Abstract: Pharmaceutical compositions which are useful for the treatment of cancer or illnesses which arise due to an abnormally elevated cell proliferation comprise acyl derivatives of aromatic aldehydes, especially arylidene diesters and .alpha.-alkoxyarylidene esters of general formula (I).

Abstract: Esters of branched C.sub.9 alcohols suitable as plasticizers are formed by esterification of a C.sub.9 alcohol produced by the aldol condensation from propanal and a C.sub.6 aldehyde and hydrogenation, the propanal optionally having been made from natural gas streams.

Abstract: A method for treating a human having elevated tumor necrosis factor levels by administrating an effective amount of one of the amino acids glycine, alanine, or serine.

Abstract: The present invention relates to optically active diphosphines. It is also targeted at their preparation according to a process for the resolution of the racemic mixture of the said phosphines to optically active isomers.The subject of the invention is new optically active bis[1-phospha-2,3-diphenyl-4,5-dimethylnorbornadiene] diphosphines and a process for resolving the racemic bis[1-phospha-2,3-diphenyl-4,5-dimethylnorbornadiene] mixture which comprises reacting it with a palladium or platinum complex as chiral auxiliary in an organic solvent, thus forming diastereoisomer complexes, and then resolving the said optically pure complexes.The invention also relates to new optically active metal complexes comprising the said phosphines and to their use in a process for the preparation of optically active carboxylic acids and/or derivatives according to a process for the hydrogenation of .alpha.,.beta.-unsaturated carboxylic acids and/or derivatives.

Abstract: Water or lipid soluble, pharmacologically active, antioxidant, anti-phospholipase compounds that are chemically defined. The compounds protect mammalian cells by inhibiting PLA.sub.2 and preventing oxidation. In particular, each compound has at least two fatty moieties and no active hydroxy group. The compound may also have at least one ionizable group, which may be a carboxyl group, and each of the fatty moieties has from sixteen to twenty carbon atoms and at least one cis-unsaturated double bond.

Abstract: The present invention relates to a process for the preparation of diacids or mixtures of diacids from aqueous solutions derived from the washing of cyclohexane oxidation products. More specifically, the present invention provides a process for the preparation of aliphatic diacids from washing waters derived from a process for the oxidation of cyclohexane and containing peroxides, the process of the invention comprising successively:(a) at least partially deperoxidizing said washing waters by subjecting them to catalytic hydrogenation at a temperature of between about 0.degree. C. and about 100.degree. C., in the presence of at least one platinum group metal;(b) oxidizing with nitric acid the products contained in the washing waters after deperoxidation.

Abstract: The invention comprises a novel pyruvate compound for the treatment of prevention of reperfusion injury following ischemia, diabetic effects, cholesterol levels, injured organs ethanol intoxication oras s foodstuff. The novel pyruvate compound is particularly a puruvate thiolester, a glucerol-pyruvate ester or a dihydoxyacetone-pyruvate ester.

Abstract: The present invention provides compounds with antioxidant activity effective in treating free radical mediated diseases.

Abstract: Disclosed is a process for the synthesis of .beta.-lactam antibacterials using soluble side chain esters in the presence of enzyme acylase. Also disclosed are novel esters useful as reactants in said process.

Abstract: The present invention relates to a novel process for preparing 3,3-dimethylbutyric acid by reaction of trimethylpyruvic acid with hydrazine hydrate and treatment of the resulting hydrazone with a base.

Abstract: Synthetic mammalian matrix metalloprotease inhibitors are disclosed that are useful for treating or preventing diseases wherein said diseases are caused by unwanted mammalian matrix metalloprotease activity and include skin disorders, keratoconus, restenosis, rheumatoid arthritis, wounds, cancer, angiogenesis and shock.

