Abstract: Benzocycloheptenes of general formula I in which R1, R2 and Y have the meanings indicated herein, have antiestrogenic activity on and are suitable for the production of pharmaceutical agents, especially for prophylaxis and therapy of osteoporosis.

Abstract: Disclosed is a process for forming an azomethine compound, comprising: (a) reacting a compound “A” having an active methylene group or methine group with an arylprimaryamine compound “B”; (b) in the presence of a base and an oxidizing agent and in a solvent medium containing a ketone compound having the formula R1C(O)R2 wherein R1 and R2 are independently C1-C4 alkyl groups; (c) at a temperature low enough to provide a yield of the azomethine product of at least 50 mole % based on compound A.

Abstract: The invention concerns a method for the condensation of aromatic derivative(s) or a sulphinic derivative by a perhalogenated, advantageously perfluorinated, carbon atom. Said method is characterized in that it consists in subjecting said sulphinic derivative and said aromatic derivative to the action of a strong acid whereof the pKa is not more that 0. The invention is applicable to organic synthesis.

Abstract: The present invention discloses highly packed polycationic ammonium, sulfonium and phosphonium lipid compounds useful for making lipid aggregates for delivery of macromolecules and other compounds into cells. They are especially useful for the DNA-dependent transformation of cells. Methods for their preparation and use as intracellular delivery agents are also disclosed.

Abstract: The present invention relates to a sulfation process comprising the steps of: a) reacting a tertiary amine with a sulfation precursor having the formula: wherein R1 is C1-C22 alkyl, C7-C22 alkylenearyl, and mixtures thereof; to form an admixture comprising a quaternized amine and a sulfating species; and b) reacting a hydroxyl species with said admixture to form a sulfated hydroxyl species. The process of the present invention is adaptable to sulfating a wide range of alcohols including the hydroxyl unit which terminates a polyalkoxylate moiety which are prevalent in the area of surfactants, inter alia, alkyl ethoxy sulfates.

Abstract: The present invention provides a process for making sulfoxides from sulfides. The process includes the step of selectively oxidizing a sulfide utilizing a perborate or a percarbonate as an oxidizing agent.

Abstract: One aspect of this invention relates to processes for solidifying dimethylsufoxide including the steps of partially solidifying a liquid phase including dimethylsulfoxide and one or more impurities, to form a mixture comprising solid dimethylsulfoxide and a liquid residue, and substantially separating the solid dimethylsulfoxide from the liquid residue, wherein the liquid residue comprises liquid dimethylsulfoxide and at least a portion of the impurities, and wherein the liquid residue is not subsequently treated by any step of partial solidification. In certain embodiments of the processes of the invention, ultra-high purity DMSO that exceeds the purity specifications for U.S.P. grade DMSO can be produced by employing solidification, fractional solidification and/or melt crystallization processes.

Abstract: The present invention provides an efficient dimethyl sulfoxide (DMSO) production process improved in the conversion from dimethyl sulfide (DMS) to DMSO by recycling the NOx used as a catalyst in the continuous oxidation reaction of DMS for producing DMSO, specifically providing a DMSO production process improved in the recovery rate and/or absorption rate of NOx by recovering NOx from the reaction off gas and/or the gas removed from the reaction product solution for re-utilization.

Abstract: This invention describes the new benzocycloheptenes of general formula I 1

Abstract: The subject invention provides a binuclear metal complex having structure (I) wherein M1, and M2 are independently selected from the group consisting of Fe, Co, Mn and Ru; wherein m and n are independently +2 or +3; wherein R1, R2, R3, R4, R5 and R6 are independently a linear C1-C6 alkyl, C5-C6 cycloalkyl, phenyl, etc.; wherein (i) R1 and R2, (ii) R3 and R4, or (iii) R5 and R6 independently and optionally are linked covalently and together with the respective adjoining C atom comprise a spirocyclic ring; wherein i, j and k are integers such that 2≦i+j+k≦4; wherein p is 1 or 2, and q is 0, 1 or 2 such that m+n−4=p×q; wherein (i) R1 or R2 and R3 or R4, (ii) R3 or R4 and R4 or R5, or (iii) R1 or R2 and R5 or R6 independently and optionally are linked covalently and together with the respective adjoining C atoms comprise a fused ring; wherein Ar is 1,2-phenylene, 1,2- or 2,3-naphthylene, etc.

