Abstract: The invention relates to a process for catalytic hydrogenation of non-hormonal unsaturated plant steroids and unsaturated plant-based fatty acids and triglycerides thereof using a metal catalyst bound to a polymer support containing grafted groups. The invention also relates to regeneration of a used catalyst.

Abstract: The invention relates to a composition, in particular a cosmetic or dermatological composition, having an aqueous dispersion of vesicles with a lipid membrane, characterized in that the lipid membrane contains at least one carbamate of following formula (I): ##STR1## wherein R.sub.1 and R.sub.2 are defined in the specification.

Abstract: The invention concerns a fat based food product comprising natural fat components which have a blood cholesterol lowering effect in amounts sufficient to obtain a blood cholesterol lowering effect, wherein the fat comprises at least 1% of a sterol composition which comprises sterols of which at least 40% is esterified with fatty acid esters.

Abstract: The present invention relates to phytosterol protein complex which is comprised of an amount of phytosterol, an amount of protein, and an amount of edible oil, with the phytosterol protein complex designed to increase the bioavailability of the phytosterol, so that if consumed on a regular basis hopefully cholesterol levels will be lowered in the subject consuming the phytosterol protein complex. The present invention also relates to methods for forming the phytosterol protein complex, methods for potentially lowering cholesterol in humans, and methods for forming food products made from the phytosterol protein complex.

Abstract: The present invention relates to transgene expression systems, related pharmaceutical compositions, and methods of making and using them. Preferred systems employ an adenovirus transgene expression vector comprising DNA sequence encoding a transgene which codes for a desired product, expressibly contained within an adenovirus vector containing at least a portion of the E3 region and certain portions of the E4 region. The E4 portions comprise the open reading frame sequence known as E4ORF3 and at least one other portion of E4. Preferably the E4 portion of the vector (or "E4 cassette") includes E4ORF3 and at least one other portion selected from E4ORF4, E4ORF6/7 and E4ORF3/4. The invention has a number of important features including improving persistency of transgene expression in a desired host cell. The transgene expression systems of the present invention are useful for a variety of applications including providing persistent cellular expression of the transgene in vitro and in vivo.

Abstract: Lanolin eaters of silicones are prepared by reacting a carboxy silicone and lanolin alcohol to form an ester. The resultant products are useful as highly water resistant lubricating coatings for skin.

Abstract: Novel compounds useful as inhibitors of estrone sulfatase are provided. The compounds have the structural formula (I) wherein r1 is an optional double bond, R.sup.1 and R.sup.2 are selected from the group consisting of hydrogen and lower alky, or together form a cyclic substituent (II) ##STR1## wherein Q is NH, O or CH.sub.2, and the other various substituents are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat estrogen-dependent disorders are provided as well.

Abstract: 16.alpha., 17.alpha.-dialkylated steroids are prepared by reacting a 16.alpha.-alkyl-17(20)-enyl-20-silyl ether with an alkylating agent and an enol silyl ether cleaving agent in a suitable solvent.

Abstract: Stanol fatty acid ester composition comprising at least 85% of stanol (saturated) fatty acid esters in which at least 85% of the fatty acid groups are saturated. Also claimed is a process for the preparation of stanol fatty acid esters, by hardening phytosterol fatty acid or a mixture thereof, or as an alternative, a process for the preparation of stanol fatty acid esters by esterification of phytosterols or a mixture thereof, followed by the hardening of the so obtained phytosterol fatty acid esters.

Abstract: Cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile.

Abstract: Cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile.

Abstract: Novel cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. By this invention, such cationic amphiphile is used in a state in which it is capable of accepting additional protons, i.e., it is not fully protonated. For purposes of this invention, cationic amphiphiles may be considered to encompass four general categories: (A) T-shaped/steroid-based amphiphiles; (B) T-shaped/non steroid-based amphiphiles; (C) non T-shaped/steroid based amphiphiles and (D) non T-shaped/non steroid-based amphiphiles.

Abstract: Fatty acid derivatives of sulfhydryl-containing compounds (for example, sulfhydryl-containing peptides or proteins) comprising fatty acid-conjugated products with a disulfide linkage are employed for delivery of the compounds to mammalian cells. This modification markedly increases the absorption of the compounds by mammalian cells relative to the rate of absorption of the unconjugated compounds, as well as prolonging blood and tissue retention of the compounds. Moreover, the disulfide linkage in the conjugate is quite labile in the cells and thus facilitates intracellular release of the intact compounds from the fatty acid moieties.

