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1. 发明申请

WO2009022013A1 INSULIN ANALOGUES WITH AN ACYL AND AKLYLENE GLYCOL MOIETY 审中-公开
标题翻译：具有ACYL和AKLYLENE GLYCOL MOIETY的胰岛素类似物
公开(公告)号：WO2009022013A1
公开(公告)日：2009-02-19
申请号：PCT/EP2008/060768
申请日：2008-08-15
申请人： NOVO NORDISK A/S , MADSEN, Peter , KJELDSEN, Thomas Børglum , HOEG-JENSEN, Thomas , TAGMOSE, Tina Møller , JAKOBSEN, Palle , KODRA, János Tibor , GARIBAY, Patrick William , GRAM, Dorte Xenia
发明人： MADSEN, Peter , KJELDSEN, Thomas Børglum , HOEG-JENSEN, Thomas , TAGMOSE, Tina Møller , JAKOBSEN, Palle , KODRA, János Tibor , GARIBAY, Patrick William , GRAM, Dorte Xenia
IPC分类号： C07K14/62 , A61K38/28
CPC分类号： C07K14/62 , A61K38/00
摘要： An acylated insulin analogue wherein the insulin analogue comprises a lysine residue connected C-terminally to the A21 amino acid residue or a peptide residue of up to 4 amino acid residues comprising a lysine residue which peptide residue is connected C-terminally to the A21 amino acid residue, characterized in that an acyl moiety comprising an alkylene glycol moiety is attached to the lysine residue in the A22 position or attached to a lysine residue present in the peptide residue that is attached to the C terminal end of the A21 amino acid residue and wherein there is only one lysine (K, Lys) in the insulin analogue, can conveniently be administered pulmonary.
摘要翻译：酰化胰岛素类似物，其中胰岛素类似物包含与A21氨基酸残基C末端连接的赖氨酸残基或至多包含赖氨酸残基的至多4个氨基酸残基的肽残基，该肽残基与C21末端连接至A21氨基酸残基，其特征在于包含亚烷基二醇部分的酰基部分连接到A22位置的赖氨酸残基，或连接到与A21氨基酸残基的C末端连接的肽残基中存在的赖氨酸残基，并且其中胰岛素类似物中只有一个赖氨酸（K，Lys），可方便地给予肺部。

2. 发明申请

WO2009022005A1 INSULIN ANALOGUES WITH AN ACYL AND ALKYLENE GLYCOL MOIETY 审中-公开
标题翻译：具有ACYL和ALGYLENE GLYCOL MOIETY的胰岛素类似物
公开(公告)号：WO2009022005A1
公开(公告)日：2009-02-19
申请号：PCT/EP2008/060733
申请日：2008-08-15
申请人： NOVO NORDISK A/S , MADSEN, Peter , KJELDSEN, Thomas Børglum , HOEG-JENSEN, Thomas , TAGMOSE, Tina Møller , JAKOBSEN, Palle , KODRA, János Tibor , GARIBAY, Patrick William , GRAM, Dorte Xenia
发明人： MADSEN, Peter , KJELDSEN, Thomas Børglum , HOEG-JENSEN, Thomas , TAGMOSE, Tina Møller , JAKOBSEN, Palle , KODRA, János Tibor , GARIBAY, Patrick William , GRAM, Dorte Xenia
IPC分类号： C07K14/62 , A61K38/28
CPC分类号： C07K14/62 , A61K38/00
摘要： An acylated insulin analogue wherein the insulin analogue comprises a lysine residue connected C-terminally to the A21 amino acid residue or a peptide residue of up to 4 amino acid residues comprising a lysine residue which peptide residue is connected C-terminally to the A21 amino acid residue, characterized in that an acyl moiety comprising an alkylene glycol moiety is attached to the lysine residue in the A22 position or attached to a lysine residue present in the peptide residue that is attached to the C terminal end of the A21 amino acid residue and wherein there is only one lysine (K, Lys) in the insulin analogue, can conveniently be administered pulmonary.
摘要翻译：酰化胰岛素类似物，其中胰岛素类似物包含与A21氨基酸残基C末端连接的赖氨酸残基或至多包含赖氨酸残基的至多4个氨基酸残基的肽残基，该肽残基与C21末端连接至A21氨基酸残基，其特征在于包含亚烷基二醇部分的酰基部分连接到A22位置的赖氨酸残基，或连接到与A21氨基酸残基的C末端连接的肽残基中存在的赖氨酸残基，并且其中胰岛素类似物中只有一个赖氨酸（K，Lys），可方便地给予肺部。

