| 摘要 |
This invention provides non-steroidal compounds with affinity for the androgen receptor and utility for androgen-receptor related treatments, having a structure according to the formula (I) wherein X is S, SO or SO2; R1 is a 5- or 6-membered monocyclic, hetero- or homocyclic, saturated or unsaturated ring structure optionally substituted with one or more substituents selected from the group consisting of halogen, CN, C1-4fluoroalkyl, nitro, C1-4alkyl, C1-4alkoxy or C1-4fluoroalkoxy; R2 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; R3 is H, halogen or C1-4alkyl; R4 is H, OH, C1-4alkoxy, or halogen; R4 is H, OH, C1-4alkoxy, NH2, CN, halogen, C1-4fluoroalkyl, NO2, hydroxyC1-4alkyl, CO2H, CO2C1-6alkyl, or R5 is NHR6, wherein R6 is C1-6acyl optionally substituted with one or more halogens, S(O)2C1-4alkyl, or S(O)2aryl optionally substituted with C1-4alkyl or one or more halogens, or R5 is C(O)N(R8,R9), wherein R8 and R9 each independently are H, C3-6cycloalkyl, or CH2R10, wherein R10 is H, C1-5alkyl, C1-5alkenyl, hydroxyC1-3alkyl, C1-4alkylester of carboxyC1-4alkyl, C1-3alkoxyC1-3alkyl, (mono- or diC1-4alkyl-aminomethyl, (mono- or diC1-4alkyl)aminocarbonyl, or a 3-, 4-, 5- or 6-membered monocyclic, homo- or heterocyclic, aromatic or non-aromatic ring, or R8 and R9 form together with the N a heterocyclic 5- or 6-membered saturated or unsaturated ring optionally substituted with C1-4alkyl; or a salt or hydrate form thereof.
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