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1. 发明申请

US20220184184A1 GLUCOSE SENSITIVE INSULIN DERIVATIVES 有权
公开(公告)号：US20220184184A1
公开(公告)日：2022-06-16
申请号：US17598010
申请日：2020-03-27
申请人： Novo Nordisk A/S
发明人： Thomas Hoeg-Jensen , Carsten Behrens , Emiliano Clo , Martin Werner Borchsenius Muenzel , Per Sauerberg , Thomas Kruse , Jane Spetzler , Ulrich Sensfuss , Claudia Ulrich Hjoerringgaard , Henning Thoegersen , Vojtech Balsanek , Zuzana Drobnakova , Ladislav Droz , Miroslav Havranek , Vladislav Kotek , Milan Stengl , Ivan Snajdr , Hana Drusanova
IPC分类号： A61K38/28 , A61K47/54 , A61K47/56 , A61P3/10
摘要： The present invention relates to novel insulin derivatives and their use in the treatment or prevention of medical conditions relating to diabetes. The insulin derivatives are glucose sensitive and display glucose-sensitive albumin binding. The invention also relates to novel intermediates. Finally, the invention provides a pharmaceutical composition comprising the insulin derivatives of the invention and the use of such a composition in the treatment or prevention of medical conditions relating to diabetes.

2. 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。

3. 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.

4. 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。

5. 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。

6. 发明申请

US20160102129A1 Stable GLP-1 Based GLP-1/Glucagon Receptor Co-Agonists 有权
标题翻译：稳定的基于GLP-1的GLP-1 /胰高血糖素受体共激动剂
公开(公告)号：US20160102129A1
公开(公告)日：2016-04-14
申请号：US14879428
申请日：2015-10-09
申请人： Novo Nordisk A/S
发明人： Steffen Reedtz-Runge , Ulrich Sensfuss , Thomas Kruse , Jane Spetzler , Henning Thoegersen , Christian W. Tornoee , Jesper F. Lau
IPC分类号： C07K14/605
CPC分类号： C07K14/605 , A61K38/00
摘要： New GLP-1 derivatives, compositions thereof and their use in medicine.
摘要翻译：新的GLP-1衍生物，其组合物及其在医学上的应用。

7. 发明申请

US20140179899A1 DOUBLE-ACYLATED GLP-1 DERIVATIVES 有权
标题翻译：双取代的GLP-1衍生物
公开(公告)号：US20140179899A1
公开(公告)日：2014-06-26
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 , Janos Tibor Kodra , Lars Linderoth , Jesper Lau , Per Sauerberg
IPC分类号： 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：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37位的位置处的第一个K残基，相对于GLP-1（7-37）的位置26的位置和与GLP-1（7-37）相比最多10个氨基酸修饰，其中第一个K残基指定为K37，第二个K残基是命名为K26，该衍生物分别包含与K26和K37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下列的伸长部分： 1，Chem。 2，Chem。 3或Chem。 4; 或其药学上可接受的盐，酰胺或酯。

8. 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.

9. 发明申请

US20210221867A1 Compounds Capable of Binding to Melanocortin 4 Receptor 有权
公开(公告)号：US20210221867A1
公开(公告)日：2021-07-22
申请号：US17055347
申请日：2019-05-15
申请人： Novo Nordisk A/S
发明人： Kilian Waldemar Conde Frieboes , Jane Spetzler , Christian Wenzel Tornoee , Line Marie Nielsen
IPC分类号： C07K14/68
摘要： The present invention relates to novel peptide compounds which are effective as melanocortin 4 receptor agonists, to the use of the compounds in medicine, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds for the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of overweight and obesity as well as a variety of diseases or conditions associated with obesity.

10. 发明申请

US20140011732A1 Peptides Derivatized with A-B-C-D- and their Therapeutical Use 审中-公开
标题翻译：用A-B-C-D衍生的肽及其治疗用途
公开(公告)号：US20140011732A1
公开(公告)日：2014-01-09
申请号：US13930079
申请日：2013-06-28
申请人： NOVO NORDISK A/S
发明人： Jane Spetzler , Lauge Schaeffer , Jesper Lau , Thomas Kruse , Patrick William Garibay , Soeren Oestergaard , Steffen Reedtz-Runge , Henning Thoegersen
IPC分类号： C07K14/00
CPC分类号： C07K14/001 , A61K38/00 , A61K38/16 , A61K38/17 , A61K38/22 , A61K38/26 , A61K47/50 , A61K47/51 , A61K47/54 , A61K47/542 , A61K47/543 , A61K47/545 , A61K47/56 , A61K47/60 , C07K14/00 , C07K14/575 , C07K14/57563 , C07K14/605
摘要： The invention relates to protracted peptide derivatives such as Glucagon-Like Peptide-1 (GLP-1), exendin-4, and analogues thereof, as well as therapeutic uses thereof. The peptide derivative of the invention comprises a peptide wherein at least one amino acid residue is derivatized with A-B—C—, or A-B—C-D-. These compounds are useful in the treatment or prevention of diabetes type 2 and related diseases. The compounds are potent, have a low ratio of binding affinity to the GLP-1 receptor in the presence of high/low albumin concentrations, have long half-lives, and have a high affinity of binding to albumin, 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：本发明涉及长时间肽衍生物如胰高血糖素样肽-1（GLP-1），毒蜥外泌肽-4及其类似物，以及其治疗用途。本发明的肽衍生物包含肽，其中至少一个氨基酸残基用A-B-C-或A-B-C-D-衍生化。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，在高/低白蛋白浓度存在下具有低的GLP-1受体结合亲和力比，具有长的半衰期，并且具有与白蛋白结合的高亲和力，所有这些都是潜在的与实现长效，稳定和活跃的GLP-1衍生物的总体目标相关，具有每周行政一次的潜力。

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