3. 发明申请

WO1992001672A1 PIPERIDINE COMPOUNDS, THEIR PREPARATION AND USE 审中-公开
标题翻译：哌啶化合物，其制备和使用
公开(公告)号：WO1992001672A1
公开(公告)日：1992-02-06
申请号：PCT/DK1991000206
申请日：1991-07-15
申请人： NOVO NORDISK A/S
发明人： NOVO NORDISK A/S , JAKOBSEN, Palle , KANSTRUP, Anders , LUNDBECK, Jane, Marie
IPC分类号： C07D211/18
CPC分类号： C07D401/04 , C07D211/22 , C07D211/26 , C07D211/34 , C07D211/90 , C07D405/12
摘要： Novel piperidine compounds having formula (I), wherein R is 3,4-methylenedioxyphenyl, phenyl, naphthyl, or a 5 or 6 membered heterocyclic group containing one or two N, O or S - atoms being saturated, partly saturated or aromatic which are optionally substituted with one or more halogen, amino, C1-6-alkyl mono- or disubstituted amino, C1-6-alkoxy, cyano, mono- or poly halogenated C1-6-alkyl, C2-6-alkenyl, C1-6-alkyl, C3-5-alkylene, trifluoromethoxy, hydroxy, hydroxy C1-4-alkyl, or trifluoromethyl; n is 0 to 4; R is hydrogen, straight or branched C1-8-alkyl, C1-8-alkoxy-C1-8-alkyl, C3-8-cycloalkyl, C2-6-alkenyl, C4-8-cycloalkylalkyl, acetyl or C2-6-alkenyl; X is one or more amino, NO2, C1-6-alkyl mono- or disubstituted amino, C1-8-alkanoylamino, carboxy, C1-6-alkyl mono- or disubstituted ureido, C1-6-alkyl substituted with amino which are optionally mono- or disubstituted with C1-6-alkyl, unsubstituted carbamoyl or C1-6-alkyl optionally substituted with phenyl and/or hydroxy N-mono or disubstituted carbamoyl, unsubstituted sulfamoyl, C1-6-alkyl N-substituted sulfamoyl, C1-6-alkyl S-substituted sulfamoyl, C1-6-alkyl N-and S-substituted sulfamoyl, or a 5 or 6 membered heterocyclic group containing one or two N, O or S - atoms being saturated, partly saturated or aromatic, the heterocyclic group can be fused to the ring and, when Y is NR and/or n is 1 to 4 X is halogen, C1-6-alkyl, C2-6-alkenyl, C3-8-cycloalkyl, C4-8-cycloalkylalkyl, C1-6-alkoxy, cyano, mono- or poly halogenated C1-6-alkyl, hydroxy or hydrogen; Y is O, S or NR wherein R is hydrogen or C1-5-alkyl, or a salt thereof with a pharmaceutically-acceptable acid. The novel compounds are useful in the treatment of anoxia, traumatic injury, ischemia, migraine, epilepsy and other neurodegenerative diseases.
摘要翻译：具有式（I）的新的哌啶化合物，其中R 3是3,4-亚甲二氧基苯基，苯基，萘基或含有一个或两个N，O或S-原子的5或6元杂环基团是饱和的，部分饱和的或芳基，其任选被一个或多个卤素，氨基，C 1-6 - 烷基单取代或二取代的氨基，C 1-6 - 烷氧基，氰基，单 - 或多卤代C 1-6 - 烷基，C 2-6 - 烯基，C 1 - C 3-6 - 烷基，C 3-5 - 亚烷基，三氟甲氧基，羟基，羟基C 1-4 - 烷基或三氟甲基; n为0〜4; R 1是氢，直链或支链C 1-8 - 烷基，C 1-8 - 烷氧基-C 1-8 - 烷基，C 3-8 - 环烷基，C 2-6 - 烯基，C 4-8 - 环烷基烷基，乙酰基或C 2-8 - 6烯基; X是一个或多个氨基，NO 2，C 1-6 - 烷基单或二取代的氨基，C 1-8 - 烷酰基氨基，羧基，C 1-6 - 烷基单或二取代的脲基，被任选被被C 1-6 - 烷基，未取代的氨基甲酰基或任选被苯基和/或羟基N-单取代或未取代的氨基甲酰基，未取代的氨磺酰基，C 1-6 - 烷基N-取代的氨磺酰基，C 1-6 - - 烷基S-取代的氨磺酰基，C 1-6 - 烷基N-和S-取代的氨磺酰基，或含有一个或两个N，O或S-原子饱和，部分饱和或芳族的5或6元杂环基，杂环基可以与环稠合，并且当Y是NR和/或n是1至4时，X是卤素，C 1-6 - 烷基，C 2-6 - 烯基，C 3-8 - 环烷基，C 4-8 - 环烷基烷基，氰基，单或多卤代C 1-6 - 烷基，羟基或氢; Y是O，S或NR，其中R是氢或C 1-5 - 烷基，或其盐与药学上可接受的酸。新型化合物可用于治疗缺氧，创伤性损伤，局部缺血，偏头痛，癫痫等神经退行性疾病。

