ANTAGONISTES DU RECEPTEUR ANDROGENE N,N'-DIARYLTHIOUREAS ET N,N'-DIARYLUREAS CYCLIQUES, AGENT ANTICANCER, METHODE DE PREPARATION ET D'UTILISATION ASSOCIEE
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. 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 are proposed, where: X is oxygen or sulphur； m = 0 or 1； R1 is C1-C3 alkyl； 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 CH2R6 group in which R6 is C1-C3 alkoxycarbonyl, 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.
