FIELD: pharmacology.
SUBSTANCE: invention relates to an oxothioimidazoline derivative of the formula
or to its mesomer, racemate, enantiomer, diastereomer, or a mixture thereof, wherein A is -CR' or N; R' is hydrogen or halogen; Z1 and Z2 each independently represents methyl; R1 and R2 each is independently selected from the group consisting of S or O; R3 is selected from the group consisting of C1-C3-alkyl, heterocyclyl selected from tetrahydrofuran, tetrahydropyran, piperidine, dioxo-tetrahydrothiopyran, azetidine, pyrrolidine, oxetane; C6-aryl and -S(O)mR6; when R3 is selected from heterocyclyl selected from tetrahydrofuran, tetrahydropyran, piperidine, dioxo-tetrahydrothiopyran, azetidine, pyrrolidine, oxetane; or C6-aryl, each of the heterocyclyl and aryl is optionally substituted by one or more groups selected from the group consisting of C1-alkyl, -OR6, -C(O)NR7R8, -S (O)mR6 and -C(O)R6; when R3 is C1-C3alkyl, alkyl is substituted by one or more groups selected from the group consisting of halogen, cyano, amino, C3-cycloalkyl, tetrahydrofuran, -OR6, -C(O)NR7R8, -S(O)mR6 and -C(O)OR6, wherein the cycloalkyl is optionally substituted by one group selected from cyano, amino, -OR6, -C(O)NR7R8 and -C(O)OR6; R4 and R5 are each independently selected from the group consisting of cyano, C1-alkyl, halogen and -CF3; R6 is hydrogen, C1-alkyl or -CF3; R7 and R8 are each independently selected from the group consisting of hydrogen and C1-alkyl, and m is 2. The invention also relates to intermediates, a process for preparation of a compound of formula (I), a pharmaceutical composition based on the compound of formula (I) and its application.
EFFECT: new oxothiohydantoin derivatives, useful for treatment of androgen receptor mediated diseases.
18 cl, 51 ex
