-
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。
-
公开(公告)号:US20110105720A1
公开(公告)日:2011-05-05
申请号:US12922117
申请日:2009-03-13
申请人: Peter Madsen , Thomas Børglum Kjeldsen , Thomas Hoeg-Jensen , Palle Jakobsen , Tina Møller Tagmose , Tine Glendorf , Jånos Tibor Kodra , Patrick William Garibay , Jacob Sten Petersen
发明人: Peter Madsen , Thomas Børglum Kjeldsen , Thomas Hoeg-Jensen , Palle Jakobsen , Tina Møller Tagmose , Tine Glendorf , Jånos Tibor Kodra , Patrick William Garibay , Jacob Sten Petersen
IPC分类号: C07K14/62
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。
-
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。
-
公开(公告)号:US08722620B2
公开(公告)日:2014-05-13
申请号:US12280851
申请日:2007-02-27
申请人: Charlotte Harkjaer Fynbo , Ib Jonassen , Thomas Børglum Kjeldsen , Peter Madsen , Patrick William Garibay , Janos Tibor Kodra , Thomas Hoeg-Jensen , Tina Møller Tagmose
发明人: Charlotte Harkjaer Fynbo , Ib Jonassen , Thomas Børglum Kjeldsen , Peter Madsen , Patrick William Garibay , Janos Tibor Kodra , Thomas Hoeg-Jensen , Tina Møller Tagmose
摘要: The present invention is related to insulin derivatives having a side chain attached to an ε-amino group of a Lys residue present in the A-chain or to an ε-amino group of a Lys residue in the B-chain.
摘要翻译: 本发明涉及具有连接在A链中存在的Lys残基的侧链或B链中的Lys残基的' - 氨基的侧链的胰岛素衍生物。
-
5.
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。
-
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。
-
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。
-
公开(公告)号:US08859493B2
公开(公告)日:2014-10-14
申请号:US13506292
申请日:2012-04-09
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
CPC分类号: A61K47/48215 , A61K38/00 , A61K47/60 , C07K14/62
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 母体胰岛素分子通过酰胺键,该侧链包含在每个末端独立地含有选自-NH 2和-COOH的一个或多个乙二醇,丙二醇和/或丁二醇残基; 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。
-
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。
-
公开(公告)号:US20120208749A1
公开(公告)日:2012-08-16
申请号:US13506292
申请日:2012-04-09
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
CPC分类号: A61K47/48215 , A61K38/00 , A61K47/60 , C07K14/62
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 母体胰岛素分子通过酰胺键,该侧链包含在每个末端独立地含有选自-NH 2和-COOH的一个或多个乙二醇,丙二醇和/或丁二醇残基; 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。
-
-
-
-
-
-
-
-
-