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21. 发明申请

US20100216715A1 FGF21 Derivatives With Albumin Binder A-B-C-D-E- And Their Use 有权
标题翻译： FGF21衍生物与白蛋白粘合剂A-B-C-D-E-及其用途
公开(公告)号：US20100216715A1
公开(公告)日：2010-08-26
申请号：US12692227
申请日：2010-01-22
申请人： Tina Møller Tagmose , Patrick William Garibay , Bírgítte Andersen , Jishu Wang , Kílían Waldemar Conde-Frieboes , Kristían Sass Bak-Jensen , Henning Thøgersen , Helle Wöldike , Peter Kresten Nielsen , Rita Slaaby , Xujia Zhang , Birgit Wieczorek
发明人： Tina Møller Tagmose , Patrick William Garibay , Bírgítte Andersen , Jishu Wang , Kílían Waldemar Conde-Frieboes , Kristían Sass Bak-Jensen , Henning Thøgersen , Helle Wöldike , Peter Kresten Nielsen , Rita Slaaby , Xujia Zhang , Birgit Wieczorek
IPC分类号： A61K38/18 , C07K14/50 , A61P3/00 , A61P3/04 , A61P9/00
CPC分类号： A61K47/48046 , A61K38/00 , A61K47/543 , A61K47/60 , A61K47/643 , C07K14/50
摘要： The present invention relates to Fibroblast Growth Factor 21 (FGF21), more in particular to derivatives of FGF21 compounds having an albumin binder of the formula A-B-C-D-E- covalently attached. The invention also relates to novel FGF21 analogues, as well as to the pharmaceutical use of these FGF21 derivatives and analogues, in particular for the treatment of diabetes, dyslipidemia, obesity, cardiovascular diseases, metabolic syndrome, and/or Non Alcoholic Fatty Liver Disease (NAFLD). The derivatives of the invention are protracted, e.g. capable of maintaining a low blood glucose level for a longer period of time, capable of increasing the in vivo half-life of FGF21, and/or result in a lower clearance of FGF21. The derivatives of the invention are preferably furthermore of an improved oxidative stability.
摘要翻译：本发明涉及成纤维细胞生长因子21（FGF21），更具体地涉及具有共价连接的式A-B-C-D-E-的白蛋白结合物的FGF21化合物的衍生物。本发明还涉及新型FGF21类似物，以及这些FGF21衍生物和类似物的药物用途，特别是用于治疗糖尿病，血脂异常，肥胖症，心血管疾病，代谢综合征和/或非酒精性脂肪肝病（ NAFLD）。本发明的衍生物是延长的，例如。能够维持较长时间的低血糖水平，能够增加FGF21的体内半衰期，和/或导致FGF21的较低清除率。本发明的衍生物优选还具有改善的氧化稳定性。

22. 发明申请

US20090137454A1 Insulin Derivatives 有权
标题翻译：胰岛素衍生物
公开(公告)号：US20090137454A1
公开(公告)日：2009-05-28
申请号：US12280851
申请日：2007-02-27
申请人： Charlotte Harkjaer Fynbo , Ib Jonassen , Thomas Borglum Kjeldsen , Peter Madsen , Patrick William Garibay , Janos Tibor Kodra , Thomas Hoeg-Jensen , Tina Moller Tagmose
发明人： Charlotte Harkjaer Fynbo , Ib Jonassen , Thomas Borglum Kjeldsen , Peter Madsen , Patrick William Garibay , Janos Tibor Kodra , Thomas Hoeg-Jensen , Tina Moller Tagmose
IPC分类号： A61K38/28 , C07K14/62
CPC分类号： C07K14/62 , A61K38/00
摘要： The present invention is related to insulin derivatives having a side chain attached to an ε-amino group of a Lys residue present in the A-chain or to an ε-amino group of a Lys residue in the B-chain.
摘要翻译：本发明涉及具有连接于存在于A链中的Lys残基的ε-氨基侧链或B链中Lys残基的ε-氨基的侧链的胰岛素衍生物。

23. 发明授权

US09758560B2 GLP-1 derivatives 有权
公开(公告)号：US09758560B2
公开(公告)日：2017-09-12
申请号：US14343152
申请日：2012-09-06
申请人： Jesper Lau , Paw Bloch , Patrick William Garibay
发明人： Jesper Lau , Paw Bloch , Patrick William Garibay
IPC分类号： C07K14/605 , A61K38/26 , A61K38/00
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 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.

