Abstract: The present invention provides cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, methods of making cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs. The present invention also provides methods of using cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs.

Abstract: A novel monomer compound having a lactone moiety of the present invention can be converted into polymers usable as resist materials with excellent properties, etc., and an alcohol compound having a lactone moiety of the invention is useful as a material for the monomer compound. The compounds are represented by the following general formula [1]: wherein one of R1 and R2 represents a hydrogen atom, an acryloyl group, or a methacryloyl group, and the other represents an alkyl group; R3 and R4 independently represent a hydrogen atom or an alkyl group; R5 and R6 both represent a hydrogen atom or are combined to form a methylene chain that may have an alkyl group; and R7 and R8 independently represent a hydrogen atom or a methyl group.

Abstract: 5-carboxyphthalide is obtained with very high purity and in high yields by a convenient process comprising reaction of terephthalic acid with paraformaldehyde HO(CH2)nH in oleum.

Abstract: A dye thin film containing a dye compound represented by the general formula (I), an optical switch, an optical distributor, an optical modulator and an optical switch array having the dye thin film, as well as a method for producing a dye thin film are provided. The method includes the step of coating the solution of the dye compound on a substrate: where R1 and R2 may be identical or different from each other and each represents, respectively, a linear alkyl group or a branched alkyl group, the dye thin film having high thermal stability, having intense absorption at approximately 1.3 ?m and having ultrafast response characteristic.

Abstract: This invention is drawn to compounds which are more easily metabolized by the metabolic drug detoxification systems. Particularly, warfarin analogs which have been designed to include esters within the structure of the compounds are taught. The invention teaches methods of reducing the toxicity of drugs comprising the introduction of ester groups into drugs during the synthesis of the drug. This invention is also drawn to methods of treating coagulation disorders comprising the administration of compounds which have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester containing warfarin, analogs are also taught.

Abstract: A dibenzofuranonylium methylate compound represented by the following formula (I), having maximum absorption wavelength of over 1 &mgr;m, high thermal stability and good solubility in organic solvents, and a production method thereof are provided: where R1 and R2 may be identical or different from each other and each represents a linear alkyl group or a branched alkyl group, respectively.

Abstract: The invention describes novel compounds of the formula (I) wherein the general symbols are as defined in claim (1) and R1 is an aromatic radical with electron withdrawing substituents, as stabilizers for protecting organic materials, in particular polymers and lubricants, against oxidative, thermal or light-induced degradation and as scavengers for oxidized developer in color photographic material.

Abstract: The present invention is related to a compound of formula (I), salts and pro-drugs of the compound (I) and methods for treating and/or preventing partial or total ischemia, methods for treating and/or preventing pathologies associated with ischemia or with mitochondrial deficiencies.

Abstract: A safe and effective process for the oxidation of a primary or secondary alcohol to the corresponding aldehyde or ketone via the reaction of said alcohol with an anhydride solution of a 1,1,1-tri(C2-C4 alkanoyloxy-1,1-dihydro-1,2-benziodoxol-3(1H)-one, and a composition useful in this process.

Abstract: The (meth)acrylate of the present invention is represented by the following formula (1). The (meth)acrylate can be produced by first producing a lactone by reducing an addition product obtained by the Diels-Alder reaction between 1,3-diene and maleic anhydride, and then hydrating the lactone to produce an alcohol followed by (meth)acrylation of the alcohol. A polymer produced by (co)polymerizing a monomer composition comprising the (meth)acrylate of the present invention is excellent in transparency, dry etching resistance, and solubility in organic solvents, and so it is preferably used as a resin for a chemically amplified resist composition.

Abstract: There is described a process for the preparation of 5-carboxy phthalide, which comprises adding terephthalic acid to fuming sulfuric acid containing at least 20% of SO3, then adding formaldehyde to the mixture, heating the mixture at a temperature of 120-145° C. and isolating 5-carboxyphthalide from the reaction mixture.

Abstract: Disclosed is a novel process for the preparation of the anti-glaucoma drug Latanoprost, in good yield, in large amounts and with desired purity. Also disclosed are novel intermediates for the above process.

