Abstract: The pharmaceutical preparations for treating side effects, such as hot flashes, prostate enlargement and gynecomastia, during and/or after treatment with analogs or antagonists of gonadotropin-releasing hormone (GnRHa therapy) contain an effective amount of a chemically modified derivative of 17&agr;-estradiol, a chemically modified derivative of 17&bgr;-estradiol and/or a chemical modified derivative of estriol. Pharmaceutical preparations containing 14&agr;, 15&agr;-methylene-1,3,5(10),8-tetraene-3,17&agr;-diol are particularly preferred.

Abstract: There is provided a compound of Formula I 1

Abstract: A method of inhibiting steroid sulphatase activity in a subject in need of same is described. The method comprises administering to said subject a steroid sulphatase inhibiting amount of a ring system compound; which ring system compound comprises a ring to which is attached sulphamate group of the formula wherein each of R1 and R2 is independently selected from H, alkyl, alkenyl, cycloalkyl and aryl, or together represent alkylene optionally containing one or more hetero atoms or groups in the alkylene chain; and wherein said compound is an inhibitor of an enzyme having steroid sulphatase activity (E.C.3.1.6.2); and if the sulphamate group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (E.C.3.1.6.2) at a pH 7.4 and 37° C. it would provide a Km value of less than 50 &mgr;M.

Abstract: This invention describes a safe method for the production of sulfamoyl chloride from chlorosulfonyl isocyanate and formic acid in the presence of a amide catalyst, taming the hazardous nature of this reaction by circumventing heat accumulation processes, as well as the sulfamoylation of alcohols and phenols with the resulting sulfamoyl chloride in N,N-dimethyl acetamide or N-methyl pyrrolidone thereby avoiding the formation of side-products which were inevitable with the methods of the prior art using dimethyl formamide or dichloromethane as a solvent. The current invention allows industrial scale applications and describes as an example the process of manufacture of the biologically active compound 17&bgr;-Hydroxyestra-1,3,5(10)-triene-3-yl sulfamate.

Abstract: Novel compounds having a formula selected from the group consisting of wherein the substituents are defined as in the specification which are intermediates for the production of vinyl compounds having a remarkable anti-estrogenic and anti-proliferative activity.

Abstract: This invention provides 3&bgr;-hydroxy-5,7,9-estratriene-17-one and a pharmaceutically acceptable salt of its 3-sulfate ester, which is useful as an estrogen.

Abstract: This invention describes the new 11&bgr;-halogen-7&agr;-substituted estratrienes of general formula I 1

Abstract: Compounds of the formula Where the substituents are defined in the application.

Abstract: Compounds of the formula 1

Abstract: A compound selected from the group consisting of the compounds of the formula wherein the substituents are defined as in the specification and their addition salts with non-toxic, pharmaceutically acceptable acids and bases having estrogenic activity at the bone level but little or no endometrial hyperplasia activity nor any activity for proliferation of mammary tumors.

Abstract: A subject of the invention is the compounds of formula (I): in which X is a halogen atom, D represents the remainder of an optionally substituted pentagonal or hexagonal ring and optionally carrying an unsaturation, R1, R2, R3, R4, Y and n are as defined in the description, their preparation process and intermediates, their use as medicaments and the compositions containing them.

Abstract: This invention provides a pharmaceutically acceptable salt of 3&bgr;-hydroxy-5(10)-estrene-17-one 3-sulfate ester and a pharmaceutically acceptable salt of 3&agr;-hydroxy-5(10)-estrene-17-one 3-sulfate ester, which are useful as an estrogens.

Abstract: Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering derivatives of 2-methoxyestradiol of the general formula: 1

Abstract: A method of inhibiting steroid sulphatase activity in a subject in need of same is described.

Abstract: New non-estrogenic derivative compounds of estradiol, which have no estrogenic activity and comparatively high anti-oxidative activity, are disclosed. These new non-estrogenic derivative compounds are potentially useful as non-estrogenic antioxidants, especially for administration in post-menopausal women and in men. The compounds of the invention can also inhibit aromatase and sulfatase.

Abstract: A subject of the invention is the compounds of formula (I): in which X is a halogen atom, D represents the remainder of an optionally substituted pentagonal or hexagonal ring and optionally carrying an unsaturation, R1, R2, R3, R4, Y and n are as defined in the description, their preparation process and intermediates, their use as medicaments and the compositions containing them.