Abstract: Novel compositions are provided. Typically, the compositions comprise one or more neutral co-lipids and also a cationic amphiphile. Therapeutic compositions are prepared according to the practice of the invention by contacting a therapeutically active molecule with a dispersion of neutral co-lipid(s) and amphiphile(s).

Abstract: Cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile.

Abstract: This invention provides for methods of reducing cholesterol uptake by a cell. The invention is premised in part on the discovery of a new mechanisms by which free cholesterol (FC) is internalized into a cell from low-density lipoproteins. Inhibition of this mechanism reduces the internalization of free cholesterol into cholesterol transport vesicles thereby reducing free cholesterol content of the cell at physiological concentrations of LDL and HDL.

Abstract: The present invention provides a protein or polypeptide substance having at least one amino group bonded to a polyethyleneglycolosy group represented by the following general formula;R.sub.1 --(OCH.sub.2 CH.sub.2).sub.n --O--(wherein R.sub.1 represents an optionally substituted cholesteryl group; and n represents a positive integer which is arbitrarily variable), and a method for producing said the protein or polypeptide.The present invention also provides a reactive polyethyleneglycol derivative as an intermediated for above the method.The chemically modified protein or polypeptide of the present invention never impairs bonding with a receptor and has a high plysiological activity. Then, a behaviors in vivo of these substance is improved. Now medical substances or drugs having a high pharmacological activity can be developed by using these substance.

Abstract: 21-norvitamin D.sub.3 analogs in which the methyl group normally attached to the side chain at carbon 20 has been replaced by a hydrogen atom. The compounds are characterized by a marked intestinal calcium transport activity while exhibiting much lower activity than 1.alpha.,25-dihydroxyvitamin D.sub.3 in their ability to mobilize calcium from bone. Because of their preferential calemic activity, these compounds would be useful for the treatment of diseases where bone formation is desired, such as osteodystrophy. Novel intermediates formed during the synthesis of the end products are also disclosed.

Abstract: Novel cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. The amphiphiles contain lipophilic groups derived from steroids, from mono or dialkylamines, or from alkyl or acyl groups; and cationic groups, protonatable at physiological pH, derived from amines, alkylamines or polyalkylamines. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile.

Abstract: Novel cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. The amphiphiles contain lipophilic groups derived from steroids, from mono or dialkylamines, or from alkyl or acyl groups; and cationic groups, protonatable at physiological pH, derived from amines, alkylamines or polyalkylamines. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile.

Abstract: Novel cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. The amphiphiles contain lipophilic groups derived from steroids, from mono or dialkylamines, or from ether or ester-linked alkyl groups, and cationic groups, protonatable at physiological pH, derived from amines, alkylamines or polyalkylamines. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile.

Abstract: A method for determination of activity of a cholesterol oxidase comprises the following steps. A monomolecule film comprising a sterol and a phospholipid is formed on a surface of a cholesterol oxidase solution. Subsequently, a surface pressure of the monomolecule film is measured in order to find a rate of increase in the surface pressure of the monomolecule film where a magnitude of the activity of the cholesterol oxidase is defined by the rate of increase in the surface pressure.

Abstract: Novel antiandrogenic agents are provided. An exemplary group of compounds has the structural formula (I) ##STR1## wherein R.sup.1 through R.sup.10, a and b are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat androgen-related clinical conditions are provided, as are methods and compositions for using the compounds as contraceptive agents.

Abstract: Novel cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. The amphiphiles contain lipophilic groups derived from steroids, from mono or dialkylamines, or from alkyl or acyl groups; and cationic groups, protonatable at physiological pH, derived from amines, alkylamines or polyalkylamines. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile.

Abstract: Disclosed are anti-obesity agents comprising 3-ketosteroidal compounds as defined in the specification. The present invention also discloses pharmaceutical compositions and use of these compounds in the prevention and treatment of obesity.

Abstract: The invention pertains to vitamin D amide derivatives of formula (I). These novel 1.alpha.-hydroxy vitamin D derivatives and their 20-epi analogues comprise compounds of formula (I) and corresponding 5,6-trans isomers, where Y represents an alkylene or alkenylene group containing up to four carbon atoms; R.sup.1 and R.sup.2 independently represent a hydrogen atom or a lower alkyl or cycloalkyl group, or R.sup.1 R.sup.2 N-- represents a heterocyclic group; and R.sup.3 and R.sup.4 independently represent a hydrogen atom or an O-protecting group. Active compounds, in which R.sup.3 and R.sup.4 are hydrogen atoms or metabolically labile O-protecting groups exhibit potent cell modulating effect, but minimal effect on calcium metabolism.