Abstract: The instant invention discloses a process for the preparation of compounds of formula I wherein the general symbols are as defined in claim 1, which process comprises hydrolyzing a compound of formula V wherein the general symbols are as defined in claim 1, in an aqueous solvent in the presence of an acid. The compounds of the formula V are new and useful as stabilizers for protecting organic materials, in particular polymers and lubricants, against oxidative, thermal or light-induced degradation.

Abstract: A product corresponding to formula (I) or its ketonic tautomer form (II) which is 3-(1-hydroxy-pentylidene)-5-nitro-3H-benzofuran-2-one, a process for the preparation and use of the product corresponding to formula (I) or its tautomeric form (II), a process for the preparation and use, particularly for the production of synthesis intermediates.

Abstract: This invention describes the novel use of alkyl, alkoxyl, halogenyl, or hydroxy substituted dicinnamoylquinides as therapeutic agents for enhancing adenosine levels in the brain and peripheral organs. These agents are particularly useful in treating human diseases or conditions that benefit from acute or chronic elevated levels of adenosine, such as reperfusion injury, coronary or cerebral ischemia, coronary vasoconstriction, paroxysmal supraventricular tachycardia, hypertension, wound healing, diabetes, inflammation, or sleep disturbances. They can also be used to protect normal cells from chemotoxicity in patients undergoing cancer therapy, and reverse the behavioral effects of caffeine intake.

Abstract: The present invention relates to a method for producing an &agr;-methylene-&ggr;-butyrolactone which is one of basic structures often shown in drugs such as an anti-cancer agent by reacting an alene compound having an aldehyde or ketone group with carbon monoxide via cyclization in a single step in the presence of a catalyst containing ruthenium, thereby improving total yield of the entire reaction and achieving effects of cost reduction.

Abstract: A process for the preparation of &agr;,&bgr;-unsaturated alcohols of general formula (I), wherein R means an alkyl group of 1-4 carbon atoms, or benzoyloxy group optionally substituted with a phenyl group; R1 means a hydrogen atom or an alkyl group of 1-4 carbon atoms, R2 means a hydrogen atom or an alkyl group of 1-4 carbon atoms; R3 means an alkyl group of 1-6 carbon atoms optionally substituted by phenyl group or cycloalkyl group of 5-7 carbon atoms; or a phenoxy group optionally substituted by a halogen atom, or a cycloalkyl group of 5-7 carbon atoms; R4 means a hydrogen atom or a halogen atom whereby at &agr;,&bgr;-unsaturated ketones of general formula (II) wherein the meanings of R, R1, R2, R3, and R4 are as given above—is diastereoselectively reduced with a borohydride type compound in an aprotic solvent, in the presence of an inorganic substance dissolublein the reaction mixture and having particle size from 0.

Abstract: The present invention relates to novel substituted (&agr;,&bgr;-fused butyrolactones, to processes for their preparation and to their use for the prevention and/or treatment of disorders caused by hyper- or hypofunction of the glutamatergic system, in particular of cerebral ischaemias, craniocerebral trauma, states of pain or CNS-mediated spasms.

Abstract: There is described a process for the preparation of 5-carboxy phthalide, which comprises adding terephthalic acid to fuming sulfuric acid containing at least 20% of SO3, then adding formaldehyde to the mixture, heating the mixture at a temperature of 120-145° C. and isolating 5-carboxyphthalide from the reaction mixture.

Abstract: Substantially pure preparations of phosphosesquiterpenes are described. The compounds inhibit farnesyl-protein transferase activity and are useful for the treatment of cancer. Methods for inhibiting farnesyl-protein transferase activity are also described.

Abstract: 5-carboxyphthalide is obtained with very high purity and in high yields by a convenient process comprising reaction of terephthalic acid with paraformaldehyde HO(CH2)nH in oleum.

