Abstract: A method of the invention industrially produces heterocyclic mercapto compounds useful as raw materials or intermediates in the synthesis of medicaments or pesticides, or as permanent wave agent, with a high yield and high productivity using easily available starting materials. A heterocyclic mercapto compound represented by Formula (1) (wherein X represents any structure of —O—, —S—, —NH—, and —NR1—; R1 represents any of an alkyl group, alkoxy group and alkoxyalkyl group each having 1 to 6 carbon atoms; Y represents an oxygen atom, a sulfur atom or —NR2—; R2 represents a hydrogen atom or alkyl group having 1 to 6 carbon atoms; and Z1 represents a divalent organic residue having at least one mercapto group) is produced by reacting a metal sulfide or a metal hydrosulfide with a compound represented by Formula (2) (wherein X and Y are as defined in Formula (1); and Z2 represents a divalent organic residue having at least one halogen group) in the presence of a solvent at a pH of 7.0 to 11.0.

Abstract: This invention provides new compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, prostate cancer, muscle wasting diseases and/or disorders or a bone-related diseases and/or disorders.

Abstract: The present invention discloses novel compounds of Formula (I): having 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I), as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11?-HSD type 1 activity.

Abstract: The present invention provides a compound of formula I and the use thereof for the inhibition of bacterial cell wall biosynthesis and for the therapeutic treatment of bacterial infection or disease in a patient in need thereof. The present invention also provides the use of the formula I compound for the control of ecto- or endoparasites in homeothermic animals.

Abstract: The present invention relates to 1,3-oxathiolane-2-thione compounds of the general formula (I): wherein R1 and R2 are the same or different, each of which denotes a straight-chain or branched alkoxy residue with 1 to 6 carbon atoms or an aryloxy or aralkyloxy residue, R3 is different or the same as R1 or R2 or an aliphatic residue, an amino residue, a halogen residue, an aromatic or heteroaromatic residue, or an araliphatic or heteroaraliphatic residue, R4 is a bridging group selected from the groups consisting of aliphatic, heteroaliphatic, araliphatic, heteroaraliphatic, aromatic and heteroaromatic groups and R5 is hydrogen, an aliphatic, heteroaliphatic, araliphatic, heteroaraliphatic, aromatic, heteroaromatic, cycloaliphatic or heterocycloaliphatic group or R4 and R5 form a cycloaliphatic, cycloheteroaliphatic, aromatic or heteroaromatic residue, which is optionally substituted with an aliphatic, heteroaliphatic residue serving as a bridging group to the silicon atom and X and Y are different and sele

Abstract: A method of an enantioselective nucleophilic addition reaction to carbonyl, which enables an asymmetric synthesis of an optically active ?-hydroxy-?-keto acid ester, an optically active ?-hydroxy-?-amino acid ester, hydroxydiketone compounds, etc. being useful as a raw material or synthesis intermediate for producing a pharmaceutical preparation, an agricultural chemical, a fragrance, a functional polymer or the like. In this method, the nucleophilic addition reaction of enamide compound accompanied by hydroxyl (—OH) formation to carbonyl is carried out in the presence of a chiral catalyst with copper or nickel.

Abstract: A compound of the formula wherein R1, R2, R3, R4, R5, R6, R?, R?, Y, CA+, and A? each, independently of the others are as defined herein.

Abstract: The present invention provides novel methods for preparing a key intermediate, 3,5-di-O-acyl-2-fluoro-2-C-methyl-D-ribono-?-lactone (2), for the preparation of 1-(2-deoxy-2-fluoro-2-C-methyl-?-D-ribofuranosyl)cytosine (1), which is a potent and selective anti-hepatitis C virus agent.

Abstract: The present invention relates to the side chain functionalization of fimbrolides (halogenated 3-alkyl-5-methylene-2(5H)-furanones) and their synthetic analogues, that yields fimbrolides substituted with a halogen, an oxygen or a nitrogen functionality in the alkyl chain, especially fimbrolide alcohols, carboxylate and sulfinate and sulfonate esters, ethers, aldehydes, ketones, acids, amides, nitro derivatives, hydrophobic, hydrophilic and fluorophilic alkyl derivatives and polymers.

