| 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 (1) wherein X is S,SO or S02; R<1 >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, (1C-4C)fluoroalkyl, nitro, (1C-4C)alkyl, (1C-4C)alkoxy or (1C-4C)fluoroalkoxy; 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; R<3> is H, halogen or (1C-4C)alkyl; R<4> is H, OH, (1C-4C)alkoxy, or halogen; R<4> is H, OH, (1C-4C)alkoxy, NH2, CN, halogen, (1C-4C)fluoroalkyl, N02, hydroxy(1C-4C)alkyl, C02H, C02(1C-6C)alkyl, or R<5> is NHR<6>, wherein R<6> is (1C-6C)acyl optionally substituted with one or more halogens, S(O)2(1C-4C)alkyl, or S(O)2aryl optionally substituted with (1C-4C)alkyl or one or more halogens, or R<5> is C(O)N(R<8>,R<9>), wherein R<8> and R<9> each independently are H, (3C-6C)cycloalkyl, or CH2R<10>, wherein R<10> is H, (1C-5C)alkyl, (1C-5C)alkenyl, hydroxy(1C-3C)alkyl, (1C-4C)alkylester of carboxy(1C-4C)alkyl, (1C-3C)alkoxy(1C-3C)alkyl, (mono- or di(1C-4C)alkyl)aminomethyl, (mono- or di(1C-4C)alkyl)aminocarbonyl, or a 3-, 4-, 5- or 6-membered monocyclic, homo- or heterocyclic, aromatic or non-aromatic ring, or R<8> and R<9 >form together with the N a heterocyclic 5- or 6-membered saturated or unsaturated ring optionally substituted with (1C-4C)alkyl; or a salt or hydrate form thereof. |