24. 发明授权

US09732137B2 Semi-recombinant preparation of GLP-1 analogues 有权
公开(公告)号：US09732137B2
公开(公告)日：2017-08-15
申请号：US12810934
申请日：2008-12-22
申请人： Jesper Færgeman Lau , Asser Sloth Andersen , Paw Bloch , Jesper Lau , Patrick William Garibay , Thomas Kruse , Inga Sig Nielsen Nørby , Claus Ulrich Jessen , Caspar Christensen , Jens Christian Norrild
发明人： Jesper Færgeman Lau , Asser Sloth Andersen , Paw Bloch , Jesper Lau , Patrick William Garibay , Thomas Kruse , Inga Sig Nielsen Nørby , Claus Ulrich Jessen , Caspar Christensen , Jens Christian Norrild
IPC分类号： C07K14/605 , C07K1/107 , C07K1/02 , C07K1/06 , C07K1/36 , C07K1/00
CPC分类号： C07K14/605 , C07K1/006 , C07K1/02 , C07K1/061 , C07K1/107 , C07K1/1077
摘要： A semi-recombinant method for the production of GLP-1 analogues and derivatives with non-proteogenic amino acids in the N-terminal part combining the use of recombinant expression techniques and chemical peptide synthesis.

25. 发明授权

US09150633B2 Insulin analogues with an acyl and alkylene glycol moiety 有权
标题翻译：具有酰基和亚烷基二醇部分的胰岛素类似物
公开(公告)号：US09150633B2
公开(公告)日：2015-10-06
申请号：US12673516
申请日：2008-08-15
申请人： Peter Madsen , Thomas Børglum Kjeldsen , Thomas Hoeg-Jensen , Tina Møller Tagmose , Palle Jakobsen , János Tibor Kodra , Patrick William Garibay , Dorte Xenia Gram
发明人： Peter Madsen , Thomas Børglum Kjeldsen , Thomas Hoeg-Jensen , Tina Møller Tagmose , Palle Jakobsen , János Tibor Kodra , Patrick William Garibay , Dorte Xenia Gram
IPC分类号： C07K14/62 , A61K38/00
CPC分类号： C07K14/62 , A61K38/00
摘要： An acylated insulin analogue wherein the insulin analogue comprises a lysine residue connected C-terminally to the A21 amino acid residue or a peptide residue of up to 4 amino acid residues comprising a lysine residue which peptide residue is connected C-terminally to the A21 amino acid residue, characterized in that an acyl moiety comprising an alkylene glycol moiety is attached to the lysine residue in the A22 position or attached to a lysine residue present in the peptide residue that is attached to the C terminal end of the A21 amino acid residue and wherein there is only one lysine (K, Lys) in the insulin analogue, can conveniently be administered pulmonary.
摘要翻译：酰化胰岛素类似物，其中胰岛素类似物包含与A21氨基酸残基C末端连接的赖氨酸残基或至多包含赖氨酸残基的至多4个氨基酸残基的肽残基，所述肽残基与C21末端连接至A21氨基酸残基，其特征在于包含亚烷基二醇部分的酰基部分连接到A22位置的赖氨酸残基，或连接到与A21氨基酸残基的C末端连接的肽残基中存在的赖氨酸残基，并且其中胰岛素类似物中只有一个赖氨酸（K，Lys），可方便地给予肺部。

