MIMETICS WITH REVERSE CONFIGURATIONS AND METHODS OF THEIR ADMINISTRATION Russian patent published in 2008 - IPC C07D487/04 A61K31/519 A61K31/53 A61P35/00 

FIELD: chemistry; pharmacology.

SUBSTANCE: present invention relates to new compounds with general formula (1), which includes compounds (VI), which relate to conformational stable compounds that imitate the secondary structures of parts of molecules of biologically active peptides and proteins with reverse configurations. The compounds can be used as antitumoral compounds for the treatment and prophylaxis of cancer such as, colorectal cancer, for treating rheumatoid arthritis and ulcerative colitis. The compound facilitates the increase of apoptosis and increases the proliferation of neurites, and inhibits survirin expression in the cell. In compounds, corresponding to the general formula (I) and (VI) , in formula (I) W denotes -Y(C=O)-, -(C=O)NH-, -(SO₂)- or is absent, Y denotes an oxygen atom, Z denotes a nitrogen atom or CH, X denotes a nitrogen atom or CH, n=0 or 1, on the condition that when Z denotes CH, X denotes a nitrogen atom and n=1; and when Z denotes a nitrogen atom, then n=0; in formula (VI) X₁ denotes a hydroxyl, and at least one of X₂ is X₃ is a hydroxyl, or X₁ denotes hydrogen, and X₂ and X₃ can be similar of different and independently selected from hydrogen, hydroxyl and halogen. Other radicals have the value specified in the formula of the invention.

EFFECT: obtaining compounds which can be used as antitumoral compounds for the treatment and prophylaxis of cancer such as, colorectal cancer, for treating rheumatoid arthritis and ulcerative colitis.

26 cl, 33 dwg, 9 tbl, 14 ex