Abstract: The present invention relates to a process for the preparation of 17?-(3-hydroxypropyl)-17?-hydroxysteroids of the formula I starting from 17-ketosteroids of the formula III via the intermediates of the formula V wherein the radicals R3, R5, R6, R7, R10, R13, R15, R16, R40, R41 and R42 have the meaning indicated in the description.

Abstract: The present invention relates to a process for the preparation of 17?-(3-hydroxypropyl)-17?-hydroxysteroids of the formula I starting from 17-ketosteroids of the formula III via the intermediates of the formula V wherein the radicals R3, R5, R6, R7, R10, R13, R15, R16, R40, R41 and R42 have the meaning indicated in the description.

Abstract: This invention describes the use of a therapeutic gestagen (e.g., drospirenone, cyproterone acetate, dienogest) for the production of a pharmaceutical agent for the treatment of premenstrual dysphoric disorder (PMDD), optionally in combination with a natural or synthetic estrogen (e.g., estradiol or ethinylestradiol).

Abstract: The invention relates to processes for preparing 3?-O-linked steroids including 3?-O-linked-androst-5-ene steroids and 3?-O-linked-5a-androstane steroids. In one process a 3?,4?-epoxy androst-5-en-17-one is predominately reduced at the epoxy moiety wherein reduction of the 3?,4? epoxy functional group occurs preferentially at position C4 with retention of configuration at position C3 to provide a 3?-O-linked-androst-5-ene steroid. In another process, conditions are provided for inversion of configuration of a 3?-hydroxy-androst-5-ene steroid by the Mitsunobu reaction to provide a 3?-O-linked-androst-5-ene steroid with reduced amounts of 3?,5?-cycloandrostane side-product impurities.

Abstract: The invention relates to a method and a device, as well as the variants thereof, which operates continuously or discontinuously for the agglomeration and/or drying of powder materials using selective infrared irradiation on a surface which is continually supplied with renewed powder, with or without the spraying of liquids. The process can be performed in sealed conditions or open to the atmosphere, with or without the recovery of volatile components.

Abstract: The present invention relates to C-ring-substituted pregn-4-ene-21,17-carbolactones of the general formula I in which R6,7 is an ?- or ?-methylene and R9 is a hydrogen atom and R11 is a bromine, chlorine or fluorine atom or R9 and R11 together are a bond. The novel compounds are progestational antimineralocorticoids.

Abstract: An in vitro synthesis of (+) cortistatin A from readily available precursors is disclosed, as are the syntheses of related 17-aryl substituted compounds, the 17-aryl substituted compounds themselves and novel compounds useful in their preparation.

Abstract: The invention relates to 15,16-methylene-17-(1?-propenyl)-17-3?-oxidoestra-4-en-3-one derivatives with the general chemical formula I, where the Z, R4, R6a, R6b, R7 and R18 have the meanings stated in claim 1, and solvates, hydrates and salts thereof, including all crystal modifications and all stereoisomers of these compounds. The invention also relates to the use of these derivatives for the production of a drug for oral contraception and for the treatment of pre-, peri- and postmenopausal problems and drugs which contain such derivatives, in particular use in the aforesaid indications. The derivatives according to the invention have a progestational and in preferable cases also an antimineralcorticoid and neutral to slight androgenic activity.

Abstract: This invention provides novel compounds comprising the following anti-inflammatory pharmacore: wherein X, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.

Abstract: Methods for separation and synthesis of the optically active 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone are provided. Preferred stereoisomerically purified 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone have fewer effects mediated by gonadal steroid receptors relative to effect mediated by minteralocorticoid progesterone receptors, compared to the stereoisomerically unpurified form of the compound. These optically active compounds can be useful for obtaining reduction in moderate essential hypertension and it the treatment of congestive heart failure in humans with minimized undesirable side effects such as gynecomastia, tender breast enlargement and menstrual irregularities in women, and loss of libido in men.

Abstract: A novel crystalline form (Form L) of the aldosterone receptor antagonist drug eplerenone is provided having relatively high physical stability at normal temperatures of storage and use. Pharmaceutical compositions are also provided comprising Form L eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form L eplerenone and for preparing compositions comprising Form L eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form L eplerenone.

