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1.发明申请Pharmaceutical Preparations Comprising Insulin, Zinc Ions and Zinc-Binding Ligand 审中-公开包含胰岛素，锌离子和锌结合配体的药物制剂公开(公告)号：US20090123563A1
公开(公告)日：2009-05-14
申请号：US11814123
申请日：2006-02-06
申请人： Niels Christian Kaarsholm , Helle Birk Olsen , Peter Madsen , Soeren Ostegaard , Palle Jakobsen , Tina Moeller Tagmose
发明人： Niels Christian Kaarsholm , Helle Birk Olsen , Peter Madsen , Soeren Ostegaard , Palle Jakobsen , Tina Moeller Tagmose
CPC分类号： A61K38/28
摘要： Novel preparations comprising branched ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer. The preparations have a prolonged action designed for flexible injection regimes.
摘要翻译： 包含R状态胰岛素六聚体的HisB10 Zn2 +位点的支链配体的新型制剂。 制剂的灵活注射方案设计时间长。
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公开(公告)号：US08691759B2
公开(公告)日：2014-04-08
申请号：US12922117
申请日：2009-03-13
申请人： Peter Madsen , Thomas Boerglum Kjeldsen , Thomas Hoeg-Jensen , Palle Jakobsen , Tina Moeller Tagmose , Janos Tibor Kodra , Patrick William Garibay
发明人： Peter Madsen , Thomas Boerglum Kjeldsen , Thomas Hoeg-Jensen , Palle Jakobsen , Tina Moeller Tagmose , Janos Tibor Kodra , Patrick William Garibay
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.
摘要翻译： 对蛋白酶具有抗性的新型酰化胰岛素类似物可以有效地被肺或口服给药。 胰岛素类似物含有B25H和A14E或A14H。
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3.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。
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公开(公告)号：US09260503B2
公开(公告)日：2016-02-16
申请号：US14126215
申请日：2012-06-14
CPC分类号： C07K14/622 , C07K1/1077 , C07K14/62
摘要： The present invention regards an insulin derivative comprising at least 2 albumin binding moieties, wherein said albumin binding moieties comprise fatty diacid substitutions and a method for preparing such an insulin derivative by acylation and/or reductive alkylation. The present invention also concern a pharmaceutical comprising such an insulin derivative.
摘要翻译： 本发明涉及包含至少2个白蛋白结合部分的胰岛素衍生物，其中所述白蛋白结合部分包含脂肪二酸取代和通过酰化和/或还原烷基化制备这种胰岛素衍生物的方法。 本发明还涉及包含这种胰岛素衍生物的药物。
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公开(公告)号：US20140228285A1
公开(公告)日：2014-08-14
申请号：US14126215
申请日：2012-06-14
IPC分类号： C07K14/62
CPC分类号： C07K14/622 , C07K1/1077 , C07K14/62
摘要： The present invention regards an insulin derivative comprising at least 2 albumin binding moieties, wherein said albumin binding moieties comprise fatty diacid substitutions and a method for preparing such an insulin derivative by acylation and/or reductive alkylation. The present invention also concern a pharmaceutical comprising such an insulin derivative.
摘要翻译： 本发明涉及包含至少2个白蛋白结合部分的胰岛素衍生物，其中所述白蛋白结合部分包含脂肪二酸取代和通过酰化和/或还原烷基化制备这种胰岛素衍生物的方法。 本发明还涉及包含这种胰岛素衍生物的药物。
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公开(公告)号：US20120035104A1
公开(公告)日：2012-02-09
申请号：US13273659
申请日：2011-10-14
申请人： Janos Tibor Kodra , Patrick William Garibay , Thomas Hoeg-Jensen , Ib Jonassen , Peter Madsen , Tina Moeller Tagmose
发明人： Janos Tibor Kodra , Patrick William Garibay , Thomas Hoeg-Jensen , Ib Jonassen , Peter Madsen , Tina Moeller Tagmose
摘要： The present invention relates to insulin derivatives having a side chain attached either to the α-amino group of the N-terminal amino acid residue of the B chain or to the ε-amino group of a Lys residue present in the B chain of the parent insulin via an amide bond which side chain comprises at least one aromatic group; at least one free carboxylic acid group or a group which is negatively charged at neutral pH, a fatty acid moiety with 4 to 22 carbon atoms in the carbon chain; and possible linkers which link the individual components in the side chain together via amide bonds.
摘要翻译： 本发明涉及具有侧链连接到B链的N末端氨基酸残基的α-氨基或存在于B链的B链中的Lys残基的' - 氨基的胰岛素衍生物 通过酰胺键的母体胰岛素，该侧链包含至少一个芳族基团; 至少一个游离羧酸基团或在中性pH下带负电荷的基团，碳链中具有4-22个碳原子的脂肪酸部分; 以及通过酰胺键将侧链中各个组分连接在一起的可能接头。
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公开(公告)号：US20090306337A1
公开(公告)日：2009-12-10
申请号：US12375678
申请日：2007-07-16
IPC分类号： C07K14/62
摘要： PEGylated, extended insulins are insulins which, compared with human insulin, has one or more extensions extended from the A1, B1, A21 and/or B30 position(s), said extension(s) consist(s) of amino acid residue(s) and wherein a PEG moiety, via a linker, is attached to one or more of the amino acid residues in the extension(s). PEG is polyethyleneglycol. Such PEGylated, extended insulins have higher bioavailability and a longer time-action profile than regulär insulin and are in particular suited for pulmonary administration and can, conveniently, be used to treat diabetes.
