Farmitalia Carlo Erba

Farmitalia Carlo Erba S.r.l.

Pharmacia & Upjohn

Societa' Farmaceutici Italia

Consiglio Nazionale Delle Ricerche

Pharmacia Corporation

Farmitalia Carlo Ebra S.r.l.

Enrico Di Salle

Paolo Lombardi

Achille Panzeri

Franco Buzzetti

Marcella Nesi

Franco Faustini

Vittoria Villa

Angelo Crugnola

Natale Barbugian

Luigi Bernardi

Antonio Longo

Aldemio Temperilli

Osvaldo Sapini

Roberto d'Alessio

Patricia Salvati

Carmelo Gandolfi

Roberto Ceserani

Roberto D'Alessio

Enzo Brambilla

Fabrizio Orzi

Daniela Ruggieri

Germano Bosisio

Bianca Patelli

Laura Chiodini

Giovanni B Falconi

Giuliano Nannini

Maristella Colombo

Gianfranco Cainelli

Anna M Caravaggi

Mauro Panunzio

Claudio Praga

Enzo Beacco

Giuseppe Spunta

Giorgio Martelli

Erminia Castegnaro

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.

Phenylsubstituted 4-azasteroid fluoroderivatives

4-azasteroids with side-chain fluoroketones

The present invention relates to a compound of formula (I) ##STR1## wherein (x) and (y) are single or double bonds; A is a ##STR2## R and R.sup.3 are hydrogen or acyl; R.sup.1 is hydrogen or fluorine; and wherein:

Fluorinated 4-aminoandrostadienone derivatives and process for their

This invention refers to compounds of formula (I) ##STR1## wherein x, y, z represent single or double bonds;

Androst-4-eno[4,5-b]pyrrole derivatives

A compound of formula (I): ##STR1## wherein R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group;

17.beta.-substituted 4-aza-5.alpha.-androstan-3-one derivatives

Compounds of formula (I) ##STR1## wherein: the symbol represents a single or a double bond;

Fluorinated 17 .beta.-substituted 4-aza-5 .alpha.-androstan-3-one

The present invention concerns steroidic 5.alpha.-reductase inhibitors having the following formula (I) ##STR1## wherein Y is oxygen or sulphur;

Unsaturated 17.beta.-subsituted 3-carboxy steroids

The present invention concerns steroidic 5.alpha.-reductase inhibitors having the formula: ##STR1## As a result of their 5.alpha.-reductase inhibiting activity, these compounds are useful in the treatment of androgen dependent conditions and diseases.

17.beta.-substituted-4-aza-5.alpha.-androstan-3-one derivatives and

The invention relates to 6-alkylidenadrosta-1,4-diene-3,17-dione derivatives, having the following general formula ##STR1## wherein each of R and R.sub.2, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sub.1 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl, which are useful in therapy, in particular in the treatment of hormone-dependent cancers.

Substituted androsta-1,4-diene-3,17-diones

The invention relates to new 17-hydroxy androsta-1,4-diene-3-one derivatives of the following formula ##STR1## wherein each of R and R.sub.3, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl;

17-Substituted androsta-1,4-dien-3-one derivatives

The invention relates to cycloalkyl substituted 4-aminophenyl halo derivatives of formula (I) ##STR1## wherein n is an integer of 1 to 5;

Cycloalkyl-substituted 4-aminophenyl halo derivatives and process for

The present invention relates to new 6-substituted 1.2.beta.methylenandrost-4-ene-3,17-diones of the following general formula: ##STR1## wherein one of R.sub.1 and R.sub.2 is hydrogen and the other is halogen, amino or azido, or R.sub.1 and R.sub.2, taken together, form a .dbd.CH.sub.2 or .dbd.O group, and, when one of R.sub.1 and R.sub.2 is amino, the pharmaceutically acceptable salts thereof. The compounds of the invention are useful in therapy, in particular as anti-cancer agents.

Androst-4-ene-3,17-diones and process for their preparation

The invention relates to new 6- or 7-methylenandrosta-1,4-diene-3,17-diones of the following formula ##STR1## wherein R is hydrogen or fluorine; R.sub.1 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.2 is hydrogen or halogen; one of R.sub.3 and R.sub.4 is .dbd.CH.sub.2 and the other is hydrogen or C.sub.1 -C.sub.4 alkyl, and when R.sub.3 is .dbd.CH.sub.2, at least one of R and R.sub.4 is other than hydrogen; and the symbol ##STR2## represents a double bond and the symbol ##STR3## represents a single bond when R.sub.3 is .dbd.CH.sub.2 or the symbol ##STR4## represents a single bond and the symbol ##STR5## represents a double bond when R.sub.4 is .dbd.CH.sub.2, which are useful in therapy, in particular as anti-cancer agents.

6- or 7-methylenandrosta-1,4-diene-3,17-dione derivatives and process

The invention relates to 4-substituted 6-alkylidenandrostene-3,17-dione derivatives of the following formula ##STR1## wherein each of R.sub.1, R.sub.2 and R.sub.3 is, independently, hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.4 is hydrogen of fluorine; (x) represents a single or double bond; and R is, especially, a hydroxy or mercapto or amino group or a functional derivative thereof. The compounds of the invention show aromatase inhibitory activity and may be useful, for instance, in the treatment of hormone-dependent tumors and of prostatic hyperplasia.

4-substituted 6-alkylidenandrosteine-3,17-dione derivatives and process

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Milan, Italy

Enrico Di Salle