Abstract: The present invention relates to compounds of the formula 1 ##STR1## wherein R.sub.1 is selected from hydrogen and -R.sub.4 -R.sub.5 where R.sub.4 is selected from nothing C.sub.1 -C.sub.20 linear or branched alkylene C.sub.3 -C.sub.20 cycloalkylene, C.sub.6 -C.sub.20 arylene, C.sub.7 -C.sub.20 alkarylene and C.sub.7 -C.sub.20 arlkylene; and R.sub.5 is one of hydrogen, hydroxy, --CO.sub.2 Z, phenyl hydroxyphenyl pyridyl, nitrophenyl, furyl, and thienyl; R.sub.2 and R.sub.3 are independently selected from a group of the formula --R.sub.4 --R.sub.6 ; where R.sub.4 is as defined above and R.sub.6 is one of hydrogen, hydroxy --CO.sub.2 Z. --CH(CO.sub.2 Z)--CH.sub.2 --CO.sub.2 Z and NR.sub.7 R.sub.8 ; where R.sub.7 and R.sub.8 are independently selected from a group of the formula: --(CH.sub.2)k--R.sub.g : where k.dbd.0-20 and R.sub.g is one of hydrogen, hydroxy, --CO.sub.2 Z. and --CH(CO.sub.2 Z)--CH.sub.2 --CO.sub.2 Z: wherein Y is selected from --CO.sub.2 Z. --SO.sub.3 Z and --C.dbd.

Abstract: This invention relates to canvanine analogs, their pharmaceutical compositions, and a method for treatment of cancer, particularly pancreatic cancer.

Abstract: A method for producing aryl alkyl hydroperoxides which comprises selectively oxidizing an aryl alkyl hydrocarbon having the formula: ##STR1## wherein P and Q are hydrogen or an alkyl and may be the same or different from each other; x is an integer of 1-3; and Ar is an aromatic hydrocarbon group having a valence of x, with an oxygen-containing gas in the presence of a transition metal complex which contains, as a ligand, a cyclic polyfunctional amine compound having at least three nitrogen atoms in the ring forming molecular chain or an open chain polyfunctional amine compound having at least three nitrogen atoms in the main chain of the molecule.

Abstract: Compositions comprising unsaturated hydroxycarboxylic compounds, a process for reacting olefinic compounds with carboxylic reagents and products prepared by the process. The compositions containing the hydroxycarboxylic compounds and the products of the process are useful as intermediates for preparing additives for lubricants and fuels.

Abstract: A nitrile compound or an amide compound is hydrolyzed in the presence of an inorganic acid or other acidic catalyst or an alkali metal hydroxide or other basic catalyst, and the by-produced ammonium salt of the acidic catalyst or the produced salt of a carboxylic acid and a base is electrodialysed to form an acid and ammonia or aqueous ammonia, or to form a base and ammonia. The obtained acid or base may be recycled as a catalyst for the hydrolysis of the nitrile compound or amide compound, and the obtained ammonia is reutilized as a nitrogen source for the nitrile compound or amide compound. Such amide compound may be produced by hydration of a nitrite compound in the presence of a manganese oxide.

Abstract: The invention relates to the production and purification of salts of 6,8-bis(amidiniumthio) octanoic acid, its enantiomers (+)-6,8-bis(amidiniumthio)octanoic acid and (-)-6,8-bis (amidiniumthio)octanoic acid and of the esters of these compounds as well as to their use to produce dihydrolipoic acid and .alpha.-lipoic acid.

Abstract: Dicarboxylic acid and diamine are recovered from polyamides by hydrolysis with nitric acid, followed by separation of the dicarboxylic acid, and hydrogenation of the nitric acid, and then recovery of the diamine.

Abstract: A guanidine derivative represented by formula (1), (2), (3) or its acid addition salt and a production process thereof ##STR1## wherein each of A and B is a C.sub.2 -C.sub.8 alkylene, D is a single bond, --CO-- or a C.sub.1 -C.sub.5 alkylene, E is H, a lower alkyl or the like, m is 1 to 6, n is 0 to 6 and R.sup.1 is H, a lower alkyl or the like, l is 1 to 10 and G is H, --OH or the like and a skin cosmetic containing the same. It can exert excellent keratin layer softening effect continuously for a long period of time.

Abstract: The present invention provides novel hydroxamic acids and carbocyclic acids and derivatives thereof and to pharmaceutical compositions and methods of use of these novel compounds for the inhibition of matrix metalloproteinases, such as stromelysin, and inhibit the production of tumor necrosis factor alpha, and for the treatment of arthritis and other related inflammatory diseases.

