Abstract: The present invention relates to novel uses of C-19 steroid compounds, in particular C-19 steroids having an androsten-17-(OR4)-3-one structure for prophylactic and/or therapeutic uses, wherein R4 is hydrogen or an unsubstituted or substituted alkyl, aryl, acyl or any group leading to hydroxyl upon biological metabolization or chemical deprotection.

Abstract: The present disclosure is generally directed to neuroactive enantiomeric 15-, 16- and 17-substituted steroids with additional optional substituents at carbons 3, 4, 6, 7, 10 and 13, and pharmaceutically acceptable salts thereof, for use as, for example, modulators for GABA type-A receptors. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

Abstract: The present invention discloses compound 2?,3?,5?-trihydroxy-androst-6-one, having the structure of formula (I). The present invention also discloses a plurality of methods for preparing the compound and a use of the compound.

Abstract: The present disclosure is generally directed to neuroactive 13,17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

Abstract: The invention relates to the use of 2-substituted estra-1,3,5(10)-triene-3-yl sulfamates of general formula I, in addition to their pharmaceutically acceptable salts for producing a medicament. Said compounds have an anti-tumour action.

Abstract: Process for the preparation of a compound of general formula (II) wherein R1 and R2 independently are hydrogen or a hydroxy- or hydrocarbyl group; or wherein R1 and R2 together are a double bonded oxygen; R3 is hydrogen; R?4 is a nitrobenzophenone group; and R5 and R6 independently are hydrogen or a hydroxy- or hydrocarbyl group; from a compound of general formula (I) wherein, R1, R2 R3, R5 and R6 are as defined above and R4 is hydrogen; wherein the compound of formula (I) is reacted under alkaline conditions with 2-chloro-5-nitrobenzophenone in the presence of an alkanolic solvent and the compound of formula (II) is directly crystallized from this alkanolic solvent. Complex of an alkanol and a compound of general formula (II) obtainable from the above process and processes wherein the above process or complex are used.

Abstract: The present invention relates to 2-alkoxy and 2-aryloxyestrogen compounds, and the intermediate compounds prepared during the preparation thereof, which intermediate compounds are useful intermediates in the preparation of certain physiologically active compounds.

Abstract: The invention provides a process for the preparation of 2-substituted-derivatives of estrone and estradiol. The invention also provides several novel compounds, which can be intermediates in the process, and processes to prepare these novel compounds. The invention also provides 2-alkoxy-estrone, 2-alkoxy-estradiol or mixtures thereof essentially free from other estrogenic intermediates.

Abstract: Substituted steroid compounds which represent selective inhibitors of 17?-hydroxysteroid dehydrogenase type I (17?-HSD1) and, in addition, which may represent inhibitors of the steroid sulfatase, salts thereof, pharmaceutical preparations containing these compounds, and a process for the preparation of these compounds. Also disclosed is a therapeutic method of using such substituted steroid compounds, particularly in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17?-hydroxysteroid dehydrogenase type I and/or steroid sulfatase enzymes and/or requiring lowering of the endogenous 17?-estradiol concentration.

Abstract: Disclosed are compounds of formula I and use thereof in a method of treating a tumor disease that can be influenced positively by the inhibition of tubulin polymerization.

Abstract: The invention relates to methods identify or characterize compounds that can be used to treat specified clinical disorders such as hyperglycemia and type 2 diabetes. Compounds that can be used in these methods include 4?-fluoro-17?-ethynylandrost-5-ene-3?,7?,17?-triol, 4?-fluoro-17?-ethynylandrost-5-ene-3?,7?,17?-triol, 4?-fluoro-17?-ethynylandrost-5-ene-3?,7?,17?-triol and 4?-fluoro-17?-ethynylandrost-5-ene-3?,17?-triol-7-one.

Abstract: Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering derivatives of 2-methoxyestradiol of the general formula: wherein the variables are defined in the specification.

Abstract: There is provided a compound comprising a steroidal ring system and a group R1 selected from any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein the D ring of the steroidal ring system is substituted by a group R2 of the formula —L-R3, wherein L is an optional linker group and R3 is an aromatic hydrocarbyl group.

Abstract: A conjugated prodrug of an estradiol compound conjugated to a biological activity modifying agent.

Abstract: Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering derivatives of 2-methoxyestradiol of the general formula: wherein the variables are defined in the specification.

Abstract: The application discloses novel 2-alkoxyestradiol analogs which exhibit anti-proliferative properties, and methods of making and using such compounds to inhibit undesired cell proliferation and tumor growth. Additionally, methods are disclosed of treating diseases associated with undesired angiogenesis and undesired proliferation, and methods of treating infectious disease wherein the infectious agent is particularly susceptible to inhibition by agents that disrupt microtubule organization and function.

Abstract: The application discloses novel 2-alkoxyestradiol analogs which exhibit anti-proliferative properties, and methods of making and using such compounds to inhibit undesired cell proliferation and tumor growth. Additionally, methods are disclosed of treating diseases associated with undesired angiogenesis and undesired proliferation, and methods of treating infectious disease wherein the infectious agent is particularly susceptible to inhibition by agents that disrupt microtubule organization and function.

Abstract: Modified 2-alkoxyestradiol compounds wherein all hydrogens of the carbon next to the oxygen of the alkoxy moiety at position 2 are substituted with a halogen, alkyl or aromatic group, or a trifluoromethyl group are provided. Methods of using compositions containing these compounds to inhibit microtubule formation and tubulin polymerization or depolymerization in cells and to treat diseases characterized by abnormal cell mitosis are also provided.

Abstract: The application discloses methods of treating mammalian diseases characterized by undesirable angiogenesis by administering compounds including those having the general formulae wherein A is a fused tropone having a general formula: wherein X is selected from the group consisting of hydrogen, hydroxy, carboxy, halogen, nitro, C1 to C12 alkenyl, C1 to C12 alkyl, C1 to C12 alkoxy, SR, NR2, OSO3−, OSO2NR2, HNSO3−, NHSO2NR2, SSO3−, SSO2NR2, wherein R is hydrogen or a C1 to C6 alkyl and the 17-ester and keto derivatives thereof, in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the method of the invention.

Abstract: Compounds represented by the following structural formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification. The compounds are disclosed as useful in the treatment of various forms of cancer.

Abstract: Disclosed is a method of preparing a compound represented by the following structural formula: ##STR1## The method comprises reacting bromine (Br.sub.2) and an aliphatic organic acid with a compound represented by the following structural formula: ##STR2## R.sub.1 and R.sub.2 are each independently a hydroxyl protecting group.

Abstract: The invention provides new androstene derivatives having anti-inflammatory activity, pharmaceutical compositions containing them, and methods of administering them to warm-blooded animals in the treatment of inflammation. The active compounds are alkyl 17.alpha.-dichloroacetoxy-11.beta.-hydroxyandrosta-1,4-dien-3-one-17.beta. -carboxylates and related androstenes.

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: 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: 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: The invention relates to a process for the alkylation of estrone derivatives, which is characterized in that a suspension of the estrone derivatives in dimethylformamide is produced and carbonic acid diester and guanidine and/or alkyl guanidines are dissolved in it and in the largely oxygen-free mixture, the reaction is performed at 100.degree.-200.degree. C. under the reaction pressure being established.

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: 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: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutial compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase including using these compounds to reduce prostate size. Also invented are intermediates used in preparing these compounds.