abstract |
This invention provides non-steroidal compounds with affinity for the androgen receptor and utility for treatments related to the androgen receptor, having a structure according to formula (1) wherein X is S, SO or SO2; R1 is a monocyclic, hetero or homociclic, saturated or unsaturated 5 or 6 membered ring structure optionally substituted with one or more substituents selected from the group consisting of halogen, CN, fluoroalkyl (1C-4C), nitro, alkyl (1C- 4C), alkoxy (1C-4C) or fluororalkoxy (1C-4C); R2 is 2-nitrophenyl, 2-cyanophenyl, 2-hydroxymethyl-phenyl, pyridin-2-yl, pyridin-2-yl-N-oxide, 2-benzamide, methyl ester of 2-benzoic acid or 2-methoxyphenyl; R3 is H, halogen or (1C-4C) alkyl; R4 is H, OH, alkoxy (1C-4C), or halogen; R5 is NHR6, wherein R6 is acyl (1C-6C) optionally substituted with one or more halogens, S (O) 2 (1C-4C) alkyl, or S (O) 2 optionally substituted with (1C-4C) alkyl or one or more halogens, or R5 is C (O) N (R8, R9), where 8 and R9 each independent are H, cycloalkyl (3C-6C), or CH2R10, where R10 is H, alkyl (1C-5C ), (1C-5C) alkenyl, hydroxy (1C-3C) alkyl, (1C-4C) alkyl (1C-4C) alkyl, alkyl (1C-3C) (1C-3C) alkyl, (mono- or dialkyl) (1C-4C)) aminomethyl, (mono- or dialkyl (1C-4C)) aminocarbonyl, or a monocyclic, homo- or heterocyclic, aromatic or non-aromatic, 3, 4, or 6-membered ring, or R8 and R9 form together with N a saturated or unsaturated 5 or 6-membered heterocyclic ring optionally substituted with (1C-4C) alkyl; or a salt or hydrate are formed thereof. |