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Claims for Patent: 5,912,226

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Claims for Patent: 5,912,226

Title: Anhydro- and isomer-A-21978C cyclic peptides
Abstract:Two new groups of A-21978C cyclic peptides, anhydro- and isomer-A21978C peptide derivatives, have antibacterial activity and are useful as intermediates. The two groups are prepared via transpeptidation of the parent cyclic peptides. Pharmaceutical formulations containing the new peptides as active ingredients and methods of treating infections caused by susceptible Gram-positive bacteria with the formulations are also provided. The invention also provides an antibacterial composition containing the new drug substance LY 146032 in substantially pure form.
Inventor(s): Baker; Patrick J. (Greenwood, IN), Debono; Manuel (Indianapolis, IN), Farid; Khadiga Z. (Lebanon, IN), Molloy; R. Michael (Danville, IN)
Assignee: Eli Lilly and Company (Indianapolis, IN)
Application Number:07/809,039
Patent Claims: 1. A compound of the formula ##STR12## in which R is C.sub.5 -C.sub.14 -alkanoyl; R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen; or a pharmaceutically acceptable salt thereof.

2. A compound of the formula ##STR13## in which R is C.sub.5 -C.sub.14 -alkanoyl; R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen; or a pharmaceutically acceptable salt thereof.

3. A compound of claim 1 wherein R is alkanoyl of the formula ##STR14## and n is an integer from 3 to 12.

4. The compound of claim 3 wherein R is octanoyl.

5. The compound of claim 3 wherein R is nonanoyl.

6. A compound of claim 1 wherein R is decanoyl.

7. A compound of claim 2 wherein R is alkanoyl of the formula ##STR15## and n is an integer from 3 to 12.

8. The compound of claim 7 wherein R is octanoyl.

9. The compound of claim 7 wherein R is nonanoyl.

10. A compound of claim 2 wherein R is decanoyl.

11. A compound of claim 2 wherein R is undecanoyl.

12. A composition useful for the treatment of bacterial infections comprising an effective antibacterial amount of a compound of claim 1 together with a vehicle.

13. A composition useful for the treatment of bacterial infections comprising an effective antibacterial amount of a compound of claim 2 together with a vehicle.

14. A method for treating bacterial infections which comprises administering an effective amount of a composition of claim 12 to an animal.

15. A method for treating bacterial infections which comprises administering an effective amount of a composition of claim 13 to an animal.
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