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1. 发明申请

WO2013037690A1 GLP-1 DERIVATIVES 审中-公开
标题翻译： GLP-1衍生物
公开(公告)号：WO2013037690A1
公开(公告)日：2013-03-21
申请号：PCT/EP2012/067364
申请日：2012-09-06
申请人： NOVO NORDISK A/S , LAU, Jesper , BLOCH, Paw , KOFOED, Jacob , GARIBAY, Patrick
发明人： LAU, Jesper , BLOCH, Paw , KOFOED, Jacob , GARIBAY, Patrick
IPC分类号： C07K14/605 , A61K38/26
CPC分类号： C07K14/605 , A61K38/00 , A61K38/26
摘要： The invention relates to a derivative of a GLP-1 peptide, which peptide has two Lys residues, namely a first and a second Lys residue, and a maximum of eight amino acid changes as compared to GLP-1(7-37) (SEQ ID NO: 3), which derivative comprises two protracting moieties attached to the epsilon amino group of said first and second Lys residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 15: HOOC-(CH 2 ) x -CO-*, and Chem. 16: HOOC-C 6 H 4 -O-(CH 2 ) y -CO-*, in which x is an integer in the range of 10-16, and y is an integer in the range of 8-12; and the linker comprises a first linker element *-NH-CH(CH 2 OH)-CO-*. A preferred linker is g Glu-Ser-Ser-Gly-Ser-Ser-Gly (SEQ ID NO: 2). The derivative of the invention has a very good potency, and a very good binding to the GLP-1 receptor. The invention also relates to the pharmaceutical use of the derivative, for example in the treatment and/or prevention of all forms of diabetes and related diseases.
摘要翻译：本发明涉及GLP-1肽的衍生物，该肽与GLP-1（7-37）（SEQ）相比具有两个Lys残基，即第一和第二Lys残基，最多八个氨基酸变化 SEQ ID NO：3），该衍生物分别包含通过接头分别连接到所述第一和第二Lys残基的ε氨基的两个伸长部分，其中伸长部分选自Chem。 15：HOOC-（CH 2）x -CO- *，和Chem。 16：HOOC-C 6 H 4 -O-（CH 2）y -CO- *，其中x是10-16的整数，y是8-12的整数; 并且连接体包含第一连接体元件* -NH-CH（CH 2 OH）-CO- *。优选的接头是g Glu-Ser-Ser-Gly-Ser-Ser-Gly（SEQ ID NO：2）。本发明的衍生物具有非常好的效力，并且与GLP-1受体具有非常好的结合。本发明还涉及衍生物的药物用途，例如用于治疗和/或预防所有形式的糖尿病和相关疾病。

2. 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。

3. 发明申请

WO2011080102A2 GLP-1 ANALOGUES AND DERIVATIVES 审中-公开
标题翻译： GLP-1类似物和衍生物
公开(公告)号：WO2011080102A2
公开(公告)日：2011-07-07
申请号：PCT/EP2010/069931
申请日：2010-12-16
申请人： NOVO NORDISK A/S , KALTHOFF, Christoph , LAU, Jesper , SPETZLER, Jane , GARIBAY, Patrick, William , KOFOED, Jacob , LINDEROTH, Lars
发明人： KALTHOFF, Christoph , LAU, Jesper , SPETZLER, Jane , GARIBAY, Patrick, William , KOFOED, Jacob , LINDEROTH, Lars
IPC分类号： C07K14/605
CPC分类号： C07K14/65 , A61K38/00 , A61K47/542 , A61K47/60 , C07K14/605 , G01N2333/605
摘要： The invention relates to a GLP-1 analogue which comprises a histidine (H) residue at a position corresponding to position 31 of GLP-1(7-37) (SEQ ID NO: 1), a glutamine (Q) residue at a position corresponding to position 34 of GLP-1 (7-37) (SEQ I D NO: 1), and a maximum of ten amino acid modifications as compared to GLP-1 (7-37) (SEQ ID NO: 1); wherein the H residue is designated H 31 , and the Q residue is designated Q 34 ; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to derivatives thereof, as well as the pharmaceutical use of these analogues and derivatives, for example in the treatment and/or prevention of all forms of diabetes and related diseases. The invention furthermore relates to corresponding novel side chain intermediates. The derivatives are suitable for oral administration.
摘要翻译：本发明涉及GLP-1类似物，其在对应于GLP-1（7-37）（SEQ ID NO：1）的位置31的位置包含组氨酸（H）残基，（7-37）（SEQ ID NO：1）的位置34处的谷氨酰胺（Q）残基，和与GLP-1（7-37）（SEQ ID NO：1）相比最多10个氨基酸修饰 ID NO：1）; 其中H残基命名为H 31，Q残基命名为Q 34。或其药学上可接受的盐，酰胺或酯。本发明还涉及其衍生物，以及这些类似物和衍生物的药物用途，例如用于治疗和/或预防所有形式的糖尿病和相关疾病。本发明还涉及相应的新型侧链中间体。这些衍生物适合口服给药。