Abstract: New non-estrogenic derivative compounds of estradiol, which have no estrogenic activity and comparatively high anti-oxidative activity, are disclosed. These new non-estrogenic derivative compounds are potentially useful as non-estrogenic antioxidants, especially for administration in post-menopausal women and in men. The compounds of the invention can also inhibit aromatase and sulfatase.

Abstract: A subject of the invention is the compounds of formula (I): 1

Abstract: A novel class of gonane type and D-homo-gonane type steroids having sulfatase-inhibiting and/or estrogenic activity is presented for application in the pharmaceutical industry. The number and location of sulfamoyloxy groups on the steroids provides for sulfatase inhibiting and estrogenic activities that independently vary over a wide range, allowing the customization of the pharmaceutical for specific purposes, including treatment and diagnosis of estrogen-dependent tumors.

Abstract: A subject of the invention is the compounds of formula (I): 1

Abstract: This invention describes new, substituted 7&agr;-(&egr;-aminoalkyl)-estratrienes of general formula I in which side chain SK is a radical of partial formula The new compounds represent compounds with very strong antiestrogenic action. The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.

Abstract: A subject of the invention is the compounds of formula (I): in which X is a halogen atom, D represents the remainder of an optionally substituted pentagonal or hexagonal ring and optionally carrying an unsaturation, R1, R2, R3, R4, Y and n are as defined in the description, their preparation process and intermediates, their use as medicaments and the compositions containing them.

Abstract: A method and kit for measurement of a steroid by means of a competitive immunoassay, preferably a competitive enzyme immunoassay. The method and kit involve the use of a steroid analogue conjugated to a label. The steroids that are amenable to detection by the method and kit of the present invention include estradiol and progesterone. The method comprises the steps of: a. incubating a mixture of a test sample suspected of containing a given steroid, a solid phase coupled to an antibody specific for that steroid, and a conjugate of an analogue of that steroid to form steroid/antibody complexes and conjugate/antibody complexes on said solid phase; b. separating said solid phase from said mixture; c. measuring the amount of label present in said mixture or in said solid phase; and d. determining the amount of steroid in said sample from the amount of label. The kit comprises a solid phase coupled to an antibody specific for a steroid and a conjugate of an analogue of that steroid.

Abstract: This invention presents alkali metal salts of 8,9-dehydroestrone, salts of its sulfate ester, and stable compositions thereof, as well as processes for their production and use in estrogen replacement therapy and cardiovascular protection.

Abstract: This invention is relating to new estra-1,3,5(10)-trien-sulfamates carrying at the 3-position an R--SO.sub.2 --O--group, with R being an R.sup.1 R.sup.2 N--group in which R.sup.1 and R.sup.2, independently of each other, represent a hydrogen atom, an alkyl residue with 1-5 C atoms or, together with the N atom, a polymethylene-imino residue with 4-6 C atoms or a morpholino residue.The compounds, according to this invention, are suitable for hormonal contraception and climacteric hormone replacement therapy (HRT) as well as for treatment of gynecological and andrological diseases. Hence, only low hepatic estrogenicity is exhibited by the compounds according to this invention.Also described are processes for preparation of the compounds according to this invention and for preparation of pharmaceutical compositions.

Abstract: Novel compounds useful as inhibitors of estrone sulfatase are provided. The compounds have the structural formula (I) wherein r1 is an optional double bond, R.sup.1 and R.sup.2 are selected from the group consisting of hydrogen and lower alky, or together form a cyclic substituent (II) ##STR1## wherein Q is NH, O or CH.sub.2, and the other various substituents are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat estrogen-dependent disorders are provided as well.

Abstract: The invention relates to a method for the preparation of a mixture of sulfated estrogens containing delta(8,9)-dehydro estrone [delta(8,9)DHE] or derivatives thereof.

Abstract: This invention describes new, substituted 7.alpha.-(.xi.-aminoalkyl)-estratrienes of general formula I ##STR1## in which side chain SK is a radical of partial formula ##STR2## as well as their physiologically compatible addition salts with organic and inorganic acids.The new compounds represent compounds with very strong antiestrogenic action.The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.