Abstract: The present invention is directed to a new process for the synthesis of vinyl sulfoxides, in particular diarylvinyl sulfoxides

Abstract: There is provided a compound of the formula[I]: wherein R represents a hydrogen atom or a protective group for a hydroxyl group; and A represents a hydrogen atom, a halogen atom or a group of the formula A1: Q represents Q3: when A represents a halogen atom or a protective group for a hydroyl group, A represents Q4:  wherein R1 and R2 represent a hydrogen atom or a protective group for a hydroxyl group; and when A represents a hydrogen atom, Q is Q2:

Abstract: Hybrid electron donor compounds, suitable for use as adhesives or as components in adhesives, contain a carbon to carbon double bond attached to an aromatic ring and conjugated with the unsaturation in the aromatic ring and a vinyl ether moiety.

Abstract: Compounds containing both electron donor and electron acceptor functionality are suitable for use in adhesives. The electron donor group is a carbon to carbon double bond attached to an aromatic ring and conjugated with the unsaturation in the ring. The electron acceptor group is a maleimide, acrylate, fumarate or maleate.

Abstract: The invention relates to novel biaromatic compounds having general formula I and their use in pharmaceutical compositions for use in human and veterinary medicine, in particular for treating dermatological, rheumatic, respiratory, cardiovascular, and ophthalmological disorders, and for use in cosmetic compositions.

Abstract: The naphthyloxyacetic acid derivatives of the formula (I) wherein A is H, -(alkylene)COOR1, -(alkylene)CONR2R3, -(alkylene)OH, -(alkylene)tetrazole, -(alkylene)CN; E is single bond or alkylene; G is —S—, —SO—, —SO2—, —O— or —NR4—; L is alkylene, —(CH2)m—CH═CH—(CH2)n— or —(CH2)x—CH(OH)— (CH2)y—; M is phenyl, phenyl(thio, oxy, amino), diphenylmethyl, diphenylmethyl(thio, oxy, amino), and pharmaceutical composition comprising them as an active ingradient. The compounds of the formula (I) can combine PGE2 receptor and exhibit the activity to antagonize or agonize for PGE2 receptor. Therefore, they are useful as anti-hyperlipemia, for the prevention of abortion, for analgesics, as antidiarrheals, sleep inducer, diuretic, anti-diabetes, abortient, cathartics, antiulcer, anti-gastritis or antihypertensive etc.

Abstract: This invention relates to new antiestrogens of the general formula ##STR1## in which the substituents have the meanings that are explained in more detail in the description.The new compounds are a) pure antiestrogens or b) antiestrogens with partial estrogenic action (tissue-selective estrogens).Based on these properties, the new compounds are suitable for the production of pharmaceutical agents: in the case of a), for example, for the treatment of breast cancer; in the case of b), for example, for hormone replacement therapy.

Abstract: A new family of crystalline manganese phosphate compositions has been prepared. These compositions have an extended network which network can be a one-, two-, or three-dimensional network. The composition has an empirical formula of:(A.sup.3+).sub.v (Mn.sup.b+)(M.sup.c+).sub.x P.sub.y O.sub.zwhere A is a structure directing agent such as an alkali metal, M is a metal such as Al, Fe.sup.3+ and "b" is the average manganese oxidation state and varies from greater than 2.0 to a maximum of 3.0. These compositions can be used as adsorbents and as catalysts in the oxidation of hydrocarbons.

Abstract: The present invention relates to novel cyclohexane-1-3-dione derivatives of formula (1) useful as herbicides and plant-growth regulants, ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 haloalkyl, nitro, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulfinyl, C.sub.1 -C.sub.6 alkylsulfonyl, C.sub.1 -C.sub.6 sulfamoyl, and N, N-di(C.sub.1 -C.sub.6 alkyl)sulfamoyl group; (X)n represents the number of X substituents which may be substituted on benzene ring, wherein n is 1, 2 or 3. Also, cyclohexyl moiety, one of the substituents on benzofuran ring, is substituted at C-4, C-5, C-6 or C-7 position on benzene ring; R.sup.1 is selected from the group consisting of hydrogen and C.sub.1 -C.sub.6 alkyl group; R.sup.2 is selected from the group consisting of C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl and C.sub.2 -C.sub.6 alkynyl group; R.sup.3 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.