Abstract: The instant invention provides potent antiandrogen compounds, such as 3?-acetoxyandrost-1,5-diene-17-ethylene ketal and 3?-hydroxyandrost-1,5-diene-17-ethylene ketal, and methods for their use in the prevention and treatment of biological conditions mediated by androgen receptors. Thus, for example, compounds of the invention are useful in the prevention and treatment of prostrate cancer. Furthermore, it has been discovered that compounds of the invention are useful in the prevention and treatment of androgen-independent cancers such as androgen-independent prostrate cancer. Finally, inventive compounds may be used to treat antiandrogen induced withdrawal syndrome.

Abstract: The present invention encompasses processes for preparing drospirenone and intermediates thereof.

Abstract: The present invention relates to a process for the preparation of 17?-(3-hydroxypropyl)-17?-hydroxysteroids of the formula I starting from 17-ketosteroids of the formula III via the intermediates of the formula V wherein the radicals R3, R5, R6, R7, R10, R13, R15, R16, R40, R41 and R42 have the meaning indicated in the description.

Abstract: A process is described for the preparation of drospirenone, a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic activity, useful for preparing pharmaceutical compositions with contraceptive action; comprising the oxidation of 17?-(3-hydroxypropyl)-6?,7?,15?,16?-dimethylene-5?-androstane-3?,5,17?-triol.

Abstract: The invention relates to an industrial process for the preparation of 17-hydroxy-6?,7?;15?,16?-bismethylene-3-oxo-17?-pregn-4-ene-21-carboxylic acid ?-lactone of formula (I), and to the key-intermediates for this process.

Abstract: The present invention describes the novel 18-methyl-19-norandrost-4-ene 17,17-spiro ethers of the general formula I in which Z is an oxygen atom, two hydrogen atoms, a group ?NOR or ?NNHSO2R, where R is a hydrogen atom or a straight- or branched-chain alkyl group having 1 to 4 or 3 to 4 carbon atoms, R4 is a hydrogen atom, a halogen atom or a trifluoromethyl group, and R6 and/or R7 may have a or a configuration, and R6 and R7 are independently of one another a hydrogen atom or a straight- or branched-chain alkyl group having 1 to 4 or 3 to 4 carbon atoms or a straight- or branched-chain alkenyl group having 2 to 4 or 3 to 4 carbon atoms or a saturated cycloalkyl group having 3 to 5 carbon atoms or together are a methylene group or a double bond. The novel compounds have progestational and antimineralocorticoid activity.

Abstract: Multiple novel keto-substituted intermediates are provided for the synthesis of epoxymexrenone, useful as an Aldosterone Receptor Antagonist.

Abstract: Intermediates in the preparation of 9,11-epoxy steroids are disclosed. Particularly, disclosed are 11,12-epoxy steroid, 4,5-9,11-diepoxy steroid and 12-keto steroid intermediates.

Abstract: Processes for the preparation of 4,5-dihydro-5,7-lactone steroid compounds are provided.

Abstract: Novel 5&bgr;-cyano steroid compounds including compounds of Formula VII: wherein A—A, B—B, R3, R8 and R9 are as defined in the specification.

Abstract: The invention relates to a steroid derivative which steroidal skeleton is bound at carbon atom 17 to a spiromethylene ring of the formula: ##STR1## wherein R.sub.a and R.sub.b are independently selected from the group consisting of hydrogen, methyl, and halogen; m is 1 or 2; and the asterisk denotes carbon atom 2 of the spiromethylene ring which is carbon atom 17 (or carbon atom 17.alpha. of a homosteroid skeleton) of the steroid. The steroids have progestational or antiprogestational activity.

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: The invention relates to a steroid derivative which steroidal skeleton is bound at carbon atom 17 to a spiromethylene ring of the formula: ##STR1## wherein R.sub.a and R.sub.b are independently selected from the group consisting of hydrogen, methyl, and halogen; m is 1 or 2; and the asterisk denotes carbon atom 2 of the spiromethylene ring which is carbon atom 17 (or carbon atom 17.alpha. of a homosteroid skeleton) of the steroid. The steroids have progestational or antiprogestational activity.

