Abstract: The present invention relates to the compounds of the general formula (I) and their salts and stereoisomers for the production of medicaments for the treatment of cardiovascular disorders.

Abstract: A catalyst suited for catalytic vapor-phase oxidation of isobutylene, t-butanol or propylene to produce respectively corresponding unsaturated aldehyde and unsaturated carboxylic acid is provided. Said catalyst consists of ring-formed shaped bodies composed of (i) a catalyst composition containing at least molybdenum and bismuth as the active ingredients and (ii) inorganic fibers. The catalyst excels in mechanical strength, can give the object products at high yield and shows little activity degradation with time.

Abstract: The present invention relates to new cinnamic acid salts of salmeterol, processes for the preparation thereof as well as the use thereof as pharmaceutical compositions.

Abstract: Compounds of formula (II) are simultaneously halogenated in the 5 position and hydroxylated in the 4 position under lactonization, the halolactone is converted into a hydroxylactone and then the hydroxy group into a leaving group, the leaving group is replaced with azide, the lactone amidated and then the azide converted to the amine group, in order to obtain compounds of formula (I).

Abstract: Compounds useful as surface coating agents, including compounds of the formula: wherein X1 comprises a first photoreactive species; X2 comprises a second photoreactive species; Y comprises a nonpolymeric core molecule comprising an aromatic group; and Z comprises at least one charged group. The Y core can include an aromatic group such as a benzene radical, the charged groups Z can be independently selected from the organic acids that include sulfonic acid, carboxylic acid, and phosphoric acid, and the photoreactive species of X1 and X2 can independently be aryl ketones, such as those selected from the group acetophenone, benzophenone, anthraquinone, anthrone, and anthrone-like heterocycles, and their substituted derivatives.

Abstract: Acylquanidines of the formula wherein the substituents are defined as in the specification which are antagonists of the vitronectin receptor and inhibitors of cell adhesion and bone resorption mediated by the osteoclasts.

Abstract: Compositions and methods for the treatment of dry eye and related diseases utilizing 6-keto-PGF1&agr; and its analogs are disclosed.

Abstract: The present invention relates to certain resorcinol derivatives and their use as skin lightening agents.

Abstract: Compounds are provided that lower blood glucose concentrations, lower serum triglyceride concentrations, lower systolic blood pressure, and increase glucose uptake by adipose tissue, but do not affect the expression of PPAR-&ggr; by adipose tissue.

Abstract: The present invention relates to production of 2-cyclohexyl-2-hydroxy-2-phenylacetic acid useful as an intermediate for pharmaceutical products, by an industrial means, economically, safely in a good yield. Novel 2-(2′-cyclohexen-1′-yl)-2-hydroxy-2-phenylacetic acid ester obtained by reacting cyclohexene and benzoylformic acid ester in the presence of a Lewis acid is hydrolyzed and reduced to give 2-cyclohexyl-2-hydroxy-2-phenylacetic acid.

Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.

Abstract: Inhibitors of the cytosolic phospholypase A2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases. The inhibitors of the present invention have the general formula where X, Z, X1, R1, R2, Ra and Rb are as defined in the specification.

Abstract: This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediated by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutical compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds. The compounds are of the formula as defined herein.

Abstract: The invention relates to a method which comprises synthesising bifunctional compounds then chiral compounds from the bifunctional compounds, also to synthesising supports comprising these chiral compounds, and the use of these supports for preparing or separating enantiomers, or for asymmetric synthesis. The invention also relates to bifunctional compounds, their use as a source of functionalised polymers, and to the chiral compounds, also to the use of these chiral compounds in a chiral support in the form of a three-dimensional network or for separating or preparing enantiomers, principally for analytical or preparative chromatography, and in a support for the production of chiral molecules by asymmetric synthesis.

Abstract: A method for producing an optically active piperidine carboxylic acid derivative, which comprises subjecting a piperidine carboxylic acid derivative of the formula (1): wherein Z is a protecting group for the carboxyl group, to optical resolution by means of an optical resolution agent of the formula (2): wherein symbol * indicates that the designated carbon atom is asymmetric.

