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31. 发明申请

WO2004056740A1 DICARBOXYLIC ACID DERIVATIVES AS PPAR-AGONISTS 审中-公开
标题翻译：二羧酸衍生物作为PPAR-AGONISTS
公开(公告)号：WO2004056740A1
公开(公告)日：2004-07-08
申请号：PCT/DK2003/000895
申请日：2003-12-18
申请人： NOVO NORDISK A/S
发明人： SAUERBERG, Per , JEPPESEN, Lone , POLIVKA, Zdenek , SINDELAR, Karel
IPC分类号： C07C59/68
CPC分类号： C07D213/74 , A61K31/215 , A61K31/216 , A61K31/225 , A61K31/341 , A61K31/381 , A61K31/395 , C07C59/68 , C07C59/72 , C07C69/734 , C07C323/20 , C07C323/52 , C07C2603/10 , C07C2603/18 , C07D263/32
摘要： A novel class of dicarboxylic acid derivatives, the use of these compounds as phar-maceutical compositions, pharmaceutical compositions comprising the compounds and meth-ods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Prolifera-tor-Activated Receptors (PPAR).
摘要翻译：一类新的二羧酸衍生物，这些化合物作为药物组合物的用途，包含这些化合物的药物组合物和使用这些化合物和组合物的处理方法。本发明化合物可用于治疗和/或预防由过氧化物酶体释放激活受体（PPAR）介导的病症。

32. 发明申请

WO2003011834A1 NOVEL VINYL N-(2-BENZOYLPHENYL)-L-TYROSINE DERIVATIVES AND THEIR USE AS ANTIDIABETICS ETC 审中-公开
标题翻译：新型乙烯基N-（2-苯甲酰基苯基）-L-酪氨酸衍生物及其作为抗病毒剂的用途
公开(公告)号：WO2003011834A1
公开(公告)日：2003-02-13
申请号：PCT/DK2002/000469
申请日：2002-07-05
申请人： NOVO NORDISK A/S
发明人： JEPPESEN, Lone , BURY, Paul, Stanley , MOGENSEN, John, Patrick , PETTERSSON, Ingrid , SAUERBERG, Per
IPC分类号： C07D235/16
CPC分类号： C07D471/04 , C07D209/82 , C07D223/26 , C07D223/28 , C07D265/38 , C07D279/22
摘要： Novel compounds of the general formula (I), the use of these compounds as medicaments, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR). The compounds exert their effects by modulating the PPARγ response in a partial agonist manner.
摘要翻译：通式（I）的新型化合物，这些化合物作为药物的用途，包含该化合物的药物组合物和使用这些化合物和组合物的治疗方法。本发明化合物可用于治疗和/或预防由核受体介导的病症，特别是过氧化物酶体增殖物激活受体（PPAR）。化合物通过以部分激动剂方式调节PPARγ反应而发挥其作用。

33. 发明申请

WO2003011814A1 NOVEL VINYL N-(2-BENZOYLPHENYL)-L-TYROSINE DERIVATIVES AND THEIR USE AS ANTIDIABETICS ETC 审中-公开
标题翻译：新型乙烯基N-（2-苯甲酰基苯基）-L-酪氨酸衍生物及其作为抗病毒剂的用途
公开(公告)号：WO2003011814A1
公开(公告)日：2003-02-13
申请号：PCT/DK2002/000470
申请日：2002-07-05
申请人： NOVO NORDISK A/S
发明人： JEPPESEN, Lone , BURY, Paul, Stanley , MOGENSEN, John, Patrick , PETTERSSON, Ingrid , SAUERBERG, Per
IPC分类号： C07C229/36
CPC分类号： C07D215/14 , C07C229/36 , C07C2603/18
摘要： Novel compounds of general formula (I), the use of thesecompounds as medicaments, pharmaceuticaly compositions comprising the compounds and methods of treatment employing these compounds and compostiones. The present compounds may be useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR). The compounds exert their effects by modulating the PPAR response in a partial agonist manner.
摘要翻译：通式（I）的新型化合物，这些化合物作为药物的用途，包含该化合物的药物组合物和使用这些化合物和组合物的治疗方法。本发明化合物可用于治疗和/或预防由核受体介导的病症，特别是过氧化物酶体增殖物激活受体（PPAR）。化合物通过以部分激动剂方式调节PPAR反应而发挥其作用。

