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NN'- NN'- Cyclic NN'-diarylthioureas and NN'-diarylureas as androgen receptor antagonists anti-cancer agent method for producing and using same
NN'- NN'- Cyclic NN'-diarylthioureas and NN'-diarylureas as androgen receptor antagonists anti-cancer agent method for producing and using same
The present invention relates to novel cyclic N , N'- diarylthiourea and N , N' -diarylurea-androgen receptor antagonists, anticancer agents, pharmaceutical compositions, medicaments, . (R) - or (S) -enantiomer of cyclic N , N'- diarylthiourea and N , N' -diarylurea compounds of Formula 1 having androgen receptor antagonist properties, Acceptable salts are provided: (here: X is oxygen or sulfur; m = 0 or 1; R1 is C 1 -C 3 alkyl; R2 and R3 are hydrogen; or R2 and R3 together with the carbon atoms to which they are attached may form a C = O group; R4 and R5 are hydrogen; or R4 is hydrogen and R5 is methyl; or R 4 is methyl, R 5 is a CH2R 6 group, R 6 is a hydroxy, carboxyl, C 1 -C 3 alkoxycarbonyl group optionally substituted with methyl or benzyl; or R4 and R5 together with the carbon atom to which they are attached form a saturated 5- or 6-membered heterocyclic ring comprising at least one oxygen or nitrogen atom, optionally substituted with methyl, or R4 and R5 together with the carbon atom to which they are attached represent an NH group.
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机译：本发明涉及新颖的环状 N ， N' -二芳基硫脲和 N ， N'< -二芳基脲-雄激素受体拮抗剂，抗癌剂，药物组合物，药物，。环状 N ， N' -二芳基硫脲和 N ，的（R）-或（S）-对映体具有雄激素受体拮抗剂特性的式 1 的I> N'-二芳基脲化合物，提供可接受的盐：（此处： X 是氧或硫; m = 0或1; R1 是C 1 -C 3 烷基; R2 和 R3 是氢;或 R2 和 R3 与它们所连接的碳原子一起可以形成C = O基团; R4 和 R5 是氢;或 R4 是氢和 R5 是甲基;或 R 4 是甲基， R 5 是 CH 2 R 6 基， R 6 是羟基，羧基，C 1 -C 3 烷氧羰基，可选地被甲基或苄基取代;或 R4 和 R5 与它们所连接的碳原子一起形成饱和的5元或6元杂环，该杂环包含至少一个氧或氮原子，可选地被取代甲基或 R4 和 R5 以及与它们相连的碳原子一起代表NH基团。
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