Oxidization metabolites of 5-.alpha.-23-methyl-4-aza-21-nor-chol

Details Oxidization metabolites of 5-.alpha.-23-methyl-4-aza-21-nor-chol Oxidization metabolites of 5-.alpha.-23-methyl-4-aza-21-nor-chol

1992-09-15

1994-06-28

Daus, Donald G.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

546 77, C07D22102, A61K 3147

Patent

active

053247345

ABSTRACT:
The compounds of formula (I) ##STR1## wherein R is selected from the group hydroxymethyl and carboxy, have been identified as metabolites of 5.alpha.-23-methyl-4-aza-21-nor-chol-1-ene-3,20-dione and are believed to be active as testosterone 5.alpha.-reductase inhibitors and would thus be useful for treatment of acne, seborrhea, female hirsutism or benign prostatic hypertrophy.

REFERENCES:
patent: 2227876 (1940-01-01), 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 (1980-02-01), Rasmusson et al.
patent: 4317817 (1982-03-01), Blohm 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: 4888336 (1989-12-01), Holt et al.
patent: 4910226 (1990-03-01), Holt et al.
patent: 5098908 (1992-03-01), Steinberg et al.
patent: 5120742 (1992-06-01), Rasmusson
patent: 5175155 (1992-12-01), Juniewicz et al.
J. Carlin et al. Drug Metabolism & Disposition, vol. 20, pp. 148-155 (1992).
J. Gilbert et al. Biolog. Mass. Spectromety, vol. 21, pp. 341-346 (1992).
Diani et al, Jour. of Clin & Metab vol. 74 pp. 345-350 (1992).
Stinson, Chem. Eng. News Jun 29, 1992, pp. 7-8.
Helliker, Wall St. Journ. 7 Jun. 1991, pp. A1, A7 (1991).
Gilbert Chem. Abstr. vol. 117 Entry 82802j (1992).
Neri, et al., Endo, vol. 91, No. 2 (1972), pp. 427-437.
Nayfeh et al., Steroids, 14, 269 (1969).
Doorenbos and Solomons, J. Pharm., Sci., 60, 8, (1973), pp. 638-640.
Doorenbos and Brown, J. Pharm. Sci., 60, 8, (1971), pp. 1234-1235.
Doorenbos and Kim, J. Pharm. Sci., 63, 4, (1974) pp. 620-622.
Rosmusson et al., J. Med. Chem., 29 (11) (1986), pp. 2298-2315.
Brooks et al., Prostate, (1) (1986), pp. 65-75.
Brooks et al. Steroids, 47 (1) (1986), pp. 1-19.
Liang et al., Endocr., 117 (2) (1985) pp. 1-19.
Rasmusson et al., J. Med. Chem., 27 (12) (1984) pp. 1690-1701.
Back, J. Org. Chem., vol. 46, No. 7 (1981) pp. 1442-1446.
Liang et al., Chem. Abstracts, vol. 95, 109055j (1981).
Kadahoma et al., JNCI, vol. 74, No. 2 (Feb. 1985) pp. 475-481.
Andriole et al., The Prostate, vol. 10, (1987) pp. 189-197.
Bingham et al. J. Endocr., vol. 57 (1973) pp. 111-121.
Kedderis, Toxicol. Appl. Pharmacol., vol. 103, (1990) pp. 222-227.
Metcalf et al., Bioorganic Chemistry, 17, (1986) pp. 372-376.
Levy et al., Biochemistry, vol. 29 (1990) pp. 2815-2824.
Holt et al., J. Med. Chem. vol. 33 (1990) pp. 943-950.
Levy et al., J. Steroid Biochem., vol. 34, Nos. 1-6 (1989) pp. 571-575.
Holt et al., J. Med. Chem., vol. 33 (1990) pp. 937-942.
Metcalf et al., TIPS, vol. 10 (Dec. 1989) pp. 491-495.
Murphy et al., Steroids, vol. 35, No. 3 (Mar. 1980) 1-7.
Stone et al., Prostate. vol. 9 (1986) pp. 311-318.
Brooks et al., Steroids, vol. 47 No. 1 (1986) pp. 1-19.
Labrie et al., Lancet, No. 8515, No. 1986 pp. 1095-1096.
Rittmaster et al., J. Clin. Endocrin. and Metabl., vol. 55, No. 1 (1987) pp. 188-193.

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