4. 发明申请

WO2012062803A1 DOUBLE-ACYLATED GLP-1 DERIVATIVES 审中-公开
标题翻译：双取代的GLP-1衍生物
公开(公告)号：WO2012062803A1
公开(公告)日：2012-05-18
申请号：PCT/EP2011/069738
申请日：2011-11-09
申请人： NOVO NORDISK A/S , MADSEN, Alice Ravn , WIECZOREK, Birgit , KOFOED, Jacob , LAU, Jesper , SPETZLER, Jane , KODRA, János Tibor , LINDEROTH, Lars , GARIBAY, Patrick William , SAUERBERG, Per , KRUSE, Thomas
发明人： MADSEN, Alice Ravn , WIECZOREK, Birgit , KOFOED, Jacob , LAU, Jesper , SPETZLER, Jane , KODRA, János Tibor , LINDEROTH, Lars , GARIBAY, Patrick William , SAUERBERG, Per , KRUSE, Thomas
IPC分类号： A61K47/48 , C07K14/605 , 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, Chem. 2, and Chem. 3: Chem. : HOOC-(CH 2 ) x -CO-* Chem. 2: HOOC-C 6 H 4 -0-(CH 2 ) y -CO-* Chem. 3: R 2 -C 6 H 4 -(CH 2 ) z -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, and R 2 is a group having a molar mass not higher than 150 Da; and the linker comprises Chem. 4: *-NH-(CH 2 ) 2 -(0-(CH 2 ) 2 ) k -0-(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18位的位置处的第一个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，Chem。 2和Chem。 3：Chem。：HOOC-（CH2）x-CO- * Chem。 2：HOOC-C6H4-0-（CH2）y-CO- * Chem。 3：R2-C6H4-（CH2）z-CO- *，其中x是6-18的整数，y是3-17的整数，z是1的整数 -5和R2是摩尔质量不高于150Da的基团; 连接体包括Chem。 4：* -NH-（CH 2）2 - （O-（CH 2）2）k -O-（CH 2）n -CO- *。其中k是1-5的整数，n是1-5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。该衍生物适用于口服给药。

5. 发明申请

WO2009030774A1 TRUNCATED GLP-1 DERIVATIVES AND THEIR THERAPEUTICAL USE 审中-公开
标题翻译：截短的GLP-1衍生物及其治疗用途
公开(公告)号：WO2009030774A1
公开(公告)日：2009-03-12
申请号：PCT/EP2008/061833
申请日：2008-09-05
申请人： NOVO NORDISK A/S , SPETZLER, Jane , SCHÄFFER, Lauge , LAU, Jesper , KODRA, János Tibor , MADSEN, Kjeld , GARIBAY, Patrick William , KOFOED, Jacob , RUNGE, Steffen , THØGERSEN, Henning , PETTERSSON, Ingrid
发明人： SPETZLER, Jane , SCHÄFFER, Lauge , LAU, Jesper , KODRA, János Tibor , MADSEN, Kjeld , GARIBAY, Patrick William , KOFOED, Jacob , RUNGE, Steffen , THØGERSEN, Henning , PETTERSSON, Ingrid
IPC分类号： C07K14/605 , A61K38/26 , C07K14/575 , A61K38/22
CPC分类号： C07K14/605 , A61K38/00
摘要： The invention relates to truncated GLP-1 analogues, in particular a GLP-1 analogue which is a modified GLP-1(7-35) (SEQ ID No 1) having : i) a total of 2, 3, 4, 5 6, 7, 8, or 9 amino acid substitutions as compared to GLP-1(7-35), including a) a GIu residue at a position equivalent to position 22 of GLP-1(7-35), and b) an Arg residue at a position equivalent to position 26 of GLP-1(7-35); as well as derivatives thereof, and therapeutic uses and compositions. These analogues and derivatives are highly potent, have a good binding affinity to the GLP-1 receptor, also to the extracellular domain of the GLP-1 receptor, which is of potential relevance achieving long-acting, stable GLP-1 compounds with a potential for once weekly administration.
摘要翻译：本发明涉及截短的GLP-1类似物，特别是GLP-1类似物，其是修饰的GLP-1（7-35）（SEQ ID No.1），其具有：i）总共2,3,4,5,6 ，7,8或9个氨基酸取代，其包括a）在等同于GLP-1（7-35）的位置22的位置处的Glu残基，和b）Arg 在等同于GLP-1（7-35）的第26位的位置上的残基; 以及其衍生物，以及治疗用途和组合物。这些类似物和衍生物是高度有效的，对GLP-1受体以及GLP-1受体的细胞外结构域具有良好的结合亲和力，这与具有潜在的长效，稳定的GLP-1化合物具有潜在的相关性每周一次行政。