Abstract: Steroid compounds active on the cardiovascular system of formula ##STR1## wherein X, n, R, R.sub.1 and R.sub.2 have the meanings mentioned in the description are described.

Abstract: A method of treatment of androgen-related diseases such as prostate cancer in susceptible male animals, including humans, comprises administering novel antiandrogens and/or novel sex steroid biosynthesis inhibitors as part of a combination therapy. Sex steroid biosynthesis inhibitors, especially those capable of inhibiting conversion of dehydroepiandrosterone (DHEA) or 4-androstenedione (.DELTA..sup.4 -dione) to natural sex steroida (and testosterone into dihydrotestosterone) in peripheral tissues, are used in combination with antiandrogens usually after blockade of testicular hormonal secretions. Antiestrogens can also be part of the combination therapy. Pharmaceutical compositions and two, three, four and five component kits are useful for such combination treatment.

Abstract: New 11.beta.-phenyl-14.beta.H-steroids of general formula (I), where Z is an oxygen atom or the hydroxyimino-grouping N.about.OH, and M and N are either jointly a second compound or L is a hydrogen atom and M is an .alpha.-permanent hydroxy group and either A and B together are a second compound and D is a hydrogen atom, where R.sup.1 is a five or six-part heteroalkyl residue or a cycloalkyl, cycloalkenyl or aryl residue or A is a hydrogen atom and B and D together are a methylene bridge, where R.sup.1 besides the aforementioned residues may be a possibly substituted hydrocarbon residue with up to 10 C atoms, a possibly substituted amino group, a hydroxy or C.sub.1-8 alkoxy, mercapto or thioalkyl group, R.sup.2 is a methyl or ethyl residue, and R.sup.3 /R.sup.4 represents the usual combination of substituents on the C17 atom in steroid chemistry, having antigestagenic and other properties.

Abstract: The invention relates to 3-phosphinic acid steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5.alpha.-reductase.

Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are intermediates used in preparing these compounds.

Abstract: Invented are sulfonic acid substituted analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase, including using these compounds to reduce or maintain prostate size. Also invented are intermediates used in preparing these compounds.

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

Abstract: Invented are phosphinic acid substituted analogues of steroidal synthetic compounds, pharamaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase, including using these compounds to reduce or maintain prostate size.

Abstract: Steroids with a 17-spiro substituent of 3,4 or 6 ring members of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of carbocyclic aryl, heterocyclic aryl and aralkyl, R.sub.2 is a hydrocarbon of 1 to 18 carbon atoms in the .alpha.-or .beta.-position, the wavy line of the spiro ether indicates the oxygen is .alpha.-or .beta.-, X is selected from the group consisting of --CH.dbd.CH--CH.sub.2 --CH.sub.2 -- and --(CH.sub.2).sub.n --, n is 1, 2 or 4, the A and B rings have a structure selected from the group consisting of ##STR2## R' and R" are individually hydrogen or alkyl of 1 to 4 carbon atoms, R.sub.e is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, substituted alkyl of 1 to 6 carbon atoms and acyl and their non-toxic, pharmaceutically acceptable acid addition salts having a remarkable antiprogestomimetic activity.

Abstract: The invention relates to new 11-arylsteroid compounds, having a strong antiprogestin and a weak or nonexistent antiglucocorticoid activity, to processes for preparing said compounds and also to pharmaceutical preparations which contain these derivatives as active constituent, characterized in that said steroids have the following formula: ##STR1## in which R.sub.1 is an aryl group with a ##STR2## group as substituent, X and Y each being separately H or a (1-4 C) hydrocarbyl group or together a (2-C) hydrocarbyl group which forms a 3- to 7-membered ring together with the nitrogen atom;R.sub.2 is hydrogen, hydroxyl, an acyloxy or an alkoxy group or a saturated or unsaturated hydrocarbyl group containing 1-8 carbon atoms, which hydrocarbyl group is provided with at least one hydroxyl, oxo, azido, cyano and/or halogen group;R.sub.3 is a hydroxyl, an acyloxy or an alkoxy group or an acyl group optionally substituted by a hydroxyl, alkoxy, acyloxy or halogen group; or R.sub.2 and R.sub.