Abstract: Methods for rapidly generating large rationally designed libraries of structurally-diverse small molecular weight compounds using a multicombinatorial approach.

Abstract: Disclosed are novel compounds which are used as linkers to bind peptides to solid support. The novel compounds can be used for the purification of synthesized peptides and are represented by the following structural formula:X--NH--(CH.sub.2).sub.n --SO.sub.2 --CH.sub.2 --CH.sub.2 --O--CO--Y;n is an integer from 1-4; X is a thiol functionalized with a protecting group that is cleavable under acidic conditions; and Y is a leaving group.

Abstract: Sulfonyl compounds have the formula ##STR1## where n is 0, 1 or 2,Y is vinyl or a radical of the formula C.sub.2 H.sub.4 Q, where Q is hydroxyl or an alkali-detachable group,E is C.sub.3 -C.sub.6 -alkylene with or without interruption by 1 or 2 oxygen atoms in ether function,Ar is the radical of benzene or naphthalene, andR.sup.1, R.sup.2 and R.sup.3 are each hydrogen, unsubstituted or substituted C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, hydroxyl, halogen, nitro, amino, hydroxysulfonyl, carboxyl, carbamoyl, sulfamoyl, cyano or a radical of the formula (NH--).sub.m (CH.sub.2 --).sub.q SO.sub.2 --Y, where m is 0 or 1, q is 0, 2 or 3, and Y is as defined above.

Abstract: Novel cyanophosphorus compounds are disclosed. The preparation, purification, and characterization of dicyanophosphinate, cyanopolyphosphates, tricyanocyclotriphosphonate and tetracyanocyclotetraphosphate are presented.

Abstract: The novel cyanophosphonate compounds of the present invention include cyanophosphonate salts, cyanophosphonate monoacid salts, cyanophosphonate monoacid esters, cyanophosphonate monoester salts and cyanophosphonate methylester salts.

Abstract: A catalyst activator, comprising a cation which is a Bronsted acid capable of donating a proton, and an inert, compatible, noncoordinating, anion, characterized by a solubility constant at 25.degree. C. in hexane, cyclohexane or methylcyclohexane of at least 5 weight percent.

Abstract: Activated aromatic compounds are more economically ring brominated by reacting the compounds with a sulfoxide/HBr brominating agent while removing water from the reaction mixture. The water removal provides high conversions and yields when employing stoichiometric quantities of reactants.

Abstract: An oxidation process for organic compounds employs stabilized bromine chloride solutions as the oxidizing agent. Organic compounds which contain an oxidizable moiety, such as thioanisole and triphenylphosphine, are rapidly converted to sulfoxides and phosphine oxides, respectively, without over-oxidation.

Abstract: A process for preparing cyanophosphonate derivatives involves contacting phosphoric anhydride (P.sub.4 O.sub.10) and a cyanide, preferably in the presence of a Lewis base, in a reaction mixture under sufficient conditions to produce a cyanophosphonate derivative. The cyanophosphonate derivative can be subsequently hydrogenated to produce an aminomethylphosphonate derivative.

Abstract: This invention describes the new triphenylethylenes of general formula I ##STR1## in which n means an integer from 1 to 10,R' means a sulfur-containing organic radical,R" means a hydrogen atom, an iodine atom or a hydroxy groups,E means a hydrogen atom,G means a hydrogen atom orE and G together mean a methylene bridge.The new compounds have strong antiestrogenic properties and are suitable for the production of pharmaceutical agents, for example for treating breast cancer.

Abstract: Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.

Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Abstract: The invention relates to a process and a nucleophilic reagent which is useful for grafting a substituted difluoromethyl group onto a compound containing at least one electrophilic function, characterized in that it comprises:a) a fluorocarboxylic acid of formula Ew--CF.sub.2 --COOH where Ew represents an electron-withdrawing atom or group, at least partially salified with an organic or inorganic cation, andb) a polar aprotic solvent;and in that the content of releasable protons carried by its various components, including their impurities, is at most equal to half the initial molar concentration of the said fluorocarboxylic acid.