6. 发明申请

WO2011117415A1 NOVEL GLUCAGON ANALOGUES 审中-公开
标题翻译：新的GLUCAGON ANALOGUES
公开(公告)号：WO2011117415A1
公开(公告)日：2011-09-29
申请号：PCT/EP2011/054712
申请日：2011-03-28
申请人： NOVO NORDISK A/S , LAU, Jesper F. , KRUSE, Thomas , LINDEROTH, Lars , THØGERSEN, Henning , KOFOED, Jacob , DAHL, Kirsten
发明人： LAU, Jesper F. , KRUSE, Thomas , LINDEROTH, Lars , THØGERSEN, Henning , KOFOED, Jacob , DAHL, Kirsten
IPC分类号： C07K14/605 , A61K38/26
CPC分类号： C07K14/605 , A61K38/00 , A61K38/26 , A61K38/28 , A61K47/542 , A61K47/545
摘要： The present invention relates to novel peptide compounds which have a protracted profile of action and improved solubility and stability, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the 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：本发明涉及新颖的肽化合物，其具有延长的作用曲线和改善的溶解性和稳定性，在治疗中使用该化合物，包括向有需要的患者施用化合物，以及使用药物制造中的化合物。本发明的化合物在治疗高血糖症，糖尿病和肥胖以及与高血糖症，糖尿病和肥胖相关的各种疾病或病症方面特别有意义。

7. 发明申请

WO2011051312A1 DERIVATIVES OF CGRP 审中-公开
标题翻译： CGRP的衍生物
公开(公告)号：WO2011051312A1
公开(公告)日：2011-05-05
申请号：PCT/EP2010/066216
申请日：2010-10-27
申请人： NOVO NORDISK A/S , NIELSEN, Anette Sams , KRUSE, Thomas , KODRA, János Tibor , LAU, Jesper F. , KOFOED, Jacob , RAUN, Kirsten , NILSSON, Cecilia
发明人： NIELSEN, Anette Sams , KRUSE, Thomas , KODRA, János Tibor , LAU, Jesper F. , KOFOED, Jacob , RAUN, Kirsten , NILSSON, Cecilia
IPC分类号： C07K14/585
CPC分类号： C07K14/57527 , A61K47/48176 , A61K47/48192 , A61K47/48215 , A61K47/48246 , A61K47/58 , A61K47/59 , A61K47/60 , A61K47/64
摘要： Acylated CGRP compounds with a linker have prolonged action and are valuable as medicaments.
摘要翻译：具有连接体的酰化CGRP化合物具有延长的作用并且作为药物是有价值的。

