Fatty acid-acylated insulin analogs

A - Human Necessities – 61 – K

Patent

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Details

A61K 38/00 (2006.01) A61K 38/02 (2006.01) A61K 38/28 (2006.01) C07K 5/00 (2006.01) C07K 7/00 (2006.01) C07K 14/62 (2006.01)

Patent

CA 2306905

Fatty acid-acylated insulin analogs are soluble at moderately acidic pH and provide long-acting basal control of glucose levels. In such a molecule, the insulin analog portion comprises an insulin A-chain, or an analog thereof, properly cross-linked to an analog of the insulin B-chain, wherein the .epsilon.-amino group of a Lys residue at either positions 28 or 29 of the B- chain analog is acylated with a fatty acid. The insulin analog portion of the molecules comprises an A-chain of insulin, or an analog thereof, with an optional Arg at position 0, properly cross-linked to a B-chain analog that includes Arg at positions 31 and 32.

Des analogues d'insuline acylée par un acide gras sont solubles à un pH modérément acide et permettent d'effectuer un contrôle basique à long terme des niveaux de glucose. Dans cette molécule, la partie analogue d'insuline est composée d'une chaîne A d'insuline, ou d'un de ses analogues, réticulée à un analogue de la chaîne B, le groupe .epsilon.-amino d'un résidu Lys dans l'une ou l'autre des positions 28 ou 29 de l'analogue de chaîne B étant acylé par un acide gras. La partie analogue d'insuline de ces molécules comprend une chaîne A d'insuline, ou d'un de ses analogues, comportant un Arg éventuel dans la position 0, réticulée à un analogue de chaîne B comprenant Arg dans les positions 31 et 32.

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