SUBSTITUTED AZOLES, ANTI-VIRAL ACTIVE INGREDIENT, PHARMACEUTICAL COMPOSITION, METHOD FOR THE PRODUCTION AND USE THEREOF

摘要

The present invention relates to novel azoles, novel anti-viral active ingredients of general formula 1A and 1B, a pharmaceutical composition, an anti-viral drug and a method for preventing and treating viral diseases, particularly those caused by hepatitis C viruses (HCV). In the general formula 1A and 1B, in which the continuous lines accompanied by dotted lines (---) represent a single or double bond, X and Y assume different meanings, one being nitrogen and the other being oxygen, sulphur or an NH group; R1 and R2 are optionally identical radicals selected from 2-(R) and (S)-substituted N-acyl pyrrolidine derivatives; N-MeTmi-N-[2-(R) and (S)-substituted 2,2-disubstituted acetamides; methyl [2-(R) and (S)-substituted (((methyl)amino)-(1-oxo-butan-2-yl)-2-(11)-] and (?)-isopropyl)-carbamates. ? stands for an aliphatic ?2-?8 biradical; dioxane, cycloaliphatic, bicycloaliphatic, alkyloxyalkyl, alkyloxyalkyleneoxyalkyl, alkenyloxyalkyl, alkynyloxyalkyl biradicals and thia analogues thereof; aryl and thiophenyl, alkynylcycloalkyl, alkynyldioxane, alkynylaryl, alkylthiophene, alkenylthiophene and alkynylthiophene, alkyloxyaryl, alkenyloxyaryl, alkynyloxyaryl, alkylthiaaryl, alkenylthiaaryl, alkynylthiaaryl, cycloalkylthiophene, aryldioxane and thiophenyldioxane biradicals. ? stands for: an aliphatic ?2-?8 radical comprising 1, 2 or 3 triple ?=? bonds; aryl and thiophenyl, alkynylcycloalkyl, alkynyldioxane, alkynylaryl, alkylthiophene, alkenylthiophene and alkynylthiophene, cycloalkylbenzene, 4-cycloalkylbiphenyl, bicycloalkylbenzene, 4-bicycloalkylbiphenyl, cycloalkylthiophene, aryldioxane and thiophenyldioxane radicals.