Abstract: The invention provides a process for preparing high-purity cholesterol, the process comprising selectively reducing the impurities (mainly desmosterol) contained in a crude cholesterol to cholesterol.According to the invention, high-purity cholesterol can be obtained in a yield of at least 85%, the cholesterol containing 0.3% or less of desmosterol, 0.5% or less of dihydrocholesterol and having a purity of at least 99% after reduction and crystallization.

Abstract: Novel cationic amphiphiles are provided that facilitate transport of biologically active molecules into cells. Typically, the amphiphiles contain lipophilic groups derived from steroids or from mono or dialkylamines, and two cationic groups, protonatable at physiological pH, derived from amines, alkylamines or polyalkylamines. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles, with or without colipids, and therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, polypeptides and low molecular weight organic compounds. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells.

Abstract: Compounds having a broad range of antimicrobial activity generally have a structure including asteroid nucleus with a cationic, preferably polyamine, side chain (X) and an anionic side chain (Y). The invention is also directed to compounds of the Formula III: ##STR1## preferably where the steroid ring nucleus is saturated; the steroid ring substituent Z.sub.5 is .alpha.-H; one Z.sub.7 is .beta.-H and the other is .alpha.-H or .alpha.-OH; both substituents Z.sub.12 are hydrogen; X' is a polyamine side chain of the formula --NH--(CH.sub.2).sub.p --NH--(CH.sub.2).sub.q --N(R.sup.II)(R.sup.III) where p and q are each independently 3 or 4, and R.sup.II and R.sup.III are each independently hydrogen or methyl; R' is methyl; and Y' is (C.sub.1 -C.sub.10)-alkyl substituted with a group such as --CO.sub.2 H or --SO.sub.3 H.

Abstract: A nucleic acid transporter to deliver a nucleic acids into cells, comprising a cationic compound having a cationic head group for binding the nucleic acid and a lipid tail for association with the membrane. A cationic compound usually is a polyamine or a short basic peptide. The lipid tail is usually selected from the group consisting of plant steroid, animal steroid, isoprenoid compound, aliphatic lipid, pore forming protein, pore forming peptides and fusogenic peptides. The cationic head and the lipid tail are linked through a carbamate linkage. When polyamine is used, it is preferably either spermidine or spermine and the nucleic acid can be any of a variety, including triplex forming oligonucleotides, antisense oligonucleotide, aptamers, ribozymes, plasmids and DNA for gene therapy. Also described is a method for treating individuals using the transporter linked to a therapeutic nucleic acid.

Abstract: The present invention provides an anti-obesity agent comprising 4-cholesten-3-one represented by the following formula: ##STR1## as an effective component. The anti-obesity agent of the present invention is useful because of inhibition effect of body weight increase and body fat accumulation. The present invention also provides a medicinal composition comprising 4-cholesten-3-one as an effective component and a pharmaceutically acceptable excipient as well as methods for preventing and treating obesity comprising administering an effective amount of 4-cholesten-3-one to a person.

Abstract: Pharmaceutical and nutritional compositions are disclosed containing, in association with a suitable diluent or carrier, at least 10% by weight of a cholesterol fatty acid ester where the fatty acid is gamma-linolenic acid, dihomo-gamma-linolenic acid, adrenic acid, the 22:5 n-6 acid, stearidonic acid, the 20:4 n-3 acid, eicosapentaenoic acid, docosahexaenoic acid, the 22:5 n-3 acid or columbinic acid. Novel cholesterol columbinic acid esters are described.

Abstract: The present invention is a method of protecting a sulfonic acid functional group in an organic molecule as a substituted or unsubstituted neopentyl sulfonate ester. The method allows the conversion of R--SO.sub.3 --H to R'--SO.sub.3 --H, wherein R and R' are different organic radicals. Also disclosed is a method of increasing the bioavailability of drugs with a sulfonic acid functional group by protecting the sulfonic acid functional group as a substituted neopentyl sulfonate ester which has a masked heteroatom nucleophile. The masked nucleophile can be liberated in vivo, resulting in removal of the neopentyl protecting group and regeneration of the parent drug.

