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21. 发明申请

WO2013041678A1 NOVEL GLUCAGON ANALOGUES 审中-公开
标题翻译：新的GLUCAGON ANALOGUES
公开(公告)号：WO2013041678A1
公开(公告)日：2013-03-28
申请号：PCT/EP2012/068649
申请日：2012-09-21
申请人： NOVO NORDISK A/S
发明人： LAU, Jesper, F. , KRUSE, Thomas , THØGERSEN, Henning , SENSFUSS, Ulrich , NIELSEN, Peter, Kresten
IPC分类号： C07K14/605 , A61K38/00
CPC分类号： C07K14/605 , A61K38/00 , A61K38/2278 , A61K38/26
摘要： The present invention relates to novel glucagon peptides, to the use of said glucagon peptides in therapy, to methods of treatment comprising administration of said glucagon peptides to patients in need thereof, and to the use of said glucagon peptides in the manufacture of medicaments. The glucagon peptides of the present invention are of particular interest in relation to the treatment of hyperglycemia, diabetes and obesity, as well as a variety of diseases or conditions associated with hyperglycemia, diabetes and obesity.
摘要翻译：本发明涉及在治疗中使用所述胰高血糖素肽的新型胰高血糖素肽涉及治疗方法，包括向有需要的患者施用所述胰高血糖素肽，以及所述胰高血糖素肽在制备药物中的用途。本发明的胰高血糖素肽与治疗高血糖症，糖尿病和肥胖症以及与高血糖症，糖尿病和肥胖相关的多种疾病或病症有特别的关注。

22. 发明申请

WO2018215525A8 MIC-1 COMPOUNDS AND USES THEREOF 审中-公开
公开(公告)号：WO2018215525A8
公开(公告)日：2018-11-29
申请号：PCT/EP2018/063476
申请日：2018-05-23
申请人： NOVO NORDISK A/S
发明人： GAO, Xiang , ZHANG, Xujia , GUAN, Hongtao , THØGERSEN, Henning , SASS-ØRUM, Kristian , IVERSEN, Lars, Fogh , NØRGAARD, Per , JØRGENSEN, Sebastian, Beck , HANSEN, Kristian, Tage , WANG, Yi , FRIEBOES, Kilian, Waldemar, Conde , WIECZOREK, Birgit
IPC分类号： C07K14/50 , A61K38/19 , C07K14/475 , G01N33/68
摘要： The invention relates to MIC-1 compounds. More specifically it relates to compounds comprising a MIC-1 polypeptide with an N-terminal amino acid extension and a protractor wherein the amino acid extension comprises 3 to 36 amino acid residues and where the MIC-1 polypeptide and the N-terminal amino acid extension together have a calculated pI lower than 6.5. The compounds of the invention have MIC-1 activity. The invention also relates to pharmaceutical compositions comprising such compounds and pharmaceutically acceptable excipients, as well as the medical use of the compounds.

23. 发明申请

WO2017118752A1 MODIFIED ENTEROKINASE LIGHT CHAIN AND ITS PREPARATION METHOD 审中-公开
标题翻译：改进的ENTEROKINASE轻链及其制备方法
公开(公告)号：WO2017118752A1
公开(公告)日：2017-07-13
申请号：PCT/EP2017/050303
申请日：2017-01-09
申请人： NOVO NORDISK A/S
发明人： LIU, Yun , GAO, Xiang , THØGERSEN, Henning
IPC分类号： C12N9/64
CPC分类号： C12Y304/21009 , C07K2319/35 , C07K2319/50 , C12N9/6424
摘要： The present invention is related to novel mammalian enterokinase analogues such as mammalian enterokinase light chain analogues and methods of making such. Also described herein is a method for cleaving proteins having an enterokinase cleavage site.
摘要翻译：本发明涉及新的哺乳动物肠激酶类似物，例如哺乳动物肠激酶轻链类似物及其制备方法。本文还描述了用于切割具有肠激酶切割位点的蛋白质的方法。