Abstract: Novel substituted steroid compounds are disclosed which are more effective than known radical-trapping agents in methods of prophylaxis and therapy of radical-mediated cell damage and of treatment of diseases due to radical-mediated cell damage. The novel substituted steroid compounds can be made from steroids having an estrane, androstane, pregnane or cholestane basic skeleton and have a radical-attracting aromatic substituent of the general formula --(CH.sub.2).sub.n X, or .dbd.CH--(CH.sub.2).sub.m X at the 17 or 6 position of the steroid nucleus, wherein X=Y, OY, SY, SeY or NHY; n=0 to 5; m=n-1 and Y is a phenyl group having five substituents A, B, C, D and E, wherein A to E is independently H, alkyl, Oalkyl, Oacyl, OH, or one of the substituents B, C or D is NR.sub.2 wherein R=alkyl and each of the other substituents is hydrogen. Pharmaceutical compositions containing the novel substituted steroid compounds and methods of making them are also part of the invention.

Abstract: Disclosed are estrane derivatives having a radical-attracting aromatic substituent of the general formula --(CH.sub.2).sub.n X attached to the 17-position of the steroid nucleus, wherein X and n are as defined by the specification. The compounds are useful as antitumor agents and in the treatment of cardiac and circulatory disorders.

Abstract: The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.

Abstract: This invention describes new, substituted 7.alpha.-(.xi.-aminoalkyl)-estratrienes of general formula I ##STR1## in which side chain SK is a radical of partial formula ##STR2## as well as their physiologically compatible addition salts with organic and inorganic acids.The new compounds represent compounds with very strong antiestrogenic action.The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.

Abstract: A 19-nor-steroid having a formula selected from the group consisting of ##STR1## wherein the A and B rings have a structure selected from the group consisting of ##STR2##

Abstract: The invention relates to new sulfamate derivatives of 1,3,5(10)-estratriene derivatives of the general formula I ##STR1## wherein the 3-sulfamate moiety is acylated, sulfonated or amidosulfonated. Furthermore, methods for the production of the compound and pharmaceutical preparations containing this compound are described. The compounds according to the invention have an estrogenic effect.

Abstract: Intermediate compounds of a formula selected from the group consisting of ##STR1## which are useful intermediates for the preparation of final products of the formula ##STR2## wherein the substituents are defined in the specification.

Abstract: Conjugates of the formula ##STR1## are prepared by reacting an estradiol derivative with a compound of the formula: ##STR2## in the presence of thionyl chloride or a metal hydride at -30.degree. to 150.degree. C. for 3 minutes to 48 hours and then recovering and purifying the product.

Abstract: Steroid sulphatase inhibitors and pharmaceutical compositions containing them for use in the treatment of oestrone dependent tumors, especially breast cancer. The steroid sulphatase are sulphamate esters of formula (I) ##STR1## where R.sub.1 and R.sub.2 are each H, alkyl, alkenyl, cycloalkyl or aryl, or together represent an alkylene group optionally containing a heteroatom e.g. --O-- or --NH--; and --O-- polycycle represents the residue of a polycyclic alcohol such as a sterol, preferably a 3-sterol.

Abstract: Steroid sulphatase inhibitors and pharmaceutical compositions containing them for use in the treatment of oestrone dependent tumors, especially breast cancer. The steroid sulphatase inhibitors are sulphonate and phosphonate esters of formula (I) ##STR1## where R is alkyl, alkenyl, cycloalkyl or aryl; X is P or S; Y is OH when X is P, and O when X is S; and --O--polycycle represents the residue of a polycyclic alcohol such as a sterol, preferably a 3--sterol.

Abstract: Estradiol derivatives of the formula: ##STR1## wherein R.sup.1 is C.sub.1-4 alky or C.sub.1-4 alkoxy; R.sup.2 is acyl or benzyl; m is an integer of 1 to 3; n is an integer of 1 to 3; and X is hydroxy or halogen are useful as tumor growth inhibiting agents.

Abstract: The invention presents 17.beta.-nitro and 11.beta., 17.beta.-dinitro esters of estradiol which are made from 3-acyloxy-17-keto- or 3,17-dihydroxy-1,3,5-estratrienes by processes known in the art. The compounds exhibit estrogenic activity.