Abstract: Phenoxyacetic acid derivatives of the formula: wherein R1, R2, Xn and A are as defined herein, and a process for preparing the derivatives. The derivatives are used as herbicides.

Abstract: 1

Abstract: A method for producing phenylenedioxydiacetic acids of high purity at high yield from crude phenylenedioxydiacetic acids which mainly contains phenylenedioxydiacetic acids represented by the following general formula (I): wherein, R represents a hologen, carboxyl group or hydrocarbon group having 1-4 carbon atoms, and n represents an integer from 0 to 3, wherein an alkaline aqueous solution of the crude phenylenedioxydiacetic acids is mixed with a mineral acid to precipitate the phenylenedioxydiacetic acids, wherein at least 10% by weight of the alkaline aqueous solution is mixed with a mineral acid at 0 to 50° C.; and, after completion of the mixing, the temperature of the mixture is kept at 80 to 110° C.

Abstract: A compound having formula (I), wherein A is selected from the group consisting of: (i) phenyl, wherein said phenyl is optionally substituted by one or more halogen atoms, C1-6alkyl, C1-3alkoxy, C1-3fluoroalkoxy, nitrile, or —NR7R8 where R7 and R8 are independently hydrogen or C1-3alkyl; (ii) a 5- or 6-membered hetrocyclic group containing at least one heteroatom selected from oxygen, nitrogen and sulfur; and (iii) a fused bicyclic ring (a), wherein ring C represents a heterocyclic group as defined in point (ii) above, which bicyclic ring is attached to group B via a ring atom of ring C; B is selected from the group consisting of: (iv) C1-6alkylene; (v) —MC1-6alkylene or C1-6alkyleneMC1-6alkylene, wherein M is O, S, or —NR2 wherein R2 represents hydrogen or C1-3alkyl; (vi) a 5- or 6-membered heterocyclic group containing at least one nitrogen heteroatom and optionally at least one further heteroatom selected from oxygen, nitrogen and sulfur and optionally substituted by C1-3alkyl; and (vii) H

Abstract: The present invention relates to a process of coding and identifying individual members of a chemical combinatorial library synthesized on a plurality of solid supports which undergo mix and split synthesis. The process provides for tagging the solid supports with a coding identifier that is attached to the solid support and which can be decoded by infrared or raman spectroscopy when directly attached to the support.

Abstract: The invention relates to compounds of the formula The compounds have agreat affinity for the neurotensin receptors.

Abstract: Carboxylic acids of formula (1): ##STR1## wherein R.sup.2 and R.sup.3 are independently hydrogen or C.sub.1 -C.sub.3 alkyl, and Q is optionally substituted phenyl, can be easily converted by ring closing into pyridazin-3-one derivatives of formula (7): ##STR2## The carboxylic acids of formula (1) can be produced by reacting hydrazone compounds of formula (5): ##STR3## wherein R.sup.3 and Q are as defined above, with malonic acid derivatives of formula (6):R.sup.2 CH(COOH).sub.2wherein R.sup.2 is as defined above in the presence of a base.

Abstract: The present invention relates to 3,4-disubstituted phenylethanolaminotetralincarboxylic acid derivatives represented by the general formula: ##STR1## [wherein Q represents a vinylene group or a group represented by the general formula:-A-(CH.sub.2).sub.m --(wherein A represents an oxygen atom or a methylene group; and m is an integer of from 1 to 6); R represents a hydrogen atom or a lower alkyl group; n is an integer of 1 or 2; the carbon atom marked with * represents a carbon atom in R configuration, S configuration or a mixture thereof; and the carbon atom marked with (S) represents a carbon atom in S configuration] and pharmaceutically acceptable salts thereof, which have a selective .beta..sub.2 -adrenergic receptor stimulating effect with relieved burdens on the heart such as tachycardia and are useful as an agent for the prevention of threatened abortion and premature labor, a bronchodilator and an agent for pain remission and promoting stone removal in urolithiasis.

