OXY-SUBSTITUTED IMIDAZOQUINOLINES, CAPABLE OF MODULATING BIOSYNTHESIS OF CYTOKINES Russian patent published in 2011 - IPC C07D471/04 A61K31/4745 A61P37/00 

FIELD: chemistry.

SUBSTANCE: present invention relates to novel derivatives of 1H-imidazo [4,5-c]quinolines of formula II or pharmaceutically acceptable salts thereof, where R₃ is selected from a group comprising -Z-Y-R₄, -Z-Y-X-Y-R₄, -Z-R₅, -Z-Het, -Z-Het'-R₄, and -Z-Het'-Y-R₄; Z is selected from a group which includes C₁-C₆alkylene; n equals 0; R₁ is selected from a group comprising R₄, -X-R₄ and -X-Y-R₄; R₂ is selected from a group comprising C₁-C₆alkyl, C₁-C₆alkoxy, hydroxyC₁-C₆alkyl and C₁-C₆alkoxy-C₁-C₆alkyl; X is selected from a group comprising C₁-C₆alkylene, C₆arylene, heteroarylene which is thienyl, and heterocyclylene which is piperzinyl, where the alkylene group can be optionally broken by -O- group; Y is selected from a group comprising -S(O)_0-2-, -C(R₆)-, -C(R₆)-O-, -O-C(R₆)-, -N(R₈)-Q-, -C(R₆)-N(R₈)-, and R₄ is selected from a group comprising hydrogen, C₁-C₆alkyl, C₂alkenyl, C₁-C₁₀aryl, C₆aryl-C₁alkylenyl, and heteroaryl selected from pyridyl, thienyl, benzodioxanyl and others (see claim 1), where C₁-C₆alkyl, C₂alkenyl and C₆-C₁₀aryl can be unsubstituted or substituted with one or two substitutes which are independently selected from a group comprising C₁-C₆alkyl, C₁-C₄alkoxy, CF₃-O-; halogen, nitro, hydroxy, mercapto, cyano, C_6-10aryl, C₆aryloxy, C₆aryl-C₁alkyleneoxy, thienyl, morpholinyl, amino, C₁alkylamino, di-C₁alkylamino, heterocyclyl group and an oxo-group; R₅ is selected from a group comprising and R₆ is selected from a group comprising =O and =S; R₇ is C_2-3akylene; R₈ is selected from a group comprising hydrogen and C₁-C₃alkyl; R₁₀ is C₄alkylene; A is selected from a group comprising -O-, -C(O)-, -S(O)_0-2-, and -N(R₄)-; Het is heterocyclyl selected from morpholinyl, pyrrolidinyl, piperidinyl, tetrahydropyranyl and others (see claim 1), which can be unsubstituted or substituted with one or more substitutes which are independently selected from a group comprising C₁-C₂alkyl, hydroxy, hydroxy-C₁-C₂alkyl, amino, C₁-C₂alkylamino, di-C₁-C₂alkylamino, heterocyclyl group and oxo; Het' is heterocyclylene selected from imidazolinyl and piperidinyl; Q is selected from a group comprising a covalent bond, -C(R₆)-, -C(R₆)-C(R₆)-, -S(O)₂-, -C(R₆)-N(R₈)-W-, -S(O)₂-N(R₈)- and -C(R₆)-O-; V is selected from a group comprising -C(R₆)-, -O-C(R₆)-, -N(R₈)-C(R₆)-, and -S(O)₂-; W is selected from a group comprising a covalent bond, , -C(O)-, and -S(O)₂-; a and b are independently integers from 1 to 6, provided that a+b≤7; provided that Z can also denote a covalent bond when R₃ is -Z-Het, -Z-Het'-R₄, or -Z-Het'-Y-R₄, or R₃ is -Z-Y-R₄ or -Z-Y-X-Y-R₄, and Y is selected from a group comprising -S(O)_0-2-, -C(R₆)-, -C(R₆)-O-, -C(R₆)-N(R₈)- and The invention also relates to a pharmaceutical composition based on the formula II compound, a method of inducing biosynthesis of cytokines, a method of treating a viral disease and an oncological disease using the compound of formula II.

EFFECT: novel derivatives of 1H-imidazo [4,5-c]quinoline, which are useful in treating viral and oncological diseases, are obtained.

37 cl, 130 ex