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|Abstract:||The present invention relates to novel derivatives of exendin-4 or exendin-4 fragments, wherein the derivatives have a lipophilic substituent attached, optionally via a spacer, to an amino acid residue, which is not the N-terminal or C-terminal amino acid residue of the derivative.|
|Inventor(s):||Knudsen; Liselotte Bjerre (Valby, DK), Huusfeldt; Per Olaf (Copenhagen K, DK), Nielsen; Per Franklin (V.ae butted.rlose, DK), Madsen; Kjeld (Vaerlose, DK)|
|Assignee:||Novo Nordisk A/S (Bagsvaerd, DK)|
|Filing Date:||Jun 21, 2001|
|Claims:||1. A derivative of exendin-4 or a fragment thereof, wherein said derivative has one lipophilic substituent attached, optionally via a spacer, to an amino acid residue of said exendin-4 or fragment thereof, which is not the N-terminal or C-terminal amino acid residue of said exendin-4 or fragment thereof, wherein said fragment has insulinotropic activity. |
2. A pharmaceutical composition comprising a derivative of claim 1 and a pharmaceutically acceptable vehicle or carrier.
3. A method of treating insulin dependent or non-insulin dependent diabetes mellitus in a patient in need of such a treatment, comprising administering to the patient a therapeutically effective amount of a derivative of claim 1 and a pharmaceutically acceptable carrier.
4. The derivative of claim 1, wherein the lipophilic substituent has 4 to 40 carbon atoms.
5. The derivative of claim 4, wherein the lipophilic substituent has 8 to 25 carbon atoms.
6. The derivative of claim 4, wherein the lipophilic substituent is attached by means of a spacer.
7. The derivative of claim 6, wherein the spacer is an unbranched alkane .alpha.,.omega.-dicarboxylic acid group having from 1 to 7 methylene groups.
8. The derivative of claim 4, wherein the lipophilic substituent is a straight-chain or branched acyl group.
9. The derivative of claim 8, wherein the acyl group is of the formula CH.sub.3(CH.sub.2).sub.nCO--, wherein n is 4 to 38.
10. The derivative of claim 9, wherein the acyl group is CH.sub.3(CH.sub.2).sub.6CO--, CH.sub.3(CH.sub.2).sub.8CO--, CH.sub.3(CH.sub.2).sub.10CO--, CH.sub.3(CH.sub.2).sub.12CO--, CH.sub.3(CH.sub.2).sub.14CO--, CH.sub.3(CH.sub.2).sub.16CO--, CH.sub.3(CH.sub.2).sub.18CO--, CH.sub.3(CH.sub.2).sub.20CO-- or CH.sub.3(CH.sub.2).sub.22CO--.
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