24. 发明申请

WO2015197446A1 MIC-1 FUSION PROTEINS AND USES THEREOF 审中-公开
标题翻译： MIC-1融合蛋白及其用途
公开(公告)号：WO2015197446A1
公开(公告)日：2015-12-30
申请号：PCT/EP2015/063596
申请日：2015-06-17
申请人： NOVO NORDISK A/S
发明人： SHAW, Allan Christian , HELGSTRAND, Charlotte , SANDRINI, Michael Paolo Bastner , JØRGENSEN, Sebastian Beck , THØGERSEN, Henning , SASS-ØRUM, Kristian , HASTRUP, Sven , ANDERSEN, Kim Vilbour
IPC分类号： A61K39/00 , C07K14/475
CPC分类号： A61K38/18 , A61K38/19 , A61K38/385 , A61K47/643 , A61K47/65 , C07K14/00 , C07K14/475 , C07K14/52 , C07K14/765 , C07K2319/31
摘要： The invention relates to MIC-1 fusion proteins. More specifically it relates to compounds comprising fusion proteins comprising a MIC-1 protein or an analogue thereof at the C-terminus of the fusion protein and a functional variant of human serum albumin at the N-terminus of the fusion protein connected via a peptide linker. The compounds of the invention have MIC-1 activity. The invention also relates to pharmaceutical compositions comprising such compounds and pharmaceutically acceptable excipients, as well as the medical use of the compounds.
摘要翻译：本发明涉及MIC-1融合蛋白。更具体地，涉及包含融合蛋白C末端的MIC-1蛋白或其类似物的融合蛋白的化合物和通过肽接头相连的融合蛋白N末端的人血清白蛋白的功能变体。本发明的化合物具有MIC-1活性。本发明还涉及包含这些化合物和药学上可接受的赋形剂的药物组合物，以及该化合物的医疗用途。

25. 发明申请

WO2017121850A1 EGF(A) ANALOGUES WITH FATTY ACID SUBSTITUENTS 审中-公开
标题翻译： EGF（A）具有脂肪酸取代基的类似物
公开(公告)号：WO2017121850A1
公开(公告)日：2017-07-20
申请号：PCT/EP2017/050668
申请日：2017-01-13
申请人： NOVO NORDISK A/S
发明人： CHEN, Jianhe , LAU, Jesper F. , KODRA, János Tibor , WIECZOREK, Birgit , LINDEROTH, Lars , THØGERSEN, Henning , RASMUSSEN, Salka Elbøl , GARIBAY, Patrick William
IPC分类号： C07K14/705 , A61K38/17
CPC分类号： C07K14/705 , A61K38/00 , A61K38/177
摘要： The invention relates to compounds derived from the EGF(A) domain of LDL-R, in particular compounds comprising a peptide analogue of the wild-type EGF(A) (LDL-R(293- 332)) sequence and at least one substituent comprising at least one fatty acid group. The invention also relates to a pharmaceutical composition thereof and use a medicament. The novel EGF(A) compounds of the invention are useful as treatment e.g. in the field of cholesterol lowering, dyslipidaemia and cardiovascular disease.
摘要翻译：本发明涉及衍生自LDL-R的EGF（A）结构域的化合物，特别是包含野生型EGF（A）的肽类似物的化合物（LDL-R（293-332 ））序列和至少一个包含至少一个脂肪酸基团的取代基。本发明还涉及其药物组合物并使用药物。本发明的新型EGF（A）化合物可用作例如治疗剂。在胆固醇降低，血脂异常和心血管疾病领域。

