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1. 发明专利

IL289504D0 Solid compositions comprising a glp-1 agonist, an sglt2 inhibitor and a salt of n-(8-(2-hydroxybenzoyl)amino)caprylic acid 未知
公开(公告)号：IL289504D0
公开(公告)日：2022-02-01
申请号：IL28950421
申请日：2021-12-29
申请人： NOVO NORDISK AS , PEDERSEN BETTY LOMSTEIN , NISSEN BIRGITTE , GARIBAY PATRICK WILLIAM , NAELAP?? KAISA , VEGGE ANDREAS
发明人： PEDERSEN BETTY LOMSTEIN , NISSEN BIRGITTE , GARIBAY PATRICK WILLIAM , NAELAP?? KAISA , VEGGE ANDREAS
IPC分类号： A61K31/192 , A61K31/70 , A61K31/7048 , A61K38/26 , A61K45/06
摘要： The invention relates to solid pharmaceutical compositions comprising a GLP-1 agonist, an SGLT2 inhibitor and a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid. The invention further relates to processes for the preparation of such compositions, and their use in medicine.

2. 发明申请

WO2011154349A3 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：WO2011154349A3
公开(公告)日：2012-03-01
申请号：PCT/EP2011059273
申请日：2011-06-06
申请人： NOVO NORDISK AS , GARIBAY PATRICK WILLIAM , WOELDIKE HELLE , ZHANG XUJIA , THOEGERSEN HENNING , NIELSEN PETER KRESTEN , ANDERSEN BIRGITTE , WANG JISHU , BAK-JENSEN KRISTIAN SASS , TAGMOSE TINA MOELLER
发明人： GARIBAY PATRICK WILLIAM , WOELDIKE HELLE , ZHANG XUJIA , THOEGERSEN HENNING , NIELSEN PETER KRESTEN , ANDERSEN BIRGITTE , WANG JISHU , BAK-JENSEN KRISTIAN SASS , TAGMOSE TINA MOELLER
IPC分类号： A61K38/18 , A61K47/48 , C07K14/50
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。

3. 发明申请

WO2006035057A1 MODIFIED PROTEINS 审中-公开
标题翻译：改良蛋白
公开(公告)号：WO2006035057A1
公开(公告)日：2006-04-06
申请号：PCT/EP2005/054901
申请日：2005-09-29
申请人： NOVO NORDISK A/S , BEHRENS, Carsten , GARIBAY, Patrick, William , ZUNDEL, Magali
发明人： BEHRENS, Carsten , GARIBAY, Patrick, William , ZUNDEL, Magali
IPC分类号： C12P21/00 , C07K14/745 , A61K38/36 , C12P19/30 , C12P19/32
CPC分类号： C12P21/005 , A61K47/60 , C07K1/1077 , C07K9/003
摘要： A method of conjugating peptides and proteins by means of glycosyltransferase is provided.
摘要翻译：提供了通过糖基转移酶缀合肽和蛋白质的方法。

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

WO2011080103A1 DOUBLE-ACYLATED GLP-1 DERIVATIVES 审中-公开
标题翻译：双酚A-GLP-1衍生物
公开(公告)号：WO2011080103A1
公开(公告)日：2011-07-07
申请号：PCT/EP2010/069932
申请日：2010-12-16
申请人： NOVO NORDISK A/S , GARIBAY, Patrick, William , SPETZLER, Jane , KODRA, János, Tibor , LINDEROTH, Lars , LAU, Jesper , SAUERBERG, Per
发明人： GARIBAY, Patrick, William , SPETZLER, Jane , KODRA, János, Tibor , LINDEROTH, Lars , LAU, Jesper , SAUERBERG, Per
IPC分类号： C07K14/605 , A61K47/48
CPC分类号： C07K14/65 , A61K38/00 , A61K47/542 , A61K47/60 , C07K14/605 , G01N2333/605
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 37 of GLP-1 (7-37) (SEQ ID NO: 1), 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 37 , and the second K residue is designated K 26 , which derivative comprises two albumin binding moieties attached to K 26 and K 37 , respectively, wherein the albumin binding moiety comprises a protracting moiety selected from: Chem. 1 : HOOC-(CH 2 ) X -CO-* Chem. 2: HOOC-C 6 H 4 -O-(CH 2 ) y -CO-* Chem. 3: R 1 -C 6 H 4 -(CH 2 ) Z -CO-* Chem. 4: HOOC-C 4 SH 2 -(CH 2 ) W -CO-* in which x is an integer in the range of 6-18, y is an integer in the range of 3-17, z is an integer in the range of 1 -5, R 1 is a group having a molar mass not higher than 150 Da, and w is an integer in the range of 6-18; with the proviso that when the protracting moiety is Chem. 1, the albumin binding moiety further comprises a linker of formula Chem. 5: *-NH-(CH 2 ) 2 -(O-(CH 2 ) 2 ) k -O-(CH 2 ) n -CO-*, wherein k is an integer in the range of 1-5, and n is an integer in the range of 1-5; 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 suitable for oral administration.
摘要翻译：本发明涉及GLP-1类似物的衍生物，其类似物包含在对应于GLP-1（7-37）（SEQ ID NO：1）的第37位的位置处的第一个K残基，相对于GLP-1（7-37）的位置26的位置和与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K37，第二个K残基是命名为K26，该衍生物分别包含与K26和K37连接的两个白蛋白结合部分，其中白蛋白结合部分包含选自下列的伸长部分： 1：HOOC-（CH2）X-CO- * Chem。 2：HOOC-C6H4-O-（CH2）y-CO- * 3：R1-C6H4-（CH2）Z-CO- * Chem。 4：HOOC-C4SH2-（CH2）W-CO- *，其中x是6-18的整数，y是3-17的整数，z是1〜 5，R1是摩尔质量不高于150Da的基团，w是6-18的整数; 条件是当伸长部分是Chem。如图1所示，白蛋白结合部分还包含式Chem的接头。 5：* -NH-（CH2）2-（O-（CH2）2）kO-（CH2）n-CO- *，其中k是1-5的整数，n是范围1-5; 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。该衍生物适合口服给药。

