REVERSE-CONFIGURATION MIMETICS AND METHODS RELATING THERETO Russian patent published in 2011 - IPC C07F9/12 C07D487/04 C40B40/04 A61K31/53 A61K31/661 A61P35/00 A61P43/00 

FIELD: chemistry.

SUBSTANCE: invention relates to novel conformationally stable compounds of general formula (I), which imitate the secondary structure of reverse-configuration regions of biologically active peptides and proteins which are reverse-configuration mimetics. The compounds can be used to inhibit or treat disorders modulated by Wnt-signalling pathway, such as cancer, especially colorectal cancer. The invention also relates to a library containing the disclosed compound. In general formula (I), A denotes -(C=O)-, B denotes -(CHR₄)-, D denotes -(C=O)-, E denotes -(ZR₆)-, G denotes -(XR₇)-, Z denotes CH, X denotes a nitrogen atom, W denotes -(C=O)NH-, R₁ denotes benzyl; R₂ denotes a heterocyclylC_1-6alkyl group, including a 9-member condensed bicyclic ring having 2-3 heteroatoms selected from nitrogen, oxygen or sulphur atoms; a substituted hetercyclylC_1-6alkyl group, including a 9-member condensed bicyclic ring having 2-3 heteroatoms selected from nitrogen, oxygen or sulphur atoms, an the ring has 1-3 substitutes independently selected from a group comprising halogen, piperidinyl, morpholinyl, C_2-6alkenyl, phenyl, hydroxyphenyl, C_1-6alkoxycarbonyl, dialkylamino, hydroxypiperidinyl, C_1-6alkyl, hydroxyC_1-6alkylpiperazinyl, amino, piperidinyl carbonyl; heterocyclyl-C_1-6alkyl group having a 9-member condensed bicyclic ring which has one or two nitrogen atoms; and other values given in the claim. R₄ denotes a substituted benzyl, having a substitute selected from disodium phosphate, monosodium phosphate, phosphate; R₆ denotes hydrogen; R₇ denotes: C_1-6alkyl; C_1-6alkynyl; C_2-6alkenyl; substituted benzyl, having one or more substitutes independently selected from halogen and C_1-6alkyl.

EFFECT: high efficiency of the compounds.

8 cl, 34 dwg, 19 tbl, 25 ex