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1. 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。

2. 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。

3. 发明申请

WO2006079641A3 INSULIN DERIVATIVES 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胰岛素衍生物
公开(公告)号：WO2006079641A3
公开(公告)日：2007-06-14
申请号：PCT/EP2006050458
申请日：2006-01-26
申请人： NOVO NORDISK AS , BEHRENS CARSTEN , LAU JESPER , KODRA JANOS TIBOR , KOFOD-HANSEN MIKAEL , HOEG-JENSEN THOMAS , MADSEN PETER , HAVELUND SVEND
发明人： BEHRENS CARSTEN , LAU JESPER , KODRA JANOS TIBOR , KOFOD-HANSEN MIKAEL , HOEG-JENSEN THOMAS , MADSEN PETER , HAVELUND SVEND
IPC分类号： A61K47/48
CPC分类号： B82Y5/00 , A61K47/59 , A61K47/595 , A61K47/60 , A61K47/641 , A61K47/6949
摘要： Insulin conjugated with structurally well defined, bifurcated and trifurcated polymers can be use by pulmonary delivery for systemic absorption through the lungs to reduce or eliminate the need for administering other insulins by injection.
摘要翻译：与结构明确定义的分叉和三叉酸聚合物结合的胰岛素可以通过肺部递送用于通过肺的全身吸收，以减少或消除通过注射施用其它胰岛素的需要。

4. 发明申请

WO0042026B1 NON-PEPTIDE GLP-1 AGONISTS 审中-公开
标题翻译：非肽GLP-1激动剂
公开(公告)号：WO0042026B1
公开(公告)日：2000-10-05
申请号：PCT/DK0000014
申请日：2000-01-14
申请人： NOVO NORDISK AS , AGOURON PHARMA , TENG MIN , TRUESDALE LARRY KENNETH , BHUMRALKAR DILIP , KIEL DAN , JOHNSON MICHAEL D , THOMAS CHRISTINE , JOERGENSEN ANKER STEEN , MADSEN PETER , OLESEN PREBEN HOULBERG , KNUDSEN LISELOTTE BJERRE , PETTERSON INGRID VIVIKA , CORNELIS DE JONG JOHANNES , BEHRENS CARSTEN , KODRA JANOS TIBOR , LAU JESPER
发明人： TENG MIN , TRUESDALE LARRY KENNETH , BHUMRALKAR DILIP , KIEL DAN , JOHNSON MICHAEL D , THOMAS CHRISTINE , JOERGENSEN ANKER STEEN , MADSEN PETER , OLESEN PREBEN HOULBERG , KNUDSEN LISELOTTE BJERRE , PETTERSON INGRID VIVIKA , CORNELIS DE JONG JOHANNES , BEHRENS CARSTEN , KODRA JANOS TIBOR , LAU JESPER
IPC分类号： C07D215/18 , A61K31/47 , A61K31/498 , A61K31/519 , A61K31/53 , A61K31/5377 , A61K31/55 , A61K45/00 , A61P3/04 , A61P3/10 , A61P43/00 , C07D215/20 , C07D215/36 , C07D215/54 , C07D241/24 , C07D241/42 , C07D241/44 , C07D241/52 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D487/04 , C07D491/10 , C07D491/20 , C07D495/04 , C07D241/00
CPC分类号： C07D401/04 , C07D241/42 , C07D241/44 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D487/04 , C07D491/10
摘要： Novel non-peptide GLP-1 agonists, pharmaceutical compositions comprising them, use of the non-peptide GLP-1 agonists for the preparation of pharmaceutical compositions and methods for the treatment and/or prevention of disorders and diseases wherein an activation of the human GLP-1 receptor is beneficial, especially metabolic disorders such as IGT, Type 1 diabetes, Type 2 diabetes and obesity.
摘要翻译：新型非肽GLP-1激动剂，包含它们的药物组合物，使用非肽GLP-1激动剂来制备用于治疗和/或预防疾病和疾病的药物组合物和方法，其中人GLP -1受体是有益的，特别是代谢疾病如IGT，1型糖尿病，2型糖尿病和肥胖。

