Abstract: An efficient and selective process, capable of scale-up, to make itaconate derivatives of formula (IV), and/or succinate derivatives of formula (V) and/or (VI) by asymmetric hydrogenation of the itaconate derivatives. wherein R, R1 and R2 are as defined herein.

Abstract: Polyhalogenated cinnamic acids and cinnamic acid derivatives are prepared by reacting diazonium salts accessible from polyhalogenated anilines with acrylic acid or acrylic acid derivatives in the presence of a homogeneous, palladium-containing catalyst at about −5 to about +100° C. Some of the cinnamic acids and cinnamic acid derivatives obtainable in this way are new. Cinnamic acids and cinnamic acid derivatives which can be prepared according to the invention can be used for the preparation of indanones which are precursors for agro- and pharmaceutical chemicals and for substances having liquid-crystalline properties.

Abstract: A process for preparing phenylacetic acid derivatives of the formula (I) by reacting benzyl chlorides of the formula (II) 1

Abstract: The present invention relates to a process wherein heterogeneous finely dispersed palladium catalysts are used for cross coupling of alkenyl halides and boronic acids in the presence of base in an aprotic solvent to produce aryl- or heteroaryl-olefin compounds. The process provides for use with either electron-withdrawing or electron-donating substituents for cross coupling of alkyl halides with boronic acids.

Abstract: The present invention relates to a novel process for the preparation of aromatic carbonyl compounds by oxidative cleavage of styrenes using lipases and hydrogen peroxide or hydrogen peroxide donors in the presence of carboxylic acids or carboxylic esters.

Abstract: The present invention is a method for acyloxylating an alkyl group substituted aromatic compound at the side chain, by letting the alkyl group substituted aromatic compound and a carboxylic acid and/or a carboxylic anhydride react with each other in the presence of an oxygen containing gas. In this case, if (1) a solid catalyst in which at least one selected from cobalt, cerium and manganese is supported on a solid material or (2) a catalyst containing at least one selected from cobalt oxides, cerium oxides and manganese oxides is used, an alkali group substituted aromatic compound and a carboxylic acid and/or a carboxylic anhydride can be caused to react with each other efficiently in the presence of an oxygen containing gas, and in addition the catalyst can be easily separated from the reaction solution. Furthermore, (3) a compound diacyloxylated at the side chains can be highly selectively produced if a cerium compound is used as a catalyst in the absence of a cobalt compound and a manganese compound.

Abstract: Process for the preparation of .alpha.-alkoxy-.alpha.-trifluoromethyl-arylacetic esters of the formula (I) ##STR1## wherein R is a component selected from the group consisting of C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.6 -C.sub.10 -aryl and C.sub.1 -C.sub.6 -halogenoalkyl, R' is selected from the group consisting of C.sub.1 -C.sub.4 -alkyl, X is selected from the group consisting of halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.2 -C.sub.4 -alkenyl, C.sub.6 -C.sub.10 -aryl or C.sub.1 -C.sub.4 -alkoxy and nitro, and n is zero or an integer from 1 to 3.

Abstract: The acrylic acid esters of Formula I are useful for the delivery of organoleptic compounds, especially for flavors, fragrances, masking agents and antimicrobial compounds. They can also deliver fluorescent whitening agents.

