| abstract |
The present invention provides nonsteroidal compounds or salts or hydrates thereof having the affinity of the androgen receptor having the structure of Formula 1 and the utility for androgen-receptor related treatments:n n n Formula 1n n n n n n n n In which X is S, SO or SO 2 ;n n n R 1 is optionally one or more substituents selected from the group consisting of halogen, CN, (1C-4C) fluoroalkyl, nitro, (1C-4C) alkyl, (1C-4C) alkoxy or (1C-4C) fluoroalkoxy Substituted 5- or 6-membered monocyclic, heterocyclic- or monocyclic, saturated or unsaturated ring structures;n n n R 2 is 2-nitrophenyl, 2-cyanophenyl, 2-hydroxymethyl-phenyl, pyridin-2-yl, pyridin-2-yl-N-oxide, 2-benzamide, 2-benzoic acid methyl ester or 2 -Methoxyphenyl;n n n R 3 is H, halogen or (1C-4C) alkyl;n n n R 4 is H, OH, (1C-4C) alkoxy or halogen;n n n R 5 is H, OH, (1C-4C) alkoxy, NH 2 , CN, halogen, (1C-4C) fluoroalkyl, NO 2 , hydroxy (1C-4C) alkyl, CO 2 H, CO 2 (1C -6C) alkyl; Or R 5 is NHR 6, wherein R 6 is (1C-6C) acyl optionally substituted with one or more halogens, S (0) 2 (1C-4C) alkyl, or (1C-4C) alkyl or one or more halogens Optionally substituted S (0) 2 aryl, or R 5 is C (O) N (R 8 , R 9 ) wherein R 8 and R 9 are each independently H, (3C-6C) cycloalkyl or CH 2 R 10, wherein R 10 is H, (1C-5C) alkyl, (1C-5C) alkenyl, hydroxy (1C-3C) alkyl, (1C-4C) alkylester of carboxyl (1C-4C) alkyl, (1C-3C) alkoxy (1C-3C) alkyl, (mono- or di (1C-4C) alkyl) aminomethyl, (mono- or di (1C-4C) alkyl) aminocarbonyl, or 3-, 4- , A 5- or 6-membered monocyclic, monocyclic or heterocyclic aromatic or non-aromatic ring, or R 8 and R 9 are heterocyclic 5- or 6- optionally substituted with (1C-4C) alkyl with N To form a circular saturated or unsaturated ring. |