| 发明名称 |
Double-acylated GLP-1 derivatives |
| 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 K37, and the second K residue is designated K26, which derivative comprises two albumin binding moieties attached to K26 and K37, respectively, wherein the albumin binding moiety comprises a protracting moiety selected from:;Chem. 1, Chem. 2, Chem. 3 or Chem. 4; or a pharmaceutically acceptable salt, amide, or ester thereof. |
| 申请公布号 |
US9556250(B2) |
申请公布日期 |
2017.01.31 |
| 申请号 |
US201314101618 |
申请日期 |
2013.12.10 |
| 申请人 |
Novo Nordisk A/S |
发明人 |
Garibay Patrick William;Spetzler Jane;Linderoth Lars;Lau Jesper;Schaeffer Lauge |
| 分类号 |
A61K38/26;A61K47/48;C07K14/65;A61K38/00;C07D233/64;C07K14/605 |
主分类号 |
A61K38/26 |
| 代理机构 |
|
代理人 |
Bork Richard W. |
| 主权项 |
1. 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), wherein the first K residue is designated K37, and the second K residue is designated K26, which analogue, in addition to K37, has a maximum of three additional amino acid modifications as compared to GLP-1(7-37), which derivative comprises two albumin binding moieties attached to K26 and K37, respectively, wherein the albumin binding moiety comprises i) a protracting moiety of formula Chem. 1:HOOC—(CH2)x—CO—* in which x is an integer in the range of 6-18 and ii) a linker of formula Chem. 5: 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. |
| 地址 |
Bagsvaerd DK |
