|Title:||Cyclic peptide antifungal agents and process for preparation thereof|
|Abstract:|| Provided are compounds of the formula (1): ##STR00001## wherein R' is hydrogen, methyl or NH.sub.2C(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 Wilson (Bloomington, IN) |
|Assignee:|| Eli Lilly and Company (Indianapolis, IN) |
|Filing Date:||Mar 10, 2005|
|Claims:||1. A pharmaceutical formulation comprising a compound having the following formula: ##STR00237## wherein R is --O(CH.sub.2).sub.3CH.sub.3, --O(CH.sub.2).sub.4CH.sub.3, --O(CH.sub.2).sub.5CH.sub.3, --O(CH.sub.2).sub.2O(CH.sub.2).sub.3CH.sub.3, or --O(CH.sub.2).sub.2OC(CH--.sub.3).sub.3, and a pharmaceutically acceptable carrier, wherein the formulation is formulated for inhalation. |
2. The pharmaceutical formulation of claim 1, wherein the formulation comprises an aerosol spray.