ANTIVIRAL SUBSTRATE ISOSTER ESTERS OF ASPARTATE PROTEASE OR THEIR SALTS, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL PREPARATION AND COMPOSITION Russian patent published in 2001 - IPC

FIELD: organic chemistry, biochemistry, pharmacy. SUBSTANCE: invention describes novel compounds of the general formula (I) where R₁ means acyl radical taken among lower alkoxy-lower alkanoyl (including lower alkoxycarbonyl) where radical of lower alkoxy-group is unsubstituted or substituted with one or more radicals taken independently each of other among halogen atom, lower alkoxy- or pyrrolidinyl-group that is unsubstituted or substituted with one or more radicals taken independently each of other among oxo- or hydroxyl-group; lower alkanoyl that is unsubstituted or substituted with piperidinyl, pyrrolidinyl, tetrahydropyranyl, tetrahydrofuranyl, thiazoli- -dinyl, thiazolyl, indolyl, 4H-1-benzopyranyl, piperidinyl- -oxy-, tetrahydropyranyloxy- or tetrahydrofuryloxy-group that in each case are unsubstituted or substituted with one or more substituents taken independently each of other among oxo-, hydroxyl-, amino-group, lower alkyl and lower alkoxycarbonyl; phenyl-lower alkoxycarbonyl; arylcarbonyl that is substituted with heterocyclyl or morpholine-lower alkyl; phenyl-lower alkanoyl that is substituted with hydroxyl, lower alkyl; and arylsulfonyl; residue that is bound by carbonyl group of amino acid valine and N-acylated by amino-group with lower alkoxy- -carbonyl; R₂ means cyclohexyl or phenyl that are unsubstituted or substituted with one or more radical taken independently each of other among hydroxyl, lower alkoxy-, phenyl-lower alkoxy-, pyridyl-lower alkoxy-group where pyridyl is bound by carbon atom in ring and lower alkoxy-lower alkoxy- -group; R₃ means cyclohexyl, cyclohexenyl, phenyl, naphthyl or tetrahydronaphthyl that are unsubstituted or substituted with one or more radicals taken independently each of other among phenyl, cyanophenyl, phenyl-lower alkyl, halogen atom, cyano-, hydroxyl-, lower alkoxy-, phenyl-lower alkoxy-, pyridyl-lower alkoxy-group where pyridyl is bound by carbon atom in ring, lower alkoxy-lower alkoxy-, alkylenedioxy-group and phenyl- -lower alkanesulfonyl that is unsubstituted or substituted in phenyl radical with one or more radicals taken independently each of other among halogen atom; R₄ means lower alkyl, cyclohexyl or phenyl; R₅ means lower alkyl; n = 1 or 2 or its salts under condition that at least salt-forming group presents. New compounds of the formula (I) show antiviral activity, they exhibit good pharmacokinetics, biological availability and/or good tolerance. Invention describes method of synthesis of compounds of the formula (I), pharmaceutical preparation and composition also. EFFECT: new compounds, improved method of synthesis, valuable medicinal properties. 12 cl, 5 tbl