Abstract: The invention provides 11?-hydroxyandrosta-4-ene-3-one compounds of Formula I, or physiologically acceptable salts or solvates thereof: wherein R4 represents a moiety selected from a group consisting of (A), (B) and (C), with a proviso that when R4 represents moiety (C), Z is S:

Abstract: The 17?-cyano-18a-homo-19-nor-androst-4-ene derivatives of the present invention possess gestagenic activity.

Abstract: The 17?-cyano-19-nor-androst-4-ene derivatives of the present invention possess gestagenic activity.

Abstract: The present invention is directed to compounds of formula (I): wherein R1 represents C4-C7 branched chain alkyl, C3-C8 cycloalkyl optionally substituted by one or more groups independently selected from C1-C3 alkyl and methoxy, C4-C6 cycloalkylmethyl wherein the methyl group is optionally substituted by a group selected from methyl or ethyl, or a bicycloalkyl group optionally substituted by one or more methyl groups; R2 represents hydrogen, a methyl group, which may be in either the a or D configuration, or a methylene group; R3 and R4 are the same or a different group and each independently represents hydrogen, halogen or a methyl group; and represents a single or a double bond; physiologically acceptable solvates thereof, pharmaceutical compositions thereof, methods of treatment using such compounds, and processes for preparing such compounds.

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 present invention is directed to compounds of formula (I): wherein R1 represents C4-C7 branched alkyl group, a bicycloalkyl group, or a C5-C6 cycloalkyl which optionally may be substituted with a C1-C4 alkyl group; R2 represents hydrogen, a methyl group, which may be in either the ? or ? configuration, or a methylene group; R3 and R4 are the same or a different group and each independently represents hydrogen, halogen or a methyl group; represents a single or a double bond; and physiologically acceptable solvates thereof, physiologically functional derivatives thereof, pharmaceutical compositions comprising the compounds, the use of the compounds for the manufacture of medicaments particularly for the treatment of inflammatory and/or allergic conditions, processes for the preparation of the compounds, and chemical intermediates in the processes for the manufacture of the compounds.

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

Abstract: There are provided compounds of formula (I) wherein the variables are as defined by the present specification; and solvates thereof, processes for preparing them and their use in therapy.

Abstract: A compound of formula (I): or a physiologically acceptable solvate thereof.

Abstract: A compound of formula (I): wherein X represents O or S; R1 represents C1-6 alkyl, C3-8 cycloalkyl, C3-8 cycloalkylmethyl or C3-8 cycloalkenyl any of which optionally may be substituted by one or more methyl groups or halogen atoms or R1 represents aryl, substituted aryl, heteroaryl or substituted heteroaryl; R2 represents hydrogen, methyl, which may be in either the ? or ? configuration, or methylene; R3 and R4 are the same or different and each independently represents hydrogen, halogen or a methyl group; and represents a single or a double bond; or a physiologically acceptable salt or solvate thereof.

Abstract: The present invention provides a convenient process for the preparation of S-fluoromethyl 6?,9?-difluoro-11?-hydroxy-16?-methyl-17?-propionyloxy-3-oxoandrosta-1,4-diene-17?-carbothioate, a compound of formula 1, comprising (a) treating 17?-[(N,N-dimethylcarbamoyl)thio]carbonyl-6?,9?-difluoro-11?-hydroxy-16?-methyl-17?-propionyloxy-3-oxoandrosta-1,4-diene, a compound of formula 3 with alkali metal carbonate-alcohol system to obtain 6?,9?-difluoro-11?-hydroxy-16?-methyl-17?-propionyloxy-3-oxoandrosta-1,4-diene-17?-carbothioic acid, a compound of formula 4; (b) reacting the compound of formula 4 with bromofluoromethane to yield the compound of formula 1.

