Abstract: The invention relates to a process for preparing a compound of (III) wherein X is a leaving group; and R1 is C1-C6 alkyl; which comprises oxidative rearrangement of a compound of formula (II) or a solvate thereof Compounds of formula (III) are key intermediates in the synthesis of Bilastine.

Abstract: Substituted phenacyl molecules are provided and employed to create molecules and polymers/copolymers that exhibit photoresponsiveness. In some instances, the substituted phenacyl molecule is incorporated into the polymer/copolymer backbone, and photoirradiation of the polymer/copolymer causes the substituted phenacyl group to break down and the polymer/copolymer to undergo degradation. In other instances, the substituted phenacyl molecules extend as a side chain from the polymer/copolymer backbone. In yet other instances the substituted phenacyl molecules extend as a side chain from the polymer/copolymer backbone, and a drug or polymer additive is linked to the photoresponsive substituted phenacyl group such that photoirradiation releases the drug or additive. In yet other embodiments the substituted phenacyl molecules extend as a side chain from the polymer/copolymer backbone, and serve to link the polymer/copolymer to another polymer/copolymer backbone, and photoirradiation breaks the links.

Abstract: The use is described of the 4-hydroxychalcone derivatives of the formula (I) wherein A may represent a single or double bond, R1, R2 and R3, mutually independently, may in each case mean H, OH or (preferably C1-C4) alkoxy, providing that at least one of the residues R1 to R3 means OH, and R4 means H, OH or (preferably C1-C4) alkoxy, and/or (ii) the salts thereof and (iii) mixtures thereof to mask or reduce the unpleasant taste impression of an unpleasant tasting substance, as are corresponding methods and preparations.

Abstract: Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula (I) or its pharmaceutically acceptable salts. The uric acid-lowering effects of the compounds of this invention are used to treat or prevent a variety of conditions including gout, hyperuricemia, elevated levels of uric acid that do not meet the levels customarily justifying a diagnosis of hyperuricemia, renal dysfunction, kidney stones, cardiovascular disease, risk for developing cardiovascular disease, tumor-lysis syndrome, cognitive impairment, early-onset essential hypertension, and Plasmodium falciparum-induced inflammation. R1 is hydrogen or alkyl having from 1 to 3 carbon atoms. R2 is alkyl having from 1 to 3 carbon atoms, alkoxy having from 1 to 3 carbon atoms, hydroxy, nitro, halo, thio, alkylthio, or cyano. R3 and R4 are each independently hydrogen, methyl, ethyl, perfluoromethyl, methoxy, ethoxy, perfluoromethoxy, halo, hydroxy, nitro, or amino.

Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.

Abstract: The present invention involves substituted 1,3-diphenylpropane derivatives, pharmaceutical compositions comprising them and the therapeutic uses thereof, in particular in the fields of human and animal health.

Abstract: The present invention concerns substituted 1,3-diphenylpropane derivatives, pharmaceutical compositions comprising them and the therapeutic uses thereof, particularly in the field of human and animal health.

Abstract: Disclosed are a curcumin derivative or a salt thereof, which contains a fluorine atom, represented by formula (I): (wherein R1a and R1b are each independently a hydrogen atom, alkyl, acetyl, or methoxycarbonyl; R2s are each independently a fluorine atom, CHF2—, CF3—, CHF2O—, or CF3O—; R3s are each independently a hydrogen atom or a fluorine atom; A is alkyl, cyano, carboxyl, alkoxycarbonyl, or R4—(CH2)m—; R4 is hydroxy, carboxy, cyano, acetyloxy, alkoxycarbonyl, alkoxyalkoxy, hydroxyalkoxy, or CONR5R6; R5 and R6 are each independently a hydrogen atom or alkyl; and m is an integer from 1 to 5), and a diagnostic imaging agent for diagnosing a disease in which an amyloid ? peptide aggregate accumulates, the diagnostic imaging agent containing a compound having a 1,3-dicarbonyl structure, wherein the compound exists in a keto form and an enol form, and the keto form and the enol form have different affinities, respectively, to the amyloid ? peptide aggregate.

