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1. 发明申请

WO2009083549A1 SEMI-RECOMBINANT PREPARATION OF GLP-1 ANALOGUES 审中-公开
标题翻译： GLP-1类似物的半重复制备
公开(公告)号：WO2009083549A1
公开(公告)日：2009-07-09
申请号：PCT/EP2008/068211
申请日：2008-12-22
申请人： NOVO NORDISK A/S , LAU, Jesper Færgeman , ANDERSEN, Asser Sloth , BLOCH, Paw , LAU, Jesper , GARIBAY, Patrick William , KRUSE, Thomas , NØRBY, Inga Sig Nielsen , JESSEN, Claus Ulrich , CHRISTENSEN, Caspar , NORRILD, Jens Christian
发明人： LAU, Jesper Færgeman , ANDERSEN, Asser Sloth , BLOCH, Paw , LAU, Jesper , GARIBAY, Patrick William , KRUSE, Thomas , NØRBY, Inga Sig Nielsen , JESSEN, Claus Ulrich , CHRISTENSEN, Caspar , NORRILD, Jens Christian
IPC分类号： C07K1/10 , C07K14/605
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.
摘要翻译：在重组表达技术和化学肽合成的N末端部分中用于生产具有非蛋白质氨基酸的GLP-1类似物和衍生物的半重组方法。

2. 发明申请

WO2006097537A2 ACYLATED GLP-1 COMPOUNDS 审中-公开
标题翻译：酰化GLP-1化合物
公开(公告)号：WO2006097537A2
公开(公告)日：2006-09-21
申请号：PCT/EP2006/060855
申请日：2006-03-20
申请人： NOVO NORDISK A/S , LAU, Jesper , DÖRWALD, Florencio Zaragoza , STEPHENSEN, Henrik , BLOCH, Paw , HANSEN, Thomas, Kruse , MADSEN, Kjeld
发明人： LAU, Jesper , DÖRWALD, Florencio Zaragoza , STEPHENSEN, Henrik , BLOCH, Paw , HANSEN, Thomas, Kruse , MADSEN, Kjeld
IPC分类号： C07K14/605 , A61K38/26 , A61K47/48
CPC分类号： C07K14/605 , A61K38/00
摘要： Protracted GLP-1 compounds and therapeutic uses thereof.
摘要翻译：延长的GLP-1化合物及其治疗用途。

3. 发明申请

WO2004002481A1 ARYL CARBONYL DERIVATIVES AS THERAPEUTIC AGENTS 审中-公开
标题翻译：作为治疗剂的ARYL CARBONYL衍生物
公开(公告)号：WO2004002481A1
公开(公告)日：2004-01-08
申请号：PCT/DK2003/000449
申请日：2003-06-27
申请人： NOVO NORDISK A/S , POLISETTI, Dharma, Rao , KODRA, János, Tibor , LAU, Jesper , BLOCH, Paw , VALCARCE-LÓPEZ,Maria,Carmen, , BLUME, Niels , GUZEL, Mustafa , SANTHOSH, Kalpathy, Chidambareswaran , MJALLI, Adnan, M., M. , ANDREWS, Robert, Carl , SUBRAMANIAN, Govindan , ANKERSEN, Michael , VEDSØ, Per , MURRAY, Anthony , JEPPESEN, Lone
发明人： POLISETTI, Dharma, Rao , KODRA, János, Tibor , LAU, Jesper , BLOCH, Paw , VALCARCE-LÓPEZ,Maria,Carmen, , BLUME, Niels , GUZEL, Mustafa , SANTHOSH, Kalpathy, Chidambareswaran , MJALLI, Adnan, M., M. , ANDREWS, Robert, Carl , SUBRAMANIAN, Govindan , ANKERSEN, Michael , VEDSØ, Per , MURRAY, Anthony , JEPPESEN, Lone
IPC分类号： A61K31/433
CPC分类号： C07D277/38 , A61K31/426 , A61K31/427 , A61K31/454 , A61K31/55 , A61K45/06 , C07D213/75 , C07D277/46 , C07D277/48 , C07D277/52 , C07D277/54 , C07D277/56 , C07D285/135 , C07D417/06 , C07D417/12 , C07D417/14 , C07D473/38
摘要： This invention relates to aryl carbonyl derivatives of the general formula (I), which are activators of glucokinase which may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.(Formul 1).
摘要翻译：本发明涉及通式（I）的芳基羰基衍生物，其是可用于治疗，治疗，控制或辅助治疗疾病的葡萄糖激酶的活化剂，其中葡萄糖激酶活性增加是有益的（Formul 1）。