Abstract: An object of the invention is to provide an aqueous solution of a No. 1 permanent waving agent through reconstitution upon use in a simple manner, which solution contains a cyclic mercapto compound as a reducing agent and realizes excellent characteristics such as high waving effect and good appearance of waved hair. The invention provides an alkylene carbonate dilution containing a cyclic mercapto compound in an amount of 7 to 80 wt. %; an alkylene carbonate for use in preparation of the alkylene carbonate dilution; and an aqueous reducing chemical agent which is prepared from the alkylene carbonate dilution and an aqueous base material.

Abstract: A catalyst for the hydrogenation of C4-dicarboxylic acids and/or derivatives thereof, preferably maleic anhydride, in the gas phase comprises a) 20-94% by weight of copper oxide (CuO), preferably 40-92% by weight of CuO, in particular 60-90% by weight of CuO, and b) 0.005-5% by weight, preferably 0.01-3% by weight, in particular 0.05-2% by weight, palladium and/or a palladium compound (calculated as metallic palladium) and c) 2-79.995% by weight, preferably 5-59.99% by weight, in particular 8-39.95% by weight, of an oxidic support selected from the group consisting of the oxides of Al, Si, Zn, La, Ce, the elements of groups IIIA to VIIIA and of groups IA and IIA of the Periodic Table of the Elements.

Abstract: Process for the continuous preparation of N-methyl-2-pyrrolidone (NMP) by reacting gamma-butyrolactone (GBL) with monomethylamine (MMA) in the liquid phase, wherein GBL and MMA are used in a molar ratio of from 1:1.08 to 1:2 and the reaction is carried out at from 320 to 380° C. and an absolute pressure of from 70 to 120 bar.

Abstract: The present invention provides a process for hydrogenating carbonyl compounds, in particular C4-dicarboxylic acids to mixtures of tetrahydrofuran and gamma-butyrolactone, over supported rhenium catalysts, wherein rhenium and at least one further metal of groups VIII or Ib of the Periodic Table of the Elements, in particular ruthenium (Ru), rhodium (Rh), palladium (Pd), osmium (Os), iridium (Ir), platinum (Pt), copper (Cu), silver (Ag) or cobalt (Co), is applied to the support in the form of at least one bimetallic precursor compound, and also to these catalysts.

Abstract: (A) A compound capable of forming a stable radical and selected from (A1) oxygen-atom-containing compounds each having a carbon-hydrogen bond at the adjacent position to an oxygen atom, (A2) carbonyl-group-containing compounds, and (A3) compounds each having a hydrocarbon group with a methine carbon atom is allowed to react with (B) a radical scavenging compound selected from, for example, (B1) unsaturated compounds, and (B2) compounds each having a hydrocarbon group with a methine carbon atom, in the presence of molecular oxygen by catalysis of, for example, an imide compound shown by the following formula (1): wherein each of R1 and R2 is a hydrogen atom or the like, where R1 and R2 may be combined to form a double bond, or an aromatic or non-aromatic ring; X is an oxygen atom or a hydroxyl group, to yield a product of an addition or substitution reaction of the compound (A) and the compound (B) or its oxidized product.

Abstract: Disclosed herein is a method for making compounds that are useful as caspase inhibitor prodrugs of formula I: wherein R1 is an optionally substituted group selected from an aliphatic group, aralkyl group, heterocyclylalkyl group or aryl group, and R2 is preferably a P2—P4 moiety of a caspase inhibitor.

Abstract: Prodrugs of carbidopa, derivatives of carbidopa prodrugs, methods of making prodrugs of carbidopa and derivatives thereof, methods of using prodrugs of carbidopa and derivatives thereof, and compositions of prodrugs of carbidopa and derivatives thereof are disclosed.

