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1. 发明申请

WO2010015668A1 CONJUGATED PROTEINS WITH PROLONGED IN VIVO EFFICACY 审中-公开
标题翻译：结合蛋白质与生殖功能有关
公开(公告)号：WO2010015668A1
公开(公告)日：2010-02-11
申请号：PCT/EP2009/060186
申请日：2009-08-06
申请人： NOVO NORDISK A/S , BEHRENS, Carsten , GARIBAY, Patrick William , ØSTERGAARD, Søren , ANDERSEN, Henrik Sune , JOHANSEN, Nils Langeland , PESCHKE, Bernd , BAK, Sonja
发明人： BEHRENS, Carsten , GARIBAY, Patrick William , ØSTERGAARD, Søren , ANDERSEN, Henrik Sune , JOHANSEN, Nils Langeland , PESCHKE, Bernd , BAK, Sonja
IPC分类号： A61K47/48 , A61P7/04
CPC分类号： A61K47/48023 , A61K47/54 , A61K47/64
摘要： The invention relates to conjugated proteins, in particular but not exclusively, blood coagulation factors, to processes for preparing said conjugates, to pharmaceutical compositions comprising said conjugates and to the use of the conjugates in therapy, in particular but not exclusively, for the treatment of diseases alleviated by blood coagulation factors such as the prophylactic treatment of hemophilia.
摘要翻译：本发明涉及缀合蛋白，特别是但不仅限于，凝血因子，制备所述缀合物的方法，包含所述缀合物的药物组合物以及所述缀合物在治疗中的用途，特别是但不排他地用于治疗通过凝血因子如血友病的预防性治疗减轻疾病。

2. 发明申请

WO2009030771A1 PEPTIDES DERIVATIZED WITH A-B-C-D- AND THEIR THERAPEUTICAL USE 审中-公开
标题翻译：用A-B-C-D及其治疗用途衍生的肽
公开(公告)号：WO2009030771A1
公开(公告)日：2009-03-12
申请号：PCT/EP2008/061830
申请日：2008-09-05
申请人： NOVO NORDISK A/S , SPETZLER, Jane , SCHÄFFER, Lauge , LAU, Jesper , KRUSE, Thomas , GARIBAY, Patrick William , ØSTERGAARD, Søren , RUNGE, Steffen , THØGERSEN, Henning
发明人： SPETZLER, Jane , SCHÄFFER, Lauge , LAU, Jesper , KRUSE, Thomas , GARIBAY, Patrick William , ØSTERGAARD, Søren , RUNGE, Steffen , THØGERSEN, Henning
IPC分类号： A61K38/22 , A61K38/26 , A61K47/48 , C07K14/575 , C07K14/605
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：本发明涉及延长的肽衍生物，例如胰高血糖素样肽-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ABC-或ABCD-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对于实现长效，稳定和活性的GLP-1衍生物的总体目标的相关性，具有每周施用一次的潜力。

3. 发明申请

WO2006003096A1 CONDENSED THIOPHENE DERIVATIVES AND THEIR USE AS CYCLIC GLP-1 AGONISTS 审中-公开
标题翻译：浓缩的THIOPHENE衍生物及其作为循环GLP-1激动剂的使用
公开(公告)号：WO2006003096A1
公开(公告)日：2006-01-12
申请号：PCT/EP2005/052873
申请日：2005-06-21
申请人： NOVO NORDISK A/S , KNUDSEN, Sanne Møller , PETTERSSON, Ingrid , LAU, Jesper , BEHRENS, Carsten , PETERSEN, Anders Klarskov , LAU, Jesper , GARIBAY, Patrick William
发明人： KNUDSEN, Sanne Møller , PETTERSSON, Ingrid , LAU, Jesper , BEHRENS, Carsten , PETERSEN, Anders Klarskov , LAU, Jesper , GARIBAY, Patrick William
IPC分类号： C07D409/12
CPC分类号： C07D495/04 , C07D333/72 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/14
摘要： The invention provides compounds of formula (I) for use as GLP-1 receptor agonists.
摘要翻译：本发明提供用作GLP-1受体激动剂的式（I）化合物。