Abstract: Compounds of the formula: ##STR1## wherein: R.sub.1, R.sub.2 and R.sub.3 are, independently, hydrogen, nitro, cyano, C.sub.1-10 haloalkoxy, amino, C.sub.1-10 alkylamino, sulfo, sulfamoyl, C.sub.1-10 alkylsulfonamido, C.sub.2-10 alkylcarboxamido C.sub.2-10 alkanoyl, C.sub.1-10 alkylsulfonyl, C.sub.1-10 haloalkylsulfonyl, C.sub.1-10 carboxyl, C.sub.1-10 haloalkyl and C.sub.6-12 aryl; with the provisos: (1) that R.sub.1, R.sub.2 and R.sub.3 may not all simultaneously be hydrogen, and (2) when R.sub.1 and R.sub.2 are hydrogen, R.sub.3 may not be meta-CF.sub.3 ;R.sub.4, R.sub.5 and R.sub.6 are, independently, hydrogen, halogen, nitro, cyano, C.sub.1-10 carboalkoxy, C.sub.1-10 haloalkoxy, amino C.sub.1-10 alkylamino, sulfo, sulfamoyl, C.sub.1-10 alkylsulfonamido, C.sub.2-10 alkylcarboxamido C.sub.2-10 alkanoyl, C.sub.1-10 alkylsulfonyl, C.sub.1-10 haloalkylsulfonyl, C.sub.1-10 carboxyl, C.sub.1-10 haloalkyl, C.sub.1-10 alkyl and C.sub.6-12 aryl;R.sub.

Abstract: A pharmaceutical or veterinary composition comprising a compound of formula I ##STR1## wherein X is a --CO.sub.2 H group and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 are as defined in the specification, or a salt, hydrate or solvate thereof, and a pharmaceutically or veterinarily acceptable excipient or carrier. A method of treatment of diseases or conditions mediated by MMPs in mammals, such as rheumatoid arthritis, osteoarthritis, periodontitis, gingivitis, corneal ulceration or tumour invasion by secondary means, by administering to the mammal an effective amount of the composition.

Abstract: The invention provides polymerizable dental, compounds, compositions, including the compounds and products for mixing the compositions and methods of using the compositions. Aryl acid compounds are provided in accordance with the invention. The compositions include at least one polymerizable aryl acid compound, an effective amount of a polymerization initiator, and at least 10 percent by weight of ceramic, metal and/or metal oxide filler particles having a particle size less than 500 microns. The dental products of the invention include a polymerizable composition in an enclosure having at least two chambers separated by a wall adapted to be ruptured prior to or during mixing of the composition. Compositions of the invention are preferred for use in these enclosures. Core build up material including a polymerizable acid containing compound is used to support dental crowns and adhere them to teeth in accordance with the invention.

Abstract: The invention relates to novel .alpha.-fluoroacrylic acid derivatives, to active compound/antidote combinations which comprise .alpha.-fluoroacrylic acid derivatives and are outstandingly suitable for use in crops of useful plants, to their use and to methods for protecting crop plants.

Abstract: Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: ##STR1## wherein r is 0-2, T is selected from ##STR2## and R.sup.40 is a mono- or bi-heterocyclic structure. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, comeal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibularjoint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture.

Abstract: .alpha., .beta.-Unsaturated acids of the formula ##STR1## wherein R.sup.1 signifies C.sub.1 -C.sub.5 -alkyl and Ar signifies an aryl group which is optionally substituted by one or more substituents selected from the group consisting of halogen, phenyl, C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -alkoxy, perfluorinated C.sub.1 -C.sub.5 -alkyl or perfluorinated C.sub.1 -C.sub.5 -alkoxy can be obtained from new or known compounds of the formula ##STR2## Compounds I can be converted by asymmetric hydrogenation into corresponding optically active saturated acids.

Abstract: Mesogens are provided based on substituted unsaturated carboxylic acids such as acrylic and methacrylic acid. Substitution of a variety of hydrophobic tails onto the carboxylic acid or acid derivative via the vinyl carbon proximal to the carbonyl of the carboxylic acid results in mesogens that are capable of forming thermotropic and single-phase lyotropic mesophases over a broad range of compositions. The mesophases can be polymerized to lock in the ordered phases.

Abstract: The present invention relates to the derivatives of formula: ##STR1## and to their use in therapeutics, especially as drugs with anti-inflammatory and analgesic properties.

Abstract: This invention relates to substituted and unsubstituted ???(aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are useful as antagonists of the pain enhancing effects of E-type prostaglandins, to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods for treating pain comprising the administration of such compounds.

