , A61K47/54 , A61K47/542 , A61K47/56 , A61K47/60 , C07K14/605
摘要： The invention relates to a derivative of a GLP-1 analogue, optionally C-terminally extended, which derivative comprises a first and a second protracting moiety in the form of a C20 or C22 diacid radical, a bis-amino branched linker, and a first and a second further linker each comprising an OEG-like linker element; wherein these elements are interconnected via amide bonds and attached to a Lys residue of the GLP-1 analogue. The invention also relates to intermediate products in the form of novel GLP-1 analogues incorporated in the derivatives of the invention, as well pharmaceutical compositions and medical uses of the derivatives. The derivatives have very long half-lives while maintaining a satisfactory potency, which makes them potentially suitable for once-monthly administration.
摘要翻译：本发明涉及任选C端延伸的GLP-1类似物的衍生物，所述衍生物包含呈C20或C22二酸基团形式的第一和第二延伸部分，双氨基分支连接子和第一和第二个另外的接头，每个接头都包含OEG样接头元件; 其中这些元件通过酰胺键相互连接并连接到GLP-1类似物的Lys残基上。本发明还涉及掺入本发明衍生物中的新型GLP-1类似物形式的中间产物，以及该衍生物的药物组合物和医学用途。衍生物具有很长的半衰期，同时保持令人满意的效力，这使得它们可能适用于每月一次的施用。

26. 发明授权

EP3033112B1 GLP-1 DERIVATIVES, AND USES THEREOF 有权
公开(公告)号：EP3033112B1
公开(公告)日：2020-10-07
申请号：EP14752614.9
申请日：2014-08-14
申请人： Novo Nordisk A/S
发明人： SAUERBERG, Per , KOFOED, Jacob
IPC分类号： A61K38/00 , A61K47/60 , A61K47/54 , A61K47/58 , C07K14/605

27. 发明授权

EP3226906B1 GLP-1 DERIVATIVES AND USES THEREOF 有权
公开(公告)号：EP3226906B1
公开(公告)日：2019-06-12
申请号：EP15801781.4
申请日：2015-11-26
申请人： Novo Nordisk A/S
发明人： SAUERBERG, Per , KOFOED, Jacob
IPC分类号： A61K38/00 , A61K47/54 , A61K47/59 , C07K14/605

28. 发明公开

EP2846824A1 DOUBLE-ACYLATED GLP-1 DERIVATIVES 有权
标题翻译：双酰化GLP-1衍生物
公开(公告)号：EP2846824A1
公开(公告)日：2015-03-18
申请号：EP13723444.9
申请日：2013-05-02
申请人： Novo Nordisk A/S
发明人： KOFOED, Jacob , GARIBAY, Patrick
IPC分类号： A61K38/26 , C07K14/605
CPC分类号： C07K14/605 , A61K38/00 , A61K38/26
摘要： The invention relates to a derivative of a GLP-1 peptide, which peptide comprises a first K residue and a second K residue, at positions corresponding to position 26, and 34, respectively, of GLP-1(7-37) (SEQ ID NO:1), and a maximum of eight 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 Chem. 2: HOOC-C
6 H
4 -0-(CH
2 )
y -CO-*, in which y is an integer in the range of 6-13; and the linker comprises Chem. 3a: *-NH-(CH
2 )
q -CH[(CH
2 )
w -NR
1 R
2 ]-CO-*, wherein q is an integer in the range of 0-5, R
1 and R
2 independently represent *-H or *-CH
3 , and w is an integer in the range of 0-5; 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 peptide and linker intermediates. The derivatives are potent, stable, protracted, and suitable for oral administration.
摘要翻译：本发明涉及GLP-1肽的衍生物，所述肽在分别对应于GLP-1（7-37）（SEQ ID NO：2）的位置26和34的位置包含第一K残基和第二K残基 NO：1），并且与GLP-1（7-37）相比最多有八个氨基酸改变; 所述衍生物包含分别通过接头连接到所述第一和第二K残基的两个延伸部分，其中所述延长部分是化学结构。 2：HOOC-C 6H 4 -O-（CH 2）y -CO- *，其中y是6-13范围内的整数; 并且接头包含Chem。 3a：* -NH-（CH 2）q -CH [（CH 2）w -NR 1 R 2] -CO- *，其中q是0-5的整数，R 1和R 2独立地表示* -H或* -CH 3，并且w是0-5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连接体中间体。衍生物有效，稳定，持久，适合口服。

