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21. 发明申请

US20140296131A1 Truncated GLP-1 Derivatives and Their Therapeutical Use 审中-公开
标题翻译：截短的GLP-1衍生物及其治疗用途
公开(公告)号：US20140296131A1
公开(公告)日：2014-10-02
申请号：US14299638
申请日：2014-06-09
申请人： Novo Nordisk A/S
发明人： Jane Spetzler , Lauge Schaeffer , Jesper Lau , Janos T. Kodra , Kjeld Madsen , Patrick W. Garibay , Jacob Kofoed , Steffen Reedtz-Runge , Henning Thoegersen , Ingrid Pettersson
IPC分类号： C07K14/605
CPC分类号： C07K14/605 , A61K38/00
摘要： The invention relates to truncated GLP-1 analogues, in particular a GLP-1 analogue which is a modified GLP-1(7-35) (SEQ ID No 1) having: i) a total of 2, 3, 4, 5 6, 7, 8, or 9 amino acid substitutions as compared to GLP-1(7-35), including a) a Glu residue at a position equivalent to position 22 of GLP-1(7-35), and b) an Arg residue at a position equivalent to position 26 of GLP-1(7-35); as well as derivatives thereof, and therapeutic uses and compositions. These analogues and derivatives are highly potent, have a good binding affinity to the GLP-1 receptor, also to the extracellular domain of the GLP-1 receptor, which is of potential relevance achieving long-acting, stable GLP-1 compounds with a potential for once weekly administration.
摘要翻译：本发明涉及截短的GLP-1类似物，特别是GLP-1类似物，其是修饰的GLP-1（7-35）（SEQ ID No.1），其具有：i）总共2,3,4,5,6 ，7,8或9个氨基酸取代，其包括a）在等同于GLP-1（7-35）的位置22的位置上的Glu残基，和b）Arg 在等同于GLP-1（7-35）的第26位的位置上的残基; 以及其衍生物，以及治疗用途和组合物。这些类似物和衍生物是高度有效的，对GLP-1受体以及GLP-1受体的细胞外结构域具有良好的结合亲和力，这与具有潜在的长效，稳定的GLP-1化合物具有潜在的相关性每周一次行政。

22. 发明授权

US11518795B2 Double-acylated GLP-1 derivatives 有权
公开(公告)号：US11518795B2
公开(公告)日：2022-12-06
申请号：US16717176
申请日：2019-12-17
申请人： Novo Nordisk A/S
发明人： Jacob Kofoed , Patrick William Garibay , Jesper Lau
IPC分类号： C07K14/605 , A61K38/26 , A61K38/00
摘要： The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue and a second K residue, at positions corresponding to position 26, and 37, 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 selected from Chem. 1: HOOC—(CH2)x—CO—*, and Chem. 2: HOOC—C6H4—O—(CH2)y—CO—*, in which x is an integer in the range of 8-16, and y is an integer in the range of 6-13; and the linker comprises Chem. 3: *—NH—(CH2)q—CH[(CH2)w—NR1R2]—CO—*, which is connected at its CO—* end to the epsilon amino group of the first or the second K residue of the GLP-1 analogue, and wherein q is an integer in the range of 0-5, R1 and R2 independently represent *—H or *—CH3, 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.

23. 发明授权

US11274135B2 Double-acylated GLP-1 derivatives 有权
公开(公告)号：US11274135B2
公开(公告)日：2022-03-15
申请号：US14399086
申请日：2013-05-02
申请人： Novo Nordisk A/S
发明人： Jacob Kofoed , Patrick W. Garibay
IPC分类号： C07K14/605 , A61K38/26 , A61K38/00
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—C6H4—O—(CH2)y—CO—*, in which y is an integer in the range of 6-13; and the linker comprises Chem. 3a: *—NH—(CH2)q—CH[(CH2)w—NR1R2]—CO—*, wherein q is an integer in the range of 0-5, R1 and R2 independently represent *—H or *—CH3, 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.

