Patent ID: 6555558
Filing Date: 2003-04-29
Classification: A61K,A61P,B82Y,Y02A

Abstract:
A pharmaceutical composition substantially free of alcohol and propylene glycol comprising:(a) a pyranone compound of Formula I as a pharmaceutically active agent, wherein R1 is Hâ€”; R2 is C3-C5 alkyl, phenyl-(CH2)2â€”, het-SO2NHâ€”(CH2)2â€”, cyclopropyl-(CH2)2â€”, F-phenyl-(CH2)2â€”, het-SO2NH-phenyl-, or F3Câ€”(CH2)2â€”; or R1 and R2 taken together are a double bond; R3 is R4â€”(CH2)nâ€”CH(R5)â€”, H3Câ€”[O(CH2)2]2â€”CH2â€”, C3-C5 alkyl, phenyl-(CH2)2â€”, het-SO2NHâ€”(CH2)2â€”, (HOCH2)3Câ€”NHâ€”C(O)â€”NHâ€”(CH2)3â€”, (HO2C)(H2N)CHâ€”(CH2)2â€”C(O)â€”NHâ€”(CH2)3â€”, piperazin-1-yl-C(O)â€”NHâ€”(CH2)3, HO3S(CH2)2â€”N(CH3)â€”C(O)â€”(CH2)6â€”C(O)â€”NHâ€”(CH2)3â€”, cyclopropyl-(CH2)2â€”, F-phenyl-(CH2)2â€”, het-SO2 NH-phenyl, or F3Câ€”(CH2)2â€”; n is 0, 1 or 2; R4 is phenyl, het, cyclopropyl, H3Câ€”[O(CH2)2]2â€”, het-SO2NHâ€”, Brâ€”, N3â€”, or HO3S(CH2)2â€”N(CH3)â€”C(O)â€”(CH2)6â€”C(O)â€”NHâ€”; R5 is â€”CH2â€”CH3, or â€”CH2-cyclopropyl; R6 is cyclopropyl, CH3â€”CH2â€”, or t-butyl; R7 is â€”NR8SO2-het, â€”NR8SO2-phenyl, optionally substituted with R9,â€”CH2â€”SO2-phenyl, optionally substituted with R9, or â€”CH2â€”SO2-het; R8 is â€”H, or â€”CH3; R9 is â€”CN, â€”F, â€”OH, or â€”NO2; wherein het is a 5-, 6- or 7-membered saturated or unsaturated ring containing from one to three heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur; and including any bicyclic group in which any of the above heterocyclic rings is fused to a benzene ring or another heterocycle, optionally substituted with â€”CH3, â€”CN, â€”OH, â€”C(O)OC2H5, â€”CF3, â€”NH2, or â€”C(O)â€”NH2; or a pharmaceutically acceptable salt thereof;(b) one or more pharmaceutically acceptable surfactants; and (c) a polyethylene glycol solvent having a mean molecular weight of greater than 300 but lower than 600.