Details for Patent: 6,384,013

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 and 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 acyl side chain. Also provided are 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:	Apr 14, 1999
Application Number:	09/291,900
Claims:	1. A compound having the following formula: ##STR245## 2. A compound represented by the formula: ##STR246## 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 prepared by acylating an amino nucleus of Echinocandin B with an active ester of a carboxylic acid represented by the formula: ##STR247## wherein R is defined the same as above. 3. The compound of claim 2 wherein R is --O(CH.sub.2).sub.4 CH.sub.3. 4. The compound of claim 2 wherein said active ester is a 2,4,5-trichlorophenyl ester. 5. A compound represented by the formula: ##STR248## 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. 6. A compound represented by the formula: ##STR249## 7. A pharmaceutically acceptable salt of a compound according to claim 6.