4. 发明申请

WO2011154349A2 FGF21 ANALOGUES AND DERIVATIVES 审中-公开
标题翻译： FGF21类似物和衍生物
公开(公告)号：WO2011154349A2
公开(公告)日：2011-12-15
申请号：PCT/EP2011/059273
申请日：2011-06-06
申请人： NOVO NORDISK A/S , GARIBAY, Patrick William , WÖLDIKE, Helle , ZHANG, Xujia , THØGERSEN, Henning , NIELSEN, Peter Kresten , ANDERSEN, Birgitte , WANG, Jishu , BAK-JENSEN, Kristian Sass , TAGMOSE, Tina Møller
发明人： GARIBAY, Patrick William , WÖLDIKE, Helle , ZHANG, Xujia , THØGERSEN, Henning , NIELSEN, Peter Kresten , ANDERSEN, Birgitte , WANG, Jishu , BAK-JENSEN, Kristian Sass , TAGMOSE, Tina Møller
IPC分类号： A61K38/18 , A61K38/26 , A61P3/10 , A61K47/48
CPC分类号： C07K14/50 , A61K38/00 , A61K47/64
摘要： Derivatives of Fibroblast Growth Factor 21 which have improved properties for treating diabetes can be prepared by a recombinant process.
摘要翻译：具有改善的用于治疗糖尿病的性质的成纤维细胞生长因子21的衍生物可以通过重组方法制备。

5. 发明申请

WO2010084169A2 FGF21 DERIVATIVES WITH ALBUMIN BINDER A-B-C-D-E- AND THEIR USE 审中-公开
标题翻译：带有铝白蛋白B-D-E-的FGF21衍生物及其使用
公开(公告)号：WO2010084169A2
公开(公告)日：2010-07-29
申请号：PCT/EP2010/050720
申请日：2010-01-22
申请人： NOVO NORDISK A/S , TAGMOSE, Tina Møller , GARIBAY, Patrick William , ANDERSEN, Birgitte , WANG, Jishu , FRIEBOES, Kilian Waldemar Conde Frieboes , BAK-JENSEN, Kristian Sass , THØGERSEN, Henning , WÖLDIKE, Helle , NIELSEN, Peter Kresten , SLAABY, Rita , ZHANG, Xujia , WIECZOREK, Birgit
发明人： TAGMOSE, Tina Møller , GARIBAY, Patrick William , ANDERSEN, Birgitte , WANG, Jishu , FRIEBOES, Kilian Waldemar Conde Frieboes , BAK-JENSEN, Kristian Sass , THØGERSEN, Henning , WÖLDIKE, Helle , NIELSEN, Peter Kresten , SLAABY, Rita , ZHANG, Xujia , WIECZOREK, Birgit
IPC分类号： A61K38/18 , A61K47/48 , A61P3/04
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。

6. 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。

7. 发明申请

WO2007128817A2 INSULIN DERIVATIVE 审中-公开
标题翻译：胰岛素衍生物
公开(公告)号：WO2007128817A2
公开(公告)日：2007-11-15
申请号：PCT/EP2007/054444
申请日：2007-05-08
申请人： NOVO NORDISK A/S , HUBALEK, Frantisek , HOEG-JENSEN, Thomas , JONASSEN, Ib , GARIBAY, Patrick William , JAKOBSEN, Palle , HAVELUND, Svend , KODRA, Janos Tibor
发明人： HUBALEK, Frantisek , HOEG-JENSEN, Thomas , JONASSEN, Ib , GARIBAY, Patrick William , JAKOBSEN, Palle , HAVELUND, Svend , KODRA, Janos Tibor
IPC分类号： A61K38/28
CPC分类号： C07K14/62 , A61K38/00
摘要： The present invention relates to novel human insulin derivatives which are soluble at physiological pH values and have a prolonged profile of action. The invention also relates to methods of providing such derivatives, to pharmaceutical compositions containing them, to methods of treating diabetes and hyperglycaemia using the insulin derivatives of the invention and to the use of such insulin derivatives in the treatment of diabetes and hyperglycaemia.
摘要翻译：本发明涉及新的人胰岛素衍生物，其在生理pH值下可溶，并具有延长的作用特征。本发明还涉及提供这样的衍生物，含有它们的药物组合物的方法，使用本发明的胰岛素衍生物治疗糖尿病和高血糖的方法以及这种胰岛素衍生物在治疗糖尿病和高血糖中的用途。

