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11. 发明专利

JP2012214486A New insulin derivative 有权
标题翻译：新胰岛素衍生物
公开(公告)号：JP2012214486A
公开(公告)日：2012-11-08
申请号：JP2012137431
申请日：2012-06-19
申请人： Novo Nordisk As , ノボ・ノルデイスク・エー/エス
发明人： FYNBO CHARLOTTE HARKJAER , JONASSEN IB , KJELDSEN THOMAS BERGLUM , MADSEN PETER , GARIBAY PATRICK WILLIAM , KODRA JANOS TIBOR , HOEG-JENSEN THOMAS , TAGMOSE TINA MOELLER
IPC分类号： C07K14/62 , A61K38/28 , A61P3/10 , C12N15/09
CPC分类号： C07K14/62 , A61K38/00
摘要： PROBLEM TO BE SOLVED: To provide a new human insulin derivative dissolving at a physiological pH value, and having an action profile over a long time.SOLUTION: This insulin derivative is provided by containing a parent insulin and a substituent, wherein the substituent bonds with any of the ε-amino group of a Lys residue presenting at A8, A9, A10, A12, A14, A15, A17, A18, A21, A22, A23 or A24 of the A-chain of the parent insulin or the ε-amino group of the Lys residue presenting at B1, B2, B3, B4, B20, B21 or B22 of the B-chain of the parent insulin, and provided that when the B3 is the Lys, B29 is not Glu; the substituent can contain a lipophilic group including 6 to 40 carbon atoms; and an example of the substituent is a 6-40C acyl, e.g. the acyl having 12 to 36 carbon atoms.
摘要翻译：要解决的问题：提供在生理pH值下溶解并且长时间具有作用特征的新的人胰岛素衍生物。解决方案：该胰岛素衍生物通过含有母体胰岛素和取代基而提供，其中取代基与A8，A9，A10，A12，A14，A15，A17上呈现的Lys残基的任何一个ε-氨基键合，母体胰岛素A链的A18，A21，A22，A23或A24或呈现在B链的B1，B2，B3，B4，B20，B21或B22的Lys残基的ε-氨基母体胰岛素，并且当B3是Lys时，B29不是Glu; 该取代基可含有包含6至40个碳原子的亲油基团; 并且取代基的实例是6-40C酰基，例如。该酰基具有12至36个碳原子。版权所有（C）2013，JPO＆INPIT

12. 发明专利

JP2011168609A Aryl carbonyl derivative as therapeutic agent 审中-公开
标题翻译： ARYL CARBONYL衍生物作为治疗剂
公开(公告)号：JP2011168609A
公开(公告)日：2011-09-01
申请号：JP2011092035
申请日：2011-04-18
申请人： Novo Nordisk As , ノボ・ノルデイスク・エー/エス
发明人： POLISETTI DHARMA RAO , KODRA JANOS TIBOR , LAU JESPER , BLOCH PAW , VALCARCE-LOPEZ MARIA CARMEN , BLUME NIELS , GUZEL MUSTAFA , SANTHOSH KALPATHY CHIDAMBARESWARAN , MJALLI ADNAN M M , ANDREWS ROBERT CARL , SUBRAMANIAN GOVINDAN , ANKERSEN MICHAEL , VEDSOE PER , MURRAY ANTHONY , JEPPESEN LONE
IPC分类号： C07D213/75 , C07D277/20 , A61K31/41 , A61K31/4196 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/4402 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/52 , A61K31/5377 , A61K31/695 , A61K45/00 , A61K45/06 , A61P1/14 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , A61P5/50 , A61P9/10 , A61P9/12 , A61P43/00 , C07D277/42 , C07D277/46 , C07D277/48 , C07D277/52 , C07D277/54 , C07D277/56 , C07D285/135 , C07D417/06 , C07D417/12 , C07D417/14 , C07D473/38 , C07F7/10 , C07F7/18
CPC分类号： C07D277/38 , A61K31/426 , A61K31/427 , A61K31/454 , A61K31/55 , A61K45/06 , C07D213/75 , C07D277/46 , C07D277/48 , C07D277/52 , C07D277/54 , C07D277/56 , C07D285/135 , C07D417/06 , C07D417/12 , C07D417/14 , C07D473/38
摘要： PROBLEM TO BE SOLVED: To provide compounds useful for the management, treatment, control, or adjunct treatment of diseases where increasing the activity of glucokinase is beneficial. SOLUTION: This invention relates to aryl carbonyl derivatives of general formula (I), which are activators of glucokinase, pharmaceutically acceptable salts, solvates, or prodrugs thereof. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供可用于治疗，治疗，控制或辅助治疗增加葡萄糖激酶活性的疾病的化合物有益的化合物。解决方案：本发明涉及通式（I）的芳基羰基衍生物，其是葡糖激酶的活化剂，其药学上可接受的盐，溶剂合物或前药。版权所有（C）2011，JPO＆INPIT