Abstract: The present invention relates to a process for the synthesis of oxandrolone from mestanolone. The process comprises the steps of: (a) oxidizing mestanolone to form 17?-hydroxy-17?-methyl-5?-androst-1-en-3-one; (b) hydroxylating the 17?-hydroxy-17?-methyl-5?-androst-1-en-3-one to form 1?, 2?, 17?-trihydroxy-17?-methylandrostan-3-one; (c) cleaving the 1?, 2?, 17?-trihydroxy-17?-methylandrostan-3-one to form 17?-hydroxy-17?-methyl-1-oxo-1,2,-seco-A-nor-5?-androstan-2-oic acid; and (d) reducing the 17?-hydroxy-17?-methyl-1-oxo-1,2,-seco-A-nor-5?-androstan-2-oic acid to form oxandrolone.

Abstract: Compounds of formula (I), where R is a monovalent cyclic organic group having from 3 to 15 atoms in the ring system, useful as pharmaceuticals

Abstract: The present invention relates to, for example, a compound of formula (XXI) 1

Abstract: The present invention relates to, for example, a compound of formula (XIII) 1

Abstract: This invention discloses a novel method for the conversion of carboxylic acids to carbothioic acids and application of the method to the preparation of androstane carbothiolates, such as fluticasone propionate, which avoids column chromatography.

Abstract: The present invention relates to a process for the synthesis of oxandrolone from mestanolone. The process comprises the steps of: (a) oxidizing mestanolone to form 17&bgr;-hydroxy-17&agr;-methyl-5&agr;-androst-1-en-3-one; (b) hydroxylating the 17&bgr;-hydroxy-17&agr;-methyl-5&agr;-androst-1-en-3-one to form 1&agr;, 2&agr;, 17&bgr;-trihydroxy-17&agr;-methylandrostan-3-one; (c) cleaving the 1&agr;, 2&agr;, 17&bgr;-trihydroxy-17&agr;-methylandrostan-3-one to form 17&bgr;-hydroxy-17&agr;-methyl-1-oxo-1,2,-seco-A-nor-5&agr;-androstan-2-oic acid; and (d) reducing the 17&bgr;-hydroxy-17&agr;-methyl-1-oxo-1,2,-seco-A-nor-5&agr;-androstan-2-oic acid to form oxandrolone.

Abstract: Steroid compounds having various oxygen substitution on the steroid nucleus are disclosed. A specific functionality present on many of the steroid compounds is oxygen substitution at both of positions 6 and 7. Thus, certain steroids have oxygen substitution at C6 and C7, and some have specific stereochemistries such as 6&agr; and 7&bgr; oxygen substitution, and an alpha hydrogen at the 5 position in addition to having 6&agr; and 7&bgr; oxygen substitution. Steroids having 3,4-epoxy functionality are also disclosed. In addition, steroids having C17 pyran and &dgr;-lactone functionality, with oxygen substitution at C6 and C7, or at C15, of the steroid nucleus, are disclosed.

Abstract: The invention provides a thiocarboxylic acid organic salt of the formula: 1

Abstract: Steroid compounds having various oxygen substitution on the steroid nucleus are disclosed. A specific functionality present on many of the steroid compounds is oxygen substitution at both of positions 6 and 7. Thus, certain steroids have oxygen substitution at C6 and C7, and some have specific stereochemistries such as 6&agr; and 7&bgr; oxygen substitution, and an alpha hydrogen at the 5 position in addition to having 6&agr; and 7&bgr; oxygen substitution. Steroids having 3,4-epoxy functionality are also disclosed. In addition, steroids having C17 pyran and &dgr;-lactone functionality, with oxygen substitution at C6 and C7, or at C15, of the steroid nucleus, are disclosed.

Abstract: The present invention relates to a process for the preparation of a compound of formula (I) which comprises the following step: 1

Abstract: There are provided according to the invention compounds of formula (I) wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 represents —C(═O)-aryl or —C(═O)-heteroaryl; R3 represents hydrogen, methyl (which may be in either the &agr; or &bgr; configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and ---- represents a single or a double bond; and salts and solvates thereof. There are also provided processes for preparing compounds of formula (I) and use of the compounds in therapy especially in the treatment of inflammatory and allergic conditions.

