FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to novel compounds, which have formula (1a):
, where R1 represents hydrogen, (C1-C4)alkyl or halogen; R2 represents hydrogen, halogen, amino, (C1-C4)alkyl, heterocyclyl, (C6-C10)aryl-(C1-C4)alkylheterocyclyl, (C3-C6)cycloalkylheterocyclyl, -NR11R12, NHR16; R3 represent hydrogen, NR11R12 or NHR16; R4 and R5 each are independently selected from: hydrogen, halogen, (C1-C4)alkyl; R6 and R8 are each independently selected from: hydrogen, (C1-C4)alkyl or halogen; R7 is hydroxy-(C1-C4)alkyl, formyl, -(CH2)nC(O)OR10 or CONHR16; R10 is hydrogen, (C1-C4)alkyl; R11 and R12 each are independently selected from hydrogen, (C1-C4)alkyl, hydroxy-(C1-C4)alkyl, halogen-(C1-C4)alkyl, amino-(C1-C4)alkyl; or R11 and R12, together with N atom, to which they are bound, form 6- or 7-member heterocycle, optionally having one or more additional heteroatoms N or O; R16 is formyl, (C1-C4)alkyl, halogen-(C1-C4)alkyl, hydroxy-(C1-C4)alkyl, (C1-C4)alkylcarbonyl, halogen-(C1-C4)alkylcarbonyl, hydroxy-(C1-C4)alkylcarbonyl, (C1-C4)alkylcarbonyloxy-(C1-C4)alkylcarbonyl or heterocyclyl-(C1-C4)alkylcarbonyl; n is 0, 1 or 2; where (C1-C4)alkyl is not substituted or is substituted with two similar or different groups, selected from: halogen, hydroxy-group and (C6-C10)aryl; heterocyclyl represents 6- or 7-member saturated monocyclic ring, containing one or two heteroatoms selected from nitrogen and oxygen, and which is not substituted or is substituted with one or two similar or different groups, which are selected from oxogroup, (C1-C4)alkyl, (C3-C6)cycloalkyl, (C6-C10)aryl, hydroxy-(C1-C4)alkyl, (C6-C10)aryl-(C1-C4)alkyl, formyl, (C1-C4)alkylcarbonyl, (C6-C10)aryl-(C1-C4)alkylcarbonyl, (C6-C10)arylcarbonyl, (C3-C6)cycloalkylcarbonyl, -SH, -S-(C1-C4)alkyl and -S(O)2-(C1-C4)alkyl; (C6-C10)aryl is not substituted or is substituted with (C1-C4)alkyl; W represents S(O)m; m equals 0, 1 or 2; and to their pharmaceutically acceptable salts. Invention also relates to compounds of formula (1a'), to methods of obtaining compounds of formula (1a), to methods of obtaining compounds of formula (1a'), to method of obtaining compounds of formula E2, to pharmaceutical compositions, as well as to application of compounds.
EFFECT: obtaining novel biologically active compounds which demonstrate inhibiting effect with respect to activity of tumour necrosis factor-α.
30 cl, 46 ex, 4 tbl
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