Abstract: The invention relates to a new process for the preparation of known aromatase inhibitors of the following formula (I) ##STR1## wherein each of R.sub.1 and R.sub.3, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl; andR.sub.4 is hydrogen or fluorine;the process comprising submitting to Mannich reaction a compound of formula (II) ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined above and R is a lower alkyl group, and then dehydrogenating the respective 6-methylene-3-oxo-.DELTA..sup.4 -steroid derivative thus obtained, by methods known per se.

Abstract: The invention relates to a new process for the preparation of know aromatase inhibitors of the following formula (I) ##STR1## wherein each of R.sub.1 R.sub.3, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl; andR.sub.4 is hydrogen or fluorine;the process comprising submitting to Mannich reaction a compound of formula (II) ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are defined above and R is a lower alkyl group, and then dehydrogenating the respective 6-methylene-3-oxo-.DELTA..sup.4 -steroid derivative thus obtained, by methods known per se.

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 a new process for the preparation of known aromatase inhibitors of the following formula ##STR1## wherein each of R.sub.1 and R.sub.3, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl andR.sub.4 is hydrogen or fluorine; the process comprising subjecting to Mannich reaction a compound of formula ##STR2## wherein R.sub.1,R.sub.2,R.sub.3 and R.sub.4 are as defined above, and then oxidizing the respective 6-methylene derivative thus obtained by methods known per se.

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: A process for the preparation of 4-aminoandrostenediones of formula (I) ##STR1## and pharmaceutically acceptable salts thereof, wherein one of R.sub.1 and R.sub.2 is hydrogen and the other is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl, and the symbol indicates that each of (x) and (y), independently, is a single bond or a double bond, comprising reacting a compound of formula (II) ##STR2## wherein E is a halogen atom and R.sub.1, R.sub.2, (x) and (y) each are as defined as above with ammonia.

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.

Abstract: The invention relates to cycloalkyl-substituted 4-pyridyl derivatives of formula (I) ##STR1## wherein R is C.sub.1 -C.sub.4 alkyl;each of R.sub.1 and R.sub.2 is, independently, hydrogen or C.sub.1 -C.sub.4 alkyl;n is an integer of 1 to 5; and either(a) A is >C.dbd.O and B is --O--, --NH-- or --CH.sub.2 --; or(b) A is --CH.sub.2 --and B is --O--, --NH--, --CH.sub.2 -- or >C.dbd.O; or(c) A is --O-- and B is >C.dbd.O or --CH.sub.2 --; or(d) A is --NH-- and B is >C.dbd.O or --CH.sub.2 --,and their pharmaceutically acceptable salts.The compounds of the invention show aromatase inhibiting activity and can be useful, e.g., in treating hormone-dependent tumors and prostatic hyperplasia.

Abstract: The invention relates to 6-substituted androsta-1,4-diene-3,17-dione derivatives wherein the 6 substituent is an azido, amino or substituted amino group.The invention provides also a process for preparing the said 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.

Abstract: The invention relates to cycloalkyl substituted 4-aminophenyl derivatives of formula (I) ##STR1## wherein R is C.sub.1 -C.sub.4 alkyl:n is an integer of 1 to 5; and either(a) A is ##STR2## and B is --O--, --NH-- or --CH.sub.2 --; or (b) A is --CH.sub.2 -- and B is --O--, --NH--, --CH.sub.2 -- or ##STR3## or (c) A is --O-- and B is ##STR4## or --CH.sub.2 --; or (d) A is --NH-- and B is ##STR5## or --CH.sub.2 -- and their pharmaceutically acceptable salts.The scope of the invention includes also a process for preparing the said compounds of formula (I) and pharmaceutical compositions containing same.The compounds of the invention show aromatase inhibiting activity and can be useful, e.g., in treating hormone-dependent tumors and prostatic hypertrophy or hyperplasia.

Abstract: The invention discloses 4-substituted androstendione derivatives of the following formula (I) ##STR1## wherein R is amino or substituted amino or azido,one of R.sub.1 and R.sub.2 is hydrogen and the other is hydrogen, alkyl, alkenyl or alkynyl, and(x) and (y) are each, independently, a single bond or a double bond.The compounds of formula (I) are useful aromatase inhibitors.

Abstract: A process is disclosed for the preparation of compounds of formula I: ##STR1## wherein R is hydrogen, lower alkyl, trichloroethyl, benzyl, p-nitrobenzyl, acetoxymethyl, pivaloyloxymethyl, phthalidyl, or a --CH(CH.sub.3)OCOOEt group;R.sup.1 is --CH.sub.2 OH, --CHO, --CH.sub.2 SH, --CH.sub.2 NH.sub.2, --CH.sub.2 OCOR.sup.2, --COOR.sup.2, --CH.sub.2 NHCOR.sup.2, --CH.sub.2 OR.sup.3, or --CH.sub.2 SR.sup.4 where R.sup.2 is a lower alkyl, aryl or a heterocyclic ring, R.sup.3 is a lower alkyl, benzyl, or trityl, and R.sup.4 is a five- or six-member heterocyclic ring containing one or more heteroatoms,which comprises reacting a 4-acetoxy azetidinone with a .beta.-thioketoester to form a mixture, reacting said mixture with thionyl chloride followed by reaction with a phosphine and a base, ozonolyzing and heating to obtain the compounds of formula I.

Abstract: There is disclosed a process for the manufacture of azetidinones related to nocardicin having the formula ##STR1## wherein R is a saturated or unsaturated alkyl having from 1 to 6 carbon atoms, .alpha.-aminobenzyl, benzyl, free or substituted phenyl, or a free or substituted heterocyclic;R.sub.1 is hydrogen, alkyl having from 1 to 4 carbon atoms, trimethylsilyl, trichloroethyl, benzhydryl or benzyl; andR.sub.2 is a free or substituted phenyl, or a free or substituted heterocyclic, using the same starting compound, but with the possibility of proceeding to the final compound via two somewhat different routes. A number of novel intermediates are also disclosed.

Abstract: Disclosed is a method for the suppression by complex conjugate cancellation of unwanted radar echoes caused both by obstacles stationary with respect to the radar transmitter as well as obstacles having a relative speed with respect to the radar transmitter. Cancellation is achieved by the use of a conventional type cancelling operator with at one input a constant weight equal to 1 and at the other input a weight variable in such a way as to make the frequency response of the cancelling operator equal to zero instant-by-instant for a Doppler frequency equal to the average frequency of the unwanted echoes.