| 摘要 |
F3 180/RJN118 181/RJN119 18222 TITLE OF THE INVENTION NEW NON-STEROIDAL AGENTS AS 5-ALPHA REDUCTASE INHIBITORS Described are new non-steroidal drugs for treatment of benign prostatic hyperplasia and other disorders mediated by high 5-alpha reductase activity, high dihydrotestosterone levels, and other conditions of hyperandrogenic stimulation, of the formula: wherein A is an 1,2-disubstituted aromatic ring selected from (a) benzene, naphthalene; F3 180/RJN118 - ii - 182; 181/RJN119 (b) 5-6 membered heteroaromatic ring, containing 1-2 N atoms, 1 S or O atom, or combination thereof; D and E are independently -COOH, CONH2, CONHRb, COORb, SO2OH, SO2NH2, SO3OH, -SSO2ONa, PH(O)(OH), P(O)(OH)2; X is O, S, SO, or SO2: R is H, C1-C4 alkyl. phenyl or substituted phenyl, halo, haloalkyl, hydroxy, carboxy, cyano, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkylsulfinyl, C1-C4 alkylsulfonyl, nitro, amino, C1-C4 mono or di-alkylamino; R' and R" are independently H, halo, C1-C4 alkyl or C1-C4 alkoxy, amino, or oxo, where CH-R' or CH-R" in the formula become -C=O; Ra is H, C1-C4 alkyl; Rb is C1-C12 alkyl, phenyl, or phenyl C1-C4 alkyl; F3 180/RJN118 - iii - 8222 181/RJN119 y is 1-6; z is 6-20; and wherein and can independently represent substituted or unsubstituted alkyl radicals or alkenyl radicals containing at least one alkene bond; and pharmaceutically acceptable salts and esters thereof.
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