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1. 发明授权

US10266577B2 GLP-1 derivatives, and uses thereof 有权
公开(公告)号：US10266577B2
公开(公告)日：2019-04-23
申请号：US14909543
申请日：2014-08-14
申请人： Novo Nordisk A/S
发明人： Per Sauerberg , Jacob Kofoed
IPC分类号： A61K38/00 , A61K47/54 , A61K47/58 , A61K47/60 , C07K14/605
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—(CH2)16—CO—*, Chem. 1a: HOOC—(CH2)18—CO—*, and Chem. 2: HO3S—(CH2)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 analogs, as well as to pharmaceutical compositions and uses of the derivatives and analogs, 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.

2. 发明申请

US20170051034A1 Novel Glucagon Analogues 审中-公开
标题翻译：新型胰高血糖素类似物
公开(公告)号：US20170051034A1
公开(公告)日：2017-02-23
申请号：US15262450
申请日：2016-09-12
申请人： Novo Nordisk A/S
发明人： Jesper F. Lau , Thomas Kruse , Lars Linderoth , Henning Thoegersen , Jacob Kofoed , Kirsten Dahl
IPC分类号： C07K14/605 , A61K38/26 , A61K47/48 , A61K38/28
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：本发明涉及新颖的肽化合物，其具有延长的作用曲线和改善的溶解性和稳定性，在治疗中使用该化合物，包括向有需要的患者施用化合物，以及使用药物制造中的化合物。本发明的化合物在治疗高血糖症，糖尿病和肥胖以及与高血糖症，糖尿病和肥胖相关的各种疾病或病症方面特别有意义。

3. 发明申请

US20170007707A1 Derivatives of GLP-1 Like Peptides, and Uses Thereof 审中-公开
标题翻译： GLP-1类似肽的衍生物及其用途
公开(公告)号：US20170007707A1
公开(公告)日：2017-01-12
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 , Christian Wenzel Tornoee , Per Sauerberg
IPC分类号： A61K47/48 , A61K38/26
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 analogues 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 analogues 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.
摘要翻译：本发明涉及作为天然GLP-1的C-末端延伸类似物的GLP-1样肽的衍生物。衍生物包含两个侧链，一个位于对应于位置42的位置，一个位于对应于位置18,23,27,31,36或38的位置，其中两个位置与GLP-1（7- 37）。侧链包含C19，C20或C22二酸延伸部分和任选的接头。本发明还涉及并入本发明衍生物中的新型GLP-1类似物形式的中间产物，以及衍生物的药物组合物和医学用途。衍生物具有非常长的半衰期，同时保持令人满意的效力，这使得它们潜在地适合于每月一次的管理。

4. 发明申请

US20160143998A1 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：US20160143998A1
公开(公告)日：2016-05-26
申请号：US14897738
申请日：2014-06-19
申请人： Novo Nordisk A/S
发明人： Steffen Reedtz-Runge , Per Sauerberg , Jacob Kofoed , Ingrid Pettersson , Christian W. Tornoee
IPC分类号： A61K38/26 , A61K47/48 , C07K14/605
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GLP-1类似物的衍生物，任选地C末端延伸，该衍生物包含C20或C22二酸基团形式的第一和第二延伸部分，双氨基支链接头和第一和第二个另外的接头，每个包含OEG样连接体元件; 其中这些元件通过酰胺键互连并连接到GLP-1类似物的Lys残基。本发明还涉及并入本发明衍生物中的新型GLP-1类似物形式的中间产物，以及衍生物的药物组合物和医学用途。衍生物具有非常长的半衰期，同时保持令人满意的效力，这使得它们潜在地适合于每月一次的管理。

