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1. 发明授权

US09657079B2 Truncated GLP-1 derivatives and their therapeutical use 有权
公开(公告)号：US09657079B2
公开(公告)日：2017-05-23
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 , Ingrid Pettersson
IPC分类号： A61K38/16 , C07K14/00 , C07K14/605 , A61K38/00
CPC分类号： C07K14/605 , A61K38/00
摘要： The invention relates to truncated GLP-1 analogs, in particular a GLP-1 analog 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 analogs 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.

2. 发明授权

US09556250B2 Double-acylated GLP-1 derivatives 有权
标题翻译：双酰化GLP-1衍生物
公开(公告)号：US09556250B2
公开(公告)日：2017-01-31
申请号：US14101618
申请日：2013-12-10
申请人： Novo Nordisk A/S
发明人： Patrick William Garibay , Jane Spetzler , Lars Linderoth , Jesper Lau , Lauge Schaeffer
IPC分类号： A61K38/26 , A61K47/48 , C07K14/65 , A61K38/00 , C07D233/64 , C07K14/605
CPC分类号： C07K14/65 , A61K38/00 , A61K47/542 , A61K47/60 , C07K14/605 , G01N2333/605
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 37 of GLP-1(7-37) (SEQ ID NO: 1), a second K residue at a position corresponding to position 26 of GLP-1(7-37), and a maximum of ten amino acid modifications as compared to GLP-1(7-37), wherein the first K residue is designated K37, and the second K residue is designated K26, which derivative comprises two albumin binding moieties attached to K26 and K37, respectively, wherein the albumin binding moiety comprises a protracting moiety selected from:Chem. 1, Chem. 2, Chem. 3 or Chem. 4; or a pharmaceutically acceptable salt, amide, or ester thereof.
摘要翻译： Chem。 1，Chem。 2，Chem。 3或Chem。 4; 或其药学上可接受的盐，酰胺或酯。

3. 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。

4. 发明申请

US20140087995A1 Polypeptides 审中-公开
标题翻译：多肽
公开(公告)号：US20140087995A1
公开(公告)日：2014-03-27
申请号：US14035501
申请日：2013-09-24
申请人： NOVO NORDISK A/S
发明人： Kirsten Dahl , Lauge Schaeffer , Thomas Kruse
IPC分类号： C07K14/47
CPC分类号： C07K14/47 , C07K14/575
摘要： The invention relates to polypeptides comprising an amino acid sequence which is an analogue of human amylin, pharmaceutical compositions comprising these polypeptides, and these polypeptides for use as medicaments.
摘要翻译：本发明涉及包含作为人胰岛淀粉样多肽的类似物的氨基酸序列的多肽，包含这些多肽的药物组合物，以及用作药物的这些多肽。

5. 发明申请

US20140018286A1 AMYLIN ANALOGUES AND PHARMACEUTICAL COMPOSITIONS THEREOF 有权
标题翻译： AMYLIN类似物及其药物组合物
公开(公告)号：US20140018286A1
公开(公告)日：2014-01-16
申请号：US14038265
申请日：2013-09-26
申请人： Novo Nordisk A/S
发明人： Lauge Schaeffer , Thomas Kruse , Henning Thoegersen
IPC分类号： C07K14/575
CPC分类号： C07K14/57527 , A61K38/00 , A61K38/225 , A61K45/06 , A61K47/542 , A61K47/643 , C07K14/575 , Y10S514/909
摘要： The invention relates to polypeptides comprising an amino acid sequence which is an analogue of pramlintide, pharmaceutical compositions comprising these polypeptides, and these polypeptides for use as medicaments.
摘要翻译：本发明涉及包含氨基酸序列的多肽，其是普兰林肽的类似物，包含这些多肽的药物组合物，以及用作药物的这些多肽。

6. 发明公开

US20240279299A1 CO-AGONISTS OF THE GLP-1 AND AMYLIN RECEPTORS 审中-公开
公开(公告)号：US20240279299A1
公开(公告)日：2024-08-22
申请号：US18591754
申请日：2024-02-29
申请人： Novo Nordisk A/S
发明人： Thomas Kruse , Anne Louise Bank Kodal , Johnny Madsen , Soeren Oestergaard , Wouter Frederik Johan Hogendorf , Christian Wenzel Tornoee , Lauge Schaeffer , Alice Ravn Madsen
IPC分类号： C07K14/605 , A61K47/54 , A61P3/04 , C07K14/575
CPC分类号： C07K14/605 , A61K47/542 , A61P3/04 , C07K14/575 , C07K2319/00
摘要： The invention relates to a compound comprising a GLP-1 receptor agonist and an amylin receptor agonist. The invention also relates to a pharmaceutical formulation, suitable for but not limited to oral administration, which comprises such a compound. The compound and pharmaceutical formulation comprising it may be used for the medical treatment of subjects with overweight, obesity and associated co-morbidities.