26. 发明申请

US20140303083A1 GLP-1 Derivatives 有权
标题翻译： GLP-1衍生物
公开(公告)号：US20140303083A1
公开(公告)日：2014-10-09
申请号：US14343152
申请日：2012-09-06
申请人： Jesper Lau , Paw Bloch , Jacob Kofoed , Patrick William Garibay
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 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。

27. 发明授权

US08691759B2 Protease stabilized, acylated insulin analogues 有权
标题翻译：蛋白酶稳定，酰化胰岛素类似物
公开(公告)号：US08691759B2
公开(公告)日：2014-04-08
申请号：US12922117
申请日：2009-03-13
申请人： Peter Madsen , Thomas Boerglum Kjeldsen , Thomas Hoeg-Jensen , Palle Jakobsen , Tina Moeller Tagmose , Janos Tibor Kodra , Patrick William Garibay
发明人： Peter Madsen , Thomas Boerglum Kjeldsen , Thomas Hoeg-Jensen , Palle Jakobsen , Tina Moeller Tagmose , Janos Tibor Kodra , Patrick William Garibay
IPC分类号： A61K38/28 , A61P3/10
CPC分类号： C07K14/62 , A61K38/00
摘要： Novel acylated insulin analogues exhibiting resistance towards proteases can, effectively, be administered pulmonary or orally. The insulin analogues contain B25H and A14E or A14H.
摘要翻译：对蛋白酶具有抗性的新型酰化胰岛素类似物可以有效地被肺或口服给药。胰岛素类似物含有B25H和A14E或A14H。

28. 发明申请

US20120329711A1 GLP-1 RECEPTOR AGONIST COMPOUNDS WITH A MODIFIED N-TERMINUS 审中-公开
标题翻译：具有修饰的N末端的GLP-1受体激动剂化合物
公开(公告)号：US20120329711A1
公开(公告)日：2012-12-27
申请号：US13516311
申请日：2010-12-16
申请人： Janos Tibor Kodra , Johnny Madsen , Patrick William Garibay
发明人： Janos Tibor Kodra , Johnny Madsen , Patrick William Garibay
IPC分类号： C07K14/605 , A61P3/10 , C07C57/30 , A61K38/26 , C07D233/64 , C07D213/56
CPC分类号： C07K14/65 , A61K38/00 , A61K47/542 , A61K47/60 , C07K14/605 , G01N2333/605
摘要： The invention relates to GLP-1 receptor agonist compounds with a modified N-terminus. The compounds are of the formula Chem. 1: Y—Z—P, wherein P represents a fragment of a GLP-1 receptor agonist peptide lacking the two N-terminal amino acid residues; and Y—Z represents novel His-Ala mimetics. Examples of GLP-1 receptor agonist compounds are derived from human GLP-1 (7-37), exendin-4(1-39), or GLP-1 A (1-37). The invention also relates to derivatives of these compounds, in particular compounds with one or more albumin binding side chains capable of protracting the duration of action in vivo of these compounds. The peptides and derivatives of the invention have a good potency, a protracted pharmacokinetic profile, are stable against degradation by gastro intestinal enzymes, and/or have a high oral bioavailability. These properties are of importance in the development of GLP-1 receptor agonist compounds for subcutaneous, intravenous, and/or in particular oral administration. The invention also relates to intermediate products for use in the preparation of the GLP-1 receptor agonist compounds of the invention.
摘要翻译：本发明涉及具有修饰的N-末端的GLP-1受体激动剂化合物。化合物具有化学式为Chem。 1：Y-Z-P，其中P表示缺少两个N-末端氨基酸残基的GLP-1受体激动剂肽的片段; Y-Z代表新型His-Ala模拟物。 GLP-1受体激动剂化合物的实例来源于人GLP-1（7-37），毒蜥外泌肽-4（1-39）或GLP-1A（1-37）。本发明还涉及这些化合物的衍生物，特别是具有能够延长这些化合物的体内作用持续时间的一种或多种白蛋白结合侧链的化合物。本发明的肽和衍生物具有良好的效力，延长的药代动力学特征对于胃肠酶的降解是稳定的，和/或具有高的口服生物利用度。这些性质在用于皮下，静脉内和/或特别是口服给药的GLP-1受体激动剂化合物的开发中是重要的。本发明还涉及用于制备本发明的GLP-1受体激动剂化合物的中间产物。