摘要翻译： 聚乙二醇化的延长胰岛素是胰岛素，其与人胰岛素相比具有从A1，B1，A21和/或B30位置延伸的一个或多个延伸，所述延伸部分包含氨基酸残基（s） ），并且其中通过接头的PEG部分连接到延伸中的一个或多个氨基酸残基。 PEG是聚乙二醇。 这种聚乙二醇化的延长胰岛素具有比调节胰岛素更高的生物利用度和更长的时间作用特征，并且特别适合于肺部给药，并且可以方便地用于治疗糖尿病。
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公开(公告)号：US20080171695A1
公开(公告)日：2008-07-17
申请号：US11814374
申请日：2006-02-01
申请人： Patrick William Garibay , Thomas Hoeg-Jensen , Ib Jonassen , Svend Havelund , Peter Madsen , Palle Jakobsen
发明人： Patrick William Garibay , Thomas Hoeg-Jensen , Ib Jonassen , Svend Havelund , Peter Madsen , Palle Jakobsen
摘要： The present invention is related to insulin derivatives having a side chain attached either to the α-amino group of the N-terminal amino acid residue of B chain or to an ε-amino group of a Lys residue present in the B chain of the parent insulin molecule via an amide bond which side chain comprises one or more residues of ethyleneglycol, propyleneglycol and/or butyleneglycol containing independently at each termini a group selected from —NH2 and —COOH; a fatty diacid moiety with 4 to 22 carbon atoms, at least one free carboxylic acid group or a group which is negatively charged at neutral pH; and possible linkers which link the individual components in the side chain together via amide or ether bonds, said linkers optionally comprising a free carboxylic acid group.
摘要翻译： 本发明涉及具有侧链连接到B链的N末端氨基酸残基的α-氨基或母体B链中存在的Lys残基的ε-氨基的胰岛素衍生物 胰岛素分子，该侧链包含一个或多个在每个末端独立地含有选自-NH 2和-COOH的乙二醇，丙二醇和/或丁二醇的残基; 具有4至22个碳原子的脂肪二酸部分，至少一个游离羧酸基团或在中性pH下带负电荷的基团; 以及通过酰胺或醚键将侧链中各个组分连接在一起的可能接头，所述接头任选地包含游离羧酸基团。
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公开(公告)号：US20060258561A1
公开(公告)日：2006-11-16
申请号：US11226870
申请日：2005-09-09
申请人： Per Balschmidt , Helle Olsen , Niels Kaarsholm , Peter Madsen , Palle Jakobsen , Svend Ludvigsen , Gerd Schluckebier , Dorte Steensgaard , Anders Petersen
发明人： Per Balschmidt , Helle Olsen , Niels Kaarsholm , Peter Madsen , Palle Jakobsen , Svend Ludvigsen , Gerd Schluckebier , Dorte Steensgaard , Anders Petersen
IPC分类号： A61K38/28 , A61K31/522 , A61K31/513 , A61K31/426 , A61K31/4196 , A61K31/4184 , A61K31/4166 , A61K33/32
CPC分类号： A61K31/4166 , A61K31/4184 , A61K31/4196 , A61K31/426 , A61K31/513 , A61K31/522 , A61K33/30 , A61K38/28 , A61K45/06
摘要： This invention relates to NPH-insulin (crystalline preparations) that are prepared in the presence of certain high-affinity ligands for the HisB10 Zn2+-sites of the R-state insulin hexamer. Preparation of NPH-insulin in the presence of high-affinity ligand results in crystalline NPH-insulin suspensions that are absorbed more slowly from subcutis than regular NPH-insulin. Hence the resulting action profile is longer and the spike is less pronounced than observed with regular NPH-insulin
摘要翻译： 本发明涉及在R状态胰岛素六聚体的HisB10 Zn 2+ 2+的某些高亲和力配体存在下制备的NPH-胰岛素（结晶制剂）。 在高亲和力配体的存在下制备NPH-胰岛素导致结晶NPH-胰岛素悬浮液比皮下组织比常规NPH-胰岛素更慢吸收。 因此，所得到的作用谱更长，并且峰值不如用常规NPH-胰岛素观察到的
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公开(公告)号：US09150633B2
公开(公告)日：2015-10-06
申请号：US12673516
申请日：2008-08-15
申请人： Peter Madsen , Thomas Børglum Kjeldsen , Thomas Hoeg-Jensen , Tina Møller Tagmose , Palle Jakobsen , János Tibor Kodra , Patrick William Garibay , Dorte Xenia Gram
发明人： Peter Madsen , Thomas Børglum Kjeldsen , Thomas Hoeg-Jensen , Tina Møller Tagmose , Palle Jakobsen , János Tibor Kodra , Patrick William Garibay , Dorte Xenia Gram
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.
摘要翻译： 酰化胰岛素类似物，其中胰岛素类似物包含与A21氨基酸残基C末端连接的赖氨酸残基或至多包含赖氨酸残基的至多4个氨基酸残基的肽残基，所述肽残基与C21末端连接至A21氨基酸 残基，其特征在于包含亚烷基二醇部分的酰基部分连接到A22位置的赖氨酸残基，或连接到与A21氨基酸残基的C末端连接的肽残基中存在的赖氨酸残基，并且其中 胰岛素类似物中只有一个赖氨酸（K，Lys），可方便地给予肺部。
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