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公开(公告)号：US08828923B2
公开(公告)日：2014-09-09
申请号：US12560833
申请日：2009-09-16
申请人： Ib Jonassen , Thomas Hoeg-Jensen , Svend Havelund , Ulla Ribel-Madsen , Tina Møller Tagmose , Peter Madsen
发明人： Ib Jonassen , Thomas Hoeg-Jensen , Svend Havelund , Ulla Ribel-Madsen , Tina Møller Tagmose , Peter Madsen
CPC分类号： C07K14/62 , A61K38/28 , A61K47/542
摘要： The present invention relates to insulin derivatives which are naturally occurring insulins or analogues thereof which have 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, the side chain being of the general formula: —W—X—Y—Z wherein W, X, Y and Z are as defined in the disclosure.
摘要翻译： 本发明涉及胰岛素衍生物，其是天然存在的胰岛素或其类似物，其具有侧链连接到B链的N-末端氨基酸残基的α-氨基或与α-链氨基的氨基 存在于母体胰岛素的B链中的Lys残基，侧链具有以下通式：-W-X-Y-Z，其中W，X，Y和Z如本公开中所定义。
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公开(公告)号：US08476228B2
公开(公告)日：2013-07-02
申请号：US13273659
申请日：2011-10-14
申请人： János Tibor Kodra , Patrick William Garibay , Thomas Hoeg-Jensen , Ib Jonassen , Peter Madsen , Tina Møller Tagmose
发明人： János Tibor Kodra , Patrick William Garibay , Thomas Hoeg-Jensen , Ib Jonassen , Peter Madsen , Tina Møller 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 胰岛素通过酰胺键，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：US20100227796A1
公开(公告)日：2010-09-09
申请号：US12781134
申请日：2010-05-17
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 ethylenglycol, 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-氨基或存在于B链的B链中的Lys残基的亚氨基的胰岛素衍生物 母体胰岛素分子，其侧链包含在每个末端独立地含有选自-NH 2和-COOH的基团的乙二醇，丙二醇和/或丁二醇的一个或多个残基; 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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14.发明申请Insulin Derivatives Conjugated with Structurally Well Defined Branched Polymers 审中-公开与结构定义良好的支化聚合物共轭的胰岛素衍生物公开(公告)号：US20090036353A1
公开(公告)日：2009-02-05
申请号：US11814184
申请日：2006-01-26
申请人： Carsten Behrens , Jesper Lau , Janos Tibor Kodra , Mikael Kofod-Hansen , Thomas Hoeg-Jensen , Peter Madsen , Svend Havelund
发明人： Carsten Behrens , Jesper Lau , Janos Tibor Kodra , Mikael Kofod-Hansen , Thomas Hoeg-Jensen , Peter Madsen , Svend Havelund
CPC分类号： B82Y5/00 , A61K47/59 , A61K47/595 , A61K47/60 , A61K47/641 , A61K47/6949
摘要： Insulin conjugated with structurally well defined, bifurcated and trifurcated polymers can be use by pulmonary delivery for systemic absorption through the lungs to reduce or eliminate the need for administering other insulins by injection.
摘要翻译： 与结构良好定义的分叉和三化聚合物结合的胰岛素可以通过肺部递送用于通过肺的全身吸收，以减少或消除通过注射施用其它胰岛素的需要。
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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：US20120071402A1
公开(公告)日：2012-03-22
申请号：US13306411
申请日：2011-11-29
摘要： Novel PEGylated insulin analogues exhibiting resistance towards proteases can, effectively, be administered pulmonary or orally. The insulin analogues contain B25H and A14E or A14H. The PEGylation is at B29K.
摘要翻译： 对蛋白酶具有抗性的新型聚乙二醇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。 PEG化为B29K。
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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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18.发明授权公开(公告)号：US08987197B2
公开(公告)日：2015-03-24
申请号：US13306411
申请日：2011-11-29
摘要： Novel PEGylated insulin analogs exhibiting resistance towards proteases can, effectively, be administered pulmonary or orally. The insulin analogs contain B25H and A14E or A14H. The PEGylation is at B29K.
摘要翻译： 对蛋白酶具有抗性的新型聚乙二醇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。 PEG化处于B29K。
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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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公开(公告)号：US20140315797A1
公开(公告)日：2014-10-23
申请号：US13823952
申请日：2011-10-14
申请人： Peter Madsen , Per Balschmidt , Svend Havelund , Thomas Hoeg-Jensen , Thomas Boerglum Kjeldsen , Charlotte Harkjaer Fynbo
发明人： Peter Madsen , Per Balschmidt , Svend Havelund , Thomas Hoeg-Jensen , Thomas Boerglum Kjeldsen , Charlotte Harkjaer Fynbo
IPC分类号： C07K14/62
CPC分类号： C07K14/62
摘要： The invention is related to novel N-terminally modified insulin derivatives, pharmaceutical compositions comprising such and methods of making such.
摘要翻译： 本发明涉及新型N-末端修饰的胰岛素衍生物，包含其的药物组合物及其制备方法。
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