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1. 发明申请

WO2015155151A1 DOUBLE-ACYLATED GLP-1 COMPOUNDS 审中-公开
标题翻译：双酚A-GLP-1化合物
公开(公告)号：WO2015155151A1
公开(公告)日：2015-10-15
申请号：PCT/EP2015/057442
申请日：2015-04-07
申请人： NOVO NORDISK A/S
发明人： LINDEROTH, Lars , KOFOED, Jacob , LAU, Jesper , BLOCH, Paw , GARIBAY, Patrick William , KODRA, János Tibor
IPC分类号： A61K38/26 , C07K14/605
CPC分类号： C07K14/605 , A61K38/00 , C07C235/20
摘要： The invention relates to a derivative of a GLP-1 peptide, which peptide comprises a first Lys residue at a position corresponding to position 36 of GLP-1(7-37) (SEQ ID NO:1), a second Lys residue at a position corresponding to position 37 of GLP-1(7-37) (SEQ ID NO : 1), and a maximum of seven amino acid changes as compared to GLP-1(7-37) (SEQ ID NO: 1); which derivative comprises two protractors attached to said first and second Lys residue, respectively, each via a linker; wherein the protractor is selected from : Chem. 1: HOOC-C 6 H 4 -0-(CH 2 ) y -CO-*, and Chem. 2: HOOC-(CH 2 ) x -CO-*, wherein y is an integer in the range of 8-11, and x is 12; and the linker comprises at least one of: Chem. 3: *-NH-CH(COOH)-(CH 2 ) 2 -CO-*, Chem. 4: *-NH-CH((CH 2 ) 2 -COOH)-CO-*, and/or Chem. 5: *-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 uses thereof, such as for the treatment of diabetes and obesity, as well as to the GLP-1 peptides forming part of these derivatives which have Lys residues at positions 36 and 37 and no other Lys residues, and the GLP-1(9-37) fragments thereof. The invention furthermore relates to an intermediate product comprising 3-carboxyphenoxy-nonanoic acid with a protection group at the carboxy group of the nonanoic acid, optionally via a linker. The derivatives have a very good potency and a long half-life which makes them potentially useful for, e.g., oral administration.
摘要翻译：本发明涉及GLP-1肽的衍生物，该肽在对应于GLP-1（7-37）（SEQ ID NO：1）的位置36的位置处的第一个Lys残基，与GLP-1（7-37）（SEQ ID NO：1）相比，对应于GLP-1（7-37）的位置37（SEQ ID NO：1）的位置和最多7个氨基酸的变化。该衍生物分别包含分别连接到所述第一和第二Lys残基的两个量角器，每个通过连接体连接; 其中所述量角器选自：Chem。 1：HOOC-C6H4-0-（CH2）y-CO- *，和Chem。 2：HOOC-（CH 2）x -CO- *，其中y是8-11的整数，x是12; 并且所述接头包含以下至少一种：Chem。 3：* -NH-CH（COOH） - （CH 2）2 -CO- *， 4：* -NH-CH（（CH 2）2 -COOH）-CO- *，和/或Chem。 5：* -NH-（CH2）2- [0-（CH2）2] k-0- [CH2] n-CO- *，其中k是1-5的整数，n是整数在1-5的范围内; 或其药学上可接受的盐，酰胺或酯。本发明还涉及其药学用途，例如用于治疗糖尿病和肥胖症，以及形成这些衍生物的一部分的GLP-1肽，其在36和37位具有Lys残基且没有其它Lys残基，以及 GLP-1（9-37）片段。本发明还涉及包含3-羧基苯氧基 - 壬酸与壬酸羧基上的保护基团的中间产物，任选地通过连接体。衍生物具有非常好的效力和长的半衰期，这使得它们可能用于例如口服给药。

2. 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。

3. 发明申请

WO2022018186A1 CO-AGONISTS AT GLP-1 AND GIP RECEPTORS SUITABLE FOR ORAL DELIVERY 审中-公开
公开(公告)号：WO2022018186A1
公开(公告)日：2022-01-27
申请号：PCT/EP2021/070485
申请日：2021-07-22
申请人： NOVO NORDISK A/S
发明人： KNERR, Patrick, J. , FINAN, Brian , DIMARCHI, Richard , LINDEROTH, Lars
IPC分类号： C07K14/605 , A61K38/26 , A61P1/16 , A61P3/04 , A61P3/10
摘要： Peptide co-agonists of the human GLP-1 and GIP receptors suitable for oral delivery, including long-acting derivatives, and their medical use in treatment and/or prevention of obesity, diabetes, and/or liver diseases are described.

