Abstract: Substituted benzoate ester prodrugs of .beta.-estradiol and ethynyl estradiol are provided which have improved bioavailability and extended duration of action when administered orally.

Abstract: The invention discloses 4-substituted androstendione derivatives of the following formula (I) ##STR1## wherein R is amino or substituted amino or azido,one of R.sub.1 and R.sub.2 is hydrogen and the other is hydrogen, alkyl, alkenyl or alkynyl, and(x) and (y) are each, independently, a single bond or a double bond.The compounds of formula (I) are useful aromatase inhibitors.

Abstract: The invention relates to ring A-diol units suitable for synthesizing 1.alpha.-hydroxyvitamin D compounds by subsequent condensation with appropriate .sup.C /.sub.D -ring fragments and to methods for preparing such ring A-diol units.

Abstract: An improvement in the epoxidation of certain 4,5-unsaturated steroids with peracetic acid, which comprises carrying out the reaction in methanol solution.

Abstract: A novel steroid of the formula ##STR1## wherein X is methylene and R is an optionally substituted carbocyclic aryl or heterocyclic aryl or optionally substituted vinyl or ethynyl or X is a simple bond or --S-- and R is optionally substituted carbocyclic aryl or heterocyclic aryl, R.sub.2 is methyl or ethyl, R.sub.3 is selected from the group consisting of optionally substituted alkyl of 1 to 8 carbon atoms and optionally substituted alkenyl and alkynyl of 2 to 8 carbon atoms, R.sub.4 is selected from the group consisting of hydrogen and acyl, ##STR2## is selected from the group consisting of ##STR3## R.sub.6 is selected from the group consisting of hydrogen and methyl, the wavy line indicates .alpha. or .beta.- and the dotted line in 1(2) indicates the optional presence of a second carbon-carbon bond and novel process and intermediates therefore having anti-glucocorticoid activity.

Abstract: The invention relates to pharmaceutical compositions comprising at least one Vitamin D derivative and a method of using the pharmaceutical compositions in suppressing immune responses.

Abstract: Thiol-substituted synthetic steriod hormones or androgens having a testosterone ring system backbone are used to inhibit aromatase's catalyzed conversion of C.sub.19 androgens having a A.sup.4,3-ketone group to estrogens in the treatment of estrogen-dependent tumors, such as metastatic breast cancer in postmenopausal females.The compounds have the general formula: ##STR1## wherein R.sub.1 =a thiol, such as --SH or --CH.sub.2 SH, and R.sub.2 =OH or =O. The preferred synthetic hormones are 17.beta.-hydroxy-10.beta.-mercaptoestr-4-en-3-one, 19-mercaptoandrost-4-en-3,17-dione, and 10.beta.-mercaptoandrost-4-en-3,17-dione.

Abstract: Compositions and methods useful for enhancing the transdermal and transmembrane drug delivery of topical and systemic agents. The compositions and methods comprise the active agent together with an effective amount of certain amides of heterocyclic amines as defined herein as penetration enhancers and topically administering to human or animal skin or other membranes the resulting compositions.

Abstract: Estriol esters of Formula I ##STR1## wherein R is, in each case, the residue of an aliphatic monocarboxylic acid of 3-10 carbon atoms,surpass estriol in strength and duration of estrogen activity.

Abstract: The present invention relates to a stabilized plant protecting agent suspension which can be characterized by containing 10 to 60% by weight of one or more active ingredients, 30 to 5% by weight of oily layer, 0 to 10% by weight of emulsifier, 10 to 20% by weight of conventionally used excipient and water needed to 100% by weight while by increasing solid concentration oil concentration decreases. The invention also provides a process for the preparation of a stabilized plant protecting agent suspension by adding oil and optionally an emulsifier and/or water containing layer to a suspension of a suitable particle size of the active ingredient and water soluble excipients, such as surfactants, optionally emulsifiers, dispersing agents, viscosity modifying agents, protective colloids and mixing together the suspension layer and the layer containing the oil with a stirrer of great shearing force and optionally adding to the obtained stabilized suspension further excipients, e.g.

Abstract: A method of treating psoriasis in a patient which comprises administering to said patient an effective amount of a vitamin D compound which is capable of stimulating the differentiation of cultured tumor cells or normal rodent or human fibroblasts or keratinocytes in vitro.