Abstract: The invention relates to a process for the preparation of cinnamic acid derivatives which involves reacting chlorinated aromatic compounds and acrylic acid derivatives in the presence of palladium catalysts.

Abstract: Disclosed is a process for the preparation of .alpha.,.beta.-unsaturated carboxylic acids and esters thereof which comprises contacting formaldehyde or a source of formaldehyde with a carboxylic acid, ester or anhydride in the presence of a catalyst comprising an oxide of niobium.

Abstract: Process for the synthesis of a-substituted acrylic acids and their application.Process for the synthesis of a-substituted acrylic acids of general formula (I) and their application to the synthesis of N- (mercaptoacyl) aminoacid derivatives of formula (II).

Abstract: The invention provides polymerizable dental, compounds, compositions, including the compounds and products for mixing the compositions and methods of using the compositions. Aryl acid compounds are provided in accordance with the invention. The compositions include at least one polymerizable aryl acid compound, an effective amount of a polymerization initiator, and at least 10 percent by weight of ceramic, metal and/or metal oxide filler particles having a particle size less than 500 microns. The dental products of the invention include a polymerizable composition in an enclosure having at least two chambers separated by a wall adapted to be ruptured prior to or during mixing of the composition. Compositions of the invention are preferred for use in these enclosures. Core build up material including a polymerizable acid containing compound is used to support dental crowns and adhere them to teeth in accordance with the invention.

Abstract: Novel pharmaceutically/cosmetically-active aromatic polyenic compounds have the structural formula (I): ##STR1## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: Neurotrophic and antiproliferative compounds related to the antiepileptic drug valproate are provided. These compounds are useful for promoting neuronal function as in neurodegenerative disorders and for treating neoplastic disease.

Abstract: A process for the carbonylation of allylic alcohols such as nerolidol, farnesol, or their monocyclic analogues with carbon monoxide at a pressure of at least 30 bar in the presence of a polar solvent and a palladium halide catalyst, optionally an alkali metal halide salt, and optionally an alcoholic solvent. The carbonylated product may then be reduced to the corresponding alcohol, which is cyclized in the presence of Lewis or Bronsted acids to afford an ambergris fragrance compound.

Abstract: The present invention relates to compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are identical or different and are hydrogen or an alkyl radical having 1 to 18 carbon atoms and optionally containing oxygen, nitrogen or halogen, the radicals X, Y and Z are identical and are a fluorine, bromine or iodine atom or if two of the radicals X, Y or Z are identical or all of the radicals X, Y, Z are different from each other, X, Y and Z are a fluorine, chlorine, bromine or iodine atom. The invention further relates to a process for the preparation of the compounds, by reacting an aryldiazonium salt of the formula ##STR2## in which the radicals X, Y and Z are identical and are a fluorine, bromine or iodine atom or, if two of the radicals X, Y and Z are identical or all of the radicals X, Y, Z are different from each other, X, Y and Z are a fluorine, chlorine, bromine or iodine atom and A.sup.(-) is an anion of an acid having a pK.sub.a <7, with a compound of the formula ##STR3## in which R.sup.

Abstract: Certain novel alicyclic compounds are effective phospholipase A.sub.2 (PLA.sub.2) inhibitors.

Abstract: The subject matter of the invention is a process for the preparation of carboxylic acids and derivatives of them of the general formula ##STR1## wherein R means hydrogen, or a C.sub.1-4 alkyl or a (C.sub.1-5 alkoxy)carbonyl group,R.sub.1 is as defined in claim 1,R.sub.7 stands for hydrogen or a C.sub.1-7 alkyl group andR.sub.8 means hydrogen or a carboxyl group.

