Claims for Patent: 6,384,013

Summary for Patent: 6,384,013

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 and Ry are independently hydroxy or hydrogen; R1 is hydroxy, hydrogen, or hydroxysulfonyloxy; R7 is hydroxy, hydrogen, hydroxysulfonyloxy or phosphonooxy; R2 is a acyl side chain. Also provided are 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:	US09/291,900
Patent Claims:	1. A compound having the following formula: 2. 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 prepared by acylating an amino nucleus of Echinocandin B with an active ester of a carboxylic acid represented by the formula: wherein R is defined the same as above. 3. The compound of claim 2 wherein R is —O(CH2)4CH3. 4. The compound of claim 2 wherein said active ester is a 2,4,5-trichlorophenyl ester. 5. 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. 6. A compound represented by the formula: 7. A pharmaceutically acceptable salt of a compound according to claim 6.