Abstract: The disclosure relates to novel 1.alpha.,7.alpha.-dithio-substituted spirolactones of general Formula I ##STR1## wherein R.sup.1 is C.sub.1-3 -alkyl and C.sub.1-3 -acyl andR.sup.2 is hydrogen, C.sub.1-3 -alkyl and C.sub.1-3 -acyl,to their preparation, and to their use as medicinal agents.The compounds of this invention exhibit anti-aldosterone activity and show the profile of effectiveness of a pro-drug.

Abstract: A new class of macrocylic polyethers having a crown ether attached to a steroid by various connector units have been prepared. These novel structures have applications as ionophores and they form unique, nonionic vesicles (niosomes).

Abstract: A non-stinging aqueous anti-inflammatory steroid formulation suitable for intranasal administration comprises: an anti-inflammatory steroid in an amount between about 0.01% and about 0.05% (w/v); propylene glycol in an amount between about 2% and about 10% (w/v); PEG 400 in an amount between about 10% and about 25% (w/v); polysorbate 20 in an amount between about 1% and about 4% (w/v); an effective amount of a preservative; an effective amount of a stabilizer; an effective amount of an antioxidant; water; and pH buffering agent sufficient to adjust the pH of the resulting solution to between about 3.5 and about 7.

Abstract: Glycoesters of estradiol (E.sub.2) and of estriol (E.sub.3) of Formula I(E.sub.2,3)--O--CO--CH.sub.2 --Z (I)whereinZ is hydroxy or the group --O--CO--R whereinR is methyl or phenyl,provide a uniform and enduring estrogen level especially when used in the form of an aqueous crystalline suspension.

Abstract: 13.alpha.-alkylgonanes of formula I ##STR1## where R is an acyl radical with as many as 10 C-atoms, andX is an oxygen atom or the grouping N--OH,have a strong antigestagenic effect and can be used for postcoital fertility control.

Abstract: A pharmaceutical or dietetic composition for the prevention and treatment of vascular, arteriosclerotic and thrombotic pathologies, comprised of lecithin and oils having a high content of eicosapentaenoic (C 20:5, n-3) and/or docosahexaenoic (C 22:6, n-3) acids, and/or esters thereof.Said composition affords a considerable enhancement of vascular pathologies therapy by the use of natural ingredients commonly employed in human nourishment without any trouble.

Abstract: There is disclosed a cholesterol level-lowering agent which comprises as a main component a strongly basic anion exchange resin having imidazolium salts as functional groups, said resin being a copolymer of (A) a high molecular quaternary salt and (B) a polyfunctional epoxy compound having two or more oxirane rings.

Abstract: 6.alpha.,16.beta.-Dimethyl corticoids of general Formula I ##STR1## wherein the bond .sub.-------- is a single bond or a double bond, andX is a hydrogen atom, a fluorine atom, a chlorine atom, or a bromine atom,Z is a hydrogen atom or, jointly with X, is a carbon-carbon bond,R.sub.1 is a formyl group, an alkanoyl group or alkoxyalkyl group of 2-8 carbon atoms, or a benzoyl group, andY is a hydrogen atom or a methyl group,are pharmacologically active compounds.

Abstract: Steroids of the formula: ##STR1## which are characterized by a 17.alpha.-cyanomethyl, azidomethyl, methoxymethyl, phenylmethyl, or ethynylmethyl substituent and a 17.beta.-hydroxy/esterified hydroxy substituent. The steroids of this invention have glucocorticoid, anti-glucocorticoid, progestational, or anti-progestational activity, depending on the particular structure.

Abstract: Urinary calculi commonly known as kidney stones are eliminated by the oral administration of triglycine or other suitable chelating agent in amounts appropriate to either the solubilization of preformed urinary calculi and/or to the prevention of the precipitation of alkaline earth compounds in the urinary track, which comprise an estimated 85% of such calculi.

Abstract: The invention relates to a novel prodrug compound useful in the treatment of tumors, of the formula:A--CO(CH.sub.2).sub.m (NHCO).sub.n --RwhereinA is a residue of an antitumor substance having >NH or --NH.sub.2 group in the molecule,R is a residue of cholesterol,m is an integer of 1 or 2 andn is 0 or 1,and its salts.