4. 发明申请

WO2013037690A1 GLP-1 DERIVATIVES 审中-公开
标题翻译： GLP-1衍生物
公开(公告)号：WO2013037690A1
公开(公告)日：2013-03-21
申请号：PCT/EP2012/067364
申请日：2012-09-06
申请人： NOVO NORDISK A/S , LAU, Jesper , BLOCH, Paw , KOFOED, Jacob , GARIBAY, Patrick
发明人： LAU, Jesper , BLOCH, Paw , KOFOED, Jacob , GARIBAY, Patrick
IPC分类号： C07K14/605 , A61K38/26
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-(CH 2 ) x -CO-*, and Chem. 16: HOOC-C 6 H 4 -O-(CH 2 ) 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(CH 2 OH)-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-C 6 H 4 -O-（CH 2）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。

5. 发明申请

WO2005027978A3 ALBUMIN-BINDING DERIVATIVES OF THERAPEUTIC PEPTIDES 审中-公开
公开(公告)号：WO2005027978A3
公开(公告)日：2005-03-31
申请号：PCT/DK2004/000624
申请日：2004-09-17
申请人： NOVO NORDISK A/S , LAU, Jesper , HANSEN, Thomas Kruse , MADSEN, Kjeld , BLOCH, Paw , DÖRWALD, Florencio Zaragoza , JOHANSEN, Nils Langeland
发明人： LAU, Jesper , HANSEN, Thomas Kruse , MADSEN, Kjeld , BLOCH, Paw , DÖRWALD, Florencio Zaragoza , JOHANSEN, Nils Langeland
IPC分类号： A61K47/48
摘要： Novel polypeptide derivatives having protracted profile of action. The present invention relates to a compound which comprises a therapeutic polypeptide linked to an albumin binding residue via a hydrophilic spacer. The present invention also relates to a compound which comprises a therapeutic polypeptide linked to an albumin binding residue via a hydrophilic spacer that separates the polypeptide and the albumin binding residue with a chemical moiety comprising at least 5 non-hydrogen atoms where 30-50% of these atoms are either N or O. In one embodiment of this invention the spacer is defined as -(CH 2 ) l D[(CH 2 ) n E] m (CH 2 ) p Q q -, wherein l, m and n independently are 1-20 and p is 0-10, Q is -Z-(CH 2 ) l D[(CH 2 ) n G] m (CH 2 ) p -, q is an integer in the range from 0 to 5, each D, E and G independently are selected from -O-, NR 3 -, -N(COR 4 )-, -PR 5 (O)-, and -P(OR 6 )(O)-, wherein R 3 , R 4 , R 5 , and R 6 independently represent hydrogen or C 1-6 -alky, Z is selected from -C(O)NH-, -C(O)NHCH 2 -, -OC(O)NH-, -C(O)NHCH 2 CH 2 -, -C(O)CH 2 -, -C(O)CH=CH-, -(CH 2 ) s -, -C(O)-, -C(O)O- or -NHC(O)-, wherein s is 0 or 1.

6. 发明申请

WO2005014049A2 SYNTHESIS AND APPLICATION OF NEW STRUCTURAL WELL DEFINED BRANCHED POLYMERS AS CONJUGATING AGENTS FOR PEPTIDES 审中-公开
标题翻译：新型结构良好支化聚合物作为肽偶联剂的合成与应用
公开(公告)号：WO2005014049A2
公开(公告)日：2005-02-17
申请号：PCT/DK2004/000531
申请日：2004-08-09
申请人： NOVO NORDISK A/S , BEHRENS, Carsten , DÖRWALD, Florencio Zaragoza , KOFOD-HANSEN, Mikael , LAU, Jesper , KODRA, János Tibor , HANSEN, Thomas Kruse , BLOCH, Paw
发明人： BEHRENS, Carsten , DÖRWALD, Florencio Zaragoza , KOFOD-HANSEN, Mikael , LAU, Jesper , KODRA, János Tibor , HANSEN, Thomas Kruse , BLOCH, Paw
IPC分类号： A61K47/48
CPC分类号： A61K38/26 , A61K38/4846 , A61K47/60 , C12Y304/21021
摘要： The invention provides synthesis and application of new structural well defined branched polymers as protraction agents for peptide and protein.
摘要翻译：本发明提供了作为肽和蛋白质的延缓剂的新的结构明确限定的支化聚合物的合成和应用。