Abstract: Disclosed herein is a process of making chiral 2-aryl-1,4-butanediamine derivatives useful as neurokinin-A antagonists of Formula 7 ##STR1##

Abstract: The preparation of 3-arylacrylic acids and their derivatives I ##STR1## where Ar is aryl which can additionally have substituents which do not react with ketene and are stable under the conditions of the reaction described below, andR.sup.1 is hydrogen, an alkali metal, an alkaline earth metal, ammonium or C.sub.1 -C.sub.20 -alkyl,comprises a first stage in which a dialkyl acetal of an aromatic aldehyde of the formula II ##STR2## where R.sup.2 is C.sub.1 -C.sub.4 -alkyl, is reacted with ketene of the formula CH.sub.2 .dbd.C.dbd.O in the presence of catalytic amounts of a protic or Lewis acid to give a 3-arylpropionic acid derivative of the formula III ##STR3## and a second stage in which this intermediate III is reacted in the presence of acid or base and, in the case where R.sup.1 is C.sub.1 -C.sub.20 -alkyl, additionally with a C.sub.1 -C.sub.20 -alkanol to give the final product I.

Abstract: The subject matter of the invention is a process for the preparation of carboxylic acids and derivatives of them of the general formula ##STR1## wherein R means hydrogen, or a C.sub.1-4 alkyl or a (C.sub.1-5 alkoxy)carbonyl group,R.sub.1 is as defined in claim 1,R.sub.7 stands for hydrogen or a C.sub.1-7 alkyl group andR.sub.8 means hydrogen or a carboxyl group,by reacting a 1,3-dioxane-4,6-dione derivative of the general formula ##STR2## wherein R.sub.9 stands for a C.sub.1-4 alkyl group or a phenyl group, optionally monosubstituted by halogen andR.sub.10 stands for hydrogen or a C.sub.1-5 alkyl group orR.sub.9 and R.sub.10 together form a pentamethylene group,and an aldehyde or ketone of the general formula ##STR3## in the presence of formic acid.

Abstract: Novel cyclic anti-tumor promoter compounds and therapeutic compositions are disclosed, along with method for their production and use as anti-cancer and cancer-prevention agents.

Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.2 ' X, Y, Z, A, B, Q and n are as described herein. Their pharmaceutically acceptable salts, and when appropriate, enantiomers, racemates, diastereomers or mixtures thereof or geometric isomer or mixtures thereof, and pharmaceutically acceptable salts thereof. The compounds of formula I inhibit enzyme carnitine acyltransferase 1 (CAT-1) and are therefore useful in the prevention of injury to ischemic tissue, and can limit infarct size, improve cardiac function and prevent arrhythmias during and following a myocardial infarction.

Abstract: Cinnamic acid derivatives, in particular 2-ethylhexyl p-methoxycinnamate and 2-isoamyl p-methoxycinnamate, are prepared avoiding particular effort for workplace hygiene and ecology by using bromoaromatic and acrylic acid derivatives in the presence of palladium catalysts and a large excess of phosphane (based on the palladium), in the presence of an inorganic base and in the presence of alcohols and/or a phase transfer catalyst.

Abstract: Novel cyclic anti-tumor promoter compounds and therapeutic compositions are disclosed, along with method for their production and use as anti-cancer and cancer-prevention agents.

Abstract: A "one-pot" process for the palladium catalyzed coupling of a diazonium salt with an olefinic bond, in the aqueous medium in which the diazonium salt is made, by employing a carboxylic acid as a solvent. Arylacrylic acids and their esters, e.g. the cinnamates, can be produced at low catalyst concentration without first isolating the diazonium salt. The process is applied to the synthesis of 2-ethylhexyl p-methoxycinnamate.

Abstract: An .alpha., .beta.-unsaturated carboxylic acid is produced by catalytically reacting an .alpha.-hydroxycarboxylic acid amide of the formula (1), ##STR1## where R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen and C.sub.1 -C.sub.4 alkyl groups, provided that at least one of R.sub.1 and R.sub.2 is the alkyl group, with water in the presence of a solid acid catalyst containing a high surface area rare earth phosphate anhydride having the monoclinic system structure producible by heating a rare earth phosphate of the hexagonal system structure at 60.degree.-200.degree. C. in a solution of an inorganic acid, an inorganic acid salt and/or an inorganic acid ester where the molar ratio of the inorganic acid component to the rare earth phosphate of the hexagonal system structure is 0.5-400.