Abstract: The present invention concerns substituted 1,3-diphenylpropane derivatives, pharmaceutical compositions comprising them and the therapeutic uses thereof, particularly in the field of human and animal health.

Abstract: The present invention is a mitochondria-targeted antioxidant prodrug useful for the prevention or treatment of diseases or conditions associated with mitochondrial dysfunction resulting from changes in the mitochondrial redox environment. Antioxidant prodrugs of the invention are produced by modifying an antioxidant to a fatty acid so that the resulting prodrug is targeted to and activated by an enzyme of mitochondrial fatty acid beta-oxidation.

Abstract: The present invention is directed to practical high-yielding synthetic processes to prepare compounds of general Formula III, IV, V, VII, VIII, IX, X, XII, XIV, and XV. Such compounds are useful as final products or can be used as intermediates and be further modified to prepare other desired products such as rho-kinase inhibitors. The present invention is also directed to certain novel compounds and/or novel solid forms of certain compounds.

Abstract: The present invention generally relates to salts of abscisic acid analogs, aqueous liquid compositions containing salts of analogs of abscisic acid and methods of their preparation for agricultural use.

Abstract: Components that demonstrate an ?-glucosidase inhibitory activity and hyperglycemic inhibitory activity have clearly been provided from among the components included in Yacon. The present inventors found that as a result of screening for a strong anti-oxidant component in a Yacon aerial portion extract, an antioxidant activity was converged in a DIAION HP-20 column chromatography 50% methanol-eluted fraction of hot water extract. Thus, since a previously unidentified high-content component was confirmed, the present inventors conducted purification thereof, and thereby separated TCAA. As a result, this TCAA was found to be the component that demonstrates the ?-glucosidase inhibitory activity and hyperglycemic inhibitory activity.

Abstract: Compounds containing both photoinitiator moieties and adhesion promoting moieties and coating formulations containing them are disclosed, in particular, durable UV cured primer layers for coil coatings. One embodiment includes a coated metal surface which comprises a metal substrate with at least one surface immediately adjacent to a coating layer comprising a photoinitiator chemically bound to an adhesion promoter is disclosed.

Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.

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 wherein X, Z, X1, R1, R2, Ra, Rb, R3, R4 and Y are as defined in the specification.

Abstract: A substrate for solid phase synthesis comprising a solid phase-linker combination of the formula I is disclosed. Also disclosed are processes for preparing the substrate and chemical intermediates useful therein. Among the novel intermediates are compounds of the formula II wherein R1 is —NO2 or —CHO; R2 is —OCH3, —CHO or —H; R3 is chosen from the group consisting of hydroxyl, the residue of a solid support having a plurality of amino groups, and the residue of an ester, and n=1 or 3-12.

Abstract: Disclosed are (i) compounds of a steroid, a &bgr;-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO2 group or a group which stimulates endogenous production of NO or EDRF in vivo; (ii) compositions of steroids, &bgr;-agonists, anticholinergics, mast cell stabilizers and PDE inhibitors, which can optionally be substituted with at least one NO or NO2 moiety or a group which stimulates endogenous production of NO or EDRF in vivo, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or that stimulates endogenous production of NO or EDRF in vivo; and (iii) uses for them in preventing and/or treating respiratory disorders.

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: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, posses an antagonistic activity on leukotriene B.sub.4.

Abstract: A new type of yellow dyes with general formula Q-CO--CO--X is disclosed. They can be used in photographic materials as antihalation dyes, acutance dyes or filter dyes. Preferably they are incorporated in UV sensitive contact materials for pre-press applications.

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: 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: This invention provides certain 1,2,4,5 substituted benzene derivatives containing "acid" substituents derived from cyclic or heterocyclic moieties. These unique compounds are leukotriene B.sub.4 antagonists and formulations of these derivatives, and a method of using these derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.