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: Novel bile acids according to the general formula ##STR1## wherein R.sub.1 represents a hydroxyl group, R.sub.2 and R.sub.3 both represent a hydrogen or a hydroxyl group, or R.sub.2 represents a hydroxyl group or a .beta. hydroxyl group and R.sub.3 represents a hydrogen or R.sub.3 represents a hydroxyl group and R.sub.2 represents a hydrogen, and R.sub.4 represents a (CH.sub.2).sub.n R.sub.5 wherein n is from 1 to 6, and R.sub.5 represents --0--PO(OH).sub.2, --CH(OH)COOH, a nitrogen containing saturated heterocyclic ring group, NR.sub.6 R.sub.7, wherein R.sub.6 and R.sub.7 are the same or different and each represent hydrogen or a C.sub.1 -C.sub.10 alkyl group or CO--R.sub.8 wherein R.sub.8 represents an amino acid moiety, R-phenylglycine, 12-aminododecanoic acid or 4-aminohippuric acid are synthesized from cholic, deoxycholic, chenodeoxycholic, ursodeoxycholic and lithocholic acids and iodo-derivatives thereof by known processes and/or by novel processes according to the present invention.

Abstract: A process for the production of 1-methyl-3-keto-.DELTA..sup.1,4 steroids of general formula I ##STR1## in which St symbolizes the radical of asteroid molecule, where a 3-keto-.DELTA..sup.1,4 steroid of general formula II ##STR2## in which St has the above-mentioned meaning, is reacted in an inert solvent in the presence of a nickel salt soluble therein with an organometallic compound of formula III, IV or V ##STR3## where X, Y.sub.1, Y.sub.2, Y.sub.3, Z.sub.1 and Z.sub.2 are as defined in the specification.

Abstract: Oligonucleotides having a low molecular weight tail molecules joined to the 3' terminus of the oligonucleotide via a linking molecule of the structure:Z is ##STR1## wherein ##STR2## m and m' are positive integers less than 11, n is 0 or 1 and Q is a connecting group, are synthesized by selectively reacting three independent functional groups on the linking molecule, i.e., an amine, a primary hydroxyl and a secondary hydroxyl, in a stepwise manner. A tail molecule R is first connected to the amino functionality of the linking molecule. Next the linking molecule-tail molecule combination is attached to a solid state support via the secondary hydroxyl group. The oligonucleotide is systematically stepwise synthesized beginning on the primary hydroxyl group followed by release of the oligonucleotide having the low molecular weight tailed joined to its 3' terminus from the solid state support.

Abstract: A process for the selective oxidation of a primary or secondary alcohol to an aldehyde or ketone and for the oxidation of a 1,2-diol to an .alpha.-ketol or .alpha.-diketone, which comprises contacting the alcohol or 1,2-diol with o-iodoxybenzoic acid. This process is suited for selective oxidation of alcohols containing easily oxidizable groups, such as amino or thioether groups and easily oxidizable heterocycles.

Abstract: Lipid-selective antioxidants of the formula I(A).sub.a (L)(X).sub.a, (I),in whichA=an antioxidative component,L=a bridging member,X=a lipophilic componenta and a'=independently of one another the numbers 1 or 2.The compounds are used for the protection of lipid-containing substances against oxidation and in pharmaceuticals for the prophylaxis and treatment of diseases in which bioradicals are involved, in particular of coronary, circulatory and vascular diseases.

Abstract: There are described spontaneously dispersible agents containing sterolester and/or sterolphosphor compounds having a pronounced antitumour activity. Novel sterolesters and sterolphosphor compounds, their use for treating tumors, and processes for their preparation are disclosed.

Abstract: The invention pertains to vitamin D amide derivatives of formula (I). These novel 1.alpha.-hydroxy vitamin D derivatives and their 20-epi analogues comprise compounds of formula (I) and corresponding 5,6-trans isomers, where Y represents an alkylene or alkenylene group containing up to four carbon atoms; R.sup.1 and R.sup.2 independently represent a hydrogen atom or a lower alkyl or cycloalkyl group, or R.sup.1 R.sup.2 N-- represents a heterocyclic group; and R.sup.3 and R.sup.4 independently represent a hydrogen atom or an 0-protecting group. Active compounds, in which R.sup.3 and R.sup.4 are hydrogen atoms or metabolically labile 0-protecting groups exhibit potent cell modulating effect, but minimal effect on calcium metabolism.