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

WO2007096431A1 INSULIN DERIVATIVES 审中-公开
标题翻译：胰岛素衍生物
公开(公告)号：WO2007096431A1
公开(公告)日：2007-08-30
申请号：PCT/EP2007/051835
申请日：2007-02-27
申请人： NOVO NORDISK A/S , FYNBO, Charlotte, Harkjaer , JONASSEN, Ib , KJELDSEN, Thomas, Børglum , MADSEN, Peter , GARIBAY, Patrick, William , KODRA, Janos, Tibor , HOEG-JENSEN, Thomas , TAGMOSE, Tina, Møller
发明人： FYNBO, Charlotte, Harkjaer , JONASSEN, Ib , KJELDSEN, Thomas, Børglum , MADSEN, Peter , GARIBAY, Patrick, William , KODRA, Janos, Tibor , HOEG-JENSEN, Thomas , TAGMOSE, Tina, Møller
IPC分类号： C07K14/62 , A61K38/28
CPC分类号： C07K14/62 , A61K38/00
摘要： The present invention is related to insulin derivatives having a side chain attached to an ε-amino group of a Lys residue present in the A-chain or to an ε -amino group of a Lys residue in the B-chain.
摘要翻译：本发明涉及具有连接在A链中存在的Lys残基的e-氨基的侧链或B链中的Lys残基的e-氨基的胰岛素衍生物。

8. 发明申请

WO2006082204A1 INSULIN DERIVATIVES 审中-公开
标题翻译：胰岛素衍生物
公开(公告)号：WO2006082204A1
公开(公告)日：2006-08-10
申请号：PCT/EP2006/050593
申请日：2006-02-01
申请人： NOVO NORDISK A/S , KODRA, János, Tibor , GARIBAY, Patrick, William , HOEG-JENSEN, Thomas , JONASSEN, Ib , MADSEN, Peter , TAGMOSE, Tina, Møller
发明人： KODRA, János, Tibor , GARIBAY, Patrick, William , HOEG-JENSEN, Thomas , JONASSEN, Ib , MADSEN, Peter , TAGMOSE, Tina, Møller
IPC分类号： C07K14/62 , A61K38/28
CPC分类号： A61K38/28 , C07K14/62
摘要： The present invention relates to insulin derivatives having a side chain attached either to the -amino group of the N-terminal amino acid residue of the B chain or to the amino group of a Lys residue present in the B chain of the parent insulin via an amide bond which side chain comprises at least one aromatic group; at least one free carboxylic acid group or a group which is negatively charged at neutral pH, a fatty acid moiety with 4 to 22 carbon atoms in the carbon chain; and possible linkers which link the individual components in the side chain together via amide bonds.
摘要翻译：本发明涉及具有侧链连接到B链的N末端氨基酸残基的氨基或存在于母体胰岛素的B链中的Lys残基的氨基的胰岛素衍生物，其通过酰胺键，该侧链包含至少一个芳族基团; 至少一个游离羧酸基团或在中性pH下带负电荷的基团，碳链中具有4-22个碳原子的脂肪酸部分; 以及通过酰胺键将侧链中各个组分连接在一起的可能接头。

9. 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。

10. 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）。

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