Abstract: There are described novel biocatalytic and chemical processes for the synthesis of various oxygenated compounds. Particularly, there are described processes for the synthesis of a useful synthon 12 made by reacting a protected diol (acetonide) with permaganate under appropriate conditions. Such synthon is useful of the synthesis of various pharmaceutically important compounds such as D-chiro-inositol and D-chiro-3-inosose. Also, there are disclosed novel compounds, including specifically the synthon 12 and compounds derived therefrom.

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 present invention relates to a chromone derivative and an aldose reductase inhibitor comprising said compound as efective component, which is represented by the following formula: ##STR1## wherein R.sub.1 and R.sub.2 each represent a lower alkyl group, etc., R.sub.3 represents an oxygen atom, a sulfur atom, etc., R.sub.7 represents a phenyl group substituted or not substituted, etc., and R represents a hydrogen atom or a lower alkoxy group. The present compounds exhibit superior inhititory action on aldose reductase and are useful for the treatment of various complications of diseases in diabetes, such as cataract, retinopathy, keratopathy, nephropathy, and neuropathy.

Abstract: This invention provides novel compounds and pharmaceutical methods comprising the administration of a compound of the Formula I: ##STR1## wherein n, m, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are variables.

Abstract: Abstract of the Disclosure: Compounds of the formula I ##STR1## where R.sup.1 is H or C.sub.1 -C.sub.4 -alkyl, R.sup.2 is C.sub.1 -C.sub.4 -alkyl and R.sup.3 is an ether, silyl ether or acetal protective group which can be converted into a hydroxyl group by hydrolysis, in particular one of the radicals ##STR2## and a process for preparing these compounds by reacting an alkenyne of the formula II ##STR3## in an inert solvent in the presence of lithium amide with a cyclohexenone of the formula III ##STR4## and the use of the compounds of the formula I for preparing astaxanthin, are described.

Abstract: Method for inhibiting aldehyde dehydrogenase activity using daidzin and/or daidzin analog and/or daidzin or daidzin analog in combination with a factor or factors which increase the bioavailability of the daidzin or daidzin analog, as ALDH-I inhibitory compounds or compositions. Such inhibitory compounds or compositions are useful as pharmaceutical compositions in methods for the treatment of alcohol dependence (i.e., alcoholism) or alcohol abuse, for alcohol sensitization, for extinguishing an alcohol-drinking response, for suppressing an urge for alcohol, for inducing alcohol intolerance, for preventing alcoholism in an individual with or without a susceptibility or predisposition to alcoholism or alcohol abuse, and for limiting alcohol consumption in an individual whether or not genetically predisposed.

Abstract: 4-(Fluorobenzoylamino)-3,4-dihydro-benzopyran derivatives are disclosed to possess anxiolytic and anti-convulsant activities.

Abstract: The present invention relates to the use of compounds of formula I ##STR1## wherein R.sup.1 is independently hydrogen, hydroxy, alkyl with 1 to 6 carbon atoms, acyloxy groups with 1 to 6 carbon atoms, alkyloxy with 1 to 6 carbon atoms or from 1 to 5 sugar moieties; and R.sup.2 is independently hydrogen, or alkyl with 1 to 6 carbon atoms, in the reduction of coagulation time in mammals.

Abstract: A process for preparing 2,2-difluoroketene silyl acetals and .alpha.,.alpha.-difluoro-.beta.-silyloxy-1,3-dioxolane-4-propanoic acid esters using these acetals.

Abstract: Starting from a mixture containing tocopherol, fats and/or fat derivatives, more particularly fatty acids, and optionally sterol and/or sterol derivatives, the free fatty acids present in the mixture are esterified with an alcohol. The mixture is then transesterified with an alcohol in the presence of a basic catalyst. After the transesterification, the excess lower alcohol is distilled off from the reaction mixture. The transesterification catalyst and the glycerol present, if any, are removed and the fatty acid alkyl ester is distilled off from the mixture. Distillation of fatty acid alkyl esters can be accomplished with a packed column in sequence with a wiped film evaporator. The simultaneous recovery of tocopherol and sterol is possible. Tocopherols and sterols can be separated by the crystallization of sterols from a blend of organic solvents.

Abstract: The present invention provides crystals of L-phenylalanine monomethyl sulfate which have low solubility compared to L-tyrosine and D-phenylalanine. The L-phenylalanine monomethylsulfate crystals are obtained by subjecting a solution containing monomethyl sulfuric acid and phenylalanine to crystallization.Further, the present invention also provides a process for recovering L-phenylalanine from a water layer by neutralizing the esterified reaction, extracting an ester of L-phenylalanine therefrom with an organic solvent, and recovering remaining L-phenylalanine in the water layer as L-phenylalanine monomethylsulfate. L-phenylalanine monomethyl sulfate is obtained by esterifying L-phenylalanine and methanol in the presence of sulfuric acid, neutralizing the esterified solution with a base in the presence of water, extracting the produced L-phenylalanine methyl ester from the neutralized solution with an organic solvent, and then crystallized the resultant water layer under acidic condition.