5. 发明申请

WO2005058845A3 NOVEL GLUCAGON ANTAGONISTS/INVERSE AGONISTS 审中-公开
标题翻译：新的GLUCAGON ANTAGONISTS / INVERSE AGONISTS
公开(公告)号：WO2005058845A3
公开(公告)日：2005-10-20
申请号：PCT/EP2004053580
申请日：2004-12-17
申请人： NOVO NORDISK AS , MADSEN PETER , LAU JESPER , KODRA JANOS TIBOR , CHRISTENSEN INGE THOEGER
发明人： MADSEN PETER , LAU JESPER , KODRA JANOS TIBOR , CHRISTENSEN INGE THOEGER
IPC分类号： A61K31/198 , A61K31/275 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/50 , C07C235/84 , C07C237/12 , C07D207/32 , C07D207/323 , C07D233/70 , C07D233/96 , C07D237/02 , C07D237/08 , C07D261/02 , C07D261/08 , C07D261/18 , C07D413/12 , A61P3/04 , A61P3/06 , A61P3/10
CPC分类号： C07D207/323 , C07C235/84 , C07C2601/02 , C07C2601/14 , C07D233/96 , C07D237/08 , C07D261/18
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. (I) wherein A is (II), (III) or (IV), Y is a valence bond, >C=O, =CR -, -(CR R )m-, -NR -,=N-, E is: C1-10-alkyl or C2-10-alkenyl; C3-10-cycloalkyl, C3-10-cycloalkenyl, C7-10-bicycloalkyl, C3-10-cycloakyl-C1-6-alkyl, C3-10-cycloalkenyl-C1-6-alkyl or C7-10-bicycloalkyl-C1-6-alkyl, wherein the rings may optionally be substituted with one or more substituents selected from halogen, C1-6-alkyl, C2-6-alkenyl, C1-6-alkoxy, C1-6-thioalkyl, -CF3, -OCF3, -SCF3, -OCHF2 and -SCHF2; aryl, aryloxy, arylthio, heteroaryl, aryl-C1-6-alkyl, aryloxy-C1-6-alkyl, arylthio-C1-6-alkyl, heteroaryl-C1-6-alkyl, diaryl-C1-6-alkyl or (C1-6 -alkyl)(aryl)-C1-7-alkyl, wherein the non-aromatic and aromatic rings may optinally be substituted with one or more substituents selected from halogen, C1-6-alkyl, C2-6-alkenyl, C1-6 -alkoxy, C1-6-thioalkyl, -CF3, -OCF3, -SCF3, -OCHF2, SCHF2, C3-10-cycloalkyl and C3-10-cycloalkenyl, or with two substituents on adjacent positions which are combined to form a bridge C1-6-alkylene, C2-6-alkenylene or -O-C1-6-alkylene-O-; (V) represents a phenyl, C3-8-cycloalkyl, or a 4-, 5-, 6- or 7-membered heterocycle, D is aryl or heteroaryl.
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。（I）其中A是（II），（III）或（IV），Y是价键，C = O，= CR 1 - ， - （CR 1 R 2）m - ，-NR 1 - ，= N-，E是：C 1-10 - 烷基或C 2-10 - 烯基; C 3-10 - 环烷基，C 3-10 - 环烯基，C 7-10 - 双环烷基，C 3-10 - 环烷基-C 1-6 - 烷基，C 3-10 - 环烯基-C 1-6 - 烷基或C 3-10 - 双环烷基-C 其中所述环可以任选地被一个或多个选自卤素，C 1-6 - 烷基，C 2-6 - 烯基，C 1-6 - 烷氧基，C 1-6 - 硫代烷基，-CF 3，-OCF 3， -SCF 3，-OCHF 2和-SCHF 2; 芳基，芳氧基，芳硫基，杂芳基，芳基-C 1-6 - 烷基，芳氧基-C 1-6 - 烷基，芳硫基-C 1-6 - 烷基，杂芳基-C 1-6 - 烷基，二芳基-C 1-6 - 烷基或（C 1 （芳基）-C 1-7 - 烷基，其中非芳族和芳族环可以选择性地被一个或多个选自卤素，C 1-6 - 烷基，C 2-6 - 烯基，C 1 -C 6 - 6-烷氧基，C 1-6 - 硫代烷基，-CF 3，-OCF 3，-SCF 3，-OCHF 2，SCHF 2，C 3-10 - 环烷基和C 3-10 - 环烯基，或与相邻位置上的两个取代基组合形成桥 C 1-6亚烷基，C 2-6亚烯基或-O-C 1-6 - 亚烷基-O-; （V）代表苯基，C 3-8 - 环烷基或4-，5-，6-或7-元杂环，D是芳基或杂芳基。