29. 发明申请

US20120208749A1 Insulin derivatives 有权
标题翻译：胰岛素衍生物
公开(公告)号：US20120208749A1
公开(公告)日：2012-08-16
申请号：US13506292
申请日：2012-04-09
申请人： Patrick William Garibay , Thomas Hoeg-Jensen , Ib Jonassen , Svend Havelund , Peter Madsen , Palle Jakobsen
发明人： Patrick William Garibay , Thomas Hoeg-Jensen , Ib Jonassen , Svend Havelund , Peter Madsen , Palle Jakobsen
IPC分类号： A61K38/28 , A61P3/10 , C07K14/62
CPC分类号： A61K47/48215 , A61K38/00 , A61K47/60 , C07K14/62
摘要： The present invention is related to insulin derivatives having a side chain attached either to the α-amino group of the N-terminal amino acid residue of B chain or to an ε-amino group of a Lys residue present in the B chain of the parent insulin molecule via an amide bond which side chain comprises one or more residues of ethyleneglycol, propyleneglycol and/or butyleneglycol containing independently at each termini a group selected from —NH2 and —COOH; a fatty diacid moiety with 4 to 22 carbon atoms, at least one free carboxylic acid group or a group which is negatively charged at neutral pH; and possible linkers which link the individual components in the side chain together via amide or ether bonds, said linkers optionally comprising a free carboxylic acid group.
摘要翻译：本发明涉及具有侧链连接到B链的N末端氨基酸残基的α-氨基或存在于B链的B链中的Lys残基的亚氨基的胰岛素衍生物母体胰岛素分子通过酰胺键，该侧链包含在每个末端独立地含有选自-NH 2和-COOH的一个或多个乙二醇，丙二醇和/或丁二醇残基; 具有4至22个碳原子的脂肪二酸部分，至少一个游离羧酸基团或在中性pH下带负电荷的基团; 以及通过酰胺或醚键将侧链中各个组分连接在一起的可能接头，所述接头任选地包含游离羧酸基团。

30. 发明申请

US20120035104A1 Insulin derivatives 有权
标题翻译：胰岛素衍生物
公开(公告)号：US20120035104A1
公开(公告)日：2012-02-09
申请号：US13273659
申请日：2011-10-14
申请人： Janos Tibor Kodra , Patrick William Garibay , Thomas Hoeg-Jensen , Ib Jonassen , Peter Madsen , Tina Moeller Tagmose
发明人： Janos Tibor Kodra , Patrick William Garibay , Thomas Hoeg-Jensen , Ib Jonassen , Peter Madsen , Tina Moeller Tagmose
IPC分类号： A61K38/28 , A61P3/10 , C07K14/62
CPC分类号： A61K38/28 , C07K14/62
摘要： The present invention relates to insulin derivatives having a side chain attached either to the α-amino group of the N-terminal amino acid residue of the B chain or to the ε-amino group of a Lys residue present in the B chain of the parent insulin via an amide bond which side chain comprises at least one aromatic group; at least one free carboxylic acid group or a group which is negatively charged at neutral pH, a fatty acid moiety with 4 to 22 carbon atoms in the carbon chain; and possible linkers which link the individual components in the side chain together via amide bonds.
摘要翻译：本发明涉及具有侧链连接到B链的N末端氨基酸残基的α-氨基或存在于B链的B链中的Lys残基的' - 氨基的胰岛素衍生物通过酰胺键的母体胰岛素，该侧链包含至少一个芳族基团; 至少一个游离羧酸基团或在中性pH下带负电荷的基团，碳链中具有4-22个碳原子的脂肪酸部分; 以及通过酰胺键将侧链中各个组分连接在一起的可能接头。

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