Cyclic N,N′-diarylthioureas and N,N′-diarylureas-androgen receptor antagonists, anticancer agent, method for preparation and use thereof
The invention relates to novel N,N′-disubstituted 2-thioxo-7-oxa-1,3-diaza-spiro[4.4]nonan-4-one-androgen receptor (AR) antagonists, an anticancer agent, a pharmaceutical composition, a medicament, and a method for treating prostate cancer. 4-[3-(4-Cyano-3-trifluoromethyl-phenyl)-4-oxo-2-thioxo-7-oxa-1,3-diaza-spiro[4.4]non-1-yl]-2-fluoro-benzamide of general formula 1 and enantiomer thereof wherein: R represents C 1 -C 3 alkyl.
1. A 4-[3-(4-Cyano-3-trifluoromethyl-phenyl)-4-oxo-2-thioxo-7-oxa-1,3-diaza-spiro[4.4]non-1-yl]-2-fluoro-benzamide compound of general formula 1
wherein:
R represents C 1 -C 3 alkyl, and enantiomers thereof.
2. The compound of claim 1 , wherein the compound is 4-[(R)-3-(4-Cyano-3-trifluoromethyl-phenyl)-4-oxo-2-thioxo-7-oxa-1,3-diaza-spiro[4.4]non-1-yl]-2-fluoro-N-methyl-benzamide represented by formula (R)-1
3. A pharmaceutical composition comprising at least one 4-[3-(4-Cyano-3-trifluoromethyl-phenyl)-4-oxo-2-thioxo-7-oxa-1,3-diaza-spiro[4.4]non-1-yl]-2-fluoro-benzamide compound of general formula 1 and enantiomers thereof.
4. The pharmaceutical composition according to claim 3 and at least one pharmaceutically acceptable carrier, inert excipient or solvent.
5. The pharmaceutical composition according to claim 4 in the form of a tablet, capsule, or injection.