Abstract: Novel glycosylated steroid derivatives for facilitating the transport of compounds across biological membranes are disclosed. A novel process for efficient synthesis of these glycosylated steroid derivatives, using activated glycosyl sulfoxide intermediates is also provided.

Abstract: Novel compounds of the general formula I ##STR1## and the pharmacologically tolerable addition salts thereof with acids are described, in which eitherIa) R.sup.11 represents a hydrogen atom in the .beta.-configuration and each of R.sup.12 and R.sup.13 represents a hydrogen atom, orIb) R.sup.11 represents a hydrogen atom in the .beta.-configuration and R.sup.12 and R.sup.13 together represent a second bond, orIc) R.sup.11 and R.sup.12 together represent a second bond and R.sup.13 represents a hydrogen atom, orId) R.sup.11 represents a hydrogen atom in the .alpha.-configuration and R.sup.12 and R.sup.13 together represent a second bond,and in Ia), Ib), Ic) or Id)X represents an oxygen atom, the hydroxyimino grouping >N.about.OH or two hydrogen atoms,R.sup.1 represents a hydrogen atom or a methyl group,R.sup.2 represents a hydroxy group, a C.sub.1 -C.sub.10 -alkoxy group or a C.sub.1 -C.sub.10 -acyloxy group, andR.sup.3 and R.sup.

Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.

Abstract: Novel glycosylated steroid derivatives for facilitating the transport of compounds across biological membranes are disclosed. A novel process for efficient synthesis of these glycosylated steroid derivatives, using activated glycosyl sulfoxide intermediates is also provided.

Abstract: The novel compounds of the invention are 19 nor-steroids of the formula: ##STR1## Where A, B, C, D, X, Y, Z, R.sub.17, and R.sup.1 are as defined in the specification, having hormonal properties and their preparation and intermediates.

Abstract: There are provided 13-alkyl-11beta-phenyl-gonanes of formula I ##STR1## wherein Z is an oxygen atom or N--OH;R.sup.2 is alpha- or beta-position methyl or ethyl;R.sup.1 is selected from heteroaryl radicals, cycloalkyl radicals, cycloalkenyl radicals, aryl radicals, alkenyl radicals, and alkyl radicals where R.sup.2 is in the alpha-position and an ethyl radical where R.sup.2 is in the beta-position; andR.sup.3 and R.sup.4 are selected from one of two different groups of substituent pairs, the group from which the selection is made being determined by the position of R.sup.2.

Abstract: 14.beta.-hydroxy-3.beta.-(.alpha.-L-rhamnopyranosyl) and-tridigitoxide-oxy-20-nitro-21-nor-5.beta.,14.beta.-pregnanes exhibit unexpectedly high cardiac potency with tolerance to high dosage levels.

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: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, insomnia and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-aminobutyric acid receptor-chloride ionophore (GR) complex.

Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionophore (GBR) complex.

Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.

Abstract: Disclosed are .DELTA..sup.9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), .DELTA..sup.16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), .DELTA..sup.17(20) -steroids (Va and Vb) and .DELTA..sup.9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.

Abstract: This invention is a compound of formula 1 and pharmaceutically acceptable salts thereof; ##STR1## wherein R.sub.1 is fluorine, chlorine or bromine; wherein R.sub.2 is hydrogen or (C.sub.1 -C.sub.3) alkyl; wherein n is one or 2; wherein R.sub.3 is phenyl, 2-furyl, 3-furyl, 2-thienyl, 3-thienyl, 2-pyridinyl, 3-pyridinyl, 4-pyridinyl; wherein phenyl is optionally substituted with one substituent selected from the group consisting of halogen, trifluoromethyl or sulfonamide. These compounds are useful as hypoglycemic agents.

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: This invention provides novel cyclic hydrocarbons of the formula: ##STR1## wherein R is selected from the group consisting of CH.sub.2 .dbd.CH--CH.sub.2 --, HO--CH.sub.2 CH.sub.2 CH.sub.2 --, and CH.sub.3 ;wherein R.sub.1 is selected from the group consisting of m-trifluoromethylphenylmethyl, 2-thienylmethyl, and p-aminosulfonylphenylethyl;wherein R.sub.2 and R.sub.3 are methyl or hydrogen;wherein R.sub.4 is hydrogen or --OH;a compound of the formula ##STR2## wherein R is (CH.sub.3).sub.2 NCH.sub.2 CH.sub.2 CH.sub.2 -- or NH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 --;or a compound of the formula ##STR3## wherein the dashed line indicates that the 2-3 bond is saturated or unsaturated and, wherein R is hydrogen or methyl.These compounds are useful for inhibiting adverse physiological symptoms associated with phospholipase A.sub.2 and for treating hyperglycemia associated diseases such as diabetes and obesity.

Abstract: The invention relates to androstane-17-carboxylic acid esters, represented by general formula (I): ##STR1## wherein R.sub.1 represents a lower alkyl group containing 1 to 4 carbon atoms, a lower alkyl group containing 2 to 4 carbon atoms substituted by an amino group, or an aralkyl group from 6 to 12 carbon atoms, R.sub.2 and R.sub.3, which may be the same or different, represent a hydrogen atom or a lower alkyl group containing 1 to 4 carbon atoms, R.sub.4 represents a hydrogen atom, a hydroxy group or an acetoxy group, R.sub.5 represents a hydroxy or acetoxy group, or R.sub.4 and R.sub.5 represent together a divalent alkylenedioxy group, R.sub.6 represents a hydroxy group, a methoxy group, or an acetoxy group, R.sub.7 represents a methyl group or a hydroxymethyl group, R.sub.8 represents an hydrogen atom or a hydroxy group and ##STR2## represents either a ##STR3## group or a ##STR4## carbon atom having the double linkage in the 4- or 5-position of the steroid nucleus.

Abstract: The invention relates to novel peptidyl derivatives of Amefalone, Pro-Amefalone, Pro-Pro-Amefalone and D-Ala-Pro-Amefalone, their halide, preferably hydrochloride, salts, to a process for their synthesis and to their use as antiarrhythmic agents.

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. This disclosure also relates to a novel class of tracer compounds employed as reagents in fluorescence polarization immunoassays.