C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 323/63 (2006.01) A61K 31/195 (2006.01) A61K 31/215 (2006.01) C07C 317/44 (2006.01) C07C 317/50 (2006.01) C07C 323/60 (2006.01) C07C 323/65 (2006.01)
Patent
CA 2074542
179/RJN117 18458 TITLE OF THE INVENTION NEW SULFUR CONTAINING 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 activity, high DHT levels and other conditions of hyperandrogenic stimulation, of the formula: Image 179/RJN117 - ii - 18458 wherein A is an 1,2-disubstituted aromatic ring, preferably a benzene ring; D is OH, NH2, NHRC; ORC; 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; 179/RJN117 - iii - 18458 Ra is H, C1-C4 alkyl; Rb, Rc are independently, C1-C12 alkyl, phenyl, phenyl-C1-C4 alkyl; n i1 0-2; y is 1-6; z is 6-20; and 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.
Tolman Richard L.
Witzel Bruce E.
Merck & Co. Inc.
Swabey Ogilvy Renault
Tolman Richard L.
Witzel Bruce E.
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