Substituted 2-thioxo-imidazolidin-4-one and spiro analogs thereof, anticancer active ingredients, pharmaceutical compositions, pharmaceutical formulations, and methods of treating prostate cancer

摘要

The invention relates to novel ( R )-stereoisomers of substituted 2-thioxo-imidazolidin-4-ones of formula 1 , or spiro analogues thereof, which exhibit androgen receptor antagonist properties, variants of a method for producing the same, and intermediate compounds for producing compounds of formula 1 . Compounds of formula 1 can be used to produce a medicinal agent suitable for treating cancers, such as prostate cancer and breast cancer. The invention also relates to a pharmaceutical composition in the form of tablets, capsules, injections. In formula 1 wherein R1 is OH, NH 2 , or an OR4 group; R2 and R3 are methyl, or R2 and R3 are a CH 2 -CH 2 group; R4 is C 1 -C 4 alkyl or cyclopropyl.