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: The invention provides a process for the preparation and isolation of compound of formula 2, comprising the following steps: 1

Abstract: A method is described for stereoselectively reducing an unsaturated alkyl ketone substituent attached to a fused ring base. In this method, the unsaturated alkyl ketone reacts with a chiral oxazaborolidine reagent. This reaction stereoselectively reduces the unsaturated alkyl ketone to an unsaturated alkyl alcohol. The unsaturated alkyl alcohol can be further reduced, if desired, to produce a saturated alkyl alcohol. The fused ring base can be, for example, a steroid ring base or a base of a vitamin D analog. The process in accordance with the invention can be used with an alkeneone substituent (e.g., a 22-ene-24-one substituent) or an alkyneone substituent (e.g., a 22-yne-24-one substituent) on a steroid ring base to make squalamine or other useful aminosterol compounds and intermediates for making aminosterol compounds.

Abstract: The invention provides novel soft steroidal anti-inflammatory agents, pharmaceutical compositions containing said agents, and methods of administering same to mammals in the treatment of inflammation. Preferred compounds of the invention include haloalkyl 17&agr;-alkoxycarbonyloxy-11&bgr;-hydroxyandrost-4-en-3-one-17&bgr;-carboxylates and the corresponding &Dgr;1,4 compounds, optionally bearing 6&agr;- and/or 9&agr;-fluorine and 16&agr;- or 16&bgr;-methyl substituents. Especially preferred compounds include haloalkyl 17&agr;-alkoxycarbonyloxy-9&agr;-fluoro-11&bgr;-hydroxy-16-methylandrosta-1,4-dien-3-one-17&bgr;-carboxylates.

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: Described are new, unsaturated 14,15-cyclopropano-androstanes of general formula (I) and their pharmaceutically acceptable salts, a process for their production and pharmaceutical preparations that contain these compounds. The compounds are characterized by hormonal (gestagenic and/or androgenic) activity and may be used for hormone replacement therapy.

Abstract: The subject of the invention is the products of formula (I): in which either R1 represents halogen, hydroxyl, (C1-C8) alkyloxy or (C1-C12) acyloxy, and R2 represents halogen or hydrogen, or R1 and R2 form together a double bond, Z is chosen from optionally substituted (C1-C8) alkylthio, optionally substituted arylthio, (C1-C8) alkyloxy, halogen, cyano, mercapto, thiocyanato and (CH2)0-1—CO2H, optionally esterified, Y represents hydrogen or methyl, the dotted line in position 1-2 or 5-6 optionally representing a second bond, as well as their addition salts, their preparation process, the intermediates of this process and the pharmaceutical compositions containing them.

Abstract: A water soluble delivery system for nucleic acids to cells having androgen receptors, preferably prostate cells, is provided comprising a steroid moiety capable of binding to said receptors, said steroid moiety being covalently linked to a polycationic material. This molecule may be complexed with therapeutic or diagnostic nucleic acids. Methods of diagnosis and therapy using these compositions are also provided, including gene therapy treatments for prostate cancer.

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: The invention relates to novel, androstane steroids which are the ligand semiochemicals which bind to neuroepithelial receptors.

Abstract: Described are new 14,15-cyclopropano steroids of the 19-norandrostane series of general formula (I) and their pharmaceutically acceptable salts, a process for their production and pharmaceutical preparations that contain these compounds. The compounds are distinguished by hormonal (gestagenic and/or androgenic) activity.

Abstract: Thiol esters of S-substituted 11&bgr;-benzaldoxime-estra-4,9-dien-carboxylic acids of the formula I their pharmaceutically acceptable salts, a method for their synthesis and pharmaceutical preparations containing these compounds are described. These compounds bind to progesterone receptors and have distinctly reduced anti-glucocorticoid action.

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 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: Novel angiostatic .DELTA..sup.4,9(11) -steroids (I), ##STR1## C.sub.21 -oxygenated steroids (II) and other known steroidal compounds have been found to be useful in treating angiogenesis in mammals who have a need for the same. These steroids are useful in treating diseases of neovascularization such as cancer, diabetes and arthritis.

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: 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: Polymorph "A" a novel polymorphic form of N-t-butyl-androst-3,5-diene-17.beta.-carboxamide-3-carboxylic acid. Novel processes for preparing polymorph "A" are also disclosed.

