CYCLIC N,N'-DIARYLTHIOUREAS AND N,N'-DIARYLUREAS AS ANDROGEN RECEPTOR ANTAGONISTS, ANTI-CANCER AGENT, METHOD FOR PRODUCING AND USING SAME

摘要

The invention relates to novel cyclic N,N'-diarylureas and N,N'-diarylthioureas as androgen receptor antagonists, an anti-cancer agent, a pharmaceutical composition, a drug and a method for treating cancerous diseases, including prostate cancer. Proposed are cyclic N,N'-diarylthioureas or N,N'-diarylureas of general formula 1, the optical (R)- and (S)-isomers thereof and pharmaceutically acceptable salts thereof, having androgen receptor antagonist properties,where X is oxygen or sulphur; m=0 or 1; R1 is C-Calkyl; R2 and R3 are hydrogen; or R2 and R3 together with the carbon atom to which they are bonded form a C=O group; R4 and R5 are hydrogen; or R4 is hydrogen and R5 is methyl; or R4 is methyl and R5 is a CHR6 group in which R6 is C-Calkoxycarbonyl, carboxyl, an optionally substituted hydroxyl group in which the substituents can be hydrogen, methyl, benzyl; or R4 and R5 together with the carbon atom to which they are bonded form a five or six-membered saturated heterocycle that includes at least one atom of oxygen or nitrogen which can be substituted with methyl, or R4 and R5 together with the carbon atom to which they are bonded are an NH group.