Method of making steroid derivatives for the treatment of prosta

Details Method of making steroid derivatives for the treatment of prosta Method of making steroid derivatives for the treatment of prosta

1996-03-20

1998-02-10

Prior, Kimberly J.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

540111, 540114, 540115, 540116, 540120, 552610, C07J 4300, C07J 1700, C07J 300

Patent

active

057170886

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: 5302621 (1994-04-01), Kojima et al.
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).
Chemical and Pharmaceutical Bulletin, vol. 33, No. 5, (1985) pp. 2164-2167, "Allylic Rearrangement of Alpha, Beta-Unsaturated Ketone-Diethyl Phosphorocyanidate Adducts".

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