Abstract: Compounds of formula (I): ##STR1## ?wherein: R.sup.1 is hydrogen, alkyl, aryl-substituted alkyl or aromatic heterocyclic-substituted alkyl; R.sup.2 is: aryl-substituted alkyl, aromatic heterocyclic-substituted alkyl or diarylamino; and R.sup.3 is carboxy or a group of formula --CONHSO.sub.2 R.sup.4 wherein R.sup.4 is alkyl!; and pharmaceutically acceptable salts and esters thereof have valuable 5.alpha.-reductase inhibitory activity and can thus be used for the treatment and prophylaxis of, inter alia, prostatic hypertrophy as well as other disorders arising from excess levels of 5.alpha.-dihydrotestosterone.

Abstract: Novel antiandrogenic agents are provided. An exemplary group of compounds has the structural formula (I) ##STR1## wherein R.sup.1 through R.sup.10, a and b are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat androgen-related clinical conditions are provided, as are methods and compositions for using the compounds as contraceptive agents.

Abstract: Compounds of formula (I): ##STR1## ?wherein: R.sup.1 is hydrogen, alkyl, aryl-substituted alkyl or aromatic heterocyclic-substituted alkyl; R.sup.2 is: aryl-substituted alkyl, aromatic heterocyclic-substituted alkyl or diarylamino; and R.sup.3 is carboxy or a group of formula --CONHSO.sub.2 R.sup.4 wherein R.sup.4 is alkyl!; and pharmaceutically acceptable salts and esters thereof have valuable 5.alpha.-reductase inhibitory activity and can thus be used for the treatment and prophylaxis of, inter alia, prostatic hypertrophy as well as other disorders arising from excess levels of 5.alpha.-dihydrotestosterone.

Abstract: The invented compound ##STR1## is useful for the production of steroidal-17-amides that have 5.alpha.-reductase inhibitory activity.

Abstract: A progesterone compound represented by the following formula (1): ##STR1## ?wherein R.sup.1 represents a C1-C23 hydrocarbon group!, and a neovascularization inhibitor containing the same as the active ingredient.The compound (1) has a potent neovascularization inhibitory effect and is hence useful in the treatment of malignant tumors, diabetic retinitis, rheumatism, etc.

Abstract: Invented are 17.alpha. and 17.beta.-substituted acyl-3-carboxy-3,5-diene analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are intermediates and processes used in preparing these compounds.

Abstract: Invented are 17.alpha. and 17.beta.-substituted acyl-3-carboxy-3,5-diene analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are intermediates and processes used in preparing these compounds.

Abstract: Invented are 17.alpha. and 17.beta.-substituted acyl-3-carboxy-3,5-diene analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are intermediates and processes used in preparing these compounds.

Abstract: The invention relates to estrene steroids, which bind to neuroepithelial receptors. The steroid is preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers.

Abstract: Invented are 17.alpha. and 17.beta.-substituted acyl-3-carboxy aromatic A ring analogues of steroidal synthetic compounds. Representative of such compounds include the following ##STR1## wherein Z is .alpha. or .beta. ##STR2## in which A is absent or present as a linear or branched, saturated or unsaturated hydrocarbon chain containing from 1-6 carbon atoms and R isa) a linear or branched, saturated or unsaturated hydrocarbon chain containing 1-12 carbon atoms substituted with one or more substituents selected from the group consisting of: --OC.sub.6 -C.sub.12 aryl, --OC.sub.1 -C.sub.4 alkyl, halogen, carboxy and --S(O).sub.n .sup.R.sup.7, where n is 0-2 and R.sup.7 is hydrogen or C.sub.1-4 alkyl;b) C.sub.3 -C.sub.8 nonaromatic, unsaturated or saturated, cycloalkyl, optionally substituted with one or more substituents selected from the group consisting of:--OC.sub.6 -C.sub.12 aryl, --(CH.sub.2).sub.m OH, --OC.sub.1 -C.sub.4 alkyl, C.sub.6 -C.sub.12 aryl, C.sub.1 -C.sub.