| 主权项 |
1. A method for preparing an anti-viral pharmaceutical formulation for pulmonary delivery to a patient in need of same, which method comprises forming an aerosolized solution of said anti-viral formulation by electrohydrodynamic spraying, wherein said anti-viral formulation comprises a compound, or a pharmaceutically acceptable salt thereof, having the formula: wherein: R1 represents a radical selected from the group consisting of—NR5R6, —SO2NR7R8, hydroxyalkyl, hydroxyalkoxy, polyhydroxyalkyl, alkoxyalkoxy, polyfluoroalkyl, dialkylaminoalkyl, R9, —OR9,and HET; n being an integer from 1 to 4;
R2 and R3 are each independently selected from the group consisting of straight or branched chain alkyl and hydrogen; R4 is a radical selected from the group consisting of a substituted or unsubstituted phenyl radical, an unsubstituted or substituted heterocyclic radical, and —NR12R13; R5 and R7 are independently selected from the group consisting of alkoxyalkyl, hydroxyalkyl, polyhydroxyalkyl, aralkyl, R9, —(C═O)R14 and —(C═O)R9; R6, R8, R12, and R13 are independently selected from the group consisting of hydrogen, alkyl, alkoxyalkyl, polyfluoroalkyl, hydroxyalkyl, polyhydroxyalkyl, aralkyl, R9, —(C═O)R15 and —(C═O)R9; or R5 and R6 taken together with the nitrogen to which they are attached form a substituted or unsubstituted heterocyclic radical, said heterocyclic radical optionally containing one to two additional heteroatoms independently selected from the group consisting of nitrogen, oxygen, and sulfur; or R7 and R8 taken together with the nitrogen to which they are attached form a substituted or unsubstituted heterocyclic radical, said heterocyclic radical optionally containing one to two additional heteroatoms independently selected from the group consisting of nitrogen, oxygen, and sulfur; said phenyl and heterocyclic radical substituents being at least one selected from the group consisting of alkyl, amino, hydroxy, carbonyl, monoalkylamino, dialkylamino, halogen, and alkoxy; R9 is a radical of the formula —W—O(C═O)—CH3, W being a straight- or branched-chain alkylene group of 1 to 6 carbon atoms; R10 and R11 are radicals independently selected from the group consisting of alkyl, halo, haloalkyl, and polyfluoroalkyl; HET represents an unsubstituted or substituted five to seven membered heterocyclic ring containing one to four heteroatoms independently selected from nitrogen, oxygen or sulfur, whereby the point of attachment to the heterocyclic ring is not at a nitrogen atom, said heterocyclic ring substituents being one or more radicals selected from the group consisting of alkyl, amino, hydroxy, carbonyl, oxo, monoalkylamino, and dialkylamino, and wherein HET is other than pyridine when R1 is in the 4-position; R14 is a hydroxyalkyl, alkoxyalkyl or cycloalkyl group; R15 is an alkyl, hydroxyalkyl, alkoxyalkyl or cycloalkyl group. |