8. 发明申请

WO2012140117A1 DOUBLE-ACYLATED GLP-1 DERIVATIVES 审中-公开
标题翻译：双取代的GLP-1衍生物
公开(公告)号：WO2012140117A1
公开(公告)日：2012-10-18
申请号：PCT/EP2012/056642
申请日：2012-04-12
申请人： NOVO NORDISK A/S , WIECZOREK, Birgit , SPETZLER, Jane , KRUSE, Thomas , LINDEROTH, Lars , KOFOED, Jacob
发明人： WIECZOREK, Birgit , SPETZLER, Jane , KRUSE, Thomas , LINDEROTH, Lars , KOFOED, Jacob
IPC分类号： A01N43/90 , A01N61/00 , A01P3/00 , A61K38/26 , C07K14/065
CPC分类号： C07K14/605 , A61K38/00 , A61K38/26 , A61K47/542 , A61K47/60
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 27 of GLP-1(7-37) (SEQ ID NO: 1 ); a second K residue at a position corresponding to position T of GLP-1(7-37), where T is an integer in the range of 7-37 except 18 and 27; and a maximum of ten amino acid changes as compared to GLP-1(7-37); wherein the first K residue is designated K 27 , and the second K residue is designated K T ; which derivative comprises two albumin binding moieties attached to K 27 and K T , respectively, via a linker, wherein the albumin binding moiety comprises a protracting moiety selected from HOOC-(CH 2 ) x -CO- and HOOC-C 6 H 4 -0-(CH 2 ) y -CO-; in which x is an integer in the range of 6-16, and y is an integer in the range of 3-17; wherein the linker comprises an element of the formula -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 GLP-1 analogues. 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）的位置27的位置处的第一个K残基; 在对应于GLP-1（7-37）的位置T的位置处的第二个K残基，其中T是除了18和27之外的7-37范围内的整数; 与GLP-1（7-37）相比最多10个氨基酸变化; 其中第一K残基指定为K27，第二K残基指定为KT; 该衍生物通过接头分别包含与K27和KT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HOOC-（CH 2）x -CO-和HOOC-C 6 H 4 O-（CH 2）y -CO-; 其中x是6-16的整数，y是3-17的整数; 其中所述接头包含式-NH-（CH 2）2 - （O-（CH 2）2）kO-（CH 2）n -CO-的元素，其中k是1-5的整数，n 是1-5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GLP-1类似物。该衍生物适用于口服给药。

9. 发明申请

WO2011033068A1 LONG-ACTING Y2 RECEPTOR AGONISTS 审中-公开
标题翻译：长期行动Y2受体激素
公开(公告)号：WO2011033068A1
公开(公告)日：2011-03-24
申请号：PCT/EP2010/063707
申请日：2010-09-17
申请人： NOVO NORDISK A/S , KOFOED, Jacob , OLSEN, Jørgen , ØSTERGAARD, Søren , JØRGENSEN, Rasmus
发明人： KOFOED, Jacob , OLSEN, Jørgen , ØSTERGAARD, Søren , JØRGENSEN, Rasmus
IPC分类号： A61K38/22 , A61K47/48 , C07K14/575
CPC分类号： C07K14/575 , A61K38/00
摘要： The present invention relates to PYY analogues or derivatives thereof comprising at least one alteration selected from the group consisting of substitutions, insertions, deletions and modifications and optionally a serum albumin binding side chain comprising an alkyl chain with at least 14 carbon atoms. Moreover, the invention relates to compositions hereof and methods of treatment of conditions responsive to Y2 receptor modulation.
摘要翻译：本发明涉及包含至少一种选自取代，插入，缺失和修饰的改变的PYY类似物或其衍生物，以及任选地包含具有至少14个碳原子的烷基链的血清白蛋白结合侧链。此外，本发明涉及本发明的组合物和治疗对Y2受体调节作用的病症的方法。

10. 发明申请

WO2011131646A1 LONG-ACTING GASTRIN DERIVATIVES 审中-公开
标题翻译：长效GASTRIN衍生物
公开(公告)号：WO2011131646A1
公开(公告)日：2011-10-27
申请号：PCT/EP2011/056197
申请日：2011-04-19
申请人： NOVO NORDISK A/S , KOFOED, Jacob , STIDSEN, Carsten Enggaard , HUBALEK, Frantisek , NIELSEN, Flemming S. , THØGERSEN, Henning , FELS, Johannes , ANDERSEN, Rikke Bjerring , KODRA, János Tibor
发明人： KOFOED, Jacob , STIDSEN, Carsten Enggaard , HUBALEK, Frantisek , NIELSEN, Flemming S. , THØGERSEN, Henning , FELS, Johannes , ANDERSEN, Rikke Bjerring , KODRA, János Tibor
IPC分类号： A61K38/22 , C07K14/00 , C07K14/595
CPC分类号： C07K14/595 , A61K38/00 , A61K38/22 , A61K38/2207 , C07K14/00
摘要： The present invention relates to gastrin derivatives comprising gastrin or an analogue or fragment thereof and a derivatisation group and therapeutic use thereof.
摘要翻译：本发明涉及包含胃泌素或其类似物或片段以及衍生化组的胃泌素衍生物及其治疗用途。

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