Claims for Patent: 6,743,777

Summary for Patent: 6,743,777

Title:	Cyclic peptide antifungal agents and process for preparation thereof
Abstract:	Provided are compounds of the formula (1): wherein R′ is hydrogen, methyl or NH2C(O)CH2—; R″ and R′″ are independently methyl or hydrogen; R adn Ry are independently hydroxy or hydrogen; R1 is hydroxy, hydrogen, or hydroxysulfonyloxy; R7 is hydroxy, hydrogen, hydroxysulfonyloxy or phosphonooxy; R2 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=H) forms of the compounds.
Inventor(s):	Frederick J. Burkhardt, Manuel Debono, Jeffrey S. Nissen, William W. Turner, Jr.
Assignee:	Eli Lilly and Co
Application Number:	US10/087,088
Patent Claims:	1. A pharmaceutical formulation comprising a compound having the following formula: and a pharmaceutically acceptable carrier. 2. A method for inhibiting parasitic activity comprising contacting a formulation of claim 1 with a parasite. 3. A method of inhibiting fungal activity comprising contacting a formulation of claim 1 with a fungus. 4. A method of inhibiting the growth of organisms responsible for opportunistic infections in immunosuppressed individuals comprising administering a formulation of claim 1 to said individual. 5. A method of inhibiting the growth of Pneumocystis carinii comprising contacting a formulation of claim 1 with Pneumocystis carinii. 6. A pharmaceutical formulation comprising a compound represented by the formula wherein R is —O(CH2)3CH3, —O(CH2)4CH3, —O(CH2)5CH3, —O(CH2)2O(CH2)3CH3, or —O(CH2)2OC(CH3)3 and a pharmaceutically acceptable carrier. 7. The formulation of claim 6, wherein R is —O(CH2)4CH3. 8. A method for inhibiting parasitic activity comprising contacting a formulation of claim 6 with a parasite. 9. The method of claim 8, wherein R is —O(CH2)4CH3. 10. A method of inhibiting fungal activity comprising contacting a formulation of claim 6 with a fungus. 11. The method of claim 10, wherein R is —O(CH2)4CH3. 12. A method of inhibiting the growth of organisms responsible for opportunistic infections in immunosuppressed individuals comprising administering a formulation of claim 6 to said individual. 13. The method of claim 12, wherein R is —O(CH2)4CH3. 14. A method of inhibiting the growth of Pneumocystis carinii comprising contacting a formulation of claim 6 with Pneumocystis carinii. 15. The method of claim 14, wherein R is —O(CH2)4CH3. 16. A pharmaceutical formulation comprising a compound represented by the formula and a pharmaceutically acceptable carrier. 17. A pharmaceutical formulation comprising a pharmaceutically acceptable salt of the formulation according to claim 16. 18. A method for inhibiting parasitic activity comprising contacting a formulation of claim 16 with a parasite. 19. A method of inhibiting fungal activity comprising contacting a formulation of claim 16 with a fungus. 20. A method of inhibiting the growth of organisms responsible for opportunistic infections in immunosuppressed individuals comprising administering a formulation of claim 16 to said individual. 21. A method of inhibiting the growth of Pneumocystis carinii comprising contacting a formulation of claim 16 with Pneumocystis carinii.