34. 发明申请

WO1996016065A1 HETEROCYCLIC COMPOUNDS AND THEIR PREPARATION AND USE 审中-公开
标题翻译：杂环化合物及其制备和使用
公开(公告)号：WO1996016065A1
公开(公告)日：1996-05-30
申请号：PCT/DK1995000456
申请日：1995-11-20
申请人： NOVO NORDISK A/S
发明人： NOVO NORDISK A/S , OLESEN, Preben, Houlberg , SAUERBERG, Per
IPC分类号： C07D513/14
CPC分类号： C07D513/04 , C07D513/14
摘要： The present invention relates to therapeutically active azacyclic or azabicyclic compounds of formula (I), wherein X is -C-, -O-, -S-, =C- or -N(R )-, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.
摘要翻译：本发明涉及式（I）的治疗活性的氮杂环或氮杂双环化合物，其中X是-C - ， - O - ， - S-，= C-或-N（R 3） - ，其制备方法和含有该化合物的药物组合物。新型化合物可用于治疗由毒蕈碱胆碱能系统功能障碍引起的中枢神经系统疾病。

35. 发明申请

WO1995005379A1 ANTIPSYCHOTIC METHOD 审中-公开
标题翻译：抗生素方法
公开(公告)号：WO1995005379A1
公开(公告)日：1995-02-23
申请号：PCT/DK1994000309
申请日：1994-08-18
申请人： NOVO NORDISK A/S
发明人： NOVO NORDISK A/S , BYMASTER, Franklin, Porter , SHANNON, Harlan, E. , SAUERBERG, Per , OLESEN, Preben, H. , WARD, John, Stanley , MITCH, Charles, H.
IPC分类号： C07D453/02
CPC分类号： C07D451/04 , C07D453/02 , C07D471/08 , C07D487/08
摘要： The method of this invention comprises administering to a patient suffering from or susceptible to schizophrenia or schizophreniform conditions an effective amount of a compound of formula (I), wherein X is oxygen or sulphur; G is selected from one of the following azabicyclic rings (a) or (b) wherein the thiadiazole or oxadiazole ring can be attached at any carbon atom of the azabicyclic ring.
摘要翻译：本发明的方法包括对患有精神分裂症或精神分裂症状况的患者施用有效量的式（I）化合物，其中X是氧或硫; G选自以下氮杂双环（a）或（b）之一，其中噻二唑或恶二唑环可以连接在氮杂双环的任何碳原子上。

36. 发明申请

WO1993014089A1 HETEROCYCLIC COMPOUNDS AND THEIR PREPARATION AND USE 审中-公开
标题翻译：杂环化合物及其制备和使用
公开(公告)号：WO1993014089A1
公开(公告)日：1993-07-22
申请号：PCT/DK1992000009
申请日：1992-01-13
申请人： NOVO NORDISK A/S
发明人： NOVO NORDISK A/S , OLESEN, Preben, H. , SAUERBERG, Per
IPC分类号： C07D417/14
CPC分类号： C07D417/14 , C07D453/02 , C07D471/08 , C07D487/08
摘要： The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful as stimulants of the cognitive function of the forebrain and hippocampus of mammals and especially in the treatment of Alzheimer's disease, severe painful conditions and glaucoma.
摘要翻译：本发明涉及治疗活性的氮杂环或氮杂双环化合物，其制备方法和包含该化合物的药物组合物。新化合物可用作哺乳动物的前脑和海马的认知功能的兴奋剂，特别是在治疗阿尔茨海默病，严重的疼痛病症和青光眼中。