Abstract: Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitriles thereof.These compounds are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, and as anti-viral and anti-fungal agents or pro-drugs of such agents. Illustrative of the disclosed compounds are fatty acid amino acid analogs of the structure ##STR1## in which X is the ethyl or t-butyl ester of an amino acid such as Gly, L-Ala, L-Ile, L-Phe, L-Trp, L-Thr or an amide such as NHCH.sub.2 C.sub.6 H.sub.5 or NH(CH.sub.2).sub.2 C.sub.6 H.sub.5.

Abstract: Tartronic acid acetalic ethers and esters of the general formula: ##STR1## are provided and are useful in treatment of bone dysmetabolism. As examples, Ra and Rb may be hydrogen, B is a C.sub.2 -C.sub.12 acyl group, R is phenyl and n is 0-12.

Abstract: A process for the continuous preparation of 3-(methylthio)propanal. A liquid reaction medium is contacted with a gaseous acrolein feed stream in a gas/liquid contact zone. The reaction medium contains 3-(methylthio)propanal, methyl mercaptan and a catalyst for the reaction between methyl mercaptan and acrolein. The gaseous acrolein feed stream comprises acrolein vapor and non-condensable gas. Acrolein is transferred from the acrolein feed stream to the reaction medium and reacts with methyl mercaptan in that medium to produce a liquid reaction product containing 3-(methylthio)propanal. The non-condensable gas is separated from the liquid reaction product. The reaction product is divided into a product fraction and a circulating fraction, and the circulating fraction is recycled to the gas/liquid contact zone.

Abstract: The present invention relates to a new class of carbohydrate based nonionic surfactant, i.e., alkyl and alkenyl glycasuccinimide, and a process for their manufacture.

Abstract: Chiral 1,4-diol cyclic sulfates and their use as precursors in the preparation of chiral phospholane ligands, and chiral complexes useful as catalysts for carrying out enantioselective reactions.

Abstract: Haloalkanoic acid impurities are decomposed in the presence of certain surfactants carboxymethyl cellulose or thioglycollic acids salts which may contain them as unconverted reactants by contacting them with dehalogenase enzyme.

Abstract: Leukotriene-B.sub.4 derivatives of formula I ##STR1## their salts with physiologically compatible bases and their cyclodextrin clathrates are described.

Abstract: A process for preparing R/S-.gamma.-lipoic acid of the formula I or R/S-.alpha.-lipoic acid of the formula II ##STR1## is disclosed.

Abstract: A monomeric diacid derivative includes at least two fatty acids coupled by a hydrolytically or enzymatically degradable bond. In a biological environment, the bond degrades forming naturally occurring fatty acid products thereby allowing elimination.

Abstract: Described are preferred processes for hydrolyzing activated esters using, as catalysts, siloxanes having 4-dialkylaminopyridyl groups incorporated into their polymer backbones. The preferred siloxane catalyst materials demonstrate unexpected catalytic efficacy in the hydrolysis as well as enzyme-like selectivity for ester substrates.

Abstract: The invention is intended to provide novel solid state displacement elements that have an extent of displacement. The solid state displacement element has an intercalation compound in which a polar compound (B) is mixed with an inorganic layered compound (A), and produces a strain when a voltage is applied.

Abstract: A process for synthesizing O-substituted oxime compounds, which includes (a) reacting an alkali metal or alkaline earth metal hydroxide compound and a solution of an oxime compound to form a first mixture including the alkali metal or alkaline earth metal salt of the oxime compound and water; and (b) adding an organohalide compound while stirring to the first mixture to form a second mixture including an O-substituted oxime compound, the alkali metal or alkaline earth metal salt of the oxime compound, water, unreacted organohalide compound and excess oxime compound. The second mixture is heated in the presence of an amount of water sufficient to react hydroxide with the unreacted organohalide compound to obtain an O-substituted oxime compound substantially free of unreacted organohalide compound.In a further embodiment, the O-substituted oxime compound can be hydrolyzed to the corresponding O-substituted hydroxylamine.

Abstract: Facile process for the production of 3-mercaptopropionitrile and 3-mercaptopropionic acid by reacting thiodipropionitrile with alkaline hydrosulfide in the presence of alkaline hydroxide. Acidification of the resulting reaction product with a strong acid, or saponification, yields the desired mercaptopropionic acid, which can be isolated in high yield.