Abstract: Thyroid hormone analogues are disclosed. Methods of using such analogues and pharmaceutical compositions containing them are also disclosed, as are novel procedures for their preparation.

Abstract: A substrate for solid phase synthesis of the formula: ##STR1## is disclosed. Also disclosed are processes for preparing the substrate and intermediates useful therein. Among the novel intermediates are compounds of the formula: ##STR2## wherein t is 0 or 1; n is 3-20; R is OH, an activated ester or the residue of a solid support having a plurality of amino functionalities; A is --O-- or --NH-- and Q is hydrogen or a protecting group for an amine or alcohol.

Abstract: A process for preparing .alpha.-hydroxy acids by heating ammonium salts of .alpha.-hydroxy acids of general formula (I), removing the formed ammonia and water, adding water to the residue, and heating the obtained mixture, wherein R is hydrogen, C.sub.1 -C.sub.6 alkyl, alkyl(C.sub.1 -C.sub.6)thioalkyl (C.sub.1 -C.sub.6), phenyl or the like. This process is freed from the problem of disposal of by-products such as ammonium bisulfate and makes it possible to prepare a free .alpha.-hydroxy acid from an ammonium salt thereof economically and in a high yield.

Abstract: Novel calix[4]arene dibenzo crown ethers useful to selectively extract cesium are represented by the formula: wherein R is a C.sub.1 -C.sub.10 normal alkyl, a phenyl or a methoxyphenyl, R' is hydrogen, p-tert-butyl or a C.sub.1 -C.sub.10 normal alkyl, R" is a C.sub.1 -C.sub.10 normal alkyl, and n is an integer of 0-2. The novel compound is prepared at high yields by introduction of benzene rings into the crown ether ring of calix[4]arene crown-6-ether. The calix[4]arene dibenzo crown ethers are superior in selective absorptivity for cesium ions by virtue of their 1,3-alternate conformational structure and thus, can be used as selective extractants able to separate cesium ions at a high efficiency.

Abstract: A substrate for solid phase synthesis of the formula: ##STR1## is disclosed. Also disclosed are processes for preparing the substrate and intermediates useful therein. Among the novel intermediates are compounds of the formula: ##STR2## wherein t is 0 or 1; n is 3-20; R is OH, an activated ester or the residue of a solid support having a plurality of amino functionalities; A is --O-- or --NH-- and Q is hydrogen or a protecting group for an amine or alcohol.

Abstract: A surfactant, an emusifier for emulsion polymerization, a dispersant for suspension polymerization and a modifier for modification of resin properties are disclosed, each of these agents being comprised of a novel compound having a dibasic carboxyl group. The compound is represented by Formula (1)[X--O--(R.sup.1 O).sub.m --OC--R.sup.2 --COO].sub.y M (1)where M is a hydrogen atom, a metal atom or a quaternary nitrogen-containing group, y is equal to the valence of M, R.sup.1 is at least one hydrocarbon group, R.sup.2 is a moiety of a dibasic acid or a moiety of its anhydride, m is 0 or an integer of 1 to 1,000, and X is a hydrocarbon group having at least one polymerizable double bond of carbon--ncarbon which may contain an oxygen atom and a fluorine atom.

Abstract: Process for preparing solid, free-flowing water-soluble salts of aryloxy-C.sub.1 -C.sub.4 -alkanecarboxylic acids by reacting the aryloxy-C.sub.1 -C.sub.4 -alkanecarboxylic acids with a salt-forming base, the salt formation taking place in the melt in the presence or absence of an entraining agent suitable for the azeotropic removal of water or in solution in the presence of an entraining agent suitable for the azeotropic removal of water and, if appropriate, removing the entraining agent from the reaction mixture during the reaction or subsequently and then isolating the solid salts in a customary manner.