Abstract: The present invention provides a reverse transcriptase inhibitor and an antiviral agent comprising at least one member selected from the group consisting of sulfated tyrosines and physiologically acceptable salts thereof as an effective component; and exhibiting less toxicity and a remarkable inhibitory effect against a reverse transcriptase existing in viruses as well as a remarkable anti-AIDS viral activity.

Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein a, b and d are all carbon atoms or one of a, b and d is a nitrogen atom or --N(O)-- and the others are carbon atoms; Y is a single bond, --CH.sub.2 --, --C(O)--, --O--, --S-- or --N(R.sup.8)--; and R.sup.1 to R.sup.7 are as defined herein. These compounds have potassium channel activating activity and are useful, therefore for example, as cardiovascular agents.

Abstract: This invention relates to a process for the preparation of a 6,7-diacyl-7-deacetylforskolin derivative represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 each stands for an acyl group and R.sup.3 stands for an aliphatic group having 2 to 3 carbon atoms, which comprises eliminating the acyl group at position 1 in a 1,6,7-triacyl-7-deacetylforskolin derivative represented by the general formula: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, by solvolysis. The compound of the formula (I) is expected as medicine.

Abstract: Tocopherol derivatives of the following formula (I) or a pharmacologically acceptable salt thereof ##STR1## wherein R.sub.l and R.sub.2 are the same or different and each represents hydrogen or methyl; R.sub.3 represents an .alpha.-amino acid, .omega.-amino acid, or peptide bonding via the N terminus thereof, except that in the case of cysteine or glutathione which has a thiol group, bonding via the thiol group, are water-soluble and can be expected to be of use as a cerebral function-improving drug and an anticataract drug. Moreover, these compounds are of value as an UV-absorber, a skin care ingredient, or a stabilizer for other cosmetic ingredients.

Abstract: A process for the preparation of a cyclic ether ketone of the general formula I ##STR1## in which R.sup.1 and R.sup.2 denote hydrogen or C.sub.1 -C.sub.4 alkyl, m and n denote integers from 1 to 5, in which a cyclic ether aldehyde of the general formula I ##STR2## in which have R.sup.1, R.sup.2, m and n have the above meanings, is reacted with an oxygen-containing gas in the presence of a solid or supported catalyst containing copper and/or manganese, at temperatures of from 50.degree. to 300.degree. C. and pressures of from 0.01 to 10 bar.

Abstract: There are described novel biocatalytic and chemical processes for the synthesis of various oxygenated compounds. Particularly, there are described processes for the synthesis of a useful synthon 12 made by reacting a protected diol (acetonide) with permaganate under appropriate conditions. Such synthon is useful of the synthesis of various pharmaceutically important compounds such as D-chiro-inositol and D-chiro-3-inosose. Also, there are disclosed novel compounds, including specifically the synthon 12 and compounds derived therefrom.

Abstract: There are described novel biocatalytic and chemical processes for the synthesis of various oxygenated compounds. Particularly, there are described processes for the synthesis of a useful synthon 12 made by reacting a protected diol (acetonide) with permaganate under appropriate conditions. Such synthon is useful of the synthesis of various pharmaceutically important compounds such as D-chiro-inositol and D-chiro-3-inosose. Also, there are disclosed novel compounds, including specifically the synthon 12 and compounds derived therefrom.

Abstract: The invention disclosed novel triterpene derivatives of azadirachtin of the formulae 2 to 11 of the drawings and a process for isolating new triterpene derivatives of azadirachtin from the various parts of the neem plant(Azadirachta indica A-Juss), which process comprises grinding the parts of the neem plant to get a powder, extracting the powder with a binary immiscible solvent consisting of one polar and another non-polar solvent in a ratio of 1:2 to obtain an extract, filtering the extract to get a filtrate having two layers, one layer containing lipids and the other layer containing the new triterpene derivatives of azadirachtin and water soluble constituents including sugars, separating the layers by known methods, concentrating the layer containing the new triterpenes of the formulae 2-11 including derviatives of azadirachtin and water soluble salts, treating the resultant concentrate with a polar solvent and if necessary, warm the concentrate having the solvent, and filtering/decanting the resultant so

Abstract: Amino acid derivatives of formula (Ia) and (Ib) and prodrugs thereof containing a group responsible for chelating the zinc atom of enkephalinase and angiotensin convertase enzymes are disclosed as inhibitors of these enzymes.