4. 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。

5. 发明申请

WO2008015099A2 PEGYLATED, EXTENDED INSULINS 审中-公开
标题翻译： PEGYLATED，延长胰岛素
公开(公告)号：WO2008015099A2
公开(公告)日：2008-02-07
申请号：PCT/EP2007/057321
申请日：2007-07-16
申请人： NOVO NORDISK A/S , MADSEN, Peter , KJELDSEN, Thomas Børglum , TAGMOSE, Tina Møller , JAKOBSEN, Palle
发明人： MADSEN, Peter , KJELDSEN, Thomas Børglum , TAGMOSE, Tina Møller , JAKOBSEN, Palle
CPC分类号： A61K38/28 , A61K47/60
摘要： PEGylated, extended insulins are insulins which, compared with human insulin, has one or more extensions extended from the A1, B1, A21 and/or B30 position(s), said extension(s) consist(s) of amino acid residue(s) and wherein a PEG moiety, via a linker, is attached to one or more of the amino acid residues in the extension(s). PEG is polyethyleneglycol. Such PEGylated, extended insulins have higher bioavailability and a longer time-action profile than regulär insulin and are in particular suited for pulmonary administration and can, conveniently, be used to treat diabetes.
摘要翻译： PEG化延长的胰岛素是与人胰岛素相比具有从A1，B1，A21和/或B30位置延伸的一个或多个延伸的胰岛素，所述延伸由（ s）的氨基酸残基并且其中PEG部分通过接头连接至延伸中的一个或多个氨基酸残基。 PEG是聚乙二醇。这种聚乙二醇化延长的胰岛素比调节胰岛素具有更高的生物利用度和更长的时间 - 作用特征，并且特别适合于肺部给药，并且可以方便地用于治疗糖尿病。

6. 发明申请

WO2007135118A1 SOLUBLE, STABLE INSULIN-CONTAINING FORMULATIONS 审中-公开
标题翻译：可溶性，稳定的含胰岛素的制剂
公开(公告)号：WO2007135118A1
公开(公告)日：2007-11-29
申请号：PCT/EP2007/054863
申请日：2007-05-21
申请人： NOVO NORDISK A/S , OLSEN, Helle, Birk , KAARSHOLM, Niels, Christian , JAKOBSEN, Palle , BALSCHMIDT, Per
发明人： OLSEN, Helle, Birk , KAARSHOLM, Niels, Christian , JAKOBSEN, Palle , BALSCHMIDT, Per
IPC分类号： A61K38/28 , A61K47/02 , A61P3/10
CPC分类号： A61K47/42 , A61K9/0019 , A61K38/28 , A61K47/12 , A61K47/34
摘要： The present invention relates to pharmaceutical formulations comprising acid stabi- lized insulin, and a salt of protamine or other positively charged peptides, to methods of pre- paring such formulations, and to uses of such formulations in the treatment of diseases and conditions for which use of the insulin peptide(s) contained in such formulations is indicated.
摘要翻译：本发明涉及包含酸稳定胰岛素和鱼精蛋白或其它带正电荷的肽的盐的药物制剂，用于制备这些制剂的方法，以及这些制剂在治疗使用的疾病和病症中的用途的这些制剂中所含的胰岛素肽。

