Novo Nordisk A/s

Ziylo Limited

Alice Ravn Madsen

Per Sauerberg

Thomas Kruse

Jesper F Lau

Patrick William Garibay

Anthony Murray

Janos Tibor Kodra

Thomas Hoeg-Jensen

Jacob Kofoed

Jane Spetzler

Lars Linderoth

Birgit Wieczorek

János Tibor Kodra

Anthony Davis

Andrew Michael Chapman

The present invention provides glucose sensitive insulin derivatives comprising a macrocycle, a glucose mimetic and human insulin or an analogue thereof, and their pharmaceutical use. Furthermore, the invention relates to pharmaceutical compositions comprising such glucose sensitive insulin derivatives, and to the use of such compounds for the treatment or prevention of medical conditions relating to diabetes.

Glucose sensitive insulins and uses thereof

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&#x2014;(CH)&#x2014;CO&#x2014;*&#x2003;&#x2003;Chem. 1:HOOC&#x2014;CH&#x2014;O&#x2014;(CH)&#x2014;CO&#x2014;*&#x2003;&#x2003;Chem. 2:R&#x2014;CH&#x2014;(CH)&#x2014;CO&#x2014;*,&#x2003;&#x2003;Chem. 3: 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.

Double-acylated GLP-1 derivatives

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Roedovre, Denmark

Alice Ravn Madsen