Abstract: A method of preventing and/or treating estrogen-dependent disorders selected from endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, fibrocystic breast disease and fibrocystic mastopathy, is disclosed which is comprised of administering to a female mammal in need of such treatment an effective amount of aromatase inactivator exemestane, alone or in combination with additional therapeutic agents. The present invention also relates to a method for treating infertility in a female mammal in need of the infertility treatment, comprising administering an effective amount of exemestane to the mammal.

Abstract: The present invention concerns the use of aromatase inhibitor exemestane, either alone or in combination with other therapeutic agents in the chemoprevention of estrogen dependent cancer in mammals, including humans, at increased risk of the disease.

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.

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.

Abstract: The present invention provides compounds of formula (D 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; A is a single bond or a straight or branched C.sub.1 -C.sub.6 alkylene chain; B is a straight or branched C.sub.1 -C.sub.12 alkylene group optionally substituted by one or more aryl groups or fluorine atoms; W is a group R.sub.1 or (a) wherein R.sub.1 is a straight or branched C.sub. -C.sub.6 alkyl group unsubstituted or substituted by one or more fluorine atoms, provided that at least a fluorine atom is present in B or W. The compounds of the invention are useful as testosterone 5.alpha.-reductase inhibitors.

Abstract: 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:when (y) is a single bond, R.sup.2 is hydrogen, fluorine methyl, trifluoromethyl;when (y) is a double bond, R.sup.2 is methylene provided that when one of (x) or (y) is a double bond the other is a single bond and at least one of R.sub.1 and R.sub.2 is fluorine or trifluoromethyl or a pharmaceutically acceptable salt thereof. The compounds of formula (I) are useful as aromatase inhibitors.

Abstract: This invention refers to compounds of formula (I) ##STR1## wherein x, y, z represent single or double bonds;R is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.1 is hydrogen or an acyl group;R.sub.2 is hydrogen; C.sub.1 -C.sub.4 alkyl unsubstituted or substituted by phenyl; phenyl unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy; andA is a >C.dbd.O, >CH OH or >CH OR.sub.3 group, in which R.sub.3 is an acyl group provided that one of z and y is a double bond and the other is a single bond.The compounds are useful as aromatase inhibitors.

Abstract: A compound of formula (I): ##STR1## wherein R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group;A is a single bond or a straight or branched C.sub.1 -C.sub.6 alkylene chain;R.sub.1 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group;R.sub.2 is a C.sub.1 -C.sub.6 alkyl group, a C.sub.5 -C.sub.7 cycloalkyl or a C.sub.6 -C.sub.10 cycloalkylalkyl group, aryl or a C.sub.7 -C.sub.10 arylalkyl group, or a C.sub.6 -C.sub.10 heterocyclylalkyl group;R.sub.3 is hydrogen, a C.sub.1 -C.sub.4 alkyl group or an aryl or a C.sub.7 -C.sub.10 arylalkyl group;Z is a C.sub.1 -C.sub.6 alkyl group, an --OR.sub.5 group wherein R.sub.5 is a C.sub.1 -C.sub.6 alkyl group, ##STR2## group wherein each of R.sub.6 and R.sub.7 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, phenyl or R.sub.6 and R.sub.7 taken together with the nitrogen to which they are linked form a pentatomic or hexatomic saturated heteromonocyclic ring; and the symbol represents a single or a double bond, is a testosterone 68 5.alpha.

Abstract: Compounds of formula (I) ##STR1## wherein: the symbol represents a single or a double bond;B is a bond or a straight or branched C.sub.1 -C.sub.6 alkylene chain;R is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or benzyl;R.sub.2 isa) hydrogen, fluorine, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl or C.sub.6 -C.sub.9 cycloalkylalkyl; orb) aryl or C.sub.7 -C.sub.10 arylalkyl;R.sub.3 isa) hydrogen, fluorine or C.sub.1 -C.sub.4 alkyl; orb) aryl or C.sub.7 -C.sub.10 arylalkyl;R.sub.4 is hydrogen, fluorine, or is absent when Y is a double bond;R.sub.5 is hydrogen, fluorine or C.sub.1 -C.sub.6 alkyl; and when Y is a single bond, A is hydrogen, fluorine or ##STR2## wherein each of R.sub.6, R.sub.7 and R.sub.8 independently is hydrogen, fluorine or C.sub.1 -C.sub.6 alkyl; and when Y is a double bond, A is a ##STR3## wherein each of R.sub.6 and R.sub.7 is independently hydrogen, fluorine or C.sub.1 -C.sub.6 alkyl; with the proviso that at least one of the groups R, R.sub.1, R.