7. 发明申请

WO2011000823A1 INSULIN DERIVATIVES 审中-公开
标题翻译：胰岛素衍生物
公开(公告)号：WO2011000823A1
公开(公告)日：2011-01-06
申请号：PCT/EP2010/059194
申请日：2010-06-29
申请人： NOVO NORDISK A/S , HOEG-JENSEN, Thomas , JAKOBSEN, Palle , SENSFUSS, Ulrich , FLEDELIUS, Christian , RIBEL-MADSEN, Ulla
发明人： HOEG-JENSEN, Thomas , JAKOBSEN, Palle , SENSFUSS, Ulrich , FLEDELIUS, Christian , RIBEL-MADSEN, Ulla
IPC分类号： C07K14/62 , A61P3/10
CPC分类号： C07K14/62 , A61K38/00
摘要： The novel insulin derivates delivers, after administration to humans, insulin as a function of the glucose concentration in the tissue.
摘要翻译：在给予人之后，新型胰岛素衍生物作为组织中葡萄糖浓度的函数递送胰岛素。

8. 发明申请

WO2004080480A1 PHARMACEUTICAL PREPARATIONS COMPRISING ACID-STABILISED INSULIN 审中-公开
标题翻译：包含酸稳定胰岛素的药物制剂
公开(公告)号：WO2004080480A1
公开(公告)日：2004-09-23
申请号：PCT/DK2004/000158
申请日：2004-03-11
申请人： NOVO NORDISK A/S , ØSTERGAARD, Søren , OLSEN, Helle, Birk , KAARSHOLM, Niels, C. , MADSEN, Peter , JAKOBSEN, Palle , LUDVIGSEN, Svend , SCHLUCKEBIER, Gerd , STEENSGAARD, Dorte, Bjerre , PETERSEN, Anders, Klarskov
发明人： ØSTERGAARD, Søren , OLSEN, Helle, Birk , KAARSHOLM, Niels, C. , MADSEN, Peter , JAKOBSEN, Palle , LUDVIGSEN, Svend , SCHLUCKEBIER, Gerd , STEENSGAARD, Dorte, Bjerre , PETERSEN, Anders, Klarskov
IPC分类号： A61K38/28
CPC分类号： A61K45/06 , A61K33/30 , A61K38/28 , A61K47/34 , C07D215/38 , C07D233/96 , C07D239/26 , C07D249/06 , C07D249/18 , C07D257/04 , C07D277/20 , C07D277/62 , C07D307/80 , C07D307/81 , C07D317/54 , C07D401/04 , C07D401/12 , C07D403/06 , C07D405/10 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D417/04 , C07D417/06 , C07D417/10 , C07D417/14 , C07D471/04 , C07D513/04 , C07K14/62 , A61K2300/00
摘要： Novel ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer that are capable of prolonging the action of insulin preparations are disclosed.
摘要翻译：公开了能够延长胰岛素制剂作用的R状态胰岛素六聚体的HisB10 Zn 2+位点的新配体。

9. 发明申请

WO2003076461A3 DIMERIC TF ANTAGONIST COMPRISING TWO FACTOR VII POLYPEPTIDES 审中-公开
公开(公告)号：WO2003076461A3
公开(公告)日：2003-09-18
申请号：PCT/DK2003/000151
申请日：2003-03-12
申请人： NOVO NORDISK A/S
发明人： KJALKE, Marianne , JAKOBSEN, Palle , STENNICKE, Henning, Ralf
IPC分类号： C12N9/96
摘要： Dimer FVII polypeptides, which binds and inhibits two TF molecules simultaneously, and thereby functions as an anticoagulant.

10. 发明申请

WO2003076461A2 DIMERIC TF ANTAGONIST 审中-公开
公开(公告)号：WO2003076461A2
公开(公告)日：2003-09-18
申请号：PCT/DK2003/000151
申请日：2003-03-12
申请人： NOVO NORDISK A/S
发明人： KJALKE, Marianne , JAKOBSEN, Palle , STENNICKE, Henning, Ralf
IPC分类号： C07K14/00
CPC分类号： A61K51/088 , A61K38/00 , A61K47/64 , C12N9/64 , C12N9/96
摘要： Dimer FVII polypeptides, which binds and inhibits two TF molecules simultaneously.
摘要翻译：二聚体FVII多肽，其同时结合并抑制两个TF分子。

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