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Serving leading biopharmaceutical companies globally:

Mallinckrodt
Farmers Insurance
Accenture
US Army
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Merck
Baxter
McKesson
Chubb
Deloitte

Generated: November 22, 2017

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Title: Cyclic peptide antifungal agents and process for preparation thereof
Abstract:Provided are compounds of the formula (1): ##STR1## wherein R' is hydrogen, methyl or NH.sub.2 C(O)CH.sub.2 --; R" and R'" are independently methyl or hydrogen; R adn R.sup.y are independently hydroxy or hydrogen; R.sub.1 is hydroxy, hydrogen, or hydroxysulfonyloxy; R.sub.7 is hydroxy, hydrogen, hydroxysulfonyloxy or phosphonooxy; R.sub.2 is a novel acyl side chain. Also provided are novel formulations, methods of inhibiting fungal and parasitic activity, and a process for preparing dideoxy (R.dbd.H) forms of the compounds.
Inventor(s): Burkhardt; Frederick J. (Indianapolis, IN), Debono; Manuel (Indianapolis, IN), Nissen; Jeffrey S. (Indianapolis, IN), Turner, Jr.; William W. (Bloomington, IN)
Assignee: Eli Lilly and Company (Indianapolis, IN)
Filing Date:Feb 27, 2003
Application Number:10/378,004
Claims:1. A compound represented by the formula ##STR237## wherein R is --O(CH.sub.2).sub.3 CH.sub.3, --O(CH.sub.2).sub.4 CH.sub.3, --O(CH.sub.2).sub.5 CH.sub.3, --O(CH.sub.2).sub.2 O(CH.sub.2).sub.3 CH.sub.3, or --O(CH.sub.2).sub.2 OC(CH.sub.3).sub.3.

2. A pharmaceutically acceptable salt of a compound according to claim 1.

3. A pharmaceutical formulation comprising a compound represented by the formula ##STR238## wherein R is --O(CH.sub.2).sub.3 CH.sub.3, --O(CH.sub.2).sub.4 CH.sub.3, --O(CH.sub.2).sub.5 CH.sub.3, --O(CH.sub.2).sub.2 O(CH.sub.2).sub.3 CH.sub.3, or --O(CH.sub.2).sub.2 OC(CH.sub.3).sub.3 and a pharmaceutically acceptable carrier.

4. A pharmaceutical formulation comprising a pharmaceutically acceptable salt of the formulation according to claim 3.

5. A method for inhibiting parasitic activity comprising contacting a formulation of claim 3 with a parasite.

6. A method of inhibiting fungal activity comprising contacting a formulation of claim 3 with a fungus.

7. A method of inhibiting the growth of organisms responsible for opportunistic infections in immunosuppressed individuals comprising administering a formulation of claim 3 to said individual.

8. A method of inhibiting the growth of Pneumocystis carinii comprising contacting a formulation of claim 3 with Pneumocystis carinii.

9. A pharmaceutical formulation comprising a compound having the following formula: ##STR239## and a pharmaceutically acceptable carrier, wherein the formulation is formulated for topical administration.

10. The pharmaceutical formulation of claim 9, wherein the pharmaceutically acceptable carrier comprises a dry powder or a solubilizing liquid.

11. The pharmaceutical formulation of claim 10, wherein the solubilizing liquid is aqueous.

12. The pharmaceutical formulation of claim 10, wherein the solubilizing liquid is non-aqueous.

13. The pharmaceutical formulation of claim 12, wherein the non-aqueous solubilizing liquid is an alcohol or glycol.

14. A method of inhibiting fungal activity comprising contacting a formulation of claim 9, with a fungus via topical administration.
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Serving leading biopharmaceutical companies globally:

Cantor Fitzgerald
Harvard Business School
Mallinckrodt
Fish and Richardson
Teva
AstraZeneca
Federal Trade Commission
Julphar
Novartis
Daiichi Sankyo

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