CYCLIC THIO-SUBSTITUTED DERIVATIVES OF ACYLAMINO ACID AMIDE AND METHOD OF THEIR SYNTHESIS Russian patent published in 2002 - IPC

FIELD: organic chemistry, chemical technology, medicine. SUBSTANCE: invention relates to cyclic thio-substituted derivatives of acylamino acid amide of the formula (I) where R means (lower) alkyl, cycloalkyl, phenyl, thienyl, pyridyl, mono- or bi-(phenyl, thienyl or pyridyl) (lower) alkyl; R₁ means (lower) alkyl, cycloalkyl, aryl taken among the group including phenyl, biphenyl, thienyl, pyridyl (phenyl, thienyl or pyridyl) (lower) alkyl; R₂ means hydrogen atom, (lower) alkyl, (lower) alkoxy-group, aryl (lower) alkyl, aryl (lower) alkoxy-group being aryl means phenyl; R₃ means hydrogen atom, (lower) alkyl, aryl (lower) alkyl being aryl means phenyl; R₄ means hydrogen atom or acyl; R₅ means acyl, (lower) alkylsulfonyl, aryl (lower) alkyl where aryl means phenyl. Invention describes also method of their synthesis and methods of treatment of diseases and states depending on tumor necrosis alpha- -factor (TNF-alpha) and matrix metalloproteinases, for example, inflammatory diseases, osteoarthritis, rheumatic arthritis and tumors in mammals using indicated compounds. EFFECT: improved method of synthesis, valuable medicinal properties. 9 cl, 3 tbl