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1. 发明专利

JP2013063984A Acylated glp-1 compound 审中-公开
标题翻译：酰化GLP-1化合物
公开(公告)号：JP2013063984A
公开(公告)日：2013-04-11
申请号：JP2012242654
申请日：2012-11-02
申请人： Novo Nordisk As , ノヴォノルディスクアー/エス
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 , A61P1/04 , A61P1/14 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P25/08 , A61P25/28 , A61P43/00
CPC分类号： C07K14/605 , A61K38/00
摘要： PROBLEM TO BE SOLVED: To provide extending glucagon-like peptide 1 (GLP-1) compounds which increase the time of action in a patient as a therapeutic peptide.SOLUTION: A GLP-1 analog has a modification of at least one non-proteogenic amino acid residue in positions 7 and/or 8 relative to the sequence GLP-1(7-37), in which a lysine residue in position 26 is acylated with a moiety comprising at least two acidic groups, wherein one acidic group is bonded terminally.
摘要翻译：待解决的问题：提供增加作为治疗性肽的患者中作用时间的胰高血糖素样肽1（GLP-1）化合物。解决方案：GLP-1类似物相对于序列GLP-1（7-37）在位置7和/或8处具有至少一个非蛋白原性氨基酸残基的修饰，其中赖氨酸残基在位置 26被包含至少两个酸性基团的部分酰化，其中一个酸性基团末端键合。版权所有（C）2013，JPO＆INPIT

2. 发明专利

JP2000143613A COMPOUND HAVING GROWTH HORMONE-RELEASING CHARACTERISTICS 失效
公开(公告)号：JP2000143613A
公开(公告)日：2000-05-26
申请号：JP32892999
申请日：1999-11-19
申请人： NOVO NORDISK AS
发明人： HANSEN THOMAS KRUSE , PESCHKE BERND , LAU JESPER , LUNDT BEHREND FRIEDRICH , ANKERSEN MICHAEL , WATSON BRETT , MADSEN KJELD
IPC分类号： C07D333/20 , A61K31/00 , A61K31/17 , A61K31/18 , A61K31/216 , A61K31/27 , A61K31/38 , A61K31/381 , A61K31/41 , A61K31/4245 , A61K31/454 , A61K38/00 , A61K38/07 , A61K38/08 , A61P3/00 , A61P5/00 , A61P5/06 , A61P5/10 , A61P15/00 , A61P15/14 , A61P19/00 , B41J19/20 , C07C237/00 , C07C237/22 , C07C311/05 , C07C335/14 , C07D213/12 , C07D227/00 , C07D271/06 , C07D333/00 , C07D333/24 , C07D333/60 , C07D409/00 , C07D413/12 , C07K5/03 , C07K5/06 , C07K5/065 , C07K5/078 , C07K5/10 , C07K7/02 , C07K14/60
摘要： PROBLEM TO BE SOLVED: To obtain a compound having growth hormone-releasing characteristics, having a more excellent property than that of a conventional compound and having an analogous property to a peptide. SOLUTION: This compound is expressed by formula I wherein, R1 and R2 are each H or a (aryl-substituted) (1-6C) alkyl; (a) and (b) are each 1 or 2; G is H, O-(CH2)k-R27 (wherein, R27 is H, a halogen or the like; (k) is 0-2) or the like; J is expressed by formula II (wherein, R32-R36 are each H, a halogen or the like) or the like; E is CONR12R13 [wherein, R12 and R13 are each H, a (substituted) (1-6C) alkyl or the like]; D is expressed by formula III [wherein, R3-R6 are each H, a (substituted) (1-6C) alkyl or the like; (n) is 0-3] or the like} and is e.g. (2E)-5-amino-5-methylhexa-2-enoic acid N-methyl-N-((1R)-1-(N- methyl-N-((1R-1-(methylcarbamoyl)-2-phenylethyl)carbamoyl)-2-(2-naphth yl)ethyl) amide. The compound of formula I is synthesized e.g. through dropping ethyl chloroformate into a solution of both 3-t-butoxycarbonylamino-3-methylbutanoic acid and triethylamine as a starting step.

