Substituted 4-aza-5.alpha.-androstan-ones as 5.alpha.-reductase

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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514284, 546 78, 544336, 544405, 544182, C07D22102, A61K 31435

Patent

active

056938098

ABSTRACT:
Described are new 16-substituted and 7,16-disubstituted 4-aza-5.alpha.-androstan-3-ones and related compounds as 5.alpha.-reductase inhibitors.

REFERENCES:
patent: 3264301 (1966-08-01), Doorenboos
patent: 3285918 (1966-11-01), Doorenboos et al.
patent: 4220775 (1980-09-01), Rasmusson et al.
patent: 4377584 (1983-03-01), Rasmusson et al.
patent: 4596812 (1986-06-01), Chidsey, III et al.
patent: 4732897 (1988-03-01), Cainelli
patent: 4760071 (1988-07-01), Rasmusson et al.
patent: 4859681 (1989-08-01), Rasmusson et al.
patent: 4882319 (1989-11-01), Holt et al.
patent: 4888336 (1989-12-01), Holt et al.
patent: 5049562 (1991-09-01), Rasmusson et al.
patent: 5110939 (1992-05-01), Holt et al.
patent: 5116983 (1992-05-01), Bhattacharya et al.
patent: 5215894 (1993-06-01), Arison et al.
patent: 5278159 (1994-01-01), Bakshi et al.
patent: 5359071 (1994-10-01), Durette et al.
patent: 5378710 (1995-01-01), Biollaz
patent: 5380728 (1995-01-01), Rasmusson
patent: 5494914 (1996-02-01), Labrie et al.
The Daily (Tuesday, May 7, 1996), "New Data on Proscar, Abbott's Hytrin Show Conflicting Results".
Wall Street Journal (Tuesday, May 7, 1996), "Study Finds Abbott's Prostate Drug is Much More Effective than Merck's", p. B4.
US News & World Report, May 20, 1996, "Zapping a problem prostate".
Stinson, "Prostate Drug Proscar Cleared for Marketing", Chem. Eng. News, Jun. 29, 1992 pp. 7-8.
Helliker, "Alopecia Sufferers Seek to Suffer Less and Not in Silence", Wall Street Journ. 7 Jun. 91, pp. A1 & A7 (1991).
Diani et al., "Hair Growth Effects of Oral Administration of Finasteride, a Steroid 5alpha-reductase Inhibitor, Alone and in Combination with Topical Minoxidil," J. Clin. & Metab. 74:345-50 (1992).
Burger, Medicinal Chemistry, 2nd Ed. Interscience, NY 1960 p. 42.
Back et al., "N-Chloroazasteroids: A Novel Class of Reactive Steroid Analogues. Preparation, Reaction with Thiols and Photochemical Conversion to Electrophilic N-Acyl Imines", J. Org. Chem., 54(8):1904-10 (1989).
Rasmusson et al., "Azasteroids as Inhibitors of Rat Prostatic 5-alpha-reductase" J. Med. Chem. 27(12):1690-1701 (1984).
Doorenbos et al., "Synthesis & Antimicrobial Properties of 17-Beta-Isopentyloxy-4-Aza-5-alpha Androstane and 4-Methyl Derivative", J. Pharm. Sci. 62(4):638-640 (1973).
Doorenbos et al., "4, 17-Alpha-Dimethyl-4-Aza-5 alpha-Androstan-17-beta-ol-Acetate & Related Azasteroids", J. Pharm. Sci. 60(8): 1234-1235 (1971).
Doorenbos et al., "Synthesis & Evaluation of Antimicrobial Properties of Amidinoaza-androstanes and Guanidinoazaandrostanes", J. Pharm. 63(4):620-622 (1974).
Rasmusson et al., "Azasteroids: Structure Activity Relationships for Inhibition of 5-alpha-reductase and of Androgen Receptor Binding", J. Med. Chem. 29(11): 2298-2315 (1986).
Brooks et al., "5-alpha-Reductase Inhibitory and Antiandrogenic Activities of some Azasteroids in the Rat", Steroids 47(1): 1-19 (1986).
Brooks et al., "Prostatic Effects Induced in Dogs by Chronic or Acute Oral Administration of 5-alpha-reductase Inhibitors", Prostate, 9(1): 65-75 (1986).
Geldof et al., "Consideration of the Use of 17Beta-N,N-Diethyl Carbamoyl-4-Methyl-4-aza-5-alpha-Androstan-3-one (4MA), a 5-alpha-Reductase Inhibitor, in Prostate Cancer Therapy", J. Cancer Res. Clin. Oncol. 118:50-55 (1992).
Rittmaster et al., "The Effects of N,N-Diethyl-4-Methyl-3-Oxo-4-Aza-5-alpha-Androstane-17beta-Carboxamide, a 5-alpha-Reductase Inhibitor and Antiandrogen, or the Development of Baldness in the Stumptail Macaque", J. Clin. Endocrin. & Metabolism 55(1): 188-193 (1987).
LaBrie et al., "Combination Therapy in Prostate Cancer", Lancet No. 8515, 1095-1096 (1986).
Metcalf eta l. "Inhibitors of Steroid 5-alpha-reductase in Benign Prostatic Hyperplasia, male Pattern Baldness & Acne" TIPS, 10:491-495 (1989).
Boyle et al., Urology, "Prostate Volume Predicts Outcome of Treatment of Benign Prostatic Hyperplasia with Finasteride: Meta-Analysis of Randomized Clinical Trials", vol. 48, No. 3, Sep. 1996, pp. 398-405.

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