Abstract: The present invention relates to the side chain functionalization of fimbrolides (halogenated 3-alkyl-5-methylene-2(5H)-furanones) and their synthetic analogues, that yields fimbrolides substituted with a halogen, an oxygen or a nitrogen functionality in the alkyl chain, especially fimbrolide alcohols, carboxylate and sulfinate and sulfonate esters, ethers, aldehydes, ketones, acids, amides, nitro derivatives, hydrophobic, hydrophilic and fluorophilic alkyl derivatives and a polymers.

Abstract: A process of the present invention produces a hydroxylactone by subjecting an unsaturated carboxylic acid having a double bond not conjugated to a carboxyl group or an ester thereof to (i) a reaction with hydrogen peroxide in the presence of a metallic compound containing a metallic element selected from W, Mo, V and Mn or (ii) a reaction with a peroxide containing the metallic element to thereby yield a corresponding hydroxylactone having a hydroxyl group combined with one of carbon atoms constituting the double bond and being cyclized at the other carbon atom position. The metallic compound may be one selected from oxides, oxoacids and salts thereof. The unsaturated carboxylic acid includes, for example, ?,?-unsaturated carboxylic acids, ?,?-unsaturated carboxylic acids, and ?,?-unsaturated carboxylic acids. The process can produce hydroxylactones in high yields at low cost.

Abstract: For the preparation of an 11-oxaprostaglandin such as [2R,(1E,3R),3S,(4Z),4R)]-7-{tetrahydro-2-[4-(3-chlorophenoxy)-3-hydroxy-1-butenyl]-4-hydroxy-3-furanyl}-4-heptenoic acid and its ester derivatives, a novel process uses a novel enantiomerically enriched compound for formula (1) wherein the bond between carbon atoms y and z is either a single or double bond; R1 is selected from vinyl, trialkylsilylethynyl, a formyl group protected as an acetal, or a protected hydroxymethyl group; R2 is C1-5 alkyl, optionally substituted at the terminus with an aryloxy or alkoxy group; and R3-R6 are independently selected from C1-6 alkyl and C6-10 aryl

Abstract: The invention relates to chiral nonracemic liquid crystal compounds which are useful as components in liquid crystal compositions to impart high polarization to the mixture. The materials of this invention can be combined with liquid crystal host materials to impart improved properties to mixtures. Chiral nonracemic compounds of this invention can function as additives or dopants in host materials to impart chirality into an LC material.

Abstract: The present invention relates to obtain novel FT-0554A substance useful for infectious disease of parasite, especially helminth and more particularly relates to the novel FT-0554A substance represented by the following formula [I] or the tautomer thereof represented by the formula [II] obtained by treating FT-0554 substance represented by the formula [II] under alkaline condition.

Abstract: The invention relates to a novel process of diastereoselective hydrogenation of 1,3-hydroxyketones of formula (I) wherein R, R′ and R″ are as defined in claim 1 which is carried out in a solvent in the presence of a magnesium salt, a heterogeneous platinum catalyst and optionally an oxidant.

Abstract: The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.

Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) 1

Abstract: The present invention provides a composition having biological activity. The composition includes from about 10 ppm to about 5000 parts iodonium salt. The composition also includes from about 100 ppm to about 300,000 ppm of a compound to act as a carrier of the iodonium compound. The carrier is selected from at least one of polyvinyl alcohols, polyvinyl acetates, polyethylene glycols, ethylene glycol and propylene glycol block copolymers, cellulosic polymers, polyesters, alkyd polymers. The composition also includes from about 50 ppm to about 50,000 ppm of a compound to render the composition compatible with a surface being treated. This component is selected from at least one of di-acids, acid anhydrides, polyfunctional acids, di-ethylene glycol, resorcinol and the like. The composition also includes an appropriate vehicle selected from at least one of water, acidified water, paint, primer, and petroleum distillates.

Abstract: Vinyl monomers having polyenic side chains derived from highly unsaturated fatty acids represented by the general formula: R1COOH wherein R1 is a C19-24 hydrocarbon having 5 or 6 unsaturated bonds, and the derivatives thereof. Vinyl monomers having polyenic side chains derived from highly polyunsaturated fatty acids and the polymers of said monomers can be provided. In addition polymers having double bonds in the side chain into which various functional groups can be introduced can be provided. Useful utilization of fatty acid esters remaining as the residue in distillation of fish oil can be provided.