Abstract: Selective thyroid hormone agonists are disclosed that are highly selective for the TR.beta. subtype with high binding affinity. Methods of using such agonists and pharmaceutical compositions containing them are also disclosed, as are novel procedures for their preparation.

Abstract: A solid phase synthesis method and intermediates useful in the process are disclosed for the preparation of diamino diol and diamino alcohol inhibitors of HIV protease.

Abstract: Process for the preparation of alkyl aryl ethers containing carboxyl groups which are suitable for the preparation of colour film couplers, or derivatives thereof, by reaction of aromatic alcohols with alkyl halides containing carboxyl groups or derivatives thereof and basic alkali metal or alkaline earth metal compounds, characterized in that the reaction is carried out in the melt of the aromatic alcohol.

Abstract: A process for preparing oxime ethers of the general formula I ##STR1## where R.sup.1 is a C-organic radical,R.sup.2 is hydrogen, alkoxy, cyano, nitro, SOR.sup.4, SO.sub.2 R.sup.4, CO.sub.2 -alkyl, P(O)(OR.sup.4).sub.2 or a C-organic radical, andR.sup.3 and R.sup.4 are unsubstituted or substituted C.sub.1 -C.sub.6 -alkyl, entails converting an oxime of the general formula II ##STR2## where the substituents R.sup.1 and R.sup.2 have the abovementioned meanings, in the presence or absence of an organic diluent, with a base into the corresponding salt, and reacting the latter with a dialkyl carbonate of the general formula III ##STR3## where R.sup.3 has the abovementioned meanings.

Abstract: Phenoxyphenylacetic acids and derivatives of general structural formula (I) have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.

Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##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: New substituted 2,2-dimethyl-.omega.-phenoxyalkanoic acids and esters of formula: ##STR1## wherein: X, A, B, R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and Z are as defined in the specification,The corresponding enantiomers and diastereoisomers, and the physiologically tolerable salts thereof with appropriate bases.The products of the invention may be used therapeutically.

Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.

Abstract: Mechanically stable, self-inverting water-in-oil polymer emulsions for use in industrial water treatment, waste water treatment, sludge conditioning, ore dressing, papermaking, secondary and tertiary oil recovery containing carboxylated ethoxylated phenols and alcohols are provided.

Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein Ar is a mono- or bicyclic aromatic group optionally containing one or two heteroatoms independently selected from nitrogen, oxygen and sulphur, said group being optionally substituted by one or more atoms or groups independently selected from halogen, nitro, amino, --NRR.sup.1 where R and R.sup.1 are independently selected from hydrogen, C.sub.1-8 alkyl and C.sub.1-8 alkanoyl, cyano, carboxyalkoxy, alkoxycarbonylalkoxy, C.sub.1-8 alkyl (including cycloalkyl and cycloalkylalkyl), C.sub.1-8 alkoxy (including cycloalkoxy and cycloalkylalkoxy), C.sub.

Abstract: Compounds of Formula I ##STR1## wherein the symbols are as defined in the specification.

Abstract: A process for the preparation of 2,2-dimethyl-5-(2,5-xylyloxy)-valeric acid, which process comprises the reaction of 2,5-dimethylphenol with a compound of formula (II), ##STR1## wherein R is an alkyl, aryl, arylalkyl group and --X is a halogen atom, and the subsequent hydrolysis to compound (I), characterized in that the reaction of compound (II) with 2,5-dimethylphenol is carried out in the absence of solvents and in the presence of an ammonium or quaternary phosphonium salt.

Abstract: Optically active .alpha.-(hydroxyphenoxy)-alkanecarboxylic acids or derivatives thereof, for example D-2-(4-hydroxyphenoxy)propionic acid or lower alkyl ester thereof, are prepared by (a) saponifying an alkyl ester of an optically active .alpha.-halogeno-alkanecarboxylic acid, in an alcoholic solvent medium, by reacting same with an aqueous solution of an alkali metal hydroxide, thereby providing a solution of an alkali metal salt of an optically active .alpha.-halogeno-alkanecarboxylic acid, (b) next reacting the step (a) solution thus provided with a dihydroxybenzene or salt thereof, in the presence of an alkali metal hydroxide and in an alcoholic solvent medium, and thence (c) recovering the optically active .alpha.-(hydroxyphenoxy)-alkanecarboxylic acid or derivative thereof from the medium of reaction.