Abstract: Novel pharmaceutically/cosmetically-active polyaromatic propynyl compounds have the structural formula (1): ##STR1## in which X is one of the radicals: ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: The present invention is directed to novel methadone derivatives which are synthesized for the covalent attachment to antigens (proteins or polypeptides) for the preparation of antibodies or receptors to methadone and methadone metabolites. The resulting novel antigens may be used for the production of antibodies or receptors using standard methods. Once generated, the antibodies or receptors and the novel derivatives which are covalently attached to proteins, polypeptides or labels may be used in the immunoassay process.

Abstract: In a process for producing trimethylsulfoxonium bromide by reacting dimethyl sulfoxide and methyl bromide, methyl bromide is added to a mixture of dimethyl sulfoxide and a stabilizing agent under atmospheric pressure intermittently or continuously so that the final molar ratio of methyl bromide to dimethyl sulfoxide becomes 0.40:1 to 0.70:1, with the temperature of dimethyl sulfoxide being maintained at a temperature of 50.degree. to 75.degree. C. This process can realize a reduction of reaction time, an improvement of yield and establishment of safety of producing operations.

Abstract: The present invention concerns the use in a cosmetic composition of a hydrofluorocarbon compound with formula (I):R.sub.F --(CH.sub.2).sub.n --X--?C.sub.3 H.sub.5 (OH)!--Y--R.sub.H(I)whereC.sub.3 H.sub.5 (OH) represents the structures: ##STR1## R.sub.F represents a perfluorinated C.sub.4 -C.sub.20 alkyl radical or a mixture of perfluorinated C.sub.4 -C.sub.20 alkyl radicals;R.sub.H represents a linear or branched C.sub.1 -C.sub.22 alkyl radical or a mixture of linear or branched C.sub.1 -C.sub.22 alkyl radicals, an aryl radical or an aralkyl radical;n is between 0 and 4;X and Y represent ##STR2## It also concerns certain sulfoxide and sulfone compounds and cosmetic compositions including the compounds of the invention.

Abstract: Lipid prodrugs of phosphonoacids and their analogs that have increased antiviral activity over the parent drugs in inhibiting cytomegalovirus and other susceptible viruses.

Abstract: A class of substituted spirodienes is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III: ##STR1## wherein R.sup.3 is methylsulfonyl or sulfamyl; and wherein R.sup.8 is selected from hydrido, fluoro, chloro, bromo, iodo, methyl, ethyl, n-propyl, isopropyl, butyl, tert-butyl, isobutyl, methoxy, ethoxy, propoxy, butoxy, hydroxyl, mercapto, methylthio, ethylthio, cyano, fluoromethyl, difluoromethyl, trifluoromethyl, chloromethyl, dichloromethyl, trichloromethyl, pentafluoroethyl, heptafluoropropyl, difluorochloromethyl, dichlorofluoromethyl, difluoroethyl, difluoropropyl, dichloroethyl, dichloropropyl, trifluoromethoxy, hydroxymethyl, methoxymethyl and ethoxymethyl; or a pharmaceutically-acceptable salt thereof.

Abstract: A class of substituted spirodienes is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.4 and R.sup.5 is hydrido; wherein R.sup.3 is methylsulfonyl or sulfamyl; and wherein each of R.sup.6 through R.sup.10 is independently selected from hydrido, halo, alkyl, alkoxy, alkylthio, cyano, haloalkyl, haloalkoxy, hydroxyalkyl, alkoxyalkyl, hydroxyl, and mercapto; and wherein n is 1, 2 or 3; or a pharmaceutically-acceptable salt thereof.

Abstract: Chiral catalysts for enantioselectively epoxidizing a prochiral olefin and for enantioselectively oxidizing a prochiral sulfide are disclosed, together with methods of using such catalysts. In accordance with one aspect of the invention, the catalyst is a salen derivative which has the following general structure: ##STR1## In accordance with another aspect of the present invention is a method of, producing an epoxychroman using a chiral catalyst. In accordance with this method, a chromene derivative, an oxygen atom source, and a chiral catalyst are reacted under such conditions and for such time as is needed to epoxidize said chromene derivative. In accordance with yet another aspect of this invention is a method of enantioselectively epoxidizing a cis-cinnamate derivative to make taxol or an analog thereof. In accordance with another aspect a method of disproportionation of hydrogen peroxide using the catalysts of the present invention is disclosed.

Abstract: The present invention is directed to new diarylvinyl sulfoxides.