Abstract: The present invention relates to a process for preparing optically pure (S)-3-hydroxy-&ggr;-butyrolactone expressed by the following Formula 1 and more particularly, to a process that enables preparing optically pure (S)-3-hydroxy-&ggr;-butyrolactone economically in large quantities, by: (a) Preparing &agr;-(1,4) linked oligosaccharide with adequate sugar distribution by reacting starch which is easily available from natural product with enzyme under a specific condition; and (b) Performing oxidation and cyclization sequentially under a specific condition.

Abstract: The present invention relates to a process for the in situ preparation of optically pure (S)-3,4-dihydroxybutyric acid derivatives represented by the Formula [2] and more particularly, to a process which enables preparing optically pure (S)-3-hydroxy-&ggr;-butyrolactone represented by Formula [1] by oxidation of &agr;- or &bgr;-(1,4) linked disaccharide or oligosaccharide with an oxidant under basic condition to give acid and cyclization sequentially under acidic condition to give (S)-3-hydroxy-&ggr;-butyrolactone.

Abstract: The invention provides compounds of Formula I and derivatives thereof, pharmaceutical compositions comprising a compound of Formula I, and methods of treatment utilizing such compounds and compositions: 1

Abstract: The present invention relates to a novel chiral compound of Hibiscus acid bearing lactone moiety of formula I, Wherein: R1═R2═alkali salt of carboxylic acid or acid chloride or lower esters or the N-substituted cyclic imides. R3═hydroxyl or protected hydroxyl group and a process for preparing the same.

Abstract: A process of the present invention produces a hydroxylactone by subjecting an unsaturated carboxylic acid having a double bond not conjugated to a carboxyl group or an ester thereof to (i) a reaction with hydrogen peroxide in the presence of a metallic compound containing a metallic element selected from W, Mo, V and Mn or (ii) a reaction with a peroxide containing the metallic element to thereby yield a corresponding hydroxylactone having a hydroxyl group combined with one of carbon atoms constituting the double bond and being cyclized at the other carbon atom position. The metallic compound may be one selected from oxides, oxoacids and salts thereof. The unsaturated carboxylic acid includes, for example, &bgr;,&ggr;-unsaturated carboxylic acids, &ggr;,&dgr;-unsaturated carboxylic acids, and &dgr;,&egr;-unsaturated carboxylic acids. The process can produce hydroxylactones in high yields at low cost.

Abstract: Acrylic esters containing fluorine at &agr;-position and having a lactone ring introduced into the ester side chain thereof are novel. Polymers obtained from the acrylic esters have a high transparency to VUV and good adhesion to substrates and are used to formulate chemically amplified resist compositions for lithographic microfabrication.

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: Furanone derivatives and the pharmaceutically acceptable salts thereof have cytoprotective activity and protective activity for neuroinflammation, and neurodegenerative disorders; they are useful in the treatment of stroke, cerebral ischemia, myocardial infarction, myocardial ischemia, chronic heart failure, inflammation and other oxidative stress-related conditions, as well as Alzheimer's disease and senile dementia; they are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.

Abstract: The invention relates to a process for the manufacture of a compound of formula 1

Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols of the formula (I) 1

Abstract: (Meth)acrylic acid is reacted with a fatty acid anhydride and the resultant reaction mixture is neutralized and washed with an aqueous alkaline solution having a pH of 7.5 to 13.5. Thus, high-purity (meth)acrylic anhydride can be industrially advantageously produced while avoiding polymerization. This (meth)acrylic anhydride is reacted with a secondary or tertiary alcohol in the presence of a basic compound which in 25° C. water has an acidity (pKa) of 11 or lower. Thus, a high-purity (meth)acrylic ester can be produced in high yield.

Abstract: Novel diphenylethylene compounds and derivatives thereof containing thiazolidinedione or oxazolidinedione moieties are provided which are effective in lowering blood glucose level, serum insulin, triglyceride and free fatty acid levels in animal models of Type II diabetes. The compounds are disclosed as useful for a variety of treatments including the treatment of inflammation, inflammatory and immunological diseases, insulin resistance, hyperlipidemia, coronary artery disease, cancer and multiple sclerosis.