8. 发明申请

WO2012062804A1 DOUBLE-ACYLATED GLP-1 DERIVATIVES WITH A LINKER 审中-公开
标题翻译：具有连接子的双取代的GLP-1衍生物
公开(公告)号：WO2012062804A1
公开(公告)日：2012-05-18
申请号：PCT/EP2011/069743
申请日：2011-11-09
申请人： NOVO NORDISK A/S , KOFOED, Jacob , LAU, Jesper , LINDEROTH, Lars , GARIBAY, Patrick William , KRUSE, Thomas
发明人： KOFOED, Jacob , LAU, Jesper , LINDEROTH, Lars , GARIBAY, Patrick William , KRUSE, Thomas
IPC分类号： A61K47/48 , A61P3/10
CPC分类号： C07K14/605 , A61K47/542
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 18 of GLP-1(7-37) (SEQ ID NO: 1), a second K residue at another position, and a maximum of twelve amino acid changes as compared to GLP-1(7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 1 : HOOC-(CH 2 ) x -CO-*, and Chem. 2: HOOC-C 6 H 4 -0-(CH 2 ) y -CO-*, in which x is an integer in the range of 6-18, and y is an integer in the range of 3-17; and the linker comprises Chem. 3: *-NH-(CH 2 ) q -CH[(CH 2 ) w -NH 2 ]-CO-*, wherein q is an integer in the range of 0-5, and w is an integer in the range of 0-5; 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 peptides and side chain intermediates. The derivatives are potent, protracted, and suitable for oral administration.
摘要翻译：本发明涉及GLP-1类似物的衍生物，其类似物在对应于GLP-1（7-37）（SEQ ID NO：1）的位置18的位置处的第一个K残基，另一个的第二个K残基位置和与GLP-1（7-37）相比最多12个氨基酸变化; 该衍生物分别包含通过接头分别连接到所述第一和第二K残基的两个伸长部分，其中伸长部分选自Chem。 1：HOOC-（CH 2）x-CO- *，和Chem。 2：HOOC-C6H4-0-（CH2）y-CO- *，其中x是6-18的整数，y是3-17的整数; 连接体包括Chem。 3：* -NH-（CH 2）q-CH [（CH 2）w -NH 2] -CO- *，其中q是0-5的整数，w是0-5的整数 ; 或其药学上可接受的盐，酰胺或酯。本发明还涉及其药物用途，例如用于治疗和/或预防所有形式的糖尿病和相关疾病，以及相应的新型肽和侧链中间体。衍生物有效，延长，适合口服。

9. 发明申请

WO2012010553A1 N-TERMINAL MODIFIED FGF21 COMPOUNDS 审中-公开
标题翻译： N-末端修饰的FGF21化合物
公开(公告)号：WO2012010553A1
公开(公告)日：2012-01-26
申请号：PCT/EP2011/062238
申请日：2011-07-18
申请人： NOVO NORDISK A/S , TAGMOSE, Tina Møller , GARIBAY, Patrick William , ZHANG, Xujia , THØGERSEN, Henning , NIELSEN, Peter Kresten , ANDERSEN, Birgitte , WANG, Jishu , BAK-JENSEN, Kristian Sass , WÖLDIKE, Helle Fabricius
发明人： TAGMOSE, Tina Møller , GARIBAY, Patrick William , ZHANG, Xujia , THØGERSEN, Henning , NIELSEN, Peter Kresten , ANDERSEN, Birgitte , WANG, Jishu , BAK-JENSEN, Kristian Sass , WÖLDIKE, Helle Fabricius
IPC分类号： A61K38/18
CPC分类号： A61K47/48038 , A61K38/1825 , A61K47/542 , A61K47/545
摘要： Analogues of FGF21 carrying a modifying, substituted ethylene or benzyl group can be used for treatment or prevention of diabetes, dyslipidemia, obesity, cardiovascular diseases, metabolic syndrome, and/or Non Alcoholic Fatty Liver Disease (NAFLD).
摘要翻译：携带改性取代的乙烯或苄基的FGF21的类似物可用于治疗或预防糖尿病，血脂异常，肥胖，心血管疾病，代谢综合征和/或非酒精性脂肪肝（NAFLD）。

10. 发明申请

WO2009115469A1 PROTEASE STABILIZED, ACYLATED INSULIN ANALOGUES 审中-公开
标题翻译：保护稳定的胰岛素类似物
公开(公告)号：WO2009115469A1
公开(公告)日：2009-09-24
申请号：PCT/EP2009/053017
申请日：2009-03-13
申请人： NOVO NORDISK A/S , MADSEN, Peter , KJELDSEN, Thomas Børglum , HOEG-JENSEN, Thomas , JAKOBSEN, Palle , TAGMOSE, Tina Møller , GLENDORF, Tine , KODRA, János Tibor , GARIBAY, Patrick William
发明人： MADSEN, Peter , KJELDSEN, Thomas Børglum , HOEG-JENSEN, Thomas , JAKOBSEN, Palle , TAGMOSE, Tina Møller , GLENDORF, Tine , KODRA, János Tibor , GARIBAY, Patrick William
IPC分类号： C07K14/62 , A61K38/28
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。

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