Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1995-01-19
1996-07-16
Prior, Kimberly J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
514172, 514174, 514175, 514176, 540108, 540109, 540111, 540116, 540120, 552610, C07J 300, C07J 4300, A61K 3158, A61K 3156
Patent
active
055367143
ABSTRACT:
The invention includes compounds of formula (I): ##STR1## in which R.sup.1 is hydrogen, alkyl, aryl-substituted alkyl or aromatic heterocyclic-substituted alkyl; R.sup.2 is aryl-substituted alkyl, aromatic heterocyclic-substituted alkyl or diarylamino; and R.sup.3 is carboxy or a group of formula --CONHSO.sub.2 R.sup.4 wherein R.sup.4 is alkyl; and pharmaceutically acceptable salts and esters of the compounds. The compounds have valuable 5.alpha.-reductase inhibitory activity and can thus be used for the treatment and prophylaxis of, inter alia, prostatic hypertrophy as well as other disorders arising from excess levels of 5.alpha.-dihydro-testosterone.
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D. A. Holt et al, "Inhibition of Steroid-5. aplha.-Reductase by Unsaturated 3-Carboxysteroids", Mar. 1990, p. 943-950, Journal of Medicinal Chemistry, Vol. 33.
Dennis A. Holt et al., "Inhibition of Steroid 5.alpha.-Reductase by Unsaturated 3-Carboxysteroids", J. Med. Chem., 33, pp. 943-950 (1990).
Mark A. Levy et al, "Inhibition of Rat Liver Steroid 5.alpha.-Reductase by 2-Androstene-3-carboxylic Acids: Mechanism of Enzyme-Inhibitor Interaction", Biochemistry, 29, pp. 2815-2824 (1990).
Hamada Takakazu
Horikoshi Hiroyoshi
Ishibashi Koki
Kojima Koichi
Kurata Hitoshi
Prior Kimberly J.
Sankyo Company Limited
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