Abstract: The invention relates to 4-substituted isoxazole derivatives of formula I: ##STR1## wherein R, R.sup.1, R.sup.2, Q and n have the meaning defined in the description which possess valuable herbicidal properties.

Abstract: Disclosed is a preparation for external application to the skin characterized by containing at least one of benzoic acid derivatives represented by formula (I) or pharmacologically acceptable salts thereof as an active ingredient, the preparation having sufficient sebaceous secretion inhibitory activity with no substantial side effect and high safety for human body. ##STR1## wherein R.sup.1 represents --OH, --OR.sup.3 or --NHR.sup.3 ; R.sup.2 represents a hydrogen atom, a lower alkyl group or a lower acyl group; R represents --O--R.sup.4 or ##STR2## R.sup.3 represents an alkyl group, an alkenyl group or a hydroxyalkyl group; R.sup.4 represents a straight-chain or branched, saturated or mono-unsaturated alkyl group or cycloalkylalkyl group having from 4 to 10 carbon atoms; X represents --O-- or --NH--; and n represents 1 or 2.

Abstract: The invention relates to caged compounds for the study of biological processes, where the caged compound has a photoremoveable .alpha.-carboxy-substituted o-nitrobenzyl group. Covalent attachment of the substituted o-nitrobenzyl to a parent compound yields a caged compound with biological and/or physical properties that are significantly altered from the original properties of the parent compound. Illumination of the caged compounds to cleave the photoremoveable group yields the parent compound with its original properties restored.

Abstract: Lactones of formula ##STR1## and their pharmacologically acceptable salts endowed with antioxiding and hypolipidaemic properties and that show the capability to prevent and/or to delay the oxidative modification of the lipoproteins by competing with the chain of propagation of the lipidic peroxidation by means of an effective scavenging of the peroxylic radicals. The compounds object of the present invention are useful in the treatment of the atherosclerosis and of many correlated vascular pathologies, like ischaemic cardiopathies (angina pectoris and myocardial infarction), cerebral thrombosis and peripheral arteriopathies, because the high plasma levels of lipids and the oxidative modifications of the low density lipoproteins (LDL) represent crucial events in the pathogenesis of the atherosclerosis.

Abstract: There are disclosed novel hydroquinone derivatives of the formula: ##STR1## The derivatives of the formula (I) have various pharmacological activities such as antioxidation in living bodies and are useful as medicaments.

Abstract: Compounds of formula (I): ##STR1## [wherein: R.sup.1 is aryl; R.sup.2 is hydrogen, alkyl, alkoxy, halogen or cyano; R.sup.3 is a group of formula --B--NR.sup.4 R.sup.5, where R.sup.4 and R.sup.5 are independently hydrogen, alkyl or substituted alkyl or R.sup.4 and R.sup.5, together with the nitrogen to which they are attached, form a heterocycle, and B is alkylene or a group of formula --CH.sub.2 CH(OR.sup.6)CH.sub.2 --, where R.sup.6 is hydrogen, alkanoyl, substituted alkanoyl or arylcarbonyl, or a group of formula --D--R.sup.7, where D is a single bond or alkylene and R.sup.7 is a heterocycle; and A is alkylene; and pharmaceutically acceptable salts and esters thereof] are useful for the treatment and prevention of circulatory diseases and psychosis.

Abstract: Novel anticholesteremic compounds capable of reducing blood cholesterol levels. Also included in this invention are (i) intermediates from which the abovementioned anticholesteremic compounds can be prepared, and (ii) methods for preparing both the intermediates and the anticholesteremic compounds.