Abstract: Invented are phosphonic acid substituted analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase, including using these compounds to reduce or maintain prostate size. Also invented are intermediates used in preparing these compounds.

Abstract: Novel 19-nor-steroids of the formula ##STR1## wherein the A ring is either ##STR2## Re is selected from the group consisting of hydrogen, acyl and optionally substituted alkyl of 1 to 6 carbon atoms, R is methyl or ethyl, R.sub.1 is selected from the group consisting of hydroxyl, protected hydroxyl, acyloxy and alkoxy, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl and alkynyl of 2 to 8 carbon atoms, acyl, aralkyl of 7 to 15 carbon atoms, the substituents other than hydrogen being optionally substituted or R.sub.1 and R.sub.2 together form a group selected from the group consisting of ##STR3## A.sub.r is an optionally substituted 5- or 6-membered aryl and their salts with non-toxic, pharmaceutically acceptable bases and acids having antiproliferative, anti-estrogenic and/or estrogenic properties.

Abstract: The present invention is concerned with 11-aryloestrane and 11-arylpregnane derivatives, characterized in that these derivatives have the following structure: ##STR1## wherein R.sub.1 is an aryl group with an ##STR2## group as substituent,X and Y each being separately H or a (1-4 C) hydrocarbon radical or together a (2-6 C) hydrocarbon radical;R.sub.2 is an alkyl group containing 1-4 carbon atoms;R.sub.3 is H, OH, a saturated or unsaturated hydrocarbon radical containing 1-8 carbon atoms, at least provided with a hydroxyl, oxo, halogen, azido or nitrile group; an acyloxy or an alkoxy group;R.sub.4 is a hydroxyl, an acyloxy or an alkoxy group or an acyl group optionally provided with a hydroxyl, alkoxy, acyloxy or halogen group; or R.sub.3 and R.sub.4 together form a ring system; andR.sub.5 is a hydrocarbon group containing 1-4 carbon atoms, and further with processes for the preparation of these compounds and with pharmaceutical preparations comprising these compounds.

Abstract: 11.beta.-substituted steroids of the formula ##STR1## wherein A and B together represent a second bond between the 6-position and 7-position carbon atoms, or, respectively, are each H;X is O, two H atoms or hydroximino;Z is the residue of a pentagonal or hexagonal ring which is optionally substituted and optionally saturated;R.sup.1 is vinyl, C.sub.3-7 -cyclo-1-alkenyl, phenyl, naphthyl or 5- or 6-membered heterocyclic aromatic having at least one N, O or S atom, each being unsubstituted or substituted by 1-3 halogen atoms, 1-3 C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, C.sub.1-4 -acyl, C.sub.2-10 -alkenyl, C.sub.1-4 -acyloxy, phenyl, nitro, hydroxy, carboxy, cyanide, COOR.sup.4 or amino optionally substituted by 1-2 C.sub.1-4 -alkyl;R.sup.2 is methyl or ethyl,R.sup.3 is H, Cl or methyl; andR.sup.4 is C.sub.1-4 -alkyl optionally substituted by phenyl which itself is optionally substituted by C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, halogen or phenylhave valuable pharmacological properties.

Abstract: 7.alpha.-acylthio-9.alpha.,11.alpha.-epoxy-20-spirox-4-ene-3,21-diones of the formula I ##STR1## in which R represents lower alkanoyl and --A--A-- represents an ethylene or cyclopropylene group, have a high aldosterone-antagonistic activity without significant sexually-specific side-effects and can be used as potassium-protecting diuretics in the treatment of various forms of hyperaldosteronism. The compounds can be obtained by conventional processes of steroid chemistry.

Abstract: A method and apparatus for dewatering an aqueous coal slurry includes imparting high shear forces to the aqueous coal slurry in the presence of a peptizing agent to render coal particles hydrophobic by stripping clay from the coal particles and peptizing the clay in the aqueous medium of the slurry. The slurry is separating to recover coal particles and the aqueous medium is draining medium from the hydrophobic surface of the coal particles.