Patent · US Active

Double-acylated GLP-1 compounds

US10689429B2 · kind B2 · utility

5Cited by
1References
11Claims
0Family size

Assignee

Inventors

Key dates

Filing dateApr 7, 2015
Grant dateJun 23, 2020
Priority date
Expiry dateApr 7, 2035

Classification

  • Technology area (CPC A)Human Necessities
  • CPC primaryA61K38/00
  • WIPO fieldPharmaceuticals
  • WIPO sectorChemistry

Abstract

The invention relates to a derivative of a GLP-1 peptide, which peptide comprises a first Lys residue at a position corresponding to position 36 of GLP-1(7-37) (SEQ ID NO: 1), a second Lys residue at a position corresponding to position 37 of GLP-1(7-37) (SEQ ID NO: 1), and a maximum of seven amino acid changes as compared to GLP-1(7-37) (SEQ ID NO: 1); which derivative comprises two protractors attached to said first and second Lys residue, respectively, each via a linker; wherein the protractor is selected from: HOOC—C6H4—O—(CH2)y—CO—*, and  Chem. 1:HOOC—(CH2)x—CO—*,  Chem. 2: wherein y is an integer in the range of 8-11, and x is 12; and the linker comprises at least one of: *—NH—CH(COOH)—(CH2)2—CO—*,  Chem. 3:*—NH—CH((CH2)2—COOH)—CO—*, and/or  Chem. 4:*—NH—(CH2)2—[O—(CH2)2]k—O—[CH2]n—CO—*,  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. The invention also relates to the pharmaceutical uses thereof, such as for the treatment of diabetes and obesity, as well as to the GLP-1 peptides forming part of these derivatives which have Lys residues at positions 36 and 37 and no …

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.