13. 发明专利

JP2010265306A Aryl carbonyl derivative as therapeutic agent 审中-公开
标题翻译： ARYL CARBONYL衍生物作为治疗剂
公开(公告)号：JP2010265306A
公开(公告)日：2010-11-25
申请号：JP2010162302
申请日：2010-07-16
申请人： Novo Nordisk As , ノボ・ノルデイスク・エー/エス
发明人： POLISETTI DHARMA RAO , KODRA JANOS TIBOR , LAU JESPER , BLOCH PAW , VALCARCE-LOPEZ MARIA CARMEN , BLUME NIELS , GUZEL MUSTAFA , SANTHOSH KALPATHY CHIDAMBARESWARAN , MJALLI ADNAN M M , ANDREWS ROBERT CARL , SUBRAMANIAN GOVINDAN , ANKERSEN MICHAEL , VEDSOE PER , MURRAY ANTHONY , JEPPESEN LONE
IPC分类号： C07D213/75 , C07D277/20 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/4402 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4523 , A61K31/454 , A61K31/496 , A61K31/506 , A61K31/52 , A61K31/5377 , A61K31/695 , A61K45/00 , A61K45/06 , A61P1/04 , A61P1/14 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , A61P5/00 , A61P5/50 , A61P9/12 , A61P43/00 , C07D277/42 , C07D277/46 , C07D277/48 , C07D277/52 , C07D277/54 , C07D277/56 , C07D285/135 , C07D417/06 , C07D417/12 , C07D417/14 , C07D473/38 , C07F7/18
CPC分类号： C07D277/38 , A61K31/426 , A61K31/427 , A61K31/454 , A61K31/55 , A61K45/06 , C07D213/75 , C07D277/46 , C07D277/48 , C07D277/52 , C07D277/54 , C07D277/56 , C07D285/135 , C07D417/06 , C07D417/12 , C07D417/14 , C07D473/38
摘要： PROBLEM TO BE SOLVED: To provide activators of glucokinase useful for the management, treatment, control, or adjuvant treatment of diseases, where increasing glucokinase activity is beneficial. SOLUTION: The aryl carbonyl derivatives represented by general formula (I), has glucokinase activating properties. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供可用于治疗，治疗，控制或辅助治疗疾病的葡萄糖激酶的活化剂，其中增加葡糖激酶活性是有益的。解决方案：由通式（I）表示的芳基羰基衍生物具有葡糖激酶活化性质。版权所有（C）2011，JPO＆INPIT

14. 发明申请

WO2004056763A3 NOVEL GLUCAGON ANTAGONISTS 审中-公开
标题翻译：新的GLUCAGON ANTAGONISTS
公开(公告)号：WO2004056763A3
公开(公告)日：2004-08-19
申请号：PCT/DK0300903
申请日：2003-12-18
申请人： NOVO NORDISK AS
发明人： KODRA JANOS TIBOR , BEHRENS CARSTEN , MADSEN PETER , JOERGENSEN ANKER STEEN , CHRISTENSEN INGE THOEGER
IPC分类号： A61K31/166 , A61K31/17 , A61K31/27 , A61K31/343 , A61K31/41 , A61P3/10 , C07C235/84 , C07C237/36 , C07C237/42 , C07C271/58 , C07C275/42 , C07C323/62 , C07D307/91 , C07C275/40
CPC分类号： C07D277/64 , A61K31/166 , A61K31/17 , A61K31/27 , A61K31/343 , A61K31/41 , C07C235/84 , C07C237/36 , C07C237/42 , C07C271/58 , C07C275/42 , C07C323/62 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07C2603/18 , C07D307/91
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.
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。

15. 发明专利

AU2013205273B2 Protease stabilized, acylated insulin analogues 未知
公开(公告)号：AU2013205273B2
公开(公告)日：2014-12-18
申请号：AU2013205273
申请日：2013-04-10
申请人： NOVO NORDISK AS
发明人： MADSEN PETER , KJELDSEN THOMAS BORGLUM , HOEG-JENSEN THOMAS , JAKOBSEN PALLE , TAGMOSE TINA MOLLER , GLENDORF TINE , KODRA JANOS TIBOR , GARIBAY PATRICK WILLIAM , PETERSEN JACOB STEN
IPC分类号： C07K14/62 , A61K38/28
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.

