Abstract: This disclosure relates to a method and reagents for determining ligands in biological fluids such as serum, plasma, spinal fluid, amnionic fluid and urine. In particular, this disclosure relates to a fluorescence polarization immunoassay procedure and to a novel class of tracer compounds employed as reagents in such procedures. The procedure disclosed combines the specificity of an immunoassay with the speed and convenience of fluorescence polarization techniques to provide a means for determining the amount of a specific ligand present in a sample.

Abstract: Estrogens characterized by an aromatic ring of the formula ##STR1## are halogenated by electrophilic substitution of a halo atom at the 1-position of the aromatic ring after protection of the sensitive 3-hydroxyl substituent and amination at the 4-position. Preferred starting materials include estrones or derivatives thereof. The estrones are preferably reduced after masking and amination to form the corresponding estradiols, which are then halogenated, deaminated and deprotected to provide the novel 1-haloestradiols.

Abstract: The invention provides novel 1.alpha.-hydroxy vitamin D compounds and a method for their preparation from 1.alpha.-hydroxy-25-hydrogen cholesta-5,7-dienes by irradiation and isomerization techniques. The invention also includes the said 1.alpha.-hydroxy-25-hydrogen-cholesta-5,7-dienes and the corresponding cholest-5-enes.The new compounds may be obtained in a crystalline form substantially free from isomeric or other impurities arising from manufacture.

Abstract: Novel radioactive steriods labelled with tritium of the formula ##STR1## wherein .sup.3 H is tritium and R and R.sub.1 are individually selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and acyl of an organic carboxylic acid of 1 to 10 carbon atoms useful for revealing receptors of glucocorticoids and in determining the number of fixation sites on glucocorticoids and novel intermediates.

Abstract: Novel radioactive estradienes labelled with tritium of the formula ##STR1## wherein .sup.3 H is tritium and R is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and acyl of an organic carboxylic acid of 1 to 10 carbon atoms and the study and radioimmunological determination of non-radioactive 11.beta.-(4-dimethylaminophenyl)-17.alpha.-(prop-1-ynyl)-.DELTA..sup.4,9 -estradiene-17.beta.-ol-3-one and its metabolites in biological fluids and novel intermediates.

Abstract: A method of preparation of halogen labeled organic compounds is described. In particular, estradiol derivatives labeled by halogen substitution at C-16 are synthesized according to the present invention. A triflate intermediate is prepared from which either 16-alpha-halo-substituted-17-beta-estradiols or 16-beta-halo-substituted-17-beta-estradiols can be rapidly formed as desired. In particular, the preparation of 16-alpha-.sup.123 I-17-beta-estradiol and 16-beta-.sup.123 I-17-beta-estradiol are shown and are synthesized from a 17-beta-estradiol-16-beta-triflate. Both 16-alpha-.sup.123 I- and 16-beta-.sup.123 I-17-beta-estradiol made according to the present invention are shown to have a high specific activity. The method of synthesis is sufficiently rapid so that the relatively short half-life of .sup.123 I is readily accommodated. The high stereospecificity of each step of the reaction sequence in preparing the labeled estradiols provides for highly efficient syntheses and little waste of radio-label.

Abstract: There is provided the novel compound 19-hydroxyaldosterone. There is provided a process for its preparation. There are further provided pharmaceutical compositions comprising this compound as active ingredient. These are useful, amongst others, as mineralocorticoid drugs and as drug against Addison's disease.

Abstract: Described for use as a key ingredient in an animal control composition and more particularly in an animal repellent composition, is the genus of steroids defined according to the structure: ##STR1## wherein X completes a substituted cyclopentyl moiety and is one of the moieties: ##STR2## wherein Y represents methylene, carbinol or keto; and wherein Z completes a substituted cyclohexyl moiety and is one of the moieties:hydroxycyclohexyl;ketocyclohexyl;ketocyclohexenyl;hydroxyphenyl;cyclohexenyl; orbicyclohexyland wherein the dashed line represents a carbon-carbon single bond or a carbon-carbon double bond.Also described are animal control articles consisting of one or more members of the above mentioned steroid genus and imbedded in a compatible polymer.

Abstract: A process for the preparation of corticosteriod esters of the formula ##STR1## in which ---- signifies that a double bond can be present;X is hydrogen, chlorine or fluorine;R.sub.1 is hydrogen, fluorine, chlorine or methyl, which may be either .alpha. or .beta.;R.sub.2 is halogen, oxo or hydroxyl;or R.sub.3 is hydrogen, .alpha.-methyl or .beta.-methyl;or R.sub.2 and X jointly form an epoxide group;R.sub.4 is an acyl group of the formula RCO, in which R is one of the following(i) an alkyl group containing 1 to 16 carbon atoms, whether straight-chained, branched or cyclic;(ii) an aralkyl group of 7 to 8 carbon atoms;(iii) a phenyl group;R.sub.5 is hydroxyl or R.sub.6 ; whereR.sub.6 is hydrogen, one or two halogen atom substituents or OR.sub.7, where R.sub.

