17.beta.-acyl-3-carboxy-androsta-3,5-dienes as testosterone 5.al

Details 17.beta.-acyl-3-carboxy-androsta-3,5-dienes as testosterone 5.al 17.beta.-acyl-3-carboxy-androsta-3,5-dienes as testosterone 5.al

1991-08-16

1993-03-23

Mars, Howard T.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

552610, C07J 300, A61K 3156

Patent

active

051964112

ABSTRACT:
17.beta.-acyl-3-carboxy-androsta-3,5-dienes as testosterone 5.alpha.-reductase inhibitors of the formula: ##STR1## wherein R is C.sub.3 -C.sub.8 cycloalkyl, which can be substituted with C.sub.1 -C.sub.4 alkoxy or C.sub.6 -C.sub.12 aryl, which can be substituted with one or more of: --OH, --OC.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkyl, --(CH.sub.2).sub.m OH, --(CH.sub.2).sub.n COOH, including protected --OH, where m is 1-4, n is 1-3, and pharmaceutically acceptable salts or esters thereof. Also described is a pharmaceutical formulation. The above compounds are active as testosterone 5.alpha.-reductase inhibitors and thus are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.

REFERENCES:
patent: 4845104 (1989-07-01), Carlin et al.
patent: 4910226 (1990-03-01), Holt et al.
Cacchi, et al. "Palladium-Catalyzed Carbonylation of Enol Triflates. A Novel Method for One-Carbon Homologation of Ketones to .alpha.,.beta.-Unsaturated Carboxylic Acid Derivatives" Tetrahedron Letters, vol. 26, No. 8, pp. 1109-1112 (1985).
J. Pharm. Sci., 60, 8, pp. 1234-1235 (1971), by Doorenbos & Brown.
J. Med. Chem. (1984) 27 (12) pp. 1690-1701, by Rasmusson, et al.

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