Abstract: New substituted phenoxyisobutyric acids and esters that can be used as medicaments and correspond to the formula: ##STR1## wherein X, A, 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 description.Those compounds and their physiologically tolerable salts can be used therapeutically.

Abstract: The invention provides a process for the preparation of fungicidally active cyclopentene derivatives of the general formula ##STR1## cyclopentane derivatives of the general formula ##STR2## and cyclohexane derivatives of the general formula ##STR3## in which n, R, R.sup.1, R.sup.2, R.sup.5, X and Y are as herein defined. Compounds of formula II and III are also provided which are useful as intermediates in the preparation of certain fungicidally active cyclopentane derivatives.

Abstract: This invention relates to novel compounds for treating inflammatory conditions by inhibition of phospholipase A.sub.2 activity of the formula ##STR1## wherein X is oxygen, sulfur or --CH.dbd.CH--; wherein R.sup.1 is hydrogen, alkyl of 1 to 6 carbons or a pharmaceutically acceptable cation;wherein R.sup.2 is phenoxy, alkoxy, methyl, trifluoromethyl or phenyl;wherein n is an integer from 1 to 20;compositions comprised of the novel compounds; and methods of treating inflammatory conditions with these compositions.

Abstract: The present invention relates to an anti-ulcer agent comprising a compound represented by the following general formula I as the effective ingredient, and a novel chalcone derivative included in the compound represented by this general formula I: ##STR1## wherein X and Y independently stand for a hydrogen atom or together form a single bond, R.sub.1 stands for a hydroxyl group, an acetoxy group, a carboxymethoxy group or a methoxycarbonylmethoxy group, R.sub.2 stands for a hydrogen atom, an isoprenyl group, isopentyl group or a propyl group, R.sub.3 stands for hydroxyl group or a methoxy group, R.sub.4 stands for a hydrogen atom, a hydroxyl group or a methoxy group, R.sub.5 stands for a hydrogen atom, a hydroxyl group, a methoxy group or an isopentyl group, R.sub.6 stands for a hydroxyl group, a methoxy group or a carboxymethoxy group, and R.sub.7 stands for a hydrogen atom or a methoxy group.

Abstract: Phenoxyalkylcarboxylic acid derivatives of the following formula, ##STR1## wherein R.sup.1 indicates a hydrogen atom, a methyl group or an ethyl group, m is equal to 2, 3 or 4, and n is equal to 3 or 4, their alkali salts and hydrates thereof are useful as antiallergic agents.

Abstract: A process has now been discovered by which an intermediate in preparation of antibiotics ##STR1## may be directly derived from the substrate ##STR2## by treatment with aqueous solutions of MHCO.sub.3 and MOH, wherein: R.sup.1, R.sup.2 and R.sup.3 are each independently alkyl, alkenyl, alkynyl, substituted alkyl, substituted alkenyl, substituted alkynyl, aryl, or substituted aryl;M is alkali metal (such as Na, Li, or K); andX is halogen.

Abstract: This invention relates to a process for making a compound of formula I ##STR1## in the form of a stereoisomer or mixture thereof, wherein R is hydrogen, lower alkyl; X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy, and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta., or a pharmaceutically acceptable, non-toxic salt of the compound wherein R is hydrogen; novel intermediates useful for preparing these compounds; processes for making the intermediates; and a stereoisomer of the compound of formula I wherein R is methyl and X is hydrogen and a process for making same.

Abstract: A novel phenoxycarboxylic acid of formula (I) is disclosed. The compound is effective as herbicide for eradicating broad-leaved weeds. A combination of the phenoxycarboxylic acid and a N-phosphonomethylglycine or a glufosinate which is known as a herbicide is very effective for eradicating both broad-leaved weeds and narrow-leaved weeds.