7. 发明授权

US10174082B2 Amylin and calcitonin receptor agonist 有权
公开(公告)号：US10174082B2
公开(公告)日：2019-01-08
申请号：US15417671
申请日：2017-01-27
申请人： Novo Nordisk A/S
发明人： Thomas Kruse , Lauge Schaeffer , Kirsten Dahl , Christian Poulsen , Kirsten Raun
IPC分类号： A61K38/00 , A61K38/16 , C07K14/00 , C07K14/575
摘要： The present invention relates to peptides comprising an amino acid sequence SEQ ID NO: 1 (EASELSTAALGRLSAELHELATLPRTETGPESP), analogs and derivatives thereof and pharmaceutical compositions comprising such peptides and derivatives. This invention further regards the use of these peptides according to SEQ ID NO: 1, analogs and derivatives thereof as medicaments.

8. 发明申请

US20170145059A1 Novel Amylin And Calcitonin Receptor Agonist 审中-公开
公开(公告)号：US20170145059A1
公开(公告)日：2017-05-25
申请号：US15417671
申请日：2017-01-27
申请人： Novo Nordisk A/S
发明人： Thomas Kruse , Lauge Schaeffer , Kirsten Dahl , Christian Poulsen , Kirsten Raun
IPC分类号： C07K14/00
CPC分类号： C07K14/001 , A61K38/00 , C07K14/575
摘要： The present invention relates to peptides comprising an amino acid sequence SEQ ID NO: 1 (EASELSTAALGRLSAELHELATLPRTETGPESP), analogues and derivatives thereof and pharmaceutical compositions comprising such peptides and derivatives. This invention further regards the use of these peptides according to SEQ ID NO: 1, analogues and derivatives thereof as medicaments.

9. 发明申请

US20150025003A1 GLUCAGON-LIKE PEPTIDE-1 DERIVATIVES AND THEIR PHARMACEUTICAL USE 审中-公开
标题翻译： GLUCAGON-LIKE PEPTIDE-1衍生物及其药物用途
公开(公告)号：US20150025003A1
公开(公告)日：2015-01-22
申请号：US14506052
申请日：2014-10-03
申请人： Novo Nordisk A/S
发明人： Jane Spetzler , Lauge Schaeffer , Jesper Lau , Thomas Kruse , Patrick W. Garibay , Steffen Reedtz-Runge , Henning Thoegersen , Ingrid Pettersson
IPC分类号： C07K14/605 , A61K38/26
CPC分类号： C07K14/605 , A61K38/26
摘要： The invention relates to protracted Glucagon-Like Peptide-1 (GLP-1) derivatives and therapeutic uses thereof. The GLP-1 derivative of the invention comprises a modified GLP-1(7-37) sequence having a total of 2-12 amino acid modifications, including Glu22 and Arg26, and being derivatised with an albumin binding residue or pegylated in position 18, 20, 23, 30, 31, 34, 36, 37, or 39. These compounds are useful in the treatment or prevention of diabetes type 2 and related diseases. The compounds are potent, stable, have long half-lives, a high affinity of binding to albumin, and/or a high affinity of binding to the extracellular domain of the GLP-1 receptor (GLP-1R), all of which is of potential relevance for the overall aim of achieving long-acting, stable and active GLP-1 derivatives with a potential for once weekly administration.
摘要翻译：本发明涉及长效的胰高血糖素样肽-1（GLP-1）衍生物及其治疗用途。本发明的GLP-1衍生物包含具有总共2-12个氨基酸修饰的修饰的GLP-1（7-37）序列，包括Glu22和Arg26，并用白蛋白结合残基衍生或在18位聚乙二醇化， 20,23,30,31,34,36,37或39.这些化合物可用于治疗或预防2型糖尿病和相关疾病。该化合物是有效的，稳定的，具有长的半衰期，与白蛋白结合的高亲和力，和/或与GLP-1受体（GLP-1R）细胞外结构域结合的高亲和力，所有这些都是对于实现长效，稳定和活性的GLP-1衍生物的总体目标的潜在相关性，具有每周一次行政的潜力。

10. 发明申请

US20130281363A1 POLYPEPTIDES 有权
公开(公告)号：US20130281363A1
公开(公告)日：2013-10-24
申请号：US13930075
申请日：2013-06-28
申请人： NOVO NORDISK A/S
发明人： Kirsten Dahl , Lauge Schaeffer , Thomas Kruse
IPC分类号： C07K14/575
CPC分类号： C07K14/47 , C07K14/575
摘要： The invention relates to polypeptides comprising an amino acid sequence which is an analogue of human amylin, pharmaceutical compositions comprising these polypeptides, and these polypeptides for use as medicaments.
摘要翻译：本发明涉及包含作为人胰岛淀粉样多肽的类似物的氨基酸序列的多肽，包含这些多肽的药物组合物，以及用作药物的这些多肽。

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