Abstract: The present invention relates to oxygen-containing heterocyclic compounds represented by the following formula (I): wherein m represents an integer of 0 to 4; R1, R2, R3 and R4 independently represent a hydrogen atom, substituted or unsubstituted lower alkyl, etc.; R5 represents substituted or unsubstituted lower alkoxy etc.; R6 represents a hydrogen atom etc.; and Y represents the following formula (II): wherein R9 represents cyano etc., R10 represents a hydrogen atom etc., R11 represents carboxy etc., and R12 represents a hydrogen atom etc.; and the like; or pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to novel substituted bicyclic lactones, to processes for their preparation and to their use for the prevention and/or treatment of disorders caused by hyper- or hypofunction of the glutamatergic system, in particular of cerebral ischaemias, cranial cerebral trauma, states of pain or CNS-mediated spasms.

Abstract: A product corresponding to formula (I) or its ketonic tautomer form (II) 1

Abstract: Substantially pure preparations of phosphosesquiterpenes are described. The compounds inhibit farnesyl-protein transferase activity and are useful for the treatment of cancer. Methods for inhibiting farnesyl-protein transferase activity are also described.

Abstract: A bisphenol derivative represented by the following formula and a manufacturing method thereof are disclosed. where R is a lower alkyl group, tetrahydropyranyl, methoxymethyl or trialkylsilyl group, and the benzene rings in the formula may be substituted by a lower alkyl group.

Abstract: Methods for treating infection and related compositions, compounds of formula I as defined in the application and methods for preparing same, are provided. In general, the compounds inhibit transfer ribonucleic acid (tRNA) synthetase and are useful as antimicrobial agents.

Abstract: This invention relates to ketones represented by the following formula ##STR1## and to drugs in which such a ketone or pharmacologically acceptable salt thereof is an effective component.The ketones of the present invention encourage the production of platelets, red blood cells, white blood cells and the like, and can be used to prevent or treat cytopaenia brought about by cancer chemotherapy, radiotherapy, bone marrow transplantation and drug therapy, or by immunological abnormality or anaemia, and the like.

Abstract: Substantially pure preparations of phosphosesquiterpenes are described. The compounds inhibit farnesyl-protein transferase activity and are useful for the treatment of cancer. Methods for inhibiting farnesyl-protein transferase activity are also described.

Abstract: Hepatic diseases can be prevented or treated by administering an isoprenylamine derivative represented by the general formula (II) ##STR1## [wherein n represents an integer of 4-12, m represents an integer of 0-3, Ar represents a phenyl group, a furyl group, a thienyl group or a pyridyl group, said group being optionally substituted with one or more of an alkyl group of 1-4 carbon atoms, and alkoxy group of 1-4 carbon atoms, a methylenedioxy group, a hydroxy group or a halogen atom, and R represents a hydrogen atom or an alkyl group of 1-4 carbon atoms] or a pharmacologically acceptable salt thereof at a daily dose of 0.01-500 .mu.g/kg.A lipid emulsion of the compound (II) is particularly useful and can be administered at a remarkably lowered dose as compared with other pharmaceutical preparations.

Abstract: The disclosure is a process for preparing a phthalide of the general formula I ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each independently of the others hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy, by catalytic hydrogenation of a phthalic anhydride of the general formula II ##STR2## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each as defined above, in a solvent, which comprises using said phthalide I, the reaction product of the catalytic hydrogenation, as solvent.

Abstract: The disclosure is a process for preparing a phthalide of the general formula I ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each independently of the others hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy, by hydrogenation of a phthalic anhydride of the general formula II ##STR2## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each as defined above, with the aid of a hydrogenation catalyst, which comprises performing the hydrogenation with the aid of a nickel catalyst doped with metals of subgroup 1, subgroup 6 and/or subgroup 7 of the Periodic Table.

