Phenylsubstituted 4-azasteroid fluoroderivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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A61K 3158

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active

061143456

ABSTRACT:
Compounds of formula (I), wherein: the symbol ---- represents a single or a double bond; R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; R.sub.f and R'.sub.f, each independently, are C.sub.1 -C.sub.4 alkyl groups substituted by one or more fluorine atoms; and R.sub.1 and R.sub.2, each independently, are selected from: a hydrogen atom; a phenyl group; a C.sub.1 -C.sub.4 alkyl group unsubstituted or substituted by one or more fluorine atoms; a halogen atom; a cyano (CN) group; a group OR.sub.4, wherein R.sub.4 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; a group SR.sub.5, wherein R.sub.5 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; and a group COR.sub.6, wherein R.sub.6 is a group OR.sub.4 in which R.sub.4 is as defined above or a C.sub.1 -C.sub.4 alkyl group unsubstituted or substituted by one or more fluorine atoms. They are useful as testosterone 5a-reductase inhibitors.

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Panzeri et al "Novel Aromatase and 5alpha-Reductase Inhibitors," J. Steroid Biochem. Molecular Biol., vol. 49, No. 4-6, pp. 289-294, 1994.
Giudici et al., "ECE 28260, a New 5-alpha-Reductase Inhibitor: In Vitro and In Vivo Effects," J. Steroid Biochem. Molec. Biol., vol. 58, No. 3, pp. 299-305, 1996.
di Salle et al., "PNU 157706, a Novel Dual type 1 and II 5-alpha-reductase inhibitor," J. Steroid Biochem. Miolec., vol. 64, No. 3-4, pp. 179-186, 1998.

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