Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1992-09-30
1994-04-19
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
Patent
active
053045629
ABSTRACT:
Compounds of the formula ##STR1## wherein carbon atoms 1 and 2 are linked by a single bond or a double bond, R.sub.1 is hydrogen, methyl or ethyl, and A is a group of the formula --N(--R.sub.2)--X-- wherein R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl and X is C.sub.1 -C.sub.12 alkylene or C.sub.3 -C.sub.6 cycloalkylidene; a group of the formula --N(--R.sub.2)--Y--Phe-- wherein R.sub.2 is as defined above, Y is a direct bond or C.sub.1 -C.sub.6 -alkylene and Phe is an unsubstituted or substituted phenylene radical; a group of the formula --O--X-- wherein X is as defined above, or a group --O--Y--Phe-- wherein Y and Phe are as defined above, are inhibitors of 5.alpha.-reductase and can be used for the therapeutic treatment of the human and animal body.
REFERENCES:
patent: 4377584 (1983-03-01), Rasmusson et al.
patent: 4760071 (1988-07-01), Rasmussen
patent: 5120847 (1992-06-01), King et al.
Rasmusson et al., Azasteroids as Inhibitors of Rat Prostatic 5.alpha.-Reductase, J. Med. Chem. 1984, 1690-1701.
Bhattacharya et al., Silylation-Mediated Oxidation of 4-Aza-3-ketosteroids with DDQ Proceeds via DDQ-Substrate Adducts J. Am. Chem. Soc. 1988.
Rasmusson et al., J. Med. Chem. 1986, 29, 2298-2315, Azasteroids; Structure Activity Relationships for Inhibition of 5.alpha.-Reductase and of Androgen Receptor Binding.
Ciba-Geigy Corporation
Daus Donald G.
Fishman Irving M.
Kaiser Karen G.
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