Patent ID: 6231887
Filing Date: 2001-05-15
Classification: A61K,A61P,Y02A,Y10S

Abstract:
A pharmaceutical composition comprising:(a) a pyranone compound of formula II as a pharmaceutically active agent, ##STR4##(b) an amine in an amount of from about 0.1% to about 10% by weight of the total composition,(c) one or more pharmaceutically acceptable solvents, and(d) one or more pharmaceutically acceptable surfactants;wherein said solvent is propylene glycol, polypropylene glycol, polyethylene glycol, glycerol, ethanol, triacetin, dimethyl isosorbide, glycofurol, propylene carbonate, dimethyl acetamide or a mixture thereof;wherein said surfactant is Polyoxyl 40 hydrogenated castor oil, Polyoxyl 35 castor oil, Polysorbate 20, Polysorbate 40, Polysorbate 60, Polysorbate 80, polyethylene glycol 12-hydroxy stearate, polyoxyethylene glyceryl trioleate, Polyoxyethylene stearates, Saturated Polyglycolyzed Glycerides, or Poloxamers;wherein R.sub.1 is H--;R.sub.2 is C.sub.3 -C.sub.5 alkyl, phenyl-(CH.sub.2).sub.2 --, het-SO.sub.2 NH--(CH.sub.2).sub.2 --, cyclopropyl-(CH.sub.2).sub.2 -, F-phenyl-(CH.sub.2).sub.2 -, het-SO.sub.2 NH-phenyl-, or F.sub.3 C-(CH.sub.2).sub.2 --; orR.sub.1 and R.sub.2 taken together are a double bond;R.sub.3 is R.sub.4 --(CH.sub.2).sub.n --CH(R.sub.5)--, H.sub.3 C--[O(CH.sub.2).sub.2 ].sub.2 --CH.sub.2 --, C.sub.3 -C.sub.5 alkyl, phenyl-(CH.sub.2).sub.2 --, het-SO.sub.2 NH--(CH.sub.2).sub.2 --, (HOCH.sub.2).sub.3 C--NH--C(O)NH--(CH.sub.2).sub.3 --, (HO.sub.2 C)(H.sub.2 N)CH--(CH.sub.2).sub.2 --C(O)--NH--(CH.sub.2).sub.3 --, piperazin-1-yl-C(O)--NH--(CH.sub.2).sub.3, HO.sub.3 S(CH.sub.2).sub.2 --N(CH.sub.3)--C(O)--(CH.sub.2).sub.6 --C(O)--NH--(CH.sub.2).sub.3 --, cyclopropyl-(CH.sub.2).sub.2 --, F-phenyl-(CH.sub.2).sub.2 --, het-SO.sub.2 NH-phenyl, or F.sub.3 C--(CH.sub.2).sub.2 --;n is 0, 1 or 2;R.sub.4 is phenyl, het, cyclopropyl, H.sub.3 C--[O(CH.sub.2).sub.2 ].sub.2 --, het-SO.sub.2 NH--, Br--, N.sub.3 --, or HO.sub.3 S(CH.sub.2).sub.2 --N(CH.sub.3)--C(O)--(CH.sub.2).sub.6 --C(O)--NH--;R.sub.5 is --CH.sub.2 --CH.sub.3, or --CH.sub.2 -cyclopropyl;R.sub.6 is cyclopropyl, CH.sub.3 --CH.sub.2 --, or t-butyl;R.sub.7 is --NR.sub.8 SO.sub.2 -het, --NR.sub.8 SO.sub.2 -phenyl, optionally substituted with R.sub.9, --CH.sub.2 --SO.sub.2 -phenyl, optionally substituted with R.sub.9, or --CH.sub.2 --SO.sub.2 -het;R.sub.8 is --H, or --CH.sub.3 ;R.sub.9 is --CN, --F, --OH, or --NO.sub.2 ;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 --CH.sub.3, --CN, --OH, --C(O)OC.sub.2 H.sub.5, --CF.sub.3, --NH.sub.2, or --C(O)--NH.sub.2 ; ora pharmaceutically acceptable salt thereof.