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Claims for Patent: 6,100,376

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Claims for Patent: 6,100,376

Title: A.sup.21, B.sup.30, modified insulin derivatives having an altered action profile
Abstract:New insulin derivatives of the formula II with an iso-electric point between 5 and 8.5, with improved stability in weakly acid aqueous medium and with a special action profile, and the physiologically tolerated salts of these insulin derivatives, for the treatment of diabetes mellitus; formula II is: ##STR1## in which R.sup.1 denotes H or H-Phe, R.sup.2 denotes a genetically encodable L-amino acid which contains no amide group, R.sup.30 represents the residue of a neutral genetically encodable L-amino acid, R.sup.31 represents 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 group which is present where appropriate can be free, in the form of an ester functionality, an amide functionality, a lactone or reduced to CH.sub.2 0H, and X represents a genetically encodable L-amino acid.
Inventor(s): Dorschug; Michael (Bochum, DE)
Assignee: Hoechst Aktiengesellschaft (Frankfurt am Main, DE)
Application Number:08/842,794
Patent Claims: 1. An insulin derivative having an isoelectric point between 5 and 8.5, or a physiologically tolerated salt thereof, of the formula II ##STR5## in which: R.sup.1 at position B1 denotes H or H-Phe,

R.sup.2 at position A21 denotes a genetically encodable L-amino acid selected from the group consisting of Gly, Ala, Val, Leu, Ile, Pro, Phe, Trp, Met, Ser, Thr, Tyr, Asp, and Glu,

R.sup.30 represents the residue of a neutral genetically encodable L-amino acid selected from the group consisting of Tyr, Gly, Phe, and Thr,

R.sup.31 represents 1, 2, or 3 neutral or basic .alpha.-amino acids, whose terminal carboxyl group can be free or in the form of an amide functionality;

X represents His at position B10; and

the sequences A1 to A20 and B2 to B29 in Formula II correspond to a mammalian insulin.

2. An insulin derivative or the physiologically tolerated salt thereof as claimed in claim 1, wherein R.sup.1 in formula II represents H-Phe.

3. An insulin derivative or the physiologically tolerated salt thereof as claimed in claim 1, wherein R.sup.2 in formula II represents Gly.

4. An insulin derivative or the physiologically tolerated salt thereof as claimed in claim 1, wherein R.sup.30 in formula II represents Thr.

5. An insulin derivative or the physiologically tolerated salt thereof as claimed in claim 1, wherein the sequences (A1 to A20) and (B2 to B9 and B11 to B29) in Formula II are the corresponding sequences of human, porcine, or bovine insulin.

6. An insulin derivative or the physiologically tolerated salt thereof as claimed in claim 1, wherein R.sup.30 in formula II represents Gly.

7. An insulin derivative or the physiologically tolerated salt thereof as claimed in claim 1, wherein R.sup.30 in formula II represents Phe.

8. An insulin derivative or the physiologically tolerated salt thereof as claimed in claim 1, wherein R.sup.30 in formula II represents Tyr.

9. A pharmaceutical composition that contains an effective amount of at least one insulin derivative of the formula II, or at least one of the physiologically tolerated salts thereof, as claimed in claim 1, in dissolved, amorphous or crystalline form.

10. A pharmaceutical composition as claimed in claim 9, which additionally contains 1 .mu.g to 2 mg, of zinc/ml.

11. A pharmaceutical composition as claimed in claim 9, which additionally contains unmodified insulin.

12. A method for treating a patient suffering from diabetes mellitus, which comprises administering to said patient a pharmaceutical composition as claimed in claim 9.
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