Abstract: A method for resolving optically impure 3-oxa-2-oxobicyclo?3.1.0!hexane-1-carboxylic acid esters. A method is provided for producing a 1-alkoxycarbonyl-2-hydroxymethylcyclopropane-1-carboxylic acid.N-benzyl-.alpha.-phenylethylamine diastereomer salt. An enantiomer of N-benzyl-.alpha.-phenylethylamine is reacted with a 1-alkoxycarbonyl-2-hydroxymethylcyclopropane-1-carboxylic acid to produce a precipitate that is enriched in one diastereomer of the salt. After isolating the optically active salt, the N-benzyl-.alpha.-phenylethylamine may be separated to produce the corresponding 1-alkoxycarbonyl-2-hydroxymethylcyclopropane-1-carboxylic acid. Under acidic conditions, the carboxylic acid and hydroxyl groups undergo ring closure to afford the optically active 3-oxa-2-oxobicyclo?3.1.0!hexane-1-carboxylic acid ester.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, acetoxy or acyl, and processes for preparing the same.

Abstract: A process for the preparation of a .gamma.-lactone of the formula ##STR1## which can be used to produce a single enantiomer of aminoazanoradamantane which is coupled to aromatic acid moieties to produce compounds useful as 5-HT agonists or antagonists.

Abstract: A difluoroprostacyclin of the following formula (V), its lower alkanol ester or its pharmaceutically acceptable salt: ##STR1## wherein A is an ethylene group, a vinylene group or an ethynylene group, R is a substituted or unsubstituted C.sub.1-10 alkyl group, a substituted or unsubstituted C.sub.1-10 alkenyl group, a substituted or unsubstituted C.sub.1-10 alkynyl group, a substituted or unsubstituted C.sub.3-8 cycloalkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryloxy group, Q is a substituted or unsubstituted C.sub.1-10 alkyl group, a substituted or unsubstituted C.sub.1-10 alkenyl group, a substituted or unsubstituted C.sub.1-10 alkynyl group, a substituted or unsubstituted C.sub.3-8 cycloalkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group.

Abstract: A compound of the formula (I) or its pharmaceutically acceptable salt or ester: ##STR1## and intermediates thereof.

Abstract: A bisphenol derivative represented by the following formula and a manufacturing method thereof are disclosed: ##STR1## where R is a lower alkyl group, tetrahydropyranyl, methoxymethyl or trialkylsilyl group, and the benzene rings in the formula may be substituted by a lower alkyl group.

Abstract: The present invention relates to the new thielocin derivatives, which exhibit phospholipase A.sub.2 inhibitory activity of the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are independently hydrogen, lower alkyl, lower alkoxy, hydroxy, or halogen;E.sub.1 and E.sub.2 are independently hydrogen, or an ester residue;m and n are independently an integer of 0 to 4;--Y-- is a bivalent group which is selected from the group consisiting of the following radicals: ##STR2## or the salts thereof.

Abstract: A method for reduction of an allyl alcohol-type compound, specific to its allylic hydroxyl group, being carried out without any side reactions such as reduction of other portions of the compound or allylic rearrangement, which comprises treating the compound with trialkylsilane in the presence of AlX.sub.3, wherein X refers to a halogen atom.

Abstract: A cyclopropane derivative represented by formula (I): ##STR1## wherein B represents a group of a purine derivative. In addition another aspect of the invention provides (3-oxa-2-oxobicyclo[3,1,0]hexan-1-yl)methanol and a method of preparing a cyclopropane derivative of formula (I) from this compound by replacing the hydroxyl group of the compound with a leaving group followed by reaction with a purine derivative.

Abstract: The present invention is directed to intermediates of the formula ##STR1## which are useful in a process for the preparation of aminoazanoradamanatanes.

Abstract: A method for producing an alkyl 3-phthalidylideneacetate has the step of treating phthalic anhydride with a monoalkyl malonate or a salt thereof having the following formula:MOCO--CH.sub.2 --COOR,wherein M represents a hydrogen atom, K, Na, Li, or NH.sub.4, and R represents a lower alkyl group having 1 to 5 carbon atoms. By using the above method, the desired alkyl 3-phthalidylideneacetate can be obtained at a high yield.

