-
1.发明授权Ligands for the HisB10 Zn2 + sites of the R-state insulin hexamer 有权用于R-state胰岛素六聚体的HisB10 Zn2 +位点的配体公开(公告)号：US07879893B2
公开(公告)日：2011-02-01
申请号：US10332541
申请日：2002-09-13
申请人： Helle Birk Olsen , Niels C. Kaarsholm , Peter Madsen , Soren Ostergaard , Svend Ludvigsen , Palle Jakobsen , Anders Klarskov Petersen , Dorte Bjerre Steensgaard
发明人： Helle Birk Olsen , Niels C. Kaarsholm , Peter Madsen , Soren Ostergaard , Svend Ludvigsen , Palle Jakobsen , Anders Klarskov Petersen , Dorte Bjerre Steensgaard
IPC分类号： A61K31/41 , A61K31/40 , C07D257/00 , C07D209/82
CPC分类号： C07D257/04 , A61K31/4192 , A61K31/426 , C07D249/18 , C07D277/20 , C07D403/04 , C07D417/06 , C07D417/10 , C07D417/14 , C07D471/04
摘要： The present invention relates to novel ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer having the formula A-B-C-D-X (III), wherein: A is a chemical group which reversibly binds to a HisB10 Zn2+ sites of an insulin hexamer; B is a linker; C is a fragment consisting of 0 to 5 neutral amino acids; D is a fragment comprising 1 to 20 positively charged groups independently selected from amino or guanidino groups; and X is —OH, —NH2 or a diamino group. The present invention also relates to R-state insulin hexamers comprising such ligands, and aqueous insulin preparations comprising such R-state insulin hexamers.
摘要翻译： 本发明涉及具有式A-B-C-D-X（III）的R状态胰岛素六聚体的HisB10 Zn 2+位点的新配体，其中：A是可逆结合胰岛素六聚体的HisB10 Zn 2+位点的化学基团; B是一个连接子; C是由0至5个中性氨基酸组成的片段; D是包含1至20个独立地选自氨基或胍基的带正电基团的片段; X为-OH，-NH 2或二氨基。 本发明还涉及包含这种配体的R状态胰岛素六聚体和包含这种R状态胰岛素六聚体的含水胰岛素制剂。
-
公开(公告)号：US08097698B2
公开(公告)日：2012-01-17
申请号：US11944757
申请日：2007-11-26
申请人： Liselotte Bjerre Knudsen , Per Olaf Huusfeldt , Per Franklin Nielsen , Niels C. Kaarsholm , Helle Birk Olsen , Soren Erik Bjorn , Freddy Zimmerdahl Pedersen , Kjeld Madsen
发明人： Liselotte Bjerre Knudsen , Per Olaf Huusfeldt , Per Franklin Nielsen , Niels C. Kaarsholm , Helle Birk Olsen , Soren Erik Bjorn , Freddy Zimmerdahl Pedersen , Kjeld Madsen
IPC分类号： A61K38/16 , C07K14/605
CPC分类号： C11D3/168 , A61K31/426 , A61K31/4439 , A61K38/2264 , A61K38/26 , A61K38/28 , A61K45/06 , A61K47/24 , C07K14/605 , C11D3/0063 , A61K2300/00
摘要： The present invention relates to a pharmaceutical composition comprising a GLP-1 derivative having a lipophilic substituent; and a surfactant.
摘要翻译： 本发明涉及包含具有亲脂性取代基的GLP-1衍生物的药物组合物; 和表面活性剂。
-
公开(公告)号：US06268343B1
公开(公告)日：2001-07-31
申请号：US09258750
申请日：1999-02-26
申请人： Liselotte Bjerre Knudsen , Per Olaf Huusfeldt , Per Franklin Nielsen , Niels C. Kaarsholm , Helle Birk Olsen , Søren Erik Bjørn , Freddy Zimmerdahl Pedersen , Kjeld Madsen
发明人： Liselotte Bjerre Knudsen , Per Olaf Huusfeldt , Per Franklin Nielsen , Niels C. Kaarsholm , Helle Birk Olsen , Søren Erik Bjørn , Freddy Zimmerdahl Pedersen , Kjeld Madsen
IPC分类号： A61K3916
CPC分类号： C11D3/168 , A61K38/2264 , A61K38/26 , A61K38/28 , C07K14/605 , C11D3/0063 , A61K2300/00
摘要： The present invention relates to GLP-1 derivatives having a lipophilic substituent, pharmaceutical compositions comprising same, and methods of making an using same. The GLP-1 derivatives of the present invention have a protracted profile of action.
