Steroid derivatives for the treatment of prostatic hypertrophy,

Details Steroid derivatives for the treatment of prostatic hypertrophy, Steroid derivatives for the treatment of prostatic hypertrophy,

1995-03-31

1998-06-02

Prior, Kimberly J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

514172, 514174, 514175, 514176, 552610, 540 2, 540107, 540108, 540110, 540111, 540113, 540114, 540115, 540116, 540120, A61K 5800, A61K 5600

Patent

active

057600252

ABSTRACT:
Compounds of formula (I): ##STR1## 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 thereof 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.-dihydrotestosterone.

REFERENCES:
patent: 5032586 (1991-07-01), Metcalf et al.
patent: 5091380 (1992-02-01), Rasmusson et al.
patent: 5137882 (1992-08-01), Holt et al.
patent: 5196411 (1993-03-01), Rasmusson et al.
patent: 5302621 (1994-04-01), Kojima et al.
Chemical and Pharmaceutical Bulletin, vol. 33, No. 5, (1985) pp. 2164-2167, "Allylic Rearrangement of Alpha, Beta-Unsaturated Ketone-Diethyl Phosphorocyanidate Adducts".
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).

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