5. 发明申请

US20150210745A1 Double-Acylated GLP-1 Derivatives with a Linker 审中-公开
标题翻译：具有接头的双酰化GLP-1衍生物
公开(公告)号：US20150210745A1
公开(公告)日：2015-07-30
申请号：US14608284
申请日：2015-01-29
申请人： Novo Nordisk A/S
发明人： Jacob Kofoed , Jesper Lau , Lars Linderoth , Patrick William Garibay , 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 HOOC—(CH2)x-CO—*, and Chem. 1: HOOC—C6H4-0-(CH2)y-CO—*, Chem. 2: in which x is an integer in the range of 6-18, and y is an integer in the range of 3-17; and the linker comprises *—NH—(CH2)q-CH[(CH2)w-NH2]-CO—*, Chem. 3: wherein q is an integer in the range of 0-5, 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 peptides and side chain intermediates. The derivatives are potent, protracted, and 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HOOC-（CH 2）x -CO- *和Chem。 1：HOOC-C6H4-0-（CH2）y-CO- *，Chem。 2：其中x是6-18的整数，y是3-17的整数; 并且连接体包含* -NH-（CH 2）q-CH [（CH 2）w -NH 2] -CO- *，Chem。 3：其中q是0-5的整数，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侧链中间体。衍生物有效，延长，适合口服。

6. 发明申请

US20150133374A1 Double-Acylated GLP-1 Derivatives 有权
标题翻译：双酰化GLP-1衍生物
公开(公告)号：US20150133374A1
公开(公告)日：2015-05-14
申请号：US14399087
申请日：2013-05-02
申请人： Novo Nordisk A/S
发明人： Jacob Kofoed , Patrick W. Garibay , Jesper Lau
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 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.
摘要翻译：本发明涉及GLP-1类似物的衍生物，其类似物分别包含第一K残基和第二K残基，分别对应于GLP-1（7-37）的位置26和37（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，其中伸长部分选自Chem。 1：HOOC-（CH 2）x-CO- *，和Chem。 2：HOOC-C6H4-O-（CH2）y-CO- *，其中x是8-16的整数，y是6-13的整数; 连接体包括Chem。 3：* -NH-（CH2）q-CH [（CH2）w-NR1R2] -CO- *，其在其CO-端连接到GLP的第一或第二K残基的ε氨基 -1类似物，其中q是0-5的整数，R 1和R 2独立地表示* -H或* -CH 3，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，以及相应的新的肽和连接物中间体。衍生物有效，稳定，延长，适合口服给药。

7. 发明授权

US11117947B2 Double-acylated GLP-1 derivatives 有权
公开(公告)号：US11117947B2
公开(公告)日：2021-09-14
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： A61K38/26 , A61K47/54 , C07K14/605 , A61K47/60 , A61K38/00
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.

8. 发明授权

US10946074B2 GLP-1 derivatives and uses thereof 有权
公开(公告)号：US10946074B2
公开(公告)日：2021-03-16
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 , A61K47/60 , C07K14/605 , A61K38/00
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.

9. 发明申请

US20160200791A1 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：US20160200791A1
公开(公告)日：2016-07-14
申请号：US14909543
申请日：2014-08-14
申请人： NOVO NORDISK A/S
发明人： Per Sauerberg , Jacob Kofoed
IPC分类号： 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—(CH2)16—CO—*, Chem. 1a: HOOC—(CH2)18—CO—*, and Chem. 2: HO3S—(CH2)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。衍生物具有半途而废，保持满意有效性，这使得它们潜在地适合于每月一次的管理。

10. 发明授权

US11572398B2 GLP-1 derivatives and uses thereof 有权
公开(公告)号：US11572398B2
公开(公告)日：2023-02-07
申请号：US15531105
申请日：2015-11-26
申请人： Novo Nordisk A/S
发明人： Per Sauerberg , Jacob Kofoed
IPC分类号： C07K14/605 , A61K47/54 , A61K47/59 , A61K38/00
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, or 38 of the GLP-1 analogue, which side chain comprises a Branched linker, a 1st and a 2nd Protractor selected from C18 diacid, C20 diacid, and sulfonic acid C16, and at least one Linker element-1 incorporating ethylene glycol units. Linker element-1 may be incorporated in an optional Pre-linker, and/or in a 1st or 2nd Post-linker. The invention also relates to novel GLP-1 analogues, novel side chain intermediate products 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.

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