Abstract: Compounds are described of formula (I) ##STR1## in which n is 1 or 2;m is 2-5 and X is --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --; or m is 1-4 and X is --CH.dbd.C.dbd.CH--;R.sup.1 is --H, alkyl, phenalkyl, phenyl, substituted phenyl or naphthyl;Y substituted or unsubstituted 3-phenoxy-2-hydroxypropyl.These compounds inhibit gastric acid secretion and provide gastrointestinal cytoprotection, and may be formulated for use in the treatment of ulcers.

Abstract: Phenoxycarboxylic acids of the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 R.sub.5, Z and n are as hereinafter set forth, are as described. The compounds of formula I are antagonists of slow reacting substance of anaphylaxis (SRS-A), which renders them useful as agents for the treatment of allergic conditions.

Abstract: This invention provides novel compounds which are leukotriene antagonists, certain novel intermediates to the compounds, formulations of the compounds, and a method of using the compounds for the treatment of conditions characterized by an excessive release of leukotrienes.

Abstract: The present invention is directed to compounds of the general formula I and pharmaceutically acceptable salts thereof: ##STR1## wherein: R=ethyl, propyl or isopropyl; andA=(CH.sub.2).sub.n wherein n is 2, 4 or 5, and C(CH.sub.2).sub.3.

Abstract: A method of producing benzoyloxyphenoxy pentanoic acid esters comprising the steps of: (a) reacting a compound of the formula ##STR1## wherein A is as defined with a compound of the formula ##STR2## wherein X is as defined, in the presence of a base selected from carbonate salts of alkaline earth or alkali metals, a catalyst and a ketonic solvent to produce a 3-(4-benzyloxyphenoxy)-2-butanone; and (b) reacting said 3-(4-benzyloxyphenoxy)-2-butanone with a dialkyl carbonate of the formula (RO).sub.2 CO, wherein R is an alkyl group having from 1 to 4 carbon atoms, in the presence of a suitable base and an organic solvent, to form alkyl 4-(4-benzyloxyphenoxy)-3-oxopentanoate.

Abstract: The present invention is directed to compounds of the general formula I and pharmaceutically acceptable salts thereof: ##STR1## wherein R=H or lower alkyl;R'=H, lower alkyl, benzyl, CH.sub.2 OH;A=(CH.sub.2).sub.1 to 5, >C(CH.sub.3).sub.2, >C (CH.sub.2).sub.3 ; andX=0 or 1.The present invention is also directed to a method of treating a person for sickle cell anemia comprising administering to the person a therapeutically effective dosage of the above compounds.In addition the invention includes the novel compound: ##STR2## which is inaccessible by synthetic procedures previously described for this general class of compounds.

Abstract: This invention provides novel alkane derivatives which are leukotriene antagonists, formulations of those derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.

Abstract: A process for the addition reaction of an unsaturated organic compound, except a rubber, having at least one carbon-carbon double bond in a molecule, which comprises reacting the unsaturated organic compound with an organic compound having a carboxyl group and an aldehyde group in the presence of a Lewis acid.

Abstract: The invention relates to compounds of the formula ##STR1## wherein R is hydrogen or lower alkyl, Z is alkylene of 1 to 10 carbon atoms, --(C*H.sub.2).sub.3 --C.tbd.C--, --C*H.sub.2 --C.tbd.C--(CH.sub.2).sub.3 --, and --(CH.sub.2).sub.2 O].sub.n (CH.sub.2).sub.2 -- wherein n is an integer of 1 to 3, the carbon atom marked with an asterisk is linked to the phenoxy moiety,and salts thereof with pharmaceutically acceptable bases. The compounds of formula I are antagonists of slow reacting substance of anaphylaxis (SRS-A; leukotrienes C.sub.4, D.sub.4 and E.sub.4), which renders them useful as agents for the treatment of allergic conditions.

