Catechol type non-steroidal drugs as 5-alpha reductase...

C - Chemistry – Metallurgy – 07 – C

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C07C 59/68 (2006.01) A61K 31/19 (2006.01) A61K 31/215 (2006.01) C07C 229/64 (2006.01) C07C 317/22 (2006.01) C07C 317/44 (2006.01) C07C 317/46 (2006.01) C07C 323/52 (2006.01) C07C 323/62 (2006.01) C07C 323/65 (2006.01)

Patent

CA 2074537

178/RJN116 18459 TITLE OF THE INVENTION NEW CATECHOL TYPE NON-STEROIDAL DRUGS AS 5-ALPHA REDUCTASE INHIBITORS ABSTRACT OF THE DISCLOSURE Described are new non-steroidal drugs for treatment of benign prostatic hyperplasia and other disorders mediated by high 5-alpha reductase acti- vity, or high dihydrotestosterone levels, and other conditions of hyperandrogenic stimulation, of the formula: Image wherein A is an 1,2-disubstituted aromatic ring; 178/RJN116 - ii - 18459 wherein X is independently 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; y is 1-6; z is 6-20; and 66/RJN116 - iii - 18459 wherein Image and Image 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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