Abstract: A process for transforming a carbonyl compound into its corresponding epoxide, which comprises contacting the carbonyl compound with either trimethylsulphonium hydrogen sulphate and/or bis(trimethylsulphonium) sulphate or trimethylsulphoxonium hydrogen sulphate and/or bis(trimethylsulphoxonium) sulphate, in the presence of a base.

Abstract: Trifluoromethanesulfonic and p-toluenesulfonic acid bis- or tris(p-tert-butoxyphenyl)sulfonium salts are novel. They are prepared from bis(p-tert-butoxyphenyl)sulfoxide which is also novel. A chemically amplified positive resist composition which contains the sulfonium salt as a photo-acid generator is highly sensitive to deep-UV rays, electron beams and X-rays, can be developed with alkaline aqueous solution to form a pattern, and is thus suitable for use in a fine patterning technique.

Abstract: A process for oxidizing a substrate susceptible to nucleophilic oxidation by reacting a bicaroate or monopersulfate solution with the substrate is disclosed. In one aspect, the substrate is introduced into the reaction mixture in an inert carrier gas, which can also serve to sweep the product out of the mixture. In a second aspect the oxidation solution is obtained by a two stage neutralization of a Caro's acid solution, the first stage to e.g. 0.5 to 2.0 and the second stage to about 7 to 9. In preferred embodiments, the substrate is introduced into partially neutralized Caro's acid, and the second stage neutralization in the presence of the substrate is most preferably carried out with an alkali salt such as sodium bicarbonate. The process can employ relatively low ratios of substrate: Caro's acid oxidant and homogeneous reaction conditions. The process is particularly useful for preparing dioxiranes from ketones.

Abstract: The present invention provides a process for preparing a sulphoxonium salt from the corresponding sulphonium salt which comprises oxidising the sulphonium salt using a peracid, under basic conditions, in a solvent other than a ketone.Some of the sulphoxonium salts are new compounds.

Abstract: A fabric softening composition containing a thiodiglycol derivative corresponding to formula IR.sup.1 --O--(C.sub.2 H.sub.4 O).sub.x --(C.sub.2 H.sub.4 --SO.sub.z --C.sub.2 H.sub.4 --O).sub.w --(C.sub.2 H.sub.4 --O).sub.y --R.sup.2 (I)wherein R.sup.1 and R.sup.2 are the same or different and represent linear or branched alkyl or alkenyl groups containing 6 to 30 carbon atoms or hydrogen, x+y=0 to 20, w is 1 to 5, and z is 1 or 2.

Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i,e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, to a patient in need of such therapy.

Abstract: A process for co-production of an alkenyl aromatic compound such as, for example, styrene and t-butylstyrene, and an oxygenated sulfur-containing compound such as, for example, a sulfoxide or a sulfone is disclosed which comprises: (1) contacting, in the presence or absence of a catalyst, an .alpha.-methyl benzylic hydroperoxide with an organic sulfide compound to produce a mixture of an .alpha.-methyl benzylic hydroxide and an oxygenated sulfur-containing compound; (2) separating the .alpha.-methyl benzylic hydroxide from the sulfur-containing compound; (3) contacting the .alpha.-methyl benzylic hydroxide with a base to convert the .alpha.-methyl benzylic hydroxide to the alkenyl aromatic compound; and optionally, (4) recovering the alkenyl aromatic compound from the oxygenated sulfur-containing compound. The sulfoxide produced can be oxidized to a sulfone. The contacting of the .alpha.-methyl benzylic hydroxide with a base can also be carried out before the .alpha.

Abstract: This invention relates to structurally novel acyclic tocotrienol analogs, which are useful for cholesterol/lipid lowering in cases of hypercholesterolemia and hyperlipidemia, and for atherosclerosis. Also provided are pharmaceutical compositions and a method of use employing those compositions.

Abstract: This invention provides 1) novel reactive fluorinated compounds derived from a specified class of telomers or cotelomers of fluoroolefins; and 2) stable products and stable polymers thereof obtained by reaction or polycondensation of the novel reactive fluorinated compounds with specified classes of hydrogenated aliphatic, alicyclic, aromatic reactive compounds, telechelic oligomers and block polymers wherein said stable products and polymers contain hetero atoms such as oxygen, sulfur or nitrogen and are characterized by high thermal and chemical resistance.