C - Chemistry – Metallurgy – 07 – J
Patent
C - Chemistry, Metallurgy
07
J
260/3
C07J 73/00 (2006.01) C07J 3/00 (2006.01) C07J 11/00 (2006.01) C07J 17/00 (2006.01) C07J 33/00 (2006.01) C07J 41/00 (2006.01) C07J 43/00 (2006.01)
Patent
CA 1142914
TITLE OF THE INVENTION ABSTRACT OF THE DISCLOSURE 4-Aza-17-substituted-5.alpha.-androstan-3-ones and their A- and D- homo analogs of the formula; Image Image Image (I) (II) (III) where Formula (I) may also have the structure of partial Formulas (II) and/or (III); wherein, A is (1) - CH2 - CH2 -; (2) - CH = CH -; (3) Image (4) Image B is (1) Image where R1 is, (a) hydrogen; (b) methyl or ethyl; (c) ethenyl; (d) ethynyl; (e) NR2R3 where R2 and R3 are hydrogen or methyl; (f) cyano; or (2) Image where x? is any anion and R4 is, (a) OR5 where R5 is C1-4 alkyl; or (b) NR6R7, where R6 and R7 are hydrogen or methyl; R' is hydrogen or methyl; R'' is hydrogen or .beta.-methyl; R''' is .beta.-methyl or hydroxy; Z is (1) oxo; (2) .beta.-hydrogen and .alpha.-hydroxy; or .alpha.-hydrogen or c- hydroxyl and (3) (Y)n Q where n = 0 or 1, Y is a straight or branched hydrocarbon chain of 1 to 12 carbon atoms and Q is (a) Image , where R8 is, (i) hydrogen, (ii) hydroxyl, (iii) C1-4 alkyl (iv) NR9R10, where R9 and R10 are each independently selected from hydrogen, C1-4 straight or branched chain alkyl, C3-6 cycloalkyl, phenyl; or R9 and R10 taken together with the nitrogen to which they are attached represent a 5-6 membered saturated ring comprising up to one other heter- atom selected from oxygen and nitrogen. (v) OR11, where R11 is M, where M is hydro- gen or alkali metal, or C1-18 straight or branched chain alkyl; benzyl; or (b) OR12, where R12 is, (i) C1-20 alkylcarbonyl, (ii) phenyl C1-6 alkylcarbonyl, (iii) C5-10 cycloalkylcarbonyl, (iv) benzoyl, or (v) C1-8 alkoxycarbonyl; (4) Image , where the dashed bond replaces the 17.alpha. hydrogen; (5) Image , where R13 is, (a) C1-12 alkyl; or (b) NR9R10; (6) cyano; or (7) tetrazolyl; and pharmaceutically acceptable salts of the above compounds; active as testosterone 5.alpha.-reductase inhibitors, and thus useful topically for treatment of acne, sebor- rhea, female hirsutism and male pattern baldness, and systemically in treatment of benign prostatic hypertrophy, breast carcinoma, and prostate carcinoma.
325640
Arth Glen E.
Jobson Ronald B.
Johnston David B.r.
Rasmusson Gary H.
Reinhold Donald F.
Goudreau Gage & Associates
Merck & Co. Inc.
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