Abstract: A process for preparing R/S-.gamma.-lipoic acid of the formula I or R/S-.alpha.-lipoic acid of the formula II ##STR1## is disclosed.

Abstract: Compounds of the formula ##STR1## wherein R.sup.21 and R.sup.22 are as defined in the specification which are intermediates useful in the preparation of compounds of the formula ##STR2## and the pharmaceutically acceptable salts thereof, wherein Q and R.sup.1 are as defined in the specification. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.

Abstract: A process for deodorizing a mercapto acid includes extracting malodorous compounds present therein by treating the mercapto acid in the presence of a polar solvent with a supercritical extraction fluid having a critical temperature ranging from 0.degree. to 135.degree. C. and a critical pressure ranging from 10.sup.6 to 10.sup.7 Pascals. The mercapto acid has the formula HS--A--COOH wherein A represents ##STR1## wherein n is an integer ranging from 1 to 4 and R is a linear or branched C.sub.1 -C.sub.3 alkyl.

Abstract: Naphthalene derivative of the formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are hydrogen atom, hydroxy group, cyclo-lower alkyloxy group, substituted or unsubstituted lower alkoxy group, or both combine each other to form lower alkylenedioxy group, R.sup.3 is substituted or unsubstituted nitrogen-containing 6-membered heterocyclic group, and groups of the formulae: --OR.sup.4 and --OR.sup.5 are the same or different and are protected or unprotected hydroxy group, processes for preparing thereof, and synthetic intermediates therefor, these compounds have excellent bronchodilating activity, and are useful in the prophylaxis and treatment of asthma.

Abstract: A process for deodorizing a mercapto acid or a polar solvent solution thereof includes extracting malodorous compounds present therein by extraction with carbon dioxide in gaseous, liquid or solid form. The mercapto acid has the formula HS-A-COOH wherein A represents ##STR1## wherein n is an integer ranging from 1-4 and R is linear or branched C.sub.1 -C.sub.3 alkyl.

Abstract: A process is disclosed for the preparation of pure ammonium thioglycolate from thioglycolic acid contaminated with the isopropyl ester of thioglycolic acid wherein the contaminated acid is reacted with aqueous ammonia or ammonium hydroxide at a pH of at least 6.5 to about 9.0 at elevated temperature.

Abstract: In a process for reacting a low molecular weight hydroxy compound with a carboxylic acid halide, a small amount of the acid halide is introduced into the reaction vessel and the remainder of the acid halide and the hydroxy compound are added gradually in an approximately stoichiometric ratio. The hydrogen halide formed is thus prevented from dissolving in the reaction medium. The heat of reaction to be dissipated is negligible.

Abstract: Immunoregulatory N-(S-3-alkyl-4-heptenoyl)- and N-(S-3-alkylheptanoyl)-D-gamma-glutamyl-glycyl-D-alanine and esters thereof are synthesized via R-trans-2-hexen-4-ols, R-3-alkyl-4-heptanoic acid and S-3-alkylheptanoic acid.

Abstract: A novel method for making .beta.-mercaptopropionic acid which comprises adding alkaline hydroxide to thiodipropionic acid to obtain alkaline thiodipropionate, mixing thus obtained alkaline thiodipropionate with an aqueous solution of alkaline sulfide, then reacting the mixed solution with addition of heating in a required time, and acidifying the reacted solution with a strong acid.

Abstract: The invention features a compound of the formulaW-Y-Q-Z or W-Y-ZwhereinW is a farnesyl group, a geranylgeranyl group, a substituted farnesyl group or a substituted geranylgeranyl group; ##STR1## wherein n=1, 2, 3, 4, 5, or 6; each of T.sub.1' . . . T.sub.n' and T.sub.1" . . . T.sub.n" is independently: Fl, Br, --NHCOCH.sub.3, --NH.sub.2, a peptide, an alkane group, an alkene group, an polyethyleneglycol group, a saturated fatty acid, an unsaturated fatty acid, a monosaccharide, or a disaccharide; andZ is --COOH or salts or esters thereof, --CONH.sub.2, --NO.sub.2, --PO.sub.3 or salts or esters thereof, --C N, or --SO.sub.3 or salts or esters thereof, provided that when W is farnesyl, Y is --S--, n=2, and either T.sub.2' or T.sub.2" is --NHCOCH.sub.3, then Z is not --COOH.The compounds of the invention are capable of interfering with enzymatic methylation of a peptide having the carboxyl-terminal motif --CAAX wherein C=cysteine, A=aliphatic amino acid, and X=any amino acid.