Abstract: The present invention concerns steroidic 5.alpha.-reductase inhibitors having the following formula (I) ##STR1## wherein Y is oxygen or sulphur;R is a group;a) --OR.sub.4, wherein R.sub.4 is hydrogen or a C.sub.1 -C.sub.6 alkyl group;b) ##STR2## wherein each of R.sub.5 and R.sub.6, independently, is hydrogen or a C.sub.1 -C.sub.6 alkyl group;c) ##STR3## wherein R.sub.7 is hydrogen or a C.sub.1 -C.sub.6 alkyl group and W is a group:(i) ##STR4## wherein R.sub.8 is a C.sub.1 -C.sub.6 alkyl group, a C.sub.5 -C.sub.6 cycloalky group, a C.sub.6 -C.sub.6 cycloalkylalkyl group, a phenyl group or a benzyl group; or(ii) ##STR5## wherein R.sub.9 is a C.sub.1 -C.sub.6 alkyl group or a C.sub.5 -C.sub.6 cycloalkyl group; or(iii) ##STR6## wherein R.sub.5 and R.sub.6 are as defined above; d) ##STR7## wherein each of R.sub.10 and R.sub.11 is, independently, hydrogen or a C.sub.1 -C.sub.

Abstract: 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.

Abstract: 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.

Abstract: 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;R.sub.1 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.4 is hydrogen or fluorine;R.sub.5 is (a) hydrogen or C.sub.1 -C.sub.6 alkyl; (b) phenyl unsubstituted or substituted by one or two substituents independently chosen from C.sub.1 -C.sub.6 alkyl, halogen and amino; (c) an acyl group; or (d) a hydroxy protecting group; and the pharmaceutically acceptable salts thereof,which are useful in therapy, in particular as anti-cancer agents.

Abstract: The invention relates to cycloalkyl substituted 4-aminophenyl halo derivatives of formula (I) ##STR1## wherein n is an integer of 1 to 5;A is >C.dbd.O or --CH.sub.2 -- and B is, independently, --O--, --NH-- or --CH.sub.2 --; andeither R is halogen and R.sub.1 is unsubstituted C.sub.1 -C.sub.4 alkyl; or R is hydrogen and R.sub.1 is C.sub.1 -C.sub.4 alkyl substituted by 1 to 4 halogen atoms,including the pharmaceutically acceptable salts thereof. The compounds of the invention show aromatase inhibiting activity and can find use, for example, in the treatment of estrogen-dependent tumors and of prostatic hyperplasia.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: The invention relates to new aromatase inhibitor agents having the general formula (I) ##STR1## wherein R.sub.1 is hydrogen or a group=CHR.sub.3 wherein R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl; the symbol indicates the presence of a single or double bond in such a way that, when R.sub.1 is hydrogen, (a) is single bond and (b) is either single or double bond, while, when R.sub.1 is a group.dbd.CHR.sub.3 as defined above, (a) is double bond and (b) is single bond; R.sub.2 is hydrogen or fluorine; and R is(1) a group --OR.sub.4 wherein R.sub.4 is(a) hydrogen;(b) C.sub.1 -C.sub.6 alkyl;(c) a phenyl or benzyl group, each unsubstituted or ring-substituted by one or more substituents chosen from C.sub.1 -C.sub.4 alkyl, halogen, trifluoromethyl, nitro, amino, hydroxy and C.sub.1 -C.sub.4 alkoxy;(d) a group--COR.sub.5 wherein R.sub.5 is(i) a C.sub.1 -C.sub.22 saturated or C.sub.2 -C.sub.22 unsaturated aliphatic hydrocarbon radical;(ii) a C.sub.4 -C.sub.

Abstract: The invention relates to 6-substituted 10.beta.-alkynylestrene derivatives wherein the 6 substituent is amino, azido, halogen or an alkylidene group and to corresponding 6,7-dihalo analogs.The invention provides also a process for the preparation of the above compounds and pharmaceutical compositions containing same.The compounds of the invention are useful aromatase inhibitors and can be used, e.g., in the treatment of hormone-dependent tumors and prostatic hyperplasia.

Abstract: The invention relates to 6-alkylidenandrosta-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.