3. 发明专利

JP2010116407A Acylated glp-1 compound 有权
标题翻译：酰化GLP-1化合物
公开(公告)号：JP2010116407A
公开(公告)日：2010-05-27
申请号：JP2010009025
申请日：2010-01-19
申请人： Novo Nordisk As , ノボノルディスクアクティーゼルスカブNovo Nordisk Aktie Selsxab
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 , A61P1/04 , A61P1/14 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P25/08 , A61P25/28 , A61P43/00
CPC分类号： C07K14/605 , A61K38/00
摘要： PROBLEM TO BE SOLVED: To provide a method which increases action time in the treating of hyperglycemia and diabetes. SOLUTION: In a glucagon like peptide (GLP-1), a GLP-1 analogue which has the remodeling of at least one nonprotein original property amino acid residue, and is the GLP-1 analogue in which a specific lysine residue is acylated by a moiety containing at least two acid groups, and one acid group combines with a terminal. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供一种增加治疗高血糖和糖尿病的作用时间的方法。解决方案：在胰高血糖素样肽（GLP-1）中，具有至少一种非蛋白原始性质氨基酸残基重构的GLP-1类似物，其中特定赖氨酸残基为由含有至少两个酸基的部分酰化，一个酸基与末端结合。版权所有（C）2010，JPO＆INPIT

4. 发明专利

JP2013100315A Amylin derivative 审中-公开
标题翻译： AMYLIN DERIVATIVE
公开(公告)号：JP2013100315A
公开(公告)日：2013-05-23
申请号：JP2013000256
申请日：2013-01-04
申请人： Novo Nordisk As , ノボ・ノルデイスク・エー/エス
发明人： HANSEN THOMAS KRUSE , SCHAEFFER LAUGE , LAU JESPER
IPC分类号： C07K14/575 , A61K38/22 , A61K47/42 , A61K47/48 , A61P1/04 , A61P1/14 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P25/28
CPC分类号： C07K14/4713 , A61K38/00 , C07K14/5759
摘要： PROBLEM TO BE SOLVED: To provide a pharmaceutical composition containing human amylin or its derivative, and a use of the derivative to prepare a pharmaceutical to treat a disease.SOLUTION: The human amylin or its derivative has a delayed action profile in which 2- to 37-position amino acid residues are substituted with a lysine residue or a cysteine residue and the lysine residue or the cysteine residue is bonded to, through a linker in some cases, an albumin bond residue or a polyethylene glycol polymer, or (b) 1-position lysine residues are bonded to, through linkers in some cases, albumin bond residues or polyethylene glycol polymers. There are provided a pharmaceutical composition containing the derivative, and a use of the derivative to treat diseases related to obesity, and diabetes and other metabolic diseases.
摘要翻译：待解决的问题：提供含有人胰岛淀粉样多肽或其衍生物的药物组合物，以及该衍生物用于制备治疗疾病的药物的用途。解决方案：人胰岛淀粉样多肽或其衍生物具有延迟作用特征，其中2至37位氨基酸残基被赖氨酸残基或半胱氨酸残基取代，赖氨酸残基或半胱氨酸残基通过在某些情况下，连接物，白蛋白键残基或聚乙二醇聚合物，或（b）1-位赖氨酸残基通过接头在某些情况下与白蛋白键残基或聚乙二醇聚合物键合。提供含有该衍生物的药物组合物，以及该衍生物用于治疗与肥胖相关的疾病以及糖尿病和其它代谢性疾病的用途。版权所有（C）2013，JPO＆INPIT

5. 发明专利

JP2008156372A Compound with growth hormone releasing property 有权
标题翻译：化合物与生长激素释放物质
公开(公告)号：JP2008156372A
公开(公告)日：2008-07-10
申请号：JP2008062381
申请日：2008-03-12
申请人： Novo Nordisk As , ノボノルディスクアクティーゼルスカブNovo Nordisk Aktie Selsxab
发明人： HANSEN THOMAS KRUSE , ANKERSEN MICHAEL
IPC分类号： C07D211/60 , C07D223/06 , A61K31/40 , A61K31/4427 , A61K31/445 , A61K31/451 , A61K31/454 , A61K31/55 , A61P5/06 , A61P5/08 , A61P5/10 , C07D207/16 , C07D209/00 , C07D211/00 , C07D211/62 , C07D401/06
CPC分类号： C07D401/06 , C07D211/62
摘要： PROBLEM TO BE SOLVED: To provide a new compound with growth hormone releasing property. SOLUTION: The invention relates to the new compounds, especially disclosed are 4,4-disubstituted and 3,3-disubstituted piperidine compounds, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：要解决的问题：提供具有生长激素释放性质的新化合物。解决方案：本发明涉及新化合物，特别公开的是4,4-二取代和3,3-二取代的哌啶化合物，含有它们的组合物及其用于治疗由生长激素缺乏引起的医学疾病的用途。版权所有（C）2008，JPO＆INPIT

6. 发明专利

JPH11209336A COMPOUND HAVING GROWTH HORMONE RELEASING CHARACTERISTIC 失效
公开(公告)号：JPH11209336A
公开(公告)日：1999-08-03
申请号：JP24793598
申请日：1998-08-13
申请人： NOVO NORDISK AS
发明人： HANSEN THOMAS KRUSE , PESCHKE BERND , LAU JESPER , LUNDT BEHREND FRIEDRICH , ANKERSEN MICHAEL , WATSON BRETT , MADSEN KJELD
IPC分类号： C07D333/20 , A61K31/00 , A61K31/17 , A61K31/18 , A61K31/216 , A61K31/27 , A61K31/38 , A61K31/381 , A61K31/41 , A61K31/4245 , A61K31/454 , A61K38/00 , A61K38/07 , A61K38/08 , A61P3/00 , A61P5/00 , A61P5/06 , A61P5/10 , A61P15/00 , A61P15/14 , A61P19/00 , B41J19/20 , C07C237/00 , C07C237/22 , C07C311/05 , C07C335/14 , C07D213/12 , C07D227/00 , C07D271/06 , C07D333/00 , C07D333/24 , C07D333/60 , C07D409/00 , C07D413/12 , C07K5/03 , C07K5/06 , C07K5/065 , C07K5/078 , C07K5/10 , C07K7/02 , C07K14/60
摘要： PROBLEM TO BE SOLVED: To obtain the subject new compound sowing more raised bioavailability than that of an already-known compound, useful for treating bodily disorders caused by deficiency of growth hormone. SOLUTION: This compound is shown by formula I [R is H or a 1-6C alkyl; R is a 1-6C alkyl; (a) and (b) are each 1 or 2; G and J are each a group of formula II or formula III (R to R are each H, a halogen or the like); D is a group of formula IV (R to R are each H, a 1-6C alkyl which may be substituted with amino or the like; (n) and (m) are each 0-3; (o) and (p) are each 0 or 1; M is O, S or the like); E is a group of the formula, CONR R (R is H or a 1-6C alkyl which may be substituted with a halogen or the like; R is a 1-6C alkyl which may be substituted with hydroxy or the like)] such as (4-(1-aminocyclobutyl)but-2-enoic acid ((1R)-1-(((1R)-1-(1-methylcarbamoyl-2- phenylethyl)methylcarbamoyl)-2-(2-naphthyl)ethyl)methylamide. The compound of formula I is obtained, for example, by starting from ethyl chloroformate and 3-tert-butoxycarbonylamino-3-methylbutanoic acid.

7. 发明申请

WO2005058958A3 NOVEL GLP-1 ANALOGUES LINKED TO ALBUMIN-LIKE AGENTS 审中-公开
标题翻译：新型GLP-1类似物与ALBUMIN-LIKE AGENTS连接
公开(公告)号：WO2005058958A3
公开(公告)日：2005-11-24
申请号：PCT/DK2004000887
申请日：2004-12-17
申请人： NOVO NORDISK AS , HANSEN THOMAS KRUSE , ZUNDEL MAGALI , MADSEN KJELD , SVENDSEN ANNE , SCHIOEDT CHRISTINE BRUUN , LAU JESPER
发明人： HANSEN THOMAS KRUSE , ZUNDEL MAGALI , MADSEN KJELD , SVENDSEN ANNE , SCHIOEDT CHRISTINE BRUUN , LAU JESPER
IPC分类号： A61K38/00 , A61K38/26 , A61K38/38 , A61K47/48 , C07K14/46 , C07K14/47 , C07K14/575 , C07K14/605 , C07K14/765 , C07K19/00 , A61P3/10
CPC分类号： C07K14/605 , A61K38/00 , A61K47/643 , C07K14/46 , C07K14/4705 , C07K14/57563 , C07K2319/00
摘要： The present invention relates to a compound having the structure of the formula (I) : GLP-1 agonist-L-RR-protraction protein (I) wherein GLP-1 agonist is a polypeptide which is an agonist of the human GLP-1 receptor, L is a linker connecting an amino acid side chain of said GLP-1 agonist with RR, RR is the remains of a reactive residue that has formed a covalent bond with an amino acid residue of the protraction protein, and protraction protein is a protein having a molar weight of at least 5 kDa, having a plasma halflife of at least 24 hours in human plasma , and said protraction protein has been synthesised by a non-mammalian organism or synthetically.
摘要翻译：本发明涉及具有式（I）结构的化合物：GLP-1激动剂-L-RR-延伸蛋白（I），其中GLP-1激动剂是作为人GLP-1受体激动剂的多肽 L是将所述GLP-1激动剂的氨基酸侧链与RR连接的接头，RR是与延伸蛋白质的氨基酸残基形成共价键的反应性残基的残基，延伸蛋白是蛋白质具有至少5kDa的摩尔重量，在人血浆中具有至少24小时的血浆半衰期，并且所述延伸蛋白已经由非哺乳动物生物合成或合成地合成。

8. 发明申请

WO2006037810A3 PROTRACTED GLP-1 COMPOUNDS 审中-公开
标题翻译：提炼的GLP-1化合物
公开(公告)号：WO2006037810A3
公开(公告)日：2006-09-08
申请号：PCT/EP2005055101
申请日：2005-10-07
申请人： NOVO NORDISK AS , LAU JESPER , HANSEN THOMAS KRUSE
发明人： LAU JESPER , HANSEN THOMAS KRUSE
IPC分类号： C07K14/605 , A61K38/26
CPC分类号： C07K14/605 , A61K38/00
摘要： Novel protracted GLP-1 compounds and therapeutic uses thereof.
摘要翻译：新颖的长效GLP-1化合物及其治疗用途。

9. 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。

10. 发明申请

WO2006087354A3 INSULINOTROPIC AGENTS CONJUGATED WITH STRUCTURALLY WELL DEFINED BRANCHED POLYMERS 审中-公开
标题翻译：结构分布良好的分离聚合物的绝缘剂
公开(公告)号：WO2006087354A3
公开(公告)日：2007-08-02
申请号：PCT/EP2006060007
申请日：2006-02-16
申请人： NOVO NORDISK AS , BEHRENS CARSTEN , LAU JESPER , KODRA JANOS TIBOR , KOFOD-HANSEN MIKAEL , HANSEN THOMAS KRUSE
发明人： BEHRENS CARSTEN , LAU JESPER , KODRA JANOS TIBOR , KOFOD-HANSEN MIKAEL , HANSEN THOMAS KRUSE
IPC分类号： A61K47/48
CPC分类号： B82Y5/00 , A61K47/595 , A61K47/60 , A61K47/641 , A61K47/6949
摘要： Novel GLP-1 conjugated with structurally well defined polymers and their therapeutically use.
摘要翻译：与结构明确定义的聚合物结合的新型GLP-1及其治疗用途。

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