| 摘要 |
medicine. SUBSTANCE: described are pyrone derivatives of general formula I: wherein X is group of formula: OR4 wherein R4 is hydrogen unbranched alkyl having 1-6 carbon atoms, branched or cyclic alkyl having 3-7 carbon atoms; y is oxygen, C(R4)2 or NR4 wherein R4 is as defined above; R1 and R2 are independently [CH2]n1-[W1]n2-[Ar]n2-[CH2]n3-[W2]n4-R5 wherein n1-n4 and R5 are as defined above; in this case, if W1 is heteroatom, then n1 is integer of 1-4, or R1 and R2 together form 3-, 4-, 5-, 6- or 7-membered ring unsubstituted or substituted by at least one of above- indicated residues of R5; R3 is group of formula [W3]-[CH2]n3-[W4]n4-[Ar]n2-[CH2]n3-[W2]n4-R5 wherein n1, n2, n3, n4 and n5 are independent and are integers of 0-4.0-1.0-4, 0-1 and 0-2, respectively. W1, W2 and W4 are independent and are oxygen, OCONR5, S(O)n5, CO, NR5, C(R5)2; W3 is selected from group consisting of oxygen, S(O)n5, NR5; R5 is independently hydrogen or residue Ar and unbranched or branched alkyl having 1-6 carbon atoms unsubstituted or substituted by at least one residue selected from group consisting of CO2R4, CON(R4)2, OR4, chlorine, bromine, fluorine, trifluoromethyl, radical Ar or two radicals R5 together form unsubstituted ring having 3-7 carbon atoms, and Ar is independently phenyl, naphthyl, benzo(1,3)dioxol, imidazolyl, pyrimidinyl, thienyl, cycloalkyl having 3-6 carbon atoms unsubstituted or substituted by residues selected form group consisting of fluorine, chlorine, bromine, cyano, amino, trifluoromethyl, and radical of formula (CH2)n6R4 and (CH2)n6OR4, wherein n6 is independently integer of 0-3, an R4 is as defined above, or pharmaceutically acceptable salts thereof. Compounds are active ingredient of pharmaceutical composition having antiviral and antimicrobial activity. Also described are intermediate compounds for preparing pyrone-derivatives of formula 1 and also method of treating retrovirus-induced infection or disease by introducing pyrone derivatives of formula I in therapeutically effective amount. EFFECT: improved properties of the title compounds. 21 cl, 113 ex, 4 tbl |
