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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

WO2006097537A3 ACYLATED GLP-1 COMPOUNDS 审中-公开
标题翻译：酰化GLP-1化合物
公开(公告)号：WO2006097537A3
公开(公告)日：2007-01-25
申请号：PCT/EP2006060855
申请日：2006-03-20
申请人： NOVO NORDISK AS , LAU JESPER , DOERWALD FLORENCIO ZARAGOZA , STEPHENSEN HENRIK , BLOCH PAW , HANSEN THOMAS KRUSE , MADSEN KJELD
发明人： LAU JESPER , DOERWALD 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

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。

4. 发明申请

WO2005014049A3 SYNTHESIS AND APPLICATION OF NEW STRUCTURAL WELL DEFINED BRANCHED POLYMERS AS CONJUGATING AGENTS FOR PEPTIDES 审中-公开
标题翻译：新型结构定义的分支聚合物作为配制剂的合成与应用
公开(公告)号：WO2005014049A3
公开(公告)日：2005-09-01
申请号：PCT/DK2004000531
申请日：2004-08-09
申请人： NOVO NORDISK AS , BEHRENS CARSTEN , DOERWALD FLORENCIO ZARAGOZA , KOFOD-HANSEN MIKAEL , LAU JESPER , KODRA JANOS TIBOR , HANSEN THOMAS KRUSE , BLOCH PAW
发明人： BEHRENS CARSTEN , DOERWALD FLORENCIO ZARAGOZA , KOFOD-HANSEN MIKAEL , LAU JESPER , KODRA JANOS TIBOR , HANSEN THOMAS KRUSE , BLOCH PAW
IPC分类号： A61K38/44 , 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：本发明提供新的结构明确的支化聚合物作为肽和蛋白质的助剂的合成和应用。

5. 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）。

6. 发明申请

WO2005027978A2 NOVEL GLP-1 DERIVATIVES 审中-公开
标题翻译：新型GLP-1衍生物
公开(公告)号：WO2005027978A2
公开(公告)日：2005-03-31
申请号：PCT/DK2004000624
申请日：2004-09-17
申请人： NOVO NORDISK AS , LAU JESPER , HANSEN THOMAS KRUSE , MADSEN KJELD , BLOCH PAW , DOERWALD FLORENCIO ZARAGOZA , JOHANSEN NILS LANGELAND
发明人： LAU JESPER , HANSEN THOMAS KRUSE , MADSEN KJELD , BLOCH PAW , DOERWALD FLORENCIO ZARAGOZA , JOHANSEN NILS LANGELAND
IPC分类号： A61K38/00 , A61K47/48 , C07K14/605
CPC分类号： C07K14/605 , A61K38/00 , A61K38/26 , A61K47/54 , A61K47/542 , A61K47/60 , C07K14/001
摘要： Novel polypeptide derivatives having protracted profile of action
摘要翻译：新型多肽衍生物具有延长的作用特征

7. 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。

8. 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.

9. 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。

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