Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Patent
1991-05-09
1992-08-11
Rivers, Diana
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
514859, C07J 7300, A61K 3158
Patent
active
051380633
ABSTRACT:
17.beta.-Acyl-4-aza-5.alpha.-androst-1-in-3-ones of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl R.sup.2 is methoxy, a monovalent radical selected from straight and branched chain alkyl of from 1-12 carbons, or monocyclic aryl optionally containing 1 or more lower alkyl substituents of from 1-2 carbon atoms and/or 1 or more halo (Cl or Br) substituents, aralkyl selected from benzyl and phenethyl and heterocyclic selected from 2- or 4-pyridyl, 2-pyrrolyl, 2-furyl or thiophenyl; and R', R" and R'" are each selected from hydrogen and methyl and pharmaceutical formulations of the above compounds are active as testosterone 5.alpha.-reductase inhibitors and thus are useful for treatment of acne, seborrhea, female hirsutism, and benign prostatic hypertrophy.
REFERENCES:
patent: 2227876 (1941-01-01), Bolt
patent: 3239417 (1966-03-01), DiTullio et al.
patent: 3264301 (1966-08-01), Doorenbos et al.
patent: 3285918 (1966-11-01), Doorenbos et al.
patent: 4220775 (1980-09-01), Rasmusson et al.
patent: 4317817 (1982-03-01), Blohn et al.
patent: 4377584 (1983-03-01), Rasmusson et al.
patent: 4732897 (1988-03-01), Cainelli et al.
patent: 4760071 (1988-07-01), Rasmusson et al.
patent: 4845104 (1989-07-01), Carlin et al.
patent: 4859681 (1989-08-01), Rasmusson et al.
patent: 4882319 (1989-11-01), Holt et al.
patent: 4910226 (1990-03-01), Holt et al.
Brooks, et al., Prostate (N.Y.), vol. 9, No. 1, pp. 65-75 (1986).
J. Med. Chem. 29: 2298-2315 (1986), Rasmusson, et al.
Endo., vol. 91, No. 2 (1972) by Neri, et al., pp. 427-437.
Steroids, 14, 269 (1969), by Nayfeh, et al.
J. Pharm. Sci., 62, 4, pp. 638-640 (1973) by Doorenbos & Solomons.
J. Pharm. Sci., 60, pp. 1234-1235 (1971), by Doorenbos & Brown.
J. Pharm., 63, 4, pp. 620-622 (1974) by Doorenbos & Kim.
J. Med. Chem. (1986) 29 (11): pp. 2298-3115 by Rasmusson, et al.
Prostate (1986) 9 (1): pp. 65-75 by Brooks, et al.
Steroids (1986) 47 (1): pp. 1-19 by Brooks, et al.
Endocr. (1985) 117 (2): pp. 571-579, by Liang, et al.
J. Med. Chem. (1984) 27 (12): pp. 1690-1701, by Rasmusson, et al.
J. Org. Chem. (1981) vol. 46, No. 7, pp. 1442-1446, by Back.
Chem. Abstracts, vol. 95, 109055j, by T. Liang, et al.
JNCI, vol. 74, No. 2, pp. 475-481 (Feb. 1985), Kadahoma, et al.
The Prostate, vol. 10, pp. 189-197 (1987) by G. L. Andriole, et al.
J. Endocr., vol. 57, pp. 111-121 (1973), by K. D. Bingham, et al.
Toxicol. Appl. Pharmacol., vol. 103, pp. 222-227 (1990), by G. L. Kedderis, et al.
Bioinorganic Chemistry, 17, pp. 372-376 (1986) by B. W. Metcalf, et al.
Biochemistry, 1990, vol. 29, pp. 2815-2824, by M. A. Levy, et al.
J. Med. Chem., 1990, vol. 33, pp. 943-950, D. A. Holt, et al.
J. Steroid Biochem., vol. 34, Nos. 1-6, pp. 571-575 (1989), by M. A. Levy, et al.
J. Med. Chem., vol. 33, pp. 937-942 (1990) by D. A. Holt, et al.
TIPS, Dec. 1989, vol. 10, pp. 491-495, by D. W. Metcalf, et al.
Prostate, vol. 9, pp. 311-318 (1986) by N. Stone, et al.
Steroids, vol. 47, No. 1, pp. 1-19 (1986) by J. R. Brooks, et al.
Lancet, No. 1986, No. 8515, pp. 1095-1096, Labrie, et al.
J. Clin. Endocrin. and Metab., vol. 55, No. 1, pp. 188-193 (1987) by Rittmaster, et al.
Steroids, 1991, vol. 56, Aug. pp. 428-433.
Rasmusson Gary H.
Reynolds Glenn F.
Caruso Charles M.
Merck & Co. , Inc.
North Robert J.
Rivers Diana
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