Abstract: An antibiotic SF2487 substance having the formula (I) 1

Abstract: This invention provides a novel process for producing optically active 3-hydroxy-&ggr;-butyrolactone in a short step, which is superior economically and in efficiency and industrially suitable by using a starting material which is inexpensive and easily available and reagents easy to handle. This invention relates to a process for producing optically active 3-hydroxy-&ggr;-butyrolactone represented by formula I: wherein the symbol * means an asymmetric carbon atom, which comprises hydrogenating an optically active 4-substituted oxy-3-hydroxybutyrate represented by formula II: wherein R1 represents a C1-4 lower alkyl group, R2 represents a protective group for a hydroxyl group deprotected by hydrogenation with a heterogeneous hydrogenation catalyst, and the symbol * has the same meaning as defined above, in the presence of a heterogeneous hydrogenation catalyst and an acidic substance followed by deprotection and simultaneous ring closure thereof.

Abstract: A new, more efficient and highly stereospecific process is described for the preparation of compounds with general formula (R)-(I) and of absolute configuration (R), where the groups M, W, Q and Q1 are as defined in the description, starting from compounds of absolute configuration (S) by hydrolysis, in the presence of acids, of the corresponding esterified derivatives. The (R)-(I) products obtained with the process described herein are chiral synthons useful for the production of enanthiomerically pure drugs. The preparation of (R)-carnitine is also provided.

Abstract: The present invention relates to compounds of formula I and to pharmaceutically acceptable salts, hydrates and prodrugs thereof, wherein R1, R2, R3, R4, R5, R10, R11, b, m, n, p and v are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and methods of treating hyperproliferative disorders in mammals by administering the above compounds.

Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) 1

Abstract: This invention affords a solution to the technical problem of obtaining one or both enantiomers of 5-substituted 4-hydroxyfuran-2-ones in pure form by resolution with enantiomerically pure bases. Racemic mixtures of 5-substituted 4-hydroxy-2(5H)-furanones, including 5-substituted and 5,5-disubstituted, 4-hydroxy and 3,4-dihydroxy furanones are separated into pure enantiomers by crystallization with an enantiomerically pure base, such as cinchonidine. In specific solvent mixtures, for example, 95% ethanol, the diastereomerically pure salt of one enantiomer crystallizes. The enantiomerically pure furanone can then be obtained simply by filtration and treatment of the salt with an acid, for example, trifluoracetic acid, followed by precipitation with water, filtration and drying. Moreover, the other enantiomer may be equally obtained in pure form by evaporation of the mother liquor, followed by the same treatment of the salt as described before.

Abstract: The invention relates to a method for producing compounds of general formula (I) wherein R1 is selected from the following groups: (a) OR5 and (b) mono-, di-, or tri-substituted phenyl; and R2 represents a group (C1-C6) alkyl. The method is characterized in that it comprises the following steps: a) reacting a compound of general formula (III) with an acid of general formula R1CH2 COOH (III) in a water-free medium; b) reacting the resulting compound with a strong base in an aprotic solvent in order to obtain an intermediate cyclic compound which forms a compound of general formula (I) after dehydration; and c) isolating said resulting compound of general formula (I).

Abstract: The present invention relates to new compounds of the formula (I) 1

Abstract: The invention relates to a new process for preparing optically active dihydropyrones, new intermediate products which may be obtained by this synthesis, and their use as starting compounds in the preparation of pharmaceutically active compounds.

Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) 1

Abstract: The present invention relates to novel anticancer agents, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The present invention more particularly relates to novel derivatives of andrographolide, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The novel derivatives of andrographolide have the general formula (I).

Abstract: Crystalline 3-hydroxylactone-containing products can be prepared in high yield and purity in a one-pot process by treating the corresponding 3,5-dihydroxy acid with a strong mineral acid in a cold, aprotic, water-miscible solvent to effect lactonization, followed by addition of excess acid to effect crystallization of the lactonized product from the reaction mixture.