Insulin derivatives, a process for the preparation thereof,...

Details Insulin derivatives, a process for the preparation thereof,... Insulin derivatives, a process for the preparation thereof,...

C - Chemistry, Metallurgy

12

P

195/128.2, 530/7

C12P 21/02 (2006.01) A61K 38/28 (2006.01) C07K 14/62 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2006818

New insulin derivatives, a process for the preparation thereof, the use thereof and a pharmaceutical formulation containing them New insulin derivatives with a basic modification - due to the basic amino acid arginine in the AO position - of the formula II Image in which a) R30 + R31 together = OH or b) R30 = residue of a neutral, genetically encodable L-amino acid and R31 = OH or a physiologically acceptable organic group which is basic in nature and has up to 50 carbon atoms, in whose structure 0 to 3 .alpha.- amino acids are involved, and whose terminal carboxyl functionality, which is present where appropriate, can be in the free form, as ester functionality, as amide functionality, as lactone or reduced to CH2OH1 2 except the case in which at the same time R30 = Ala, R31 = OH and the A- and B-chains are the sequences of bovine insulin, and the physiologically tolerated salts thereof, are obtained by a variety of processes. The compounds are suitable for the treatment of diabetes mellitus, have a delayed profile of action and are very well tolerated.

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