1351185-75-5Relevant academic research and scientific papers
CYCLIC N,N'-DIARYLTHIOUREAS AND N,N'-DIARYLUREAS - ANDROGEN RECEPTOR ANTAGONISTS, ANTICANCER AGENT, METHOD FOR PREPARATION AND USE THEREOF
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Paragraph 0076, (2013/05/21)
The present invention relates to novel cyclic N,N′-diarylureas and N,N′-diarylthioureas—androgen receptor antagonists, anti-cancer agent, pharmaceutical composition, medicament, and method for treatment of cancerous diseases, among them prostate cancer. Cyclic N,N′-diarylthioureas or N,N′-diarylureas of the general formula 1, their optical (R)- and (S)-isomers and pharmaceutically acceptable salts thereof exhibiting properties of androgen receptor antagonists have been proposed, wherein: X represents oxygen or sulfur; m=0 or 1;R1 represents C1-C3alkyl;R2 and R3 represent hydrogen; orR2 and R3 together with C-atom they are attached to form C═O group; R4 and R5 represent hydrogen; orR4 represents hydrogen, R5 represents methyl; orR4 represents methyl, R5 represents CH2R6 group in which R6 represents C1-C3 alkoxycarbonyl, carboxyl, hydroxyl group optionally substituted with methyl or benzyl; orR4 and R5 together with C-atom they are attached to form 5- or 6-membered heterocycle comprising at least one oxygen atom or nitrogen atom optionally substituted with methyl; orR4 and R5 together with C-atom they are attached to form NH group.
