The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Apr. 23, 2019

Filed:

Aug. 14, 2014
Applicant:

Novo Nordisk A/s, Bagsvaerd, DK;

Inventors:

Per Sauerberg, Farum, DK;

Jacob Kofoed, Vaerloese, DK;

Assignee:

Novo Nordisk A/S, Bagsvaerd, DK;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
A61K 38/00 (2006.01); A61K 47/54 (2017.01); A61K 47/58 (2017.01); A61K 47/60 (2017.01); C07K 14/605 (2006.01);
U.S. Cl.
CPC ...
C07K 14/605 (2013.01); A61K 47/54 (2017.08); A61K 47/58 (2017.08); A61K 47/60 (2017.08); A61K 38/00 (2013.01);
Abstract

The present invention relates to tri-acylated GLP-1 derivatives, acylated at positions corresponding to positions (18, 22, 30), (18, 26, 37), (18, 27, 37), (26, 30, 37), or (27, 30, 37) of the native human glucagon-like peptide 1 (GLP-1 (7-37) (SEQ ID NO: 1); or pharmaceutically acceptable salts, amides, or esters thereof. The acylated side chains comprise a protracting moiety selected from Chem. 1: HOOC—(CH)—CO—*, Chem. 1a: HOOC—(CH)—CO—*, and Chem. 2: HOS—(CH)—CO—*, and the protracting moieties are connected, via a linker, to a Lys residue of the GLP-1 peptide. The GLP-1 peptide has a maximum of seven amino acid changes as compared to GLP-1 (7-37) (SEQ ID NO: 1). The invention also relates to intermediate products in the form of novel GLP-1 analogs, as well as to pharmaceutical compositions and uses of the derivatives and analogs, in particular for the treatment of type 2 diabetes. The derivatives have very long half-lives while maintaining a satisfactory potency, which makes them potentially suitable for once-monthly administration.


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