Abstract: This invention provides a method of lowering cholesterol and blood lipid levels, preventing hypercholesterolemia, hyperlipidemia, cardiovascular disease, atherosclerosis, and peripheral vascular disease comprising administering an effective amount of 17.alpha.-dihydroequilenin or a mammalian metabolic conjugate thereof to a mammal in need thereof.

Abstract: The invention relates to 11 .beta.-substituted 14,17-ethanoestratrienes of the general formula 1 ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are defined in the specification. The compound have antiestrogenic activity and are, therefore, useful for the treatment of estrogen dependent disorders.

Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein the substituents are defined as in the specification having anti-estrogen activity.

Abstract: Disclosed is a method of inhibiting the growth of tumors by administering an estradiol derivative-alkylating agent conjugate of the formula (I'): ##STR1## wherein R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy; R.sup.2 is acyl or benzyl; m is an integer of 1 to 3; and n is an integer of 0 to 3. Also disclosed is a method of inhibiting the growth of tumors by administering a compound of the formula (II); ##STR2## wherein R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy; R.sup.2 is acyl or benzyl; m is an integer of 1 to 3; n is an integer of 0 to 3; and X is hydroxy or halogen.

Abstract: Disclosed is a method for treating prostatic hypertrophy with an estradiol derivative-alkylating agent conjugate of the formula (1'): ##STR1## wherein R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy; R.sup.2 is acyl or benzyl; m is an integer of 1 to 3; and n is an integer of 0 to 3. Also disclosed is the treatment of prostatic hypertrophy with an estradiol derivative of the formula (II): ##STR2## wherein R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy; R.sup.2 is acyl or benzyl; m is an integer of 1 to 3; and n is an integer of 0 to 3; and X is hydroxy or halogen.

Abstract: Disclosed is an estradiol derivative-alkylating agent conjugate of the formula (I'): ##STR1## wherein R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy; R.sup.2 is acyl or benzyl; m is an integer of 1 to 3; and n is an integer of 0 to 3, which is useful a growth inhibiting agent.

Abstract: An estradiol derivative-chlorambucil conjugate of the formula (I): ##STR1## wherein R.sup.1 is alkyl or alkoxyl of 1 to 4 carbon atoms; R.sup.2 is acyl, dansyl, or alkyl; R.sup.3, R.sup.4, and R.sup.5 independently are H, oxo, OH, or acyloxy; m is an integer of 1 to 3; and n is an integer of 0 to 3; provided that when n is 0, all of R.sup.3, R.sup.4, and R.sup.5 are not H at the same time, and at least one of R.sup.3, R.sup.4, and R.sup.5 is a group other than H and OH; and further, when n is 2 or 3, the groups R.sup.1 are the same or different; a process for preparing the same, and a pharmaceutical composition containing the conjugate are described.

Abstract: This invention presents alkali metal salts of 8,9-dehydroestrone, its sulfate ester, and stable compositions thereof, as well as processes for their production. The sulfate ester salts are useful in estrogen replacement therapy.

Abstract: This invention presents alkali metal salts of 8,9-dehydroestrone, its sulfate ester, and stable compositions thereof, as well as processes for their production. The sulfate ester salts are useful in estrogen replacement therapy.

Abstract: Novel compounds for the inhibition of sex steroid activity for the treatment of both androgen-related and estrogen-related diseases include for example 15- and 16-halo substituted compounds such as: ##STR1## The compounds are characterized by an estrogenic nucleus substituted with a substituent of the formula --R.sup.1 [B--R.sup.2 --].sub.x L--G whereinat least one of L and G is a polar moiety distanced from a ring carbon of the estrogenic nucleus by a least three intervening atoms:x is an integer from 0-6;R.sup.1 and R.sup.2 are independently either absent or selected from the group consisting of straight- or branched-chain alkylene, straight- or branched-chain alkynylene, straight- or branched-chain alkenylene, phenylene, and fluoro-substituted analogs of the foregoing; andB is either absent or selected from the group consisting of --O--, --Se--, --SO--, --SO.sub.2 --, --NR.sup.3 --, --SiR.sup.3.sub.2, --CR.sup.3 OR.sup.3 --, NR.sup.3 CO--, NR.sup.3 CS--, --CONR.sup.3 --, CSNR.sup.