24. 发明申请

US20180258153A1 GLP-1 Derivatives and Uses Thereof 审中-公开
公开(公告)号：US20180258153A1
公开(公告)日：2018-09-13
申请号：US15534644
申请日：2015-12-17
申请人： Novo Nordisk A/S
发明人： Jacob Kofoed
IPC分类号： C07K14/605 , A61P3/10 , A61P3/04
CPC分类号： C07K14/605 , A61K38/00 , A61P3/04 , A61P3/10
摘要： The invention relates to a derivative of a GLP-1 analogue of a general Formula I, which derivative comprises a side chain attached to a Lys residue at position 34, 35, 36, 37, 38, or 39 of the GLP-1 analogue. The side chain comprises a Branched linker, a 1st and a 2nd Protractor and a Pre-linker. The Branched linker is connected to the Lys residue of the GLP-1 analogue via the Pre-linker and to the 1st and the 2nd Protractor via a 1st and 2nd Post-linker, respectively. The Branched linker may, e.g., be a tri-radical of Lys. The 1st and the 2nd Protractor is C20 diacid. Various linker elements may be used in the Prelinker as well as the two Post-linkers. The invention also relates to novel GLP-analogues, novel side chain intermediates and their manufacture and use to prepare derivatives of biologically active peptides and proteins, as well as pharmaceutical compositions and medical uses of the analogues and derivatives. The derivatives have very long half-lives while maintaining a satisfactory potency, which makes them potentially suitable for once-monthly administration.

25. 发明申请

US20170145069A1 GLP-1 Derivatives 审中-公开
公开(公告)号：US20170145069A1
公开(公告)日：2017-05-25
申请号：US15404808
申请日：2017-01-12
申请人： Novo Nordisk A/S
发明人： Jesper Lau , Paw Bloch , Jacob Kofoed , Patrick William Garibay
IPC分类号： 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 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—(CH2))x—CO—*, and Chem. 16: HOOC—C6H4—O—(CH2)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(CH2OH)—CO—*. A preferred linker is gGlu-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.

26. 发明申请

US20170114116A1 Double-Acylated GLP-1 Compounds 审中-公开
公开(公告)号：US20170114116A1
公开(公告)日：2017-04-27
申请号：US15301960
申请日：2015-04-07
申请人： Novo Nordisk A/S
发明人： Lars Linderoth , Jacob Kofoed , Jesper Lau , Paw Bloch , Patrick William Garibay , Janos Tibor Kodra
IPC分类号： C07K14/605 , C07C235/20
摘要： The invention relates to a derivative of a GLP-1 peptide, which peptide comprises a first Lys residue at a position corresponding to position 36 of GLP-1(7-37) (SEQ ID NO:1), a second Lys residue at a position corresponding to position 37 of GLP-1(7-37) (SEQ ID NO: 1), and a maximum of seven amino acid changes as compared to GLP-1(7-37) (SEQ ID NO: 1); which derivative comprises two protractors attached to said first and second Lys residue, respectively, each via a linker; wherein the protractor is selected from: Chem. 1: HOOC—C6H4-0-(CH2)y—CO—*, and Chem. 2: HOOC—(CH2)x—CO—*, wherein y is an integer in the range of 8-11, and x is 12; and the linker comprises at least one of: Chem. 3: *—NH—CH(COOH)—(CH2)2—CO—*, Chem. 4: *—NH—CH((CH2)2—COOH)—CO—*, and/or Chem. 5: *—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 uses thereof, such as for the treatment of diabetes and obesity, as well as to the GLP-1 peptides forming part of these derivatives which have Lys residues at positions 36 and 37 and no other Lys residues, and the GLP-1(9-37) fragments thereof. The invention furthermore relates to an intermediate product comprising 3-carboxyphenoxy-nonanoic acid with a protection group at the carboxy group of the nonanoic acid, optionally via a linker. The derivatives have a very good potency and a long half-life which makes them potentially useful for, e.g., oral administration.