29. 发明公开

EP2753642A1 GLP-1 DERIVATIVES 有权转让
标题翻译： GLP-1衍生物
公开(公告)号：EP2753642A1
公开(公告)日：2014-07-16
申请号：EP12805429.3
申请日：2012-09-06
申请人： Novo Nordisk A/S , Lau, Jesper
发明人： LAU, Jesper , BLOCH, Paw , KOFOED, Jacob , GARIBAY, Patrick
IPC分类号： C07K14/605 , A61K38/26
CPC分类号： C07K14/605 , A61K38/00 , A61K38/26
摘要： The invention relates to a derivative of a GLP-1 peptide, which peptide has two Lys residues, namely a first and a second Lys residue, and a maximum of eight amino acid changes as compared to GLP-1(7-37) (SEQ ID NO: 3), which derivative comprises two protracting moieties attached to the epsilon amino group of said first and second Lys residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 15: HOOC-(CH 2 ) x -CO-*, and Chem. 16: HOOC-C 6 H 4 -O-(CH 2 ) y -CO-*, in which x is an integer in the range of 10-16, and y is an integer in the range of 8-12; and the linker comprises a first linker element *-NH-CH(CH 2 OH)-CO-*. A preferred linker is g Glu-Ser-Ser-Gly-Ser-Ser-Gly (SEQ ID NO: 2). The derivative of the invention has a very good potency, and a very good binding to the GLP-1 receptor. The invention also relates to the pharmaceutical use of the derivative, for example in the treatment and/or prevention of all forms of diabetes and related diseases.
摘要翻译：本发明涉及GLP-1肽的衍生物，该肽与GLP-1（7-37）（SEQ）相比，具有两个Lys残基，即第一和第二Lys残基，最多八个氨基酸变化 SEQ ID NO：3），该衍生物分别包含通过接头分别连接到所述第一和第二Lys残基的ε氨基的两个伸长部分，其中伸长部分选自Chem。 15：HOOC-（CH 2）x-CO- *，和Chem。 16：HOOC-C6H4-O-（CH2）y-CO- *，其中x是10-16的整数，y是8-12的整数; 并且连接体包含第一连接体元件* -NH-CH（CH 2 OH）-CO- *。优选的接头是g Glu-Ser-Ser-Gly-Ser-Ser-Gly（SEQ ID NO：2）。本发明的衍生物具有非常好的效力，并且与GLP-1受体具有非常好的结合。本发明还涉及衍生物的药物用途，例如用于治疗和/或预防所有形式的糖尿病和相关疾病。

30. 发明公开

EP2552950A1 NOVEL GLUCAGON ANALOGUES 审中-公开
标题翻译：新的胰高血糖素类似物
公开(公告)号：EP2552950A1
公开(公告)日：2013-02-06
申请号：EP11710218.6
申请日：2011-03-28
申请人： Novo Nordisk A/S
发明人： LAU, Jesper F. , KRUSE, Thomas , LINDEROTH, Lars , THØGERSEN, Henning , KOFOED, Jacob , DAHL, Kirsten
IPC分类号： C07K14/605 , A61K38/26
CPC分类号： C07K14/605 , A61K38/00 , A61K38/26 , A61K38/28 , A61K47/542 , A61K47/545
摘要： The present invention relates to novel peptide compounds which have a protracted profile of action and improved solubility and stability, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of hyperglycemia, diabetes and obesity, as well as a variety of diseases or conditions associated with hyperglycemia, diabetes and obesity.
摘要翻译：本发明涉及具有长效作用特征和改善的溶解度和稳定性的新型肽化合物，涉及该化合物在治疗中的用途，涉及包括将化合物给予有需要的患者的治疗方法，以及涉及在药物制造中的化合物。本发明化合物在治疗高血糖症，糖尿病和肥胖症以及与高血糖症，糖尿病和肥胖症有关的各种疾病或病症方面特别感兴趣。

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