Invention Grant
- Patent Title: Double-acylated GLP-1 derivatives
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Application No.: US13882947Application Date: 2011-11-09
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Publication No.: US09708383B2Publication Date: 2017-07-18
- Inventor: Alice Ravn Madsen , Birgit Wieczorek , Jacob Kofoed , Jesper Lau , Jane Spetzler , Janos Tibor Kodra , Lars Linderoth , Patrick William Garibay , Per Sauerberg , Thomas Kruse
- Applicant: Alice Ravn Madsen , Birgit Wieczorek , Jacob Kofoed , Jesper Lau , Jane Spetzler , Janos Tibor Kodra , Lars Linderoth , Patrick William Garibay , Per Sauerberg , Thomas Kruse
- Applicant Address: DK Bagsvaerd
- Assignee: Novo Nordisk A/S
- Current Assignee: Novo Nordisk A/S
- Current Assignee Address: DK Bagsvaerd
- Agent Richard W. Bork
- Priority: EP10190515 20101109; EP11169276 20110609
- International Application: PCT/EP2011/069738 WO 20111109
- International Announcement: WO2012/062803 WO 20120518
- Main IPC: A61K38/00
- IPC: A61K38/00 ; C07K14/605 ; A61K47/48

Abstract:
The invention relates to a derivative of a GLP-1 analog, which analog comprises a first K residue at a position corresponding to position 18 of GLP-1(7-37) (SEQ ID NO: 1), a second K residue at another position, and a maximum of twelve amino acid changes as compared to GLP-1(7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 1, Chem. 2, and Chem. 3: HOOC—(CH2)x—CO—* Chem. 1: HOOC—C6H4—O—(CH2)y—CO—* Chem. 2: R2—C6H4—(CH2)z—CO—*, Chem. 3: in which x is an integer in the range of 6-18, y is an integer in the range of 3-17, z is an integer in the range of 1-5, and R2 is a group having a molar mass not higher than 150 Da; and the linker comprises *—NH—(CH2)2—(O—(CH2)2)k—O—(CH2)n—CO—*. Chem. 4: 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. The invention also relates to the pharmaceutical use thereof, for example in the treatment and/or prevention of all forms of diabetes and related diseases, as well as to corresponding novel peptides and side chain intermediates. The derivatives are suitable for oral administration.
Public/Granted literature
- US20130288960A1 Double-Acylated GLP-1 Derivatives Public/Granted day:2013-10-31
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