7. 发明申请

WO2015155151A1 DOUBLE-ACYLATED GLP-1 COMPOUNDS 审中-公开
标题翻译：双酚A-GLP-1化合物
公开(公告)号：WO2015155151A1
公开(公告)日：2015-10-15
申请号：PCT/EP2015/057442
申请日：2015-04-07
申请人： NOVO NORDISK A/S
发明人： LINDEROTH, Lars , KOFOED, Jacob , LAU, Jesper , BLOCH, Paw , GARIBAY, Patrick William , KODRA, János Tibor
IPC分类号： A61K38/26 , C07K14/605
CPC分类号： C07K14/605 , A61K38/00 , 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-C 6 H 4 -0-(CH 2 ) y -CO-*, and Chem. 2: HOOC-(CH 2 ) 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)-(CH 2 ) 2 -CO-*, Chem. 4: *-NH-CH((CH 2 ) 2 -COOH)-CO-*, and/or Chem. 5: *-NH-(CH 2 ) 2 -[0-(CH 2 ) 2 ] k -0-[CH 2 ] 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.
摘要翻译：本发明涉及GLP-1肽的衍生物，该肽在对应于GLP-1（7-37）（SEQ ID NO：1）的位置36的位置处的第一个Lys残基，与GLP-1（7-37）（SEQ ID NO：1）相比，对应于GLP-1（7-37）的位置37（SEQ ID NO：1）的位置和最多7个氨基酸的变化。该衍生物分别包含分别连接到所述第一和第二Lys残基的两个量角器，每个通过连接体连接; 其中所述量角器选自：Chem。 1：HOOC-C6H4-0-（CH2）y-CO- *，和Chem。 2：HOOC-（CH 2）x -CO- *，其中y是8-11的整数，x是12; 并且所述接头包含以下至少一种：Chem。 3：* -NH-CH（COOH） - （CH 2）2 -CO- *， 4：* -NH-CH（（CH 2）2 -COOH）-CO- *，和/或Chem。 5：* -NH-（CH2）2- [0-（CH2）2] k-0- [CH2] n-CO- *，其中k是1-5的整数，n是整数在1-5的范围内; 或其药学上可接受的盐，酰胺或酯。本发明还涉及其药学用途，例如用于治疗糖尿病和肥胖症，以及形成这些衍生物的一部分的GLP-1肽，其在36和37位具有Lys残基且没有其它Lys残基，以及 GLP-1（9-37）片段。本发明还涉及包含3-羧基苯氧基 - 壬酸与壬酸羧基上的保护基团的中间产物，任选地通过连接体。衍生物具有非常好的效力和长的半衰期，这使得它们可能用于例如口服给药。

8. 发明申请

WO2004002480A1 NOVEL GLUCAGON ANTAGONISTS/INVERSE AGONISTS 审中-公开
标题翻译：新的GLUCAGON ANTAGONISTS / INVERSE AGONISTS
公开(公告)号：WO2004002480A1
公开(公告)日：2004-01-08
申请号：PCT/DK2003/000350
申请日：2003-05-27
申请人： NOVO NORDISK A/S
发明人： LAU, Jesper , CHRISTENSEN, Inge, Thøger , MADSEN, Peter , BLOCH, Paw , BEHRENS, Carsten , KODRA, János, Kodra , NIELSEN, Poul, Enrico
IPC分类号： A61K31/426
CPC分类号： A61K45/06 , A61K31/195 , A61K31/41 , A61K31/4439 , A61K2300/00
摘要： Novel compounds that act to antagonize the action of the glucagon peptide hormone on the glucagon receptor. More particularly, it relates to glucagon antagonists or inverse agonists.
摘要翻译：用于拮抗胰高血糖素肽激素对胰高血糖素受体的作用的新型化合物。更具体地，涉及胰高血糖素拮抗剂或反向激动剂。

9. 发明申请

WO2019243502A1 NOVEL COMPOUNDS FOR TREATMENT OF OBESITY 审中-公开
公开(公告)号：WO2019243502A1
公开(公告)日：2019-12-26
申请号：PCT/EP2019/066358
申请日：2019-06-20
申请人： NOVO NORDISK A/S
发明人： ROED, Nikolaj, Kulahin , GRUHLER, Albrecht , RAMIREZ-ANDERSEN, Henrik, Sune , PADKJÆR, Søren , SANDRINI, Michael, Paulo, Bastner , LAU, Jesper , BLOCH, Paw , SECHER, Anna , JENSEN, Casper, Bo , MCGUIRE, Jim , CHAMBERS, Adam, Paul
IPC分类号： A61K38/26 , A61K47/68 , A61P3/04
摘要： The invention relates to a construct comprising a compound targeting areas in the brain involved in the regulation of body weight and an allosteric ligand to a receptor located in the blood-brain barrier (BBB). The invention also relates to compositions and uses of such construct, for example in the prevention or treatment of overweight and obesity. Preferred compounds for regulation of body weight include GLP-1 receptor agonists (GLP-1RA), and preferred receptors located in the BBB include the transferrin receptor (TfR). Exemplary fusions and conjugates of GLP-1 RA's and anti TfR-Fab's exhibit an increased binding to brain regions expressing the GLP-1 receptor as compared to fusions or conjugates with inactive control Fab's, in particular in brain areas protected by the BBB. In vivo mice studies confirm increased reduction in food intake as well as weight loss for the active construct compared to the inactive one.

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