Abstract: 16-Fluoro-16,17-didehydro prostanoids, processes for their preparation, compositions containing them and methods of using them are disclosed. The compounds and compositions have pharmaceutical utility including, for example, luteolytic activity.

Abstract: The invention relates to novel substituted [2,3-dihydro-4-(3-oxo-1-cyclohexen-1-yl)phenoxy]-alkanoic acids their derivatives and their salts. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections and various brain concussions.

Abstract: This invention covers a compound of the formula ##STR1## wherein R is hydrogen, lower alkyl or a pharmaceutically acceptable, non-toxic salt of a compound wherein R is hydrogen; and X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy; and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta..

Abstract: Compounds of the formula (I): ##STR1## in which R.sub.1 represents alkyl containing from 1 to 18 carbon atoms, R.sub.2 represents hydrogen or alkyl containing from 1 to 8 carbon atoms and R represents hydrogen or alkyl containing from 1 to 8 carbon atoms, as well as the alkali metal, alkaline-earth metal or amine salts thereof, in which R represents hydrogen. Also, method of preparing same, compositions containing same and therapeutic treatment therewith.

Abstract: A process for the preparation of an optically-active (mixed) anhydride of an alpha-chiral (optically-active) carboxylic acid by treating a non-symmetrical ketene with a carboxylic acid in the presence of an optically-active (chiral) tertiary amine catalyst. Hydrolysis of the resulting (mixed) anhydride yields the optically-active acid corresponding to the non-symmetrical ketene.

Abstract: A process for the production of aryloxyalkylpyruvic acid of the general formula:(R).sub.n --A--O--(CR'.sub.2).sub.m --CR"H--COCOOHwherein:A represents an aromatic hydrocarbon radical containing 1 or 2 condensed benzene rings,R, R' and R" may be the same or different, and are selected from hydrogen and linear or branched alkyl radicals having up to about 6 carbon atoms,n is 0 or an integer from 1-5 when A contains one benzene ring, and n is 0 or an integer from 1-7 when A contains two condensed benzene rings and m is 0-20, which comprises carbonylating an aryloxyalkyl halide of the general formula:(R).sub.n --A--O--(CR'.sub.2).sub.m --CR"H--Xwhere R, R', R", n, A and m are as defined above and X represents halogen in a liquid solvent medium with carbon monoxide at elevated temperature and elevated pressure in the presence of a catalytic amount of a metal carbonyl compound and an alkali metal inorganic base or an alkaline earth metal inorganic base.

Abstract: Ascochlorin derivatives of the formula: ##STR1## wherein R is a hydroxyl group, a lower alkoxy group, a pyridyl group, an amino group, a dialkylamino group, a phenoxyalkyl group which may have a substituent in the nucleus, or a phenyl group which may have a substituent in the nucleus; and n is an integer of 0 to 5, a process for preparing the same and a pharmaceutical composition containing the same are disclosed.The derivatives are useful to treat diabetes, improve lipid metabolism and control tumors.

Abstract: The present invention provides chalcone derivatives of the general formulae: ##STR1## wherein R.sub.1 is a hydroxyl, carboxylic or sulphonic acid group or a carboxyalkoxy or sulphoalkoxy radical, R.sub.2 is an unsaturated, straight-chained or branched aliphatic hydroxycarbonyloxy radical, R.sub.3 is a hydrogen atom, a hydroxyl group or an alkoxy radical, R.sub.4 is an alkyl, hydroxyalkyl, alkoxy, carboxyalkoxy, sulphoalkoxy or carboxyalkylcarbonyloxyalkyl radical or a carboxylic acid or sulphonic acid group and R.sub.5 is a hydrogen or halogen atom, with the proviso that compounds of general formula (IIa) always contain at least one carboxylic or sulphonic acid group; and the nontoxic inorganic and organic salts of those compounds containing at least one carboxylic acid or sulphonic acid group.The present invention also provides a process for the preparation of these chalcone derivatives, as well as pharmaceutical compositions containing them.