4. 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。

5. 发明申请

WO2017149070A1 GLP-1 DERIVATIVES AND USES THEREOF 审中-公开
标题翻译： GLP-1衍生物及其用途
公开(公告)号：WO2017149070A1
公开(公告)日：2017-09-08
申请号：PCT/EP2017/054895
申请日：2017-03-02
申请人： NOVO NORDISK A/S
发明人： KOFOED, Jacob , KODRA, János, Tibor , LINDEROTH, Lars , GARIBAY, Patrick, William
IPC分类号： C07K14/605 , A61K38/26
摘要： The invention relates to GLP-1 analogues and derivatives having a Trp at a position corresponding to position 8 of GLP-1(7-37), and their pharmaceutical use e.g. in the treatment of type 2 diabetes. These Trp8 compounds are very stable against degradation by DPP-IV, while maintaining the capability to bind to and activate the GLP-1 receptor. The derivatives have one or two substituents (P-L) attached to a Lys residue of the GLP-1 analogue via an optional Branching group (B), wherein P is a Protracting moiety such as a fatty diacid, and L is a linker consisting of one or more linker elements such as, for example, 8-amino-3,6-dioxaoctanoic acid. Examples of compounds of the invention include the 8W variants of liraglutide and dulaglutide. The invention also relates to a method for the fully recombinant preparation of 8W GLP-1 analogues and derivatives which is more simple and thereby cheaper as compared to the preparation of known GLP-1 analogues that have been DPP-IV stabilised by inclusion of one or more non-coded amino acids.
摘要翻译：本发明涉及在对应于GLP-1（7-37）的8位的位置具有Trp的GLP-1类似物和衍生物及其药物用途，例如，用于治疗2型糖尿病。这些Trp8化合物对抗DPP-IV降解非常稳定，同时保持结合并激活GLP-1受体的能力。该衍生物通过任选的支化基团（B）具有一个或两个与GLP-1类似物的赖氨酸残基连接的取代基（PL），其中P是伸长部分如脂肪二酸，并且L是由一个或更多接头元件，例如8-氨基-3,6-二氧杂辛酸。本发明化合物的实例包括利拉鲁肽和杜拉鲁肽的8W变体。本发明还涉及用于完全重组制备8W GLP-1类似物和衍生物的方法，与制备通过包含一个或两个以上的DPP-IV而稳定的已知GLP-1类似物相比，该方法更简单并因此更便宜更多的非编码氨基酸。

6. 发明申请

WO2017121850A1 EGF(A) ANALOGUES WITH FATTY ACID SUBSTITUENTS 审中-公开
标题翻译： EGF（A）具有脂肪酸取代基的类似物
公开(公告)号：WO2017121850A1
公开(公告)日：2017-07-20
申请号：PCT/EP2017/050668
申请日：2017-01-13
申请人： NOVO NORDISK A/S
发明人： CHEN, Jianhe , LAU, Jesper F. , KODRA, János Tibor , WIECZOREK, Birgit , LINDEROTH, Lars , THØGERSEN, Henning , RASMUSSEN, Salka Elbøl , GARIBAY, Patrick William
IPC分类号： C07K14/705 , A61K38/17
CPC分类号： C07K14/705 , A61K38/00 , A61K38/177
摘要： The invention relates to compounds derived from the EGF(A) domain of LDL-R, in particular compounds comprising a peptide analogue of the wild-type EGF(A) (LDL-R(293- 332)) sequence and at least one substituent comprising at least one fatty acid group. The invention also relates to a pharmaceutical composition thereof and use a medicament. The novel EGF(A) compounds of the invention are useful as treatment e.g. in the field of cholesterol lowering, dyslipidaemia and cardiovascular disease.
摘要翻译：本发明涉及衍生自LDL-R的EGF（A）结构域的化合物，特别是包含野生型EGF（A）的肽类似物的化合物（LDL-R（293-332 ））序列和至少一个包含至少一个脂肪酸基团的取代基。本发明还涉及其药物组合物并使用药物。本发明的新型EGF（A）化合物可用作例如治疗剂。在胆固醇降低，血脂异常和心血管疾病领域。

7. 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。

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

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

WO2011117416A1 NOVEL GLUCAGON ANALOGUES 审中-公开
标题翻译：新的GLUCAGON ANALOGUES
公开(公告)号：WO2011117416A1
公开(公告)日：2011-09-29
申请号：PCT/EP2011/054714
申请日：2011-03-28
申请人： NOVO NORDISK A/S , LAU, Jesper, F. , KRUSE, Thomas , LINDEROTH, Lars , THØGERSEN, Henning
发明人： LAU, Jesper, F. , KRUSE, Thomas , LINDEROTH, Lars , THØGERSEN, Henning
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 an improved physical stability in solution and improved solubility at neutral pH, 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：本发明涉及在溶液中具有改善的物理稳定性和在中性pH下改善的溶解度，化合物在治疗中的用途的新型肽化合物，包括向有需要的患者施用化合物的治疗方法，以及化合物在制造药物中的用途。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。

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