37. 发明申请

WO1992003430A1 HETEROCYCLIC COMPOUNDS AND THEIR PREPARATION AND USE 审中-公开
标题翻译：杂环化合物及其制备和使用
公开(公告)号：WO1992003430A1
公开(公告)日：1992-03-05
申请号：PCT/DK1991000234
申请日：1991-08-20
申请人： NOVO NORDISK A/S
发明人： NOVO NORDISK A/S , SAUERBERG, Per , OLESEN, Preben, H. , MITCH, Charles, H.
IPC分类号： C07D417/04
CPC分类号： C07D413/04 , C07D417/04 , C07D417/14
摘要： The present invention relates to therapeutically active azacyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful as stimulants of the cognitive function of the forebrain and hippocampus of mammals and especially in the treatment of Alzheimer's disease, severe painful conditions and glaucoma.
摘要翻译：本发明涉及治疗活性的azacyclic化合物，其制备方法和包含该化合物的药物组合物。新化合物可用作哺乳动物的前脑和海马的认知功能的兴奋剂，特别是在治疗阿尔茨海默病，严重的疼痛病症和青光眼中。

38. 发明授权

EP3326620B1 SOLID COMPOSITIONS COMPRISING A GLP-1 AGONIST AND A SALT OF N-(8-(2- HYDROXYBENZOYL)AMINO)CAPRYLIC ACID 有权
公开(公告)号：EP3326620B1
公开(公告)日：2020-03-04
申请号：EP17204363.0
申请日：2011-12-16
申请人： Novo Nordisk A/S
发明人： BJERREGAARD, Simon , SAUERBERG, Per , Seier, NIELSEN, Flemming
IPC分类号： A61K9/20 , A61K38/26 , A61K31/195 , A61P3/04 , A61P3/10

39. 发明公开

EP3010546A1 GLP-1 DERIVATIVES AND USES THEREOF 有权
标题翻译： GLP-1衍生物及其用途
公开(公告)号：EP3010546A1
公开(公告)日：2016-04-27
申请号：EP14731951.1
申请日：2014-06-19
申请人： Novo Nordisk A/S
发明人： REEDTZ-RUNGE, Steffen , SAUERBERG, Per , KOFOED, Jacob , PETTERSSON, Ingrid , TORNØE, Christian, Wenzel
IPC分类号： A61K47/48 , C07K14/605
CPC分类号： A61K38/26 , A61K47/54 , A61K47/542 , A61K47/56 , A61K47/60 , C07K14/605
摘要： The invention relates to a derivative of a GLP-1 analogue, optionally C-terminally extended, which derivative comprises a first and a second protracting moiety in the form of a C20 or C22 diacid radical, a bis-amino branched linker, and a first and a second further linker each comprising an OEG-like linker element; wherein these elements are interconnected via amide bonds and attached to a Lys residue of the GLP-1 analogue. The invention also relates to intermediate products in the form of novel GLP-1 analogues incorporated in the derivatives of the invention, as well pharmaceutical compositions and medical uses of the derivatives. The derivatives have very long half-lives while maintaining a satisfactory potency, which makes them potentially suitable for once-monthly administration.
摘要翻译：本发明涉及任选C端延伸的GLP-1类似物的衍生物，所述衍生物包含呈C20或C22二酸基团形式的第一和第二延伸部分，双氨基分支连接子和第一和第二个另外的接头，每个接头都包含OEG样接头元件; 其中这些元件通过酰胺键相互连接并连接到GLP-1类似物的Lys残基上。本发明还涉及掺入本发明衍生物中的新型GLP-1类似物形式的中间产物，以及该衍生物的药物组合物和医学用途。衍生物具有很长的半衰期，同时保持令人满意的效力，这使得它们可能适用于每月一次的施用。

40. 发明公开

EP3000482A1 DOUBLE-ACYLATED GLP-1 DERIVATIVES 有权
标题翻译：双酰化GLP-1衍生物
公开(公告)号：EP3000482A1
公开(公告)日：2016-03-30
申请号：EP15188731.2
申请日：2010-12-16
申请人： Novo Nordisk A/S
发明人： SAUERBERG, Per , LAU, Jesper , LINDEROTH, Lars , KODRA, János Tibor , SPETZLER, Jane , GARIBAY, Patrick William
IPC分类号： A61K47/48 , C07D233/64 , 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 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.

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