Abstract: 1.alpha.,25-Dihydroxy-24R-fluorocholecalciferol and 1.alpha.,25-dihydroxy-24S-fluorocholecalciferol, analogs of 1.alpha.,25-dihydroxy-cholecalciferol which is physiologically the most active metabolite of vitamin D.sub.3, are synthesized in a multistep process from the known substance 1.alpha.,3.beta.-dihydroxyandrost-5-en-17-one. The new analogs are characterized by the ability to increase intestinal calcium transport, increase serum calcium and phosphate concentrations and to increase the deposition of these minerals in bones. These compounds will find a ready application as substitutes for natural 1.alpha.,25-dihydroxycholecalciferol in the treatment of disease states characterized by metabolic calcium and phosphate deficiencies.

Abstract: Androstane carbothioic acids of the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, a hydroxy group in the .alpha.-configuration, a methyl group which may be in either the .alpha.- or .beta.-configuration, or a methylene group;R.sup.2 represents a hydroxy or protected hydroxy group in either the .alpha.- or .beta.-configuration or an oxo group;R.sup.3 represents a hydrogen, bromine, chlorine or fluorine atom; or R.sup.2 and R.sup.3 together represent a carbon-carbon bond or an epoxy group in the .beta.-configuration;R.sup.4 represents a hydrogen or fluorine atom; and the symbol represents a single or double bond and the salts thereof are useful as intermediates in the preparation of anti-inflammatory androstane 17.beta.-carbothioate esters.The compounds of formula I are prepared by reaction of a reactive derivative of a 17.beta.-carboxylic acid corresponding to the compound of formula I with hydrogen sulphide or a sulphide or hydrosulphide salt.

Abstract: A compound of the formula, ##STR1## wherein R may be H or acyl; X may be H, acyl, or lower alkyl; Z may be H, hydroxy, or acyloxy; Y may be lower alkyl, aryl, alkyl substituted aryl or vinyl; and the non-toxic pharmaceutically acceptable salts thereof.This invention was made in the course of work performed under a grant from the United States National Heart Lung and Blood Institute.

Abstract: 6.alpha.-Methyl corticoids of formula I ##STR1## wherein is a single bond or a double bond, R is acyloxy of up to 8 carbon atoms, and X is chlorine, hydroxy, or acyloxy of up to 8 carbon atoms, are pharamacologically effective substances.

Abstract: An eye drops composition containing estradiol-17beta dissolved therein or in a crystalline form, said composition being suitable for treating chronic catarrh disorders of the ocular conjunctiva, that is chronic conjunctivitis simplex.

Abstract: The invention relates to a contraceptive composition of a prolactin elevag benzamide, such as N-[(1-ethyl-2-pyrrolidinyl)methyl]2-methoxy 5-sulfamoyl benzamide, and a progestogen.

Abstract: There is disclosed a new therapeutic use of cyproterone acetate, to block the estrogen signal in the treatment of functional and tumoral estrogen-dependant pathology, in women, caused by intrafollicular iperestrogenism in a pharmaceutically-acceptable dosage.

Abstract: Novel radioactive estradienes labelled with iodine of the formula ##STR1## in the form of their syn or anti isomers or mixtures thereof wherein the wavy line indicates anti or syn position, R is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and acyl of an organic carboxylic acid of 1 to 12 carbon atoms and R.sub.1 is the residue of an amino acid R.sub.1 NH.sub.2 possessing an iodine acceptor group or a derivative thereof labelled with iodine .sup.125 or .sup.131 and their preparation and novel intermediates, antigens prepared from the compounds of formula I and bovine seric albumin or human seric albumin and their preparation and their use for the preparation of antibodies.

Abstract: A water-swellable, water-insoluble polymer is loaded with a biologically active substance or substance convertible into a biologically active substance in vivo by preparing and grinding a mixture of a said substance with a water-swellable, water-insoluble polymer in a weight ratio of the said substance:polymer of from 1:0.1 to 1:100. The thus-loaded polymer is useful as a pharmaceutical composition.

Abstract: A compound of the formula ##STR1## wherein Z is hydrogen and Y is nitro, inhibits the growth of murine ductal carcinoma (MXT mammary tumors).

Abstract: Novel 19-nor steroids and 19-nor-D-homo-steroids of the formula ##STR1## wherein R.sub.1 is an organic radical of 1 to 18 carbon atoms containing at least one atom selected from the group consisting of nitrogen, phosphorous and silicon with the atom immediately adjacent to the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is selected from the group consisting of a pentagonal ring and a hexagonal ring optionally substituted and optionally containing a double bond, B and C together form a double bond or an epoxy group, the C.dbd.A group at position 3 is selected from the group consisting of C.dbd.O, ketal, which may be open or closed ##STR2## are selected from the group consisting of alkyl of 1 to 8 carbon atoms and aralkyl of 7 to 15 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having anti-glucocorticoid activity and a process for their preparation.