16. 发明专利

ES2428510T3 Derivados de insulina 未知
公开(公告)号：ES2428510T3
公开(公告)日：2013-11-08
申请号：ES06707955
申请日：2006-02-01
申请人： NOVO NORDISK AS
发明人： MADSEN PETER , TAGMOSE TINA MOELLER , KODRA JANOS TIBOR , GARIBAY PATRICK WILLIAM , HOEG-JENSEN THOMAS , JONASSEN IB
IPC分类号： C07K14/62 , A61K38/28
摘要： Derivado de insulina con la fórmula **Fórmula**donde Ins es la fracción de insulina progenitora la cual por vía del grupo α-amino del residuo de aminoácido Nterminalde la cadena B o un grupo ε-amino de un residuo de Lys presente en la cadena B de la fracción deinsulina se enlaza al grupo CO- en la cadena lateral por medio de un enlace amida; X1 es - un enlace W es un enlace; m es 0; X es - un enlace; Y es - -(CR1R2)q-NR-CO-, donde R1 y R2 independientemente uno del otro independientemente eindependientemente para cada valor de q puede ser H, -COOH, un enlace u OH, q es 1-6; y R es hidrógeno o- (CH2)p -COOH; -(CH2)p-SO3H; -(CH2)p-PO3H2 ; -(CH2)p-O-SO3H2 ; -(CH2)p-O-PO3H2 ; arilenosustituido con 1 o 2 -(CH2)p -O-COOH grupos; -(CH2)p-tetrazolilo, donde p es un número entero en elintervalo de 1 a 6; Q es - -(CH2)r - donde r es un número entero de 4 a 22; - una cadena de hidrocarburo bivalente que comprende 1,2 o 3 grupos -CH>=CH- y varios grupos -CH2-suficientes para dar un número total de átomos de carbono en la cadena en el intervalo de 4 a 22 o - una cadena de hidrocarburo bivalente de la fórmula-(CH2)s -Q1 -(C6 H4)v1 -Q2 - (CH2)w -Q3 - (C6H4)v2 -Q4 - (CH2)t -Q5 - (C6 H4)v3 -Q6 - (CH2)z -

18. 发明专利

ZA201204436B DOUBLE-ACYLATED GLP-1 DERIVATIVES 未知
公开(公告)号：ZA201204436B
公开(公告)日：2013-08-28
申请号：ZA201204436
申请日：2012-06-15
申请人： NOVO NORDISK AS
发明人： GARIBAY PATRICK WILLIAM , LAU JESPER , KODRA JANOS TIBOR , SPETZLER JANE , LINDEROTH LARS , SAUERBERG PER
IPC分类号： A61K20060101 , C07K20060101
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: €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒChem. 1:€ƒ€ƒ€ƒ€ƒ€ƒHOOC-(CH 2 ) x -CO-* €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒChem. 2:€ƒ€ƒ€ƒ€ƒ€ƒHOOC-C 6 H 4 -O-(CH 2 ) y -CO-* €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒChem. 3:€ƒ€ƒ€ƒ€ƒ€ƒR 1 -C 6 H 4 -(CH 2 ) z -CO-* €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒChem. 4:€ƒ€ƒ€ƒ€ƒ€ƒHOOC-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.

19. 发明专利

AU2010338387A1 Double-acylated GLP-1 derivatives 未知
公开(公告)号：AU2010338387A1
公开(公告)日：2012-05-31
申请号：AU2010338387
申请日：2010-12-16
申请人： NOVO NORDISK AS
发明人： GARIBAY PATRICK WILLIAM , SPETZLER JANE , KODRA JANOS TIBOR , LINDEROTH LARS , LAU JESPER , SAUERBERG PER
IPC分类号： C07K14/605 , A61K47/48
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, and the second K residue is designated K, which derivative comprises two albumin binding moieties attached to K and K, respectively, wherein the albumin binding moiety comprises a protracting moiety selected from: Chem. 1 : HOOC-(CH)-CO-* Chem. 2: HOOC-CH-O-(CH)-CO-* Chem. 3: R-CH-(CH)-CO-* Chem. 4: HOOC-CSH-(CH)-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 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)-(O-(CH))-O-(CH)-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.

20. 发明专利

CA2695970A1 INSULIN ANALOGUES WITH AN ACYL AND AKLYLENE GLYCOL MOIETY 未知
公开(公告)号：CA2695970A1
公开(公告)日：2009-02-19
申请号：CA2695970
申请日：2008-08-15
申请人： NOVO NORDISK AS
发明人： MADSEN PETER , KJELDSEN THOMAS BOERGLUM , HOEG-JENSEN THOMAS , TAGMOSE TINA MOELLER , JAKOBSEN PALLE , KODRA JANOS TIBOR , GARIBAY PATRICK WILLIAM , GRAM DORTE XENIA
IPC分类号： C07K14/62 , A61K38/28
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.

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