Abstract: A method of inhibiting angiogenesis in a warm blooded animal which comprises administering to said animal an anti-angiogenic effective amount of a compound of the formula: ##STR1## wherein the dotted line between positions C-1 and C-2 means the presence or absence of a double bond; the .about.bond at C-6 denotes .alpha. or .beta.;wherein R.sub.1 is CH.sub.3 or --C.sub.2 H.sub.5 ;wherein R.sub.2 is H, and R.sub.3 is in the .alpha.-position and is --OH, --O-alkyl(C.sub.1 -C.sub.12), --OC(.dbd.O)alkyl(C.sub.1 -C.sub.12), --OC(.dbd.O)aryl, --OC(.dbd.O)N(R).sub.2, or --OC(.dbd.O)OR.sub.7, wherein aryl is furyl, thienyl, pyrrolyl, or pyridyl wherein each of said hetero moiety is optionally substituted with one or two (C.sub.1 -C.sub.4)-alkyl groups or aryl is --(CH.sub.2).sub.f -phenyl wherein f is 0 to 2 and wherein the phenyl ring is optionally substituted with one to three groups selected from chlorine, fluorine, bromine, alkyl(C.sub.1 -C.sub.3), alkoxy(C.sub.1 -C.sub.3), thioalkoxy(C.sub.1 -C.sub.3), Cl.sub.

Abstract: The invention relates to 6-substituted androsta-1,4-diene-3,17-dione derivatives wherein the 6 substituent is an azido, amino or substituted amino group.The invention provides also a process for preparing the said compounds and pharmaceutical compositions containing same.The compounds of the invention are useful aromatase inhibitors and can be used, e.g., in the treatment of hormone-dependent tumors.

Abstract: The invention is directed to the preparation of hydroxylated compounds of the vitamin D.sub.2 series and specifically to a process for synthesizing 1.alpha.,25-dihydroxyvitamin D.sub.2, 1.beta.,25-dihydroxyvitamin D.sub.2, their corresponding 5,6-trans isomers and the C-24 epimers of these compounds.The hydroxylated vitamin D.sub.2 compounds obtained exhibit vitamin D-like activity and can be substituted for vitamin D.sub.3 or various of its known metabolites where such compounds are applied.

Abstract: The endometrial maturation in the post-ovulatory phase (luteal phase) of mammals is delayed with reference to the nidation point by administration of antigestagens.

Abstract: Compounds of the formula: ##STR1## wherein one X is COOR, CH.sub.2 COOR, CH(COOR).sub.2, CONHR, CH.sub.2 CONHR, or CNremaining X's are H, F, CH.sub.3, OH, COOR, CH.sub.2 COOR, CH(COOR).sub.2, CONHR, CH.sub.2 CONHR, or CN;Y is ##STR2## R is H, alkyl of 1-5 carbon atoms, or benzyl; R.sub.1 is CH.sub.2 OR.sub.3, COOR, or CONHR;R.sub.2 is H, OR.sub.3, or BR;R.sub.3 is H, COR.sub.4, or tetrahydropyranyl;R.sub.4 is alkyl of 1-5 carbon atoms or benzyl;R.sub.5 is H or COR.sub.4 ;represents a single or double bond;represents .alpha.-position, .beta.-position, or a mixture of .alpha.- and .beta.-positions; and--- represents .alpha.-position;and methods for preparing the same.

Abstract: This invention relates to a method of controlling phytopathogenic rust and smut fungi of the Uredinales order in a plant locus which comprises applying a fungicidally effective amount of an ornithine decarboxylase inhibitor.

Abstract: A novel process for the stereospecific preparation of a 24(R),25- and 24(S),25-dihydroxycholecalciferol. Also provided are novel intermediates used in the above process, being 22-p-toluenesulfonyl derivatives of 23,24,25,26,27-pentanorcholecalciferol and of 24(R)- and 24(S),25-dihydroxycholecalciferol.

Abstract: New processes for preparing new steroid derivatives including ergosta-1,5,7,22-tetraen-3.beta.-ol, 1.alpha.-hydroxyergosteryl diacetate, etc. which are useful intermediates in the synthesis of 1.alpha.-hydroxy vitamin D.sub.2. The processes include the new steps of reacting ergosta-1,4,6,22-tetraen-3-one with isopropenyl acetate in the presence of an acid catalyst followed by reduction to ergosta-1,5,7,22-tetraen-3.beta.-ol. The overall yield leading to 1.alpha.-hydroxy vitamin D.sub.2 is dramatically increased.

Abstract: The invention relates to biodegradable compositions which continuously release estradiol in a uniform manner over extended periods of time and do not exhibit initial release of undesirably high levels of active ingredient.The invention also relates to a method for preparation of the compositions, and a method for administering estradiol parenterally to feedlot animals in a continuous and uniform fashion over extended periods of time.