abstract |
A pharmaceutical composition comprising: (a) a pyranone compound of formula II or a pharmaceutically acceptable salt thereof as a pharmaceutically active agent; (b) a basic amine in an amount of from 0.1% to 10% by weight of the total composition, (c) one or more pharmaceutically acceptable solvents and (d) one or more pharmaceutically acceptable surfactants. In formula II: R1 is H-; R2 is alkyl, phenyl-(CH2)2-, het-SO2NH-(CH2)2-, cyclopropyl-(CH2)2-, F-phenyl-(CH2)2-, het-SO2NH-phenyl- or F3C-(CH2)2- or R1 and R2 taken together are a double bond; R3 is R4-(CH2)n-CH(R5)-, H3C-[O(CH2)2]2-CH2-, phenyl-(CH2)2-, het-SO2NH-(CH2)2-, (HOCH2)3C-NH-C(O)-NH-(CH2)3-, (HO2C)(H2N)CH-(CH2)2-C(O)-NH-(CH2)3-, piperazin-1-yl-C(O)-NH-(CH2)3, HO3S-(CH2)2-N(CH3)-C(O)-(CH2)6-C(O)-NH-(CH2)3-, cyclopropyl-(CH2)2-, F-phenyl-(CH2)2-, het-SO2NH-phenyl, or F3C-(CH2)2-; n is 0, 1 or 2; R4 is phenyl, het, cyclopropyl, H3C-[O-(CH2)2]2-, het-SO2NH-, Br-, N3-, or HO3S-(CH2)2-N(CH3)-C(O) -(CH2)6-C(O)-NH-; R6 is cyclopropyl, -CH3CH2 or t-butyl; R7 is -NR8SO2-het, -NR8SO2-phenyl optionally substituted with R9, -CH2-SO2phenyl optionally substituted with R9, or -CH2-SO2-het and R8 and R9 are as defined in the specification. |