Abstract: A process is disclosed for the enantioselective hydrogenation of olefins of the formula: ##STR1## where R is hydrogen or C.sub.1 to C.sub.6 linear or branched alkyl, Z is ##STR2## where R' is hydrogen or C.sub.1 to C.sub.6 linear or branched alkyl, --CN, C(NH)OR" where R" is C.sub.1 to C.sub.6 linear or branched alkyl, or --C(O)NH.sub.2 ; and Ar is phenyl or naphthyl unsubstituted or substituted with benzoyl or substituted benzoyl, C.sub.1 to C.sub.6 linear or branched alkyl, C.sub.1 to C.sub.6 linear or branched alkoxy, halo, or carboxylic acid or C.sub.1 to C.sub.6 linear or branched alkyl ester thereof, which comprises contacting said aromatic-substituted olefin with a catalytically effective amount of a ruthenium phosphite complex.

Abstract: There is here disclosed a method for obtaining high-purity cinnamic acid containing less metals from crude cinnamic acid containing a metallic catalyst which is a mixture prepared by the synthetic reaction of a cinnamic acid ester. A disclosed purifying means is the combination of alkali hydrolysis, active carbon adsorption, solvent extraction and precipitation with an acid.

Abstract: Novel 8-alkenyl, alkynyl, allenyl and cycloalkyl-quinolinecarboxylic acids are described as antibacterial agents as well as methods of manufacture including novel intermediates used in said manufacture.

Abstract: Novel 8-alkenyl, alkynyl, allenyl and cycloalkyl-quinolinecarboxylic acids are described as antibacterial agents as well as methods of manufacture including novel intermediates used in said manufacture.

Abstract: Novel 8-alkenyl, alkynyl, allenyl and cycloalkyl-quinolinecarboxylic acids are described as antibacterial agents as well as methods of manufacture including novel intermediates used in said manufacture.

Abstract: Substituted ethylamines of the formula ##STR1## wherein R.sub.1 is phenyl optionally mono-, di- or trisubstituted by halogen, lower alkyl, lower haloalkyl or lower alkoxy, or is an aromatic heterocycle having 5 to 7 chains wherein the heteroatom is nitrogen, oxygen or sulfur,R.sub.2 is lower alkyl,R.sub.3 and R.sub.4, each independently, represent hydrogen, lower alkyl or lower alkenyl,R.sub.5 is phenyl optionally mono-, di- or trisubstituted by halogen or lower alkoxy or is an aromatic heterocycle having 5 to 7 chains wherein the heteroatom is nitrogen, oxygen or sulfur andQ represents a --CH.dbd.CH-- ethylene group or a 1,2-diyl ##STR2## propane group, their acid addition salts and their optically active forms. These substituted ethylamines have psycotropic properties and are useful as medicines.

Abstract: Catalyst and process are disclosed for the improved preparation of alpha, beta-unsaturated acids. The catalyst comprises a porous silica gel component and a Group IA alkali metal component, which is present in an amount of from 200 to 20,000 parts per million and optionally another component such as tin (IV) oxide, and mixtures thereof. The process comprises reacting formaldehyde and an aliphatic carboxylic acid in the presence of said catalyst while maintaining catalyst activity and selectivity during the process by addition of a source of the alkali metal component.

Abstract: Catalyst and process are disclosed for preparation of alpha, beta-unsaturated acids. Catalyst comprises a silica component and a Group IA alkali metal component which is present in an amount of from 200 to 15,000 parts per million, said silica component containing less than about 500 parts per million individually of aluminum, zirconium, titanium, iron and mixtures thereof. Process comprises reacting formaldehyde and a carboxylic acid of the formula RHC.sub.2 COOH wherein R is a member of the class consisting of --H, -alkyl, -aryl, -aralkyl, -cycloalkyl, and -alkylaryl radicals in the presence of said catalyst. Catalyst activity is maintained during process by addition of source of alkali metal component.