摘要翻译： 本发明涉及具有亲油性取代基的GLP-1衍生物，包含其的药物组合物及其使用方法。 本发明的GLP-1衍生物具有延长的作用。
-
公开(公告)号：US20090176700A1
公开(公告)日：2009-07-09
申请号：US11944757
申请日：2007-11-26
申请人： Liselotte Bjerre Knudsen , Per Olaf Huusfeldt , Per Franklin Nielsen , Niels C. Kaarsholm , Helle Birk Olsen , Soren Erik Bjorn , Freddy Zimmerdahl Pedersen , Kjeld Madsen
发明人： Liselotte Bjerre Knudsen , Per Olaf Huusfeldt , Per Franklin Nielsen , Niels C. Kaarsholm , Helle Birk Olsen , Soren Erik Bjorn , Freddy Zimmerdahl Pedersen , Kjeld Madsen
IPC分类号： A61K38/16
CPC分类号： C11D3/168 , A61K31/426 , A61K31/4439 , A61K38/2264 , A61K38/26 , A61K38/28 , A61K45/06 , A61K47/24 , C07K14/605 , C11D3/0063 , A61K2300/00
摘要： The present invention relates to a pharmaceutical composition comprising a GLP-1 derivative having a lipophilic substituent; and a surfactant.
摘要翻译： 本发明涉及包含具有亲脂性取代基的GLP-1衍生物的药物组合物; 和表面活性剂。
-
公开(公告)号：US06521738B2
公开(公告)日：2003-02-18
申请号：US09736611
申请日：2000-12-14
IPC分类号： C07K1462
CPC分类号： C07K14/62
摘要： Novel insulin precursors and insulin precursor analogs having a mini C-peptide comprising at least one aromatic amino acid residue have an increased folding stability. The novel insulin precursors and insulin precursor analogs can be expressed in yeast in high yields and are preferably not more 15 amino acid residues in length. Also provided are polynucleotide sequences encoding the claimed precursors or precursor analogs, and vectors and cell lines containing such polynucleotide sequences.
-
公开(公告)号：US07087408B2
公开(公告)日：2006-08-08
申请号：US10316421
申请日：2002-12-11
CPC分类号： C07K14/62
摘要： Novel insulin precursors and insulin precursor analogs having a mini C-peptide comprising at least one aromatic amino acid residue have an increased folding stability. The novel insulin precursors and insulin precursor analogs can be expressed in yeast in high yields and are preferably not more 15 amino acid residues in length. Also provided are polynucleotide sequences encoding the claimed precursors or precursor analogs, and vectors and cell lines containing such polynucleotide sequences.
-
公开(公告)号：US20180110863A1
公开(公告)日：2018-04-26
申请号：US15564805
申请日：2016-04-04
申请人： Danqing FENG , Erin N. GUIDRY , Pei HUO , Niels C. KAARSHOLM , Songnian LIN , Ravi P. NARGUND , Lin YAN , Merck Sharp & Dohme Corp.
发明人： Danqing Feng , Erin N. Guidry , Pei Huo , Niels C. Kaarsholm , Songnian Lin , Ravi P. Nargund , Lin Yan
摘要： Insulin conjugates comprising an insulin analog molecule covalently attached to at least one bi-dentate linker having two arms, each arm independently attached to a ligand comprising a saccharide and wherein the saccharide for at least one ligand of the linker is fucose are disclosed. The insulin conjugates display a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose even when administered to a subject in need thereof in the absence of an exogenous multivalent saccharide-binding molecule such as Con A.
-
公开(公告)号：US06489292B1
公开(公告)日：2002-12-03
申请号：US09441702
申请日：1999-11-16
申请人： Svend Havelund , Niels C. Kaarsholm
发明人： Svend Havelund , Niels C. Kaarsholm
IPC分类号： A61K3828
CPC分类号： A61K38/28
摘要： Stable, aqueous insulin formulations without phenol and m-cresol which are suitable for pulmonary delivery and for delivery when phenol and m-cresol are undesirable are disclosed. The formulations provide increased convenience for the patient.
摘要翻译： 公开了不含酚和间甲酚的稳定的含水胰岛素制剂，其适用于肺部输送和当苯酚和间甲酚不期望时的递送。 该制剂为患者提供了更多的便利。
-
公开(公告)号：US06384016B1
公开(公告)日：2002-05-07
申请号：US09265141
申请日：1999-03-08
申请人： Niels C. Kaarsholm
发明人： Niels C. Kaarsholm
IPC分类号： A61K3800
CPC分类号： A61K38/26 , A61K47/24 , Y10S514/866
摘要： Aqueous compositions comprising at least one peptide selected from glucagon, GLP-1, and analogues and derivatives thereof together with a stabilizing and solubilizing amount of at least one detergent, said detergent having at least 2 positive charges, at least 2 negative charges, or a combination of at least one positive charge and at least one negative charge.
摘要翻译： 包含选自胰高血糖素，GLP-1及其类似物和衍生物的至少一种肽以及稳定和增溶量的至少一种洗涤剂的水性组合物，所述洗涤剂具有至少2个正电荷，至少2个负电荷或 至少一个正电荷和至少一个负电荷的组合。
-
-
-
-
-
-
-
-
搜索结果
9 条记录 (耗时 0.037 秒)
