Abstract: A process produces a 2-benzoyloxyacetaldehyde derivative represented by following Formula (3): wherein R1 and R2 may be the same as or different from each other and are each a hydrocarbon group, wherein R1 and R2 may be combined to form a ring with the adjacent oxygen-carbon-oxygen bond