Abstract: The invention relates to the preparation of 9.beta.,10.alpha.-5,7-diene steroids by irradiating the corresponding 9.alpha.,10.beta. steroids with filtered ultraviolet light of an antimony lamp.

Abstract: This invention discloses novel glycosides which are potent inhibitors of cholesterol absorption and therefore useful in treating hypercholesterolemia and atherosclerosis. Particularly useful in this respect is glycoside tigogenin cellobioside. The method of use for treatment of hypercholesterolemia and atherosclerosis, and the suitable pharmaceutical compositions are also disclosed.

Abstract: 16-Alkylated and 16-alkylated-7-hydroxy 5.beta.-androstan-3-ol-17-one, and the esters and ethers thereof, are used as an anti-diabetic, anti-obesity and erythropoietic agent in mammals.

Abstract: The process of the present invention transforms 17-keto steroids (I) to the corresponding corticoids (IV) in three steps.

Abstract: This invention provides a method for inhibiting angiogenesis in mammals. A pharmaceutically acceptable formulation containing a compound of the formula ##STR1## where X.sub.1 X.sub.2 and X.sub.3 are H, C1, or F and X.sub.3 must be H if the substituent of R.sub.1 is .alpha.OH;R.sup.1 is chosen from the group consisting of hydroxyl and hydrogen;R.sub.2 is chosen from the group of alkyloxy or thioalkyls wherein said alkyls have less than 5 carbon atomsR.sub.3 is H or an alkyl having less than 6 carbon atoms, is administered to the mammal having undesirable angiogenesis.The wavy line at C-16 refers to either .alpha. or .beta..

Abstract: A multistep process for production of 17.alpha.-acetoxy-1,2-methylene-4,6-pregnadiene-3,20-dione involves ketalization of the 20-keto group of 17.alpha.-hydroxy-1,4,6-pregnatriene-3,20-dione, then methylenation in the 1,2-position with trimethylsulfoxonium iodide, hydrolysis and simultaneous acetylation of the 17.alpha.-hydroxy group.

Abstract: A combination of an aromatase-inhibitor and an antiandrogen in a weight ratio of aromatase-inhibitor to antiandrogen of 20:1 to 1:1 is useful in a method of prophylaxis and/or of treatment by therapy of prostatic hyperplasia. The aromatase-inhibitor is, for example, testolactone and the antiandrogen is, for example, cyproterone acetate.

Abstract: Aromatase-inhibitors are used in a method of prophylaxis and/or treatment by therapy of prostatic hyperplasia. Pharmaceutical preparations suitable for such a use comprise an aromatase-inhibitor. A particularly preferred aromatase-inhibitor is, for example, testolactone.

Abstract: The invention provides new derivatives of vitamin D.sub.3, 2.alpha.-fluorovitamin D.sub.3 and the acylates thereof.The compounds are characterized by vitamin D-like activity in their ability to increase intestinal calcium transport and serum calcium indicating their ready application as substitutes for vitamin D.

Abstract: The syntheses of 25,26-dehydro-1.alpha.,24R-dihydroxycholecalciferol and 25,26-dehydro-1.alpha.,24S-dihydroxycholecalciferol and the epimeric mixture which are useful as differentiation inducing agent and anti-proliferation agents are described. 25,26-dehydro-1.alpha.,24R-dihydroxycholecalciferol, 25,26-dehydro-1.alpha.,24S-dihydroxycholecalciferol, and the epimeric mixture are useful in treating osteoporosis, tumors and leukemia.

Abstract: There is provided the novel compound 11-hydroxypregn-4-en-3-one-20-carbaldehyde, as well as a microbial method for production of the same. This novel compound is of value as a starting material for antiinflammatory corticoids such as hydrocortisone, cortisone, prednisolone and prednisone.

Abstract: This invention relates to a selective acylation process for the preparation of phenolic N-disubstituted carbamate esters of steroids, comprising reacting in an inert solvent an acylating agent being a carbamoyl halogenide, a 4-(tertiary amino)-pyridine, or a complex thereof, optionally as a part of a polymer and a steroid having at least two free hydroxy groups, where at least one is phenolic and at least one is alcoholic, optionally in the presence of an acid acceptor.