Abstract: The present invention relates to an oligonucleotide or analog thereof conjugated to a molecule comprising a structure, which structure (a) is of substantially fixed conformation; (b) contains, is directly attached to, or is attached to a carbon atom that is directly attached to, an first amine; and (c) contains, is directly attached to, or is attached to an atom that is directly attached to a phosphate, a second amine, or a cationic sulfur. In a preferred embodiment, the structure consists of at least a nonaromatic cyclic portion or substituted derivative thereof. In a specific embodiment, the structure is a nonaromatic cyclic compound. In another embodiment, the molecule is a steroid. In yet another particular aspect, the structure is an aromatic compound. In another embodiment, the structure can bind to a nucleic acid sequence in a nonintercalative manner.

Abstract: 8-En-19,11.beta.-bridged steroids of general formula I ##STR1## that have the 8,9-double bond as a new structural feature, and a process for their production are described. The substituents R.sup.1 R.sup.4 -Y, R.sup.4' -Y.sup.', X and Z have the meaning indicated in the description. The new compounds especially have at their disposal pronounced antigestagen effectivenss and are suitable for the production of pharmaceutical preparations.

Abstract: Mixtures of compounds of ##STR1## or a mixture of the latter and a compound of the formula ##STR2## which are useful intermediates for the preparation 20-keto-21(S)-hydroxy steroids.

Abstract: The present invention relates to N-acylglutamine derivatives of formula (I): ##STR1## The N-acylglutamine derivatives are well compatible with oily bases and have good skin-moisturizing activity and hair growth-stimulative effect. These are useful as cosmetics and hair growth stimulants.

Abstract: A process for the preparation of a compound of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 3 carbon atoms, R.sub.2 is alkyl of 1 to 12 carbon atoms, R.sub.3 is alkyl of 1 to 4 carbon atoms comprising reacting a compound of the formula ##STR2## wherein R.sub.4 is a remainder of an easily cleavable ether, K is a protected ketone function in the form of ketal, thioketal or mixed ketal and R.sub.1 has the above definition with a magnesium organic compound reagent of the formulaHalMg--CH.sub.2 --R.sub.2 Awherein Hal is a halogen and R.sub.2 is defined as above to obtain a compound of the formula ##STR3## wherein R.sub.1, R.sub.2 and K are defined as above, reacting the latter with an acylation agent to obtain a compound of the formula ##STR4## wherein R.sub.5 is alkyl of 1 to 6 carbon atoms or aryl of 6 to 10 carbon atoms and R.sub.1, R.sub.2 and K are defined as above, reacting the latter with an appropriate alkylation agent to obtain a compound of the formula ##STR5## wherein R.sub.1, R.sub.2, R.sub.

Abstract: An improved process for the preparation of 20-keto-21(S)-hydroxy steroids of the Formula ##STR1## wherein R.sub.1 is alkyl of 1 to 3 carbon atoms, R.sub.2 is alkyl of 1 to 12 carbon atoms, and R.sub.3 is alkyl of 1 to 4 carbon atoms and novel intermediates therefrom.

Abstract: There are provided pregnane derivatives represented by formula ##STR1## wherein A.sup.1 represents a hydrogen atom or a hydroxyl group, A.sup.2 represents a substituent such as a hydroxyl group when A.sup.1 represents a hydrogen atom, or A.sup.2 represents a hydrogen atom when A.sup.1 represents a hydroxyl group, or A.sup.1 and A.sup.2 are combined together to form an oxo group; D.sup.1 represents a substituent such as a hydroxyl group, and D.sup.2 represents a hydrogen atom, or D.sup.1 and D.sup.2 are combined together to form an epoxy group or a single bond; D.sup.3, D.sup.5 and D.sup.7 each represents a hydrogen atom, D.sup.4 represents a hydroxyl group, and D.sup.6 represents a substituent such as a hydroxyl group, or D.sup.3 and D.sup.4 may be combined together to form an epoxy group or a single bond, or D.sup.4 and D.sup.5 may be combined together to form a single bond, or D.sup.5 and D.sup.6 may be combined together to form an epoxy group or a single bond, or D.sup.6 and D.sup.

Abstract: The process of the invention comprises reacting a C-22-halo-23,24-bisnorsteroid or C-22-halo-23,24-bisnor-9,10-secosteroid with a nickel complex of an electron withdrawing alkene of the formula ##STR1## wherein R.sub.1 is hydrogen, hydroxycarbonyl, lower alkoxycarbonyl, lower alkylcarbonyl or unsubstituted or substituted lower alkyl, and R.sub.2 is hydroxyl, lower alkoxy, or unsubstituted or substituted lower alkyl, to yield a C-25 or C-26 precursor of the formula ##STR2## which is appropriately functionalized for conversion into the corresponding steroid or secosteroid by treatment as hereinafter described.

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.