26. 发明申请

WO2016055610A1 STABLE GLP-1 BASED GLP-1/GLUCAGON RECEPTOR CO-AGONISTS 审中-公开
标题翻译：稳定的基于GLP-1的GLP-1 / GLUCAGON受体共同作用
公开(公告)号：WO2016055610A1
公开(公告)日：2016-04-14
申请号：PCT/EP2015/073372
申请日：2015-10-09
申请人： NOVO NORDISK A/S
发明人： REEDTZ-RUNGE, Steffen , SENSFUSS, Ulrich , KRUSE, Thomas , SPETZLER, Jane , THØGERSEN, Henning , WENZEL TORNØE, Christian , LAU, Jesper F.
IPC分类号： C07K14/605 , A61K38/26
CPC分类号： C07K14/605 , A61K38/00
摘要： The application concerns stable and protracted GLP-1 derivatives which are GLP-l/glucagon receptor co-agonists, compositions thereof, use of the GLP-1 derivatives in medicine, and to methods of treatment comprising administration of the GLP-1 derivatives to patients, including treatment of diabetes, obesity and related diseases and conditions. Prefered GLP-1 derivatives comprise a polypeptide consisting of the amino acid sequence of Formula I: lmp-X8-His-Gly-Thr-Phe-Thr-Ser-Asp-Xl 6-Ser-Xi 8-Tyr-Leu-Glu-X22- X23-Ala-Ala -X26-X27-Phe-I le-Ala-Trp-Leu-X33-X34-X35-X36-X37 [I], wherein - X8 is Ala, Aib, Acb, or Gly; - X16 is Val, Leu, lie, or Tyr; - X18 is Lys or Arg; - X22 is Gly, Ala, Glu, Lys, Arg, Ser, orAib; - X23 is Gin, Arg, or Lys; - X26 is Lys or Arg; - X27 is Glu or Lys; - X33 is Val, Leu, or lle; - X34 is Lys or Arg; - X35 is Gly, Thr, Lys, or is absent; - X36 is Ala, Gly, Lys, Ser, or is absent; - X37 is Gly or is absent; wherein said GLP-i derivative further comprises a substituent comprising a lipophilic moiety and at least two negatively charged moieties, wherein one of said negatively charged moieties is distal of a lipophilic moiety; wherein said polypeptide optionally comprises a C-terminal amide; or a pharmaceutically acceptable salt and/or ester thereof.
摘要翻译：本申请涉及GLP-1 /胰高血糖素受体共激动剂，其组合物，GLP-1衍生物在医药中的用途以及包括向患者施用GLP-1衍生物的治疗方法的稳定和延长的GLP-1衍生物，包括治疗糖尿病，肥胖症及相关疾病和病症。优选的GLP-1衍生物包含由式I的氨基酸序列组成的多肽：1mp-X8-His-Gly-Thr-Phe-Thr-Ser-Asp-X116-Ser-Xi 8-Tyr-Leu-Glu- X22-X23-Ala-Ala -X26-X27-Phe-Ile-Ala-Trp-Leu-X33-X34-X35-X36-X37 [I]，其中-X8是Ala，Aib，Acb或Gly; - X16是Val，Leu，lie或Tyr; -X18是Lys或Arg; - X22是Gly，Ala，Glu，Lys，Arg，Ser或Aib; - X23是Gin，Arg或Lys; - X26是Lys或Arg; - X27是Glu或Lys; - X33是Val，Leu或lle; - X34是Lys或Arg; - X35是Gly，Thr，Lys，或不存在; - X36是Ala，Gly，Lys，Ser，或不存在; - X37是Gly或不存在; 其中所述GLP-1衍生物还包含包含亲脂部分和至少两个带负电荷的部分的取代基，其中所述带负电荷的部分之一是亲脂性部分的远端; 其中所述多肽任选地包含C-末端酰胺; 或其药学上可接受的盐和/或酯。

27. 发明申请

WO2004048345A2 COMPOUNDS FOR USE IN TREATING OBESITY 审中-公开
标题翻译：化合物用于治疗肥胖
公开(公告)号：WO2004048345A2
公开(公告)日：2004-06-10
申请号：PCT/DK2003/000797
申请日：2003-11-20
申请人： NOVO NORDISK A/S , BOEHRINGER INGELHEIM INTERNATIONAL GMBH
发明人： CONDE-FRIEBOES, Kilian, Waldemar , ANKERSEN, Michael , SENSFUSS, Ulrich , WULFF, Birgitte, Schjellerup , THØGERSEN, Henning , LUSTENBERGER, Philipp , RUDOLF, Klaus , KRIST, Bernd , MÜLLER, Stephan , STENKAMP, Dirk , SCHINDLER, Marcus , WIELAND, Heike , ARNDT, Kirsten
IPC分类号： C07D241/00
CPC分类号： C07D401/06 , C07D241/08 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , C07D413/14
摘要： The present invention relates to novel compounds of the general formula (I) as well as any optical or geometric isomer or tautomer form thereof, or a pharmaceutically acceptable salt thereof, as agonists of melanocortin receptors, such as agonists of the MC4 receptor. The compounds may for instance be used in the treatment of obesity.
摘要翻译：本发明涉及通式（I）的新颖化合物及其任何光学或几何异构体或互变异构体形式或其药学上可接受的盐作为黑皮质素受体的激动剂，例如MC4受体的激动剂。该化合物可用于治疗肥胖症。