Abstract: P,P-dihydrocarbylphosphinoacetic acids are prepared by reacting a 2-methyl-4,4-dialkyl-2-oxazoline (preferably 2,4,4-trimethyl-2-oxazoline) with a basic alkali metal compound (preferably potassium hydride), followed by coupling with at least one halodihydrocarbylphosphine (preferably chlorodiphenylphosphine or chlorodiethylphosphine or chlorodi(t-butyl)phosphine or chlorodicyclohexylphosphine), and subsequent hydrolysis under acidic conditions.

Abstract: A process is provided for producing alkylthio-substituted carboxylic acids and arylthio-substituted carboxylic acids and their corresponding alkylthio-substituted thioesters and arylthio-substituted thioesters. The process comprises reacting a mercaptan with a lactone in the presence of an acidic catalyst at temperatures of about 100.degree. C. to about 350.degree. C. The process for preparing the thio-substituted carboxylic acids and thio-substituted thioesters may be a continuous process or a batch process.

Abstract: There is disclosed a process for preparing sulfonyl acids from mercaptans in a single reactor. The mercaptan is converted to a mercaptide and reacted with an acrylic acid or salt thereof in a basic reaction medium. After formation of the thioether, the reaction medium is treated with chlorine gas to oxidize the thioether to the sulfone. Mild conditions and readily available starting materials render the method capable of preparing such acids efficiently in large scale amounts.

Abstract: A catalyst system, which containsa) a source of a group VIII metal, andb) a phosphine of general formula: ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 are independently selected from an optionally substituted aryl group and a group of general formula: ##STR2## wherein eachh of A, X, Y and Z is independently selected from a nitrogen atom, a CH group and a group of formula CR wherein R represents a hydroxyl group, an amino group, an amido group, a cyano group, an aryl group, an aryloxy group, a halogen atom, an optionally substituted hydrocarbyl group or an optionally substituted hydrocarbyloxy group, it also being possible for two adjacent CR groups to form a ring, provided that at least one of R.sup.1, R.sup.2 and R.sup.3 represents a group of formula (II) in which at least one of A and Z represents a group of formula CR; or an acid addition salt thereof.Also disclosed is the use of the catalyst system in the selective carbonylation of unsaturated hydrocarbons.

Abstract: P,P-dihydrocarbylphosphinoacetic acids are prepared by reacting an alkyl ethynyl ether (preferably ethyl ethynyl ether) and/or a haloacetaldehyde acetal (preferably bromoacetaldehyde diethyl acetal) with a basic alkali metal compound (preferably lithium diisopropylamide), followed by coupling with a least one halodihydrocarbylphosphine (preferably chlorodiphenylphosphine or chlorodiethylphosphine or chlorodi(t-butyl)phosphine or chlorodicyclohexylphosphine) and subsequent hydrolysis.

Abstract: A process is provided for the preparation of mercaptopropionic acid esters by reaction of an acrylic acid ester with hydrogen sulfide in the presence of a weakly basic amine as a catalyst, a polyether as a co-catalyst, a polythiodipropionic acid ester as a reactive solvent, and added elemental sulfur.

Abstract: A method for controlling the release of durgs or other passenger molecules form carrier conjugates, and a class of conjugates that releases drugs when ingested by a cell or subjected to acidic conditions, are disclosed. These conjugates contain a passenger molecule which is attached to a spacer molecule through an acidic bonding group, such as carboxyl, that is in a "cis" configuration with another acidic group, and a carrier molecule that is bonded to the spacer molecule at another site. When subjected to a mild increase in acidity, such as occurs within a lysosome of a cell, the drug or other passenger molecule is hydrolyzed from the the conjugate and released in unmodified, active form.