6. 发明申请

WO2007128817A3 INSULIN DERIVATIVE 审中-公开
标题翻译：胰岛素衍生物
公开(公告)号：WO2007128817A3
公开(公告)日：2008-03-06
申请号：PCT/EP2007054444
申请日：2007-05-08
申请人： NOVO NORDISK AS , 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： C07K14/62 , 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值下是可溶的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。

7. 发明申请

WO2008145721A3 N-TERMINAL MODIFICATION OF POLYPEPTIDES FOR PROTECTION AGAINST DEGRADATION BY AMINOPEPTIDASES 审中-公开
标题翻译：用于保护抗微生物剂降解的多肽的N-末端修饰
公开(公告)号：WO2008145721A3
公开(公告)日：2009-03-12
申请号：PCT/EP2008056673
申请日：2008-05-30
申请人： NOVO NORDISK AS , SENSFUSS ULRICH , HUBALEK FRANTISEK , SCHAEFFER LAUGE , HOEG-JENSEN THOMAS , KODRA JANOS TIBOR
发明人： SENSFUSS ULRICH , HUBALEK FRANTISEK , SCHAEFFER LAUGE , HOEG-JENSEN THOMAS , KODRA JANOS TIBOR
IPC分类号： C07K14/435 , C07K14/62
CPC分类号： C07K14/62 , C07K1/003 , C07K14/605
摘要： N-terminally modified polypeptides comprising one or more N-terminal modifications consisting of an organic molecular substituent having a MW below 100 g per mol are ob- tained by the invention. Also compositions comprising such and the use thereof are com- prised by the invention.
摘要翻译：包含一个或多个N末端修饰的N-末端修饰的多肽由MW低于100g / mol的有机分子取代基组成，得到本发明。包含该组合物的组合物及其用途也包括本发明。

8. 发明申请

WO2004085471A3 GLP-2 DERIVATIVES 审中-公开
标题翻译： GLP-2衍生物
公开(公告)号：WO2004085471A3
公开(公告)日：2004-11-04
申请号：PCT/DK2004000198
申请日：2004-03-23
申请人： NOVO NORDISK AS , KODRA JANOS TIBOR , JOHANSEN NILS LANGELAND , THIM LARS , PESCHKE BERND
发明人： KODRA JANOS TIBOR , JOHANSEN NILS LANGELAND , THIM LARS , PESCHKE BERND
IPC分类号： A61K38/00 , A61K47/48 , A61P1/00 , C07K14/605 , A61K38/26
CPC分类号： C07K14/605 , A61K38/00 , A61K47/60
摘要： The present invention relates to novel derivatives of human glucagon-like peptide-2 (GLP-2) peptides which have a protracted profile of action, as well as pharmaceutical compositions, uses and methods of treatment.
摘要翻译：本发明涉及具有长期作用特征的人胰高血糖素样肽-2（GLP-2）肽的新衍生物，以及药物组合物，用途和治疗方法。