Abstract: An antifungal pastille formulation, preferably containing nystatin as the antifungal agent, is provided which is soft and smooth in texture and when dissolved slowly in the mouth does not cause irritation of and will not adhere to oral mucosa and yet distributes nystatin in sufficiently high saliva concentrations, throughout the oral cavity, for long enough periods of time so as to be particularly effective in the treatment of candidiasis in the oral cavity and esophagus. A method for treating candidiasis in the oral cavity and esophagus employing the antifungal pastille and a method for preparing a nystatin pastille formulation are also provided.

Abstract: 17.alpha.-bromo-.alpha. and 17.alpha.-iodo-vinyl-estrane derivatives of general formula I ##STR1## wherein X is a bromine or iodine atom in Z or E position,R.sup.1 is hydrogen, hydroxy or acyloxy with up to 3 C atoms,R.sup.2 is hydrogen, alkyl with up to 3 C atoms and alkanoyl and aroyl with up to 7 C atoms,R.sup.3 is hydrogen or methyl,R.sup.4 is a hydrogen atom in the .alpha. or .beta. position,R.sup.5 is hydrogen, methyl or methoxy andR.sup.6 is hydrogen or methyl,are pharmacologically effective with a profile of action like ethinylestradiol and in the form of their radioactively labeled compounds are also valuable diagnostic media.The Z-isomers can be prepared by a new process by reaction of the corresponding 17.alpha.-ethinyl steroids with trialkyl (or phenyl) tin hydride with addition of a free radical former.

Abstract: Insect infestation of grain is controlled by contacting the grain, or a locus separating the grain from an insect population, with an insecticidally effective amount of a liquid comprising a concentration of phosphatides greater than that found in crude vegetable oils. The dust associated with the grain is controlled as well when the grain is contacted with the liquid.

Abstract: Anionic, surface-active trehalose lipids, in which different organic acids are bound to a trehalose molecule by an ester linkage, are prepared by aerobically cultivating trehalose-producing microorganisms, capable of assimilating hydrocarbons, under growth-limiting conditions, but without limiting the oxygen.

Abstract: This invention is concerned with the selective production of ethyl acetate and acetaldehyde by microorganisms, for example of the genus Candida and of the genus Hansenula. Ethyl acetate or acetaldehyde may be produced by altering the concentration of ethanol in the medium.

Abstract: A process for making a known 6-methyl, 19-nor-pregna-4, 6-diene, 3.20-dione which begins with formylating a 3-alcoxy, 19-nor-pregna-3,5,17(20)-triene at the 6 position. The 6-formylated derivative is reduced to yield a 6-hydroxy methylated derivative, which is in turn dehydrated to a 3-keto, 6-methylenic derivative. The 3-keto derivative is then isomerized to a 3-keto, 4,6,17-pregnatriene. This latter triene is then coverted to the known product by reaction with a bis-hydroxylating agent and a catalyst based on osmium tetroxide. Optionally, the product can be acylated at the 17-alpha position. The process reduces the cost of producing the known product by allowing it to be manufactured from starting materials less costly than those previously required.

Abstract: The rate and character of human hair growth including androgen-stimulated beard hair growth in intact, sexually mature males is altered by the topical application out of a dermatologically acceptable carrier of a material capable of inhibiting the action of the enzyme ornithine decarboxylase. In a preferred practice of the invention, compositions containing such materials along with anti-androgen material are employed.

Abstract: Novel 1-hydroxylated vitamin D compounds containing a 22, 23-cis double bond in the side chain are provided. The compounds are characterized by an unexpectedly high binding affinity for the protein receptor forecasting their ready applicability as substitutes for vitamin D or various of its metabolites in their various known applications and in the treatment of various metabolic bone diseases.

Abstract: The invention provides, as novel vitamin D derivatives, analogs of vitamin D.sub.2 compounds which lack the 24-methyl substituent and are identified as 1.alpha.-hydroxy-28-norvitamin D.sub.2 and 1.alpha.,25-dihydroxy-28-norvitamin D.sub.2.The compounds of the invention are characterized by unexpectedly high vitamin D-like activity as well as a novel activity pattern. Because of such activity they would find ready application as substitutes for vitamin D or various of the known vitamin D metabolites in their various application for the treatment of calcium disorders.