Abstract: A compound of formula (I) ##STR1## its isomers and its salts in which R.sub.1, R.sub.3 and R.sub.4 are each independently hydrogen, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -alkoxy, halogen, C.sub.1 -C.sub.8 acyloxy or hydroxyl;R' is hydrogen or C.sub.1 -C.sub.6 -alkyl;R" is either a polyene chain or a benzene ring are useful in cosmetics and in the treatment of various dermatological and other complaints.

Abstract: This invention provides a novel catalyst composed of a complex of an organic acid or its ester and a Lewis acid, preferably boron trichloride that can add olefin monomers to increase the molecular weight of the complex from as low as 200 to in excess of a million, with the complex being active viz., living, until the complex dies, viz., is decomposed or destroyed so that polymers in the liquid or easily liquefiable range of 300 to about 20,000 can be made or those more difficult to be liquefied or unliquefiable, viz., those of over 10,000 up to 100,000 or in some cases 500,000 and then those in the range of the elastomers, or moldable or extrudable plastics range having very high molecular weights, generally in excess of 100,000 up to in excess of 500,000 and having useful end groups such as the halogens and specifically chloride, allyl, acryl or methacryl, acetate or formate to name some of the more useful ones.

Abstract: The present invention relates to 1-substituted derivatives of 4-methoxy-2,3,6-trimethylbenzene which are useful in cosmetic or pharmaceutical preparations for use in the treamtnet of dermatological complaints connected with a keratinisation disorder, dermatological complaints having an inflammatory and/or immuno-alleric component or ophthalmological complaints.

Abstract: An aromatic naphthyl compound of the formula ##STR1## wherein n is 0 or 1,R' is hydrogen, OH, acyloxy, alkoxy or NH.sub.2,R" is hydrogen or lower alkoxy, or R' and R" taken together form an oxo, methano or hydroxy-imino radical,R is --CH.sub.2 OH or --COR.sub.8,R.sub.8 is hydrogen, --OR.sub.9 or ##STR2## R.sub.9 is hydrogen, alkyl having 1-20 carbon atoms, mono or polyhydroxyalkyl, aryl, aralkyl, the residue of a sugar or ##STR3##is 1, 2 or 3,r' and r" each independently represent hydrogen, alkyl, monohydroxyalkyl, polyhydroxyalkyl, aryl, benzyl, the residue of amino acid or the residue of aminated sugar, or r' and r" together form a heterocycle,R.sub.1, R.sub.2, R.sub.3 and R.sub.4 represent hydrogen, lower alkyl, alkoxy having 1-4 carbon atoms, fluoroalkoxy, CF.sub.3, cycloalkyl, lower acyl, halogen, OH, amino, acylamino or alkoxy carbonyl,R.sub.5, R.sub.6 and R.sub.7 represent hydrogen or methyl or when n=1, R.sub.5 and R.sub.

Abstract: (Z)-2-(2-arylethenyl)arylcarboxylic acids of the general formula I ##STR1## where A is a group for completing an aromatic ring system and Ar is an aromatic radical, are prepared by reacting a 2-formylarylcarboxylic acid of the general formula II ##STR2## with an (arylmethyl)phosphonium salt of the general formula III ##STR3## where R.sup.1, R.sup.2 and R.sup.3 are each organic radicals and X is halogen, in the presence of a base at from (-20.degree.) to +30.degree. C. by carrying out the reaction in the presence of a C.sub.1 -C.sub.5 -alkanol and/or a C.sub.2 -C.sub.4 -alkanediol.

Abstract: Neurotrophic and antiproliferative compounds related to the antiepileptic drug valproate are provided. These compounds are useful for promoting neuronal function as in neurodegenerative disorders and for treating neoplastic disease.