Abstract: Disorders of the skin resulting from over androgenicity, such as acne vulgaris, may be treated by applying, to affected areas of the skin, a composition containing a therapeutically effective amount of pregnenolone.

Abstract: 1-Alkyl androsta-1,4-diene-3,17-diones of the formula ##STR1## wherein R.sub.1 is a methyl, ethyl, hydroxymethyl, C.sub.1 -C.sub.3 -alkoxymethyl, or C.sub.1 -C.sub.4 -alkanoyloxymethyl group, R.sub.6 is a hydrogen atom or a methyl group, and R.sub.7 is a hydrogen atom or a methyl group in the 7.alpha.- or 7.beta.-position, are useful for fertility control and for the treatment of estrogen-triggered diseases.

Abstract: Disclosed herein is a pharmaceutical composition in dosage unit form, which comprises a dosage effective for treating osteoporosis of a compound of 24,25-dihydroxycholecalciferol and a pharmaceutically acceptable carrier.

Abstract: A compound of the formula ##STR1## wherein St represents a corticosteroid moiety bonded to the carbonyl via the21-hydroxy group of said corticosteroid;whereinZ is a bond or --O--;whereinn is an integer from 4 to 9;whereinQ is(1) Y--CH.sub.2 COOH wherein Y is --S--, --S(0)--, --S(0.sub.2)--, --SO.sub.2 N(R)--, or --N(R)SO.sub.2 ; R is hydrogen or lower alkyl(C.sub.1 -C.sub.4) with the proviso that the total carbon atoms in R and (CH.sub.2).sub.n is not greater than 10;(2) ##STR2## or (3) ##STR3## wherein R.sub.1 is hydrogen and R.sub.2 is H, CH.sub.3,CH.sub.2 COOH, CH.sub.2 CH.sub.2 COOH, CH.sub.2 OH, CH.sub.2 SH, CH.sub.2 CH.sub.2 SCH.sub.3, or CH.sub.2 Ph--(OH) wherein Ph is phenyl and Ph--(OH) is p-hydroxyphenyl; or R.sub.1 is CH.sub.3 and R.sub.2 is H; or R.sub.1 and R.sub.2 taken together are --CH.sub.2 CH.sub.2 CH.sub.2 --; or N(R.sub.1)CH(R.sub.2) COOH taken together is NHCH.sub.2 CONHCH.sub.2 COOH; and pharmaceutically salts thereof.

Abstract: The invention provides new derivatives of vitamin D.sub.3 and specifically (22E,24R)-1,24-dihydroxy-.DELTA..sup.22 -vitamin D.sub.3 and (22E,24S)-1,24-dihdroxy-.DELTA..sup.22 -vitamin D.sub.3.The compounds exhibit vitamin D-like activity in their ability to stimulate intestinal calcium transport, increase serum inorganic phosphorous and mineralize bone indication ready application of the compounds in the treatment of various metabolic bone diseases. The characteristic of the compounds to not mobilize bone indicates that the compositions would find ready application in combination with vitamin D and various of its derivatives to achieve controlled bone mineralization.

Abstract: Oxymercuration reaction products (I) and/or mercury contaminated steroids (I) are purified by dissolving the compound in a suitable solvent and contacting with a metal dust selected from zinc, copper or iron and a suitable acid.

Abstract: The present invention relates to novel compounds, vitamin supplements, diet pills, and methods for making the same. The vitamin supplements include one or more phytosterol esters, such as esters of sitosterol or stigmasterol, and/or one or more novel substituted fructose compounds. The diet pills within the scope of the invention include antitrypsin, and may be combined with the vitamin supplements to provide diet vitamin supplements.

Abstract: Prodrug compounds for dermal application of topical medicaments, such as 6-aminonicotinamide for treatment of psoriasis, are linked by an enzyme cleavable group to a carrier side chain, such as succinyl piperidate or morpholidate. The neutral lipophilic compounds are rapidly absorbed into the epithelial cells where they are enzymatically cleaved to release the active drug in an ionic form which is retained within the cells.