27. 发明申请

US20150152157A1 Double-Acylated GLP-1 Derivatives 审中-公开
标题翻译：双酰化GLP-1衍生物
公开(公告)号：US20150152157A1
公开(公告)日：2015-06-04
申请号：US14399086
申请日：2013-05-02
申请人： Novo Nordisk A/S
发明人： Jacob Kofoed , Patrick W. Garibay
IPC分类号： 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—C6H4-0-(CH2)y—CO—*, in which y is an integer in the range of 6-13; and the linker comprises Chem. 3a: *—NH—(CH2)q—CH[(CH2)w—NR1R2]—CO—*, wherein q is an integer in the range of 0-5, R1 and R2 independently represent *—H or *—CH3, 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。

28. 发明申请

US20200079834A1 DOUBLE-ACYLATED GLP-1 DERIVATIVES 审中-公开
公开(公告)号：US20200079834A1
公开(公告)日：2020-03-12
申请号：US16692260
申请日：2019-11-22
申请人： Novo Nordisk A/S
发明人： Birgit Wieczorek , Jane Spetzler , Thomas Kruse , Lars Linderoth , Jacob Kofoed
IPC分类号： C07K14/605 , A61K47/54 , A61K47/60 , A61K38/26
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 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 analogues. The derivatives are suitable for oral administration.

29. 发明申请

US20190038721A1 GLP-1 DERIVATIVES AND USES THEREOF 审中-公开
公开(公告)号：US20190038721A1
公开(公告)日：2019-02-07
申请号：US16077759
申请日：2017-03-02
申请人： Novo Nordisk A/S
发明人： Jacob Kofoed , Janos Tibor Kodra , Lars Linderoth , Patrick William Garibay
IPC分类号： A61K38/26 , A61K47/54
摘要： The invention relates to GLP-1 analogues and derivatives having a Trp at a position corresponding to position 8 of GLP-1(7-37), and their pharmaceutical use e.g. in the treatment of type 2 diabetes. These Trp8 compounds are very stable against degradation by DPP-IV, while maintaining the capability to bind to and activate the GLP-1 receptor. The derivatives have one or two substituents (P-L) attached to a Lys residue of the GLP-1 analogue via an optional Branching group (B), wherein P is a Protracting moiety such as a fatty diacid, and L is a linker consisting of one or more linker elements such as, for example, 8-amino-3,6-dioxaoctanoic acid. Examples of compounds of the invention include the 8W variants of liraglutide and dulaglutide. The invention also relates to a method for the fully recombinant preparation of 8W GLP-1 analogues and derivatives which is more simple and thereby cheaper as compared to the preparation of known GLP-1 analogues that have been DPP-IV stabilised by inclusion of one or more non-coded amino acids.

30. 发明授权

US10010614B2 Derivatives of GLP-1 like peptides, and uses thereof 有权
公开(公告)号：US10010614B2
公开(公告)日：2018-07-03
申请号：US15278501
申请日：2016-09-28
申请人： Novo Nordisk A/S
发明人： Steffen Reedtz-Runge , Jacob Kofoed
IPC分类号： A61K38/26 , C07K14/605 , A61K47/48
CPC分类号： A61K47/545 , A61K38/26 , A61K47/542 , C07K14/605
摘要： The invention relates to derivatives of GLP-1 like peptides which are C-terminally extended analogs of native GLP-1. The derivatives comprise two side chains, one at a position corresponding to position 42, and one at a position corresponding to position 18, 23, 27, 31, 36, or 38, wherein both positions are when compared to GLP-1(7-37). The side chains comprise a C19, C20, or C22 diacid protracting moiety and optionally a linker. The invention also relates to intermediate products in the form of novel GLP-1 analogs incorporated in the derivatives of the invention, as well as 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.

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