Abstract: Compounds of the formula (1) ##STR1## in which R.sub.2, R.sub.3, R.sub.4 and R.sub.5 independently of one another, are hydrogen, C.sub.1 -C.sub.25 alkyl, C.sub.7 -C.sub.9 phenylalkyl, unsubstituted or C.sub.1 -C.sub.4 alkyl-substituted phenyl, unsubstituted or C.sub.1 -C.sub.4 alkyl-substituted C.sub.5 -C.sub.8 cycloalkyl; C.sub.1 -C.sub.18 alkoxy, hydroxyl, C.sub.1 -C.sub.25 alkanoyloxy, C.sub.3 -C.sub.25 alkenoyloxy, C.sub.3 -C.sub.25 alkanoyloxy which is interrupted by oxygen, sulfur or >N--R.sub.16 ; C.sub.6 -C.sub.9 cycloalkylcarbonyloxy, benzoyloxy or C.sub.1 -C.sub.12 alkyl-substituted benzoyloxy, where R.sub.16 is hydrogen or C.sub.1 -C.sub.8 alkyl, or, furthermore, the radicals R.sub.2 and R.sub.3 or the radicals R.sub.4 and R.sub.5 together with the carbon atoms to which they are bound form a phenyl ring, R.sub.4 is additionally --(CH.sub.2).sub.n --COR.sub.11, in which n is 0, 1 or 2, R.sub.11 is hydroxyl, ##STR2## R.sub.14 and R.sub.15, independently of one another, are hydrogen or C.sub.1 -C.

Abstract: Improvement in the technique of synthesizing prostaglandins, particularly those having at least one halogen atom at the 16- or 17-position, which comprises introducing a .omega. chain into the aldehyde thereby to enable considerable yield improvement in the production of .alpha.,.beta.-unsaturated ketones, and which does not involve hydrogen generation and can insure safe operation.A method of producing .alpha.,.beta.-unsaturated ketones by reacting aldehyde with 2-oxoalkyl phosphonate, wherein the reaction was carried out under the presence of a base and a zinc compound.

Abstract: A method for reducing an .alpha.,.beta.-unsaturated ketone of the present invention includes the step of treating the .alpha.,.beta.-unsaturated ketone with a silyl compound in the presence of a Lewis acid and alcohol to selectively reduce the carbonyl group of the .alpha.,.beta.-unsaturated ketone. According to this method, a deoxy-compound can be obtained from the .alpha.,.beta.-unsaturated ketone by selectively reducing the carbonyl group without reducing an .alpha.,.beta.-unsaturated bond.

Abstract: The disclosed 6-substituted derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil.

Abstract: Novel compounds of formula (1) ##STR1## wherein R.sub.1 is hydrogen, alkyl or alkaryl, R.sub.2 to R.sub.5 are independently hydrogen, chloro, alkyl phenylalkyl, aryl, cycloalkyl, alkoxy, alkylthio, hydroxy, amino or substituted amino, R.sub.6 is hydrogen, R.sub.7 and R.sub.8 are hydrogen or alkyl, R.sub.9 and R.sub.9 ' are hydrogen, alkyl or phenyl, and R.sub.10 is hydrogen or alkyl, are disclosed as stabilisers for protecting organic materials against thermal, oxidative or light-induced degradation.

Abstract: Novel compounds of the formula (1), ##STR1## in which R.sub.1 is hydrogen or acyl, R.sub.2 to R.sub.5 are independently hydrogen, chloro, alkyl phenylalkyl, aryl, cycloalkyl, alkoxy, alkylthio, hydroxy, amino or substituted amino, R.sub.6 is hydrogen, R.sub.7 to R.sub.10 are independently hydrogen, alkyl or alkoxy, R.sub.17 or R.sub.19 is hydrogen or alkyl, and R.sub.18 is hydrogen, alkyl, aralkyl or aryl, are described for use as stabilizers for organic materials against thermal, oxidative or light-induced degradation.

Abstract: Disclosed are pH dyes containing a suitable compatible substituent which permits binding of the dye to a solid support. Also disclosed are methods for synthesizing such dyes prior to their coupling to the solid supports.