28. 发明申请

WO2019092125A1 GLUCOSE-SENSITIVE ALBUMIN-BINDING DERIVATIVES 审中-公开
公开(公告)号：WO2019092125A1
公开(公告)日：2019-05-16
申请号：PCT/EP2018/080650
申请日：2018-11-08
申请人： NOVO NORDISK A/S
发明人： KRUSE, Thomas , HANSEN, Mikael, Kofoed , MÜNZEL, Martin, Werner, Borchsenius , THØGERSEN, Henning , SAUERBERG, Per , RASMUSSEN, Jakob, Ewald , BEHRENS, Carsten , HØEG-JENSEN, Thomas , BALŠÁNEK, Vojtech , DROBNÁKOVÁ, Zuzana , DROŽ, Ladislav , HAVRÁNEK, Miroslav , KOTEK, Vladislav , ŠTENGL, Milan , ŠNAJDR, Ivan , VÁNOVÁ, Hana
IPC分类号： C07F5/02 , A61K31/69 , G01N24/08 , G01N33/52 , A61P3/08 , A61K33/00 , C12Q1/00 , C12Q3/00 , C40B30/00 , C40B30/04 , C40B30/10 , G01N33/48 , G01N33/50
CPC分类号： C07F5/025 , A61K31/69 , A61K33/00 , C12Q1/00 , C12Q3/00 , C40B30/00 , C40B30/04 , C40B30/10 , G01N24/088 , G01N33/542 , G01N33/66 , G01N33/6827 , G01N2333/76 , G01N2800/042
摘要： This invention relates to glucose-sensitive albumin-binding diboron conjugates. More particularly the invention provides novel diboron compounds, and in particular diboronate or diboroxole compounds, useful as intermediate compounds for the synthesis of diboron conjugates. The diboron compounds are characterized by formula (I), which is: R1-X-R2, and wherein "X" is a mono- to multiatomic linker and where R 1 and R 2 , which may be identical or different, each represents a group of Formula (lla) or (IIb) Also described are diboron conjugates represented by the general Formula (I'), which is: R1'-X'-R2', in which either the moeities R1' or R2' or X' carry a drug that is covalently attached to the diboron compound.

29. 发明申请

WO2018215525A1 MIC-1 COMPOUNDS AND USES THEREOF 审中-公开
公开(公告)号：WO2018215525A1
公开(公告)日：2018-11-29
申请号：PCT/EP2018/063476
申请日：2018-05-23
申请人： NOVO NORDISK A/S
发明人： GAO, Xiang , ZHANG, Xujia , GUAN, Hongtao , THØGERSEN, Henning , SASS-ØRUM, Kristian , IVERSEN, Lars, Fogh , NØRGAARD, Per , JØRGENSEN, Sebastian, Beck , HANSEN, Kristian, Tage , WANG, Yi , FRIEBOES, Kilian, Waldemar, Conde , WIECZOREK, Birgit
IPC分类号： C07K14/50 , A61K38/19 , C07K14/475 , G01N33/68
摘要： The invention relates to MIC-1 compounds. More specifically it relates to compounds comprising a MIC-1 polypeptide with an N-terminal amino acid extension and a protractor wherein the amino acid extension comprises 3 to 36 amino acid residues and where the MIC-1 polypeptide and the N-terminal amino acid extension together have a calculated pI lower than 6.5. The compounds of the invention have MIC-1 activity. The invention also relates to pharmaceutical compositions comprising such compounds and pharmaceutically acceptable excipients, as well as the medical use of the compounds.

30. 发明申请

WO2017202936A1 MIC-1 COMPOUNDS AND USE THEREOF 审中-公开
标题翻译： MIC-1化合物及其用途
公开(公告)号：WO2017202936A1
公开(公告)日：2017-11-30
申请号：PCT/EP2017/062583
申请日：2017-05-24
申请人： NOVO NORDISK A/S
发明人： ZHANG, Xujia , GAO, Xiang , GUAN, Hongtao , THØGERSEN, Henning , SASS-ØRUM, Kristian , IVERSEN, Lars, Fogh , NØRGAARD, Per , JØRGENSEN, Sebastian, Beck , HANSEN, Kristian, Tage , WANG, Yi
IPC分类号： A61K38/00 , A61K38/27 , C07K14/475
摘要： 160031WO03 56 ABSTRACT The invention relates to MIC-1 compounds. More specifically it relates to compounds comprising a MIC-1 polypeptide and an N-terminal amino acid extension, wherein said extension consists of 3 to 36 amino acid residues and where the compound has a calculated pI lower than 6.5. The compounds of the invention have MIC-1 activity. 5 The invention also relates to pharmaceutical compositions comprising such compounds and pharmaceutically acceptable excipients, as well as the medical use of the compounds.
摘要翻译：本发明涉及MIC-1化合物。更具体地说，它涉及包含MIC-1多肽和N端氨基酸延伸的化合物，其中所述延伸由3至36个氨基酸残基组成，并且其中化合物具有低于6.5的计算pI。本发明的化合物具有MIC-1活性。本发明还涉及包含此类化合物和药学上可接受的赋形剂的药物组合物，以及这些化合物的医学用途。

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