9. 发明专利

JP2013144684A Double-acylated glp-1 derivative 有权
标题翻译：双取代的GLP-1衍生物
公开(公告)号：JP2013144684A
公开(公告)日：2013-07-25
申请号：JP2013030695
申请日：2013-02-20
申请人： Novo Nordisk As , ノヴォノルディスクアー/エス
发明人： GARIBAY PATRICK WILLIAM , JANE SPETZLER , KODRA JANOS TIBOR , LINDEROTH LARS , LAU JESPER , SAUERBERG PER
IPC分类号： C07K14/605 , A61K38/26 , A61K47/48 , A61P1/00 , A61P3/04 , A61P3/10 , A61P9/00 , A61P15/00 , A61P43/00
CPC分类号： C07K14/65 , A61K38/00 , A61K47/48038 , A61K47/48215 , A61K47/542 , A61K47/60 , C07K14/605 , G01N2333/605
摘要： PROBLEM TO BE SOLVED: To provide a derivative of a GLP-1 analogue suitable for oral administration and capable of being used, for example in treatment and/or prevention of all forms of diabetes and related diseases.SOLUTION: The invention relates to: a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 37 of GLP-1(7-37), a second K residue at a position corresponding to position 26 of GLP-1(7-37), and a maximum of ten amino acid modifications as compared to GLP-1(7-37), wherein the first K residue is designated K, and the second K residue is designated K. The derivative comprises two albumin binding moieties attached to Kand K, respectively; or a pharmaceutically acceptable salt, amide, or ester thereof.
摘要翻译：要解决的问题：提供适于口服给药并能够用于例如治疗和/或预防所有形式的糖尿病和相关疾病的GLP-1类似物的衍生物。解决方案：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）的位置37的位置处的第一个K残基，对应于GLP-1（7- 37），并且与GLP-1（7-37）相比最多10个氨基酸修饰，其中第一个K残基指定为K，第二个K残基用K表示。该衍生物包含两个白蛋白结合部分 Kand K; 或其药学上可接受的盐，酰胺或酯。

10. 发明专利

JP2011006435A Amide derivative as gk activator 审中-公开
标题翻译：酰胺衍生物作为GK激活剂
公开(公告)号：JP2011006435A
公开(公告)日：2011-01-13
申请号：JP2010178083
申请日：2010-08-06
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 , KODRA JANOS TIBOR , GUZEL MUSTAFA , SANTOSH KALPATHY CHIDAMBARESWARAN , MJALLI ADNAN M M , ANDREWS ROBERT CARL , POLISETTI DHARMA RAO
IPC分类号： C07D213/75 , C07D239/42 , A61K31/16 , A61K31/18 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/4402 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/505 , A61K45/00 , A61K45/06 , A61P1/00 , A61P1/18 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/50 , A61P9/00 , A61P9/10 , A61P9/12 , A61P43/00 , C07D277/20 , C07D277/44 , C07D277/46 , C07D277/48 , C07D285/135 , C07D405/12 , C07D409/12 , C07D417/12
CPC分类号： C07D277/46 , A61K31/16 , A61K31/18 , A61K45/06 , C07D213/75
摘要： PROBLEM TO BE SOLVED: To provide a glucokinase activator which is useful for the management, treatment, regulation or adjunct treatment of diseases or conditions, where increasing glucokinase activity is beneficial, e.g. for diseases such as impaired glucose tolerance (IGT), syndrome X, type II diabetes, type I diabetes, dyslipidemia, hyperlipidemia, hypertension and obesity.SOLUTION: The compound is expressed by general formula (I), in which Rin the formula (I) is such as a thiazole, thiadiazole, isothiazole, pyridine and pyrimidine, etc., which may be substituted.
摘要翻译：要解决的问题：提供可用于治疗，治疗，调节或辅助治疗疾病或病症的葡糖激酶活化剂，其中增加葡糖激酶活性是有益的，例如，对于葡萄糖耐量异常（IGT），X综合征，II型糖尿病，I型糖尿病，血脂异常，高脂血症，高血压和肥胖等疾病。解决方案：该化合物由通式（I）表示，其中Rin为式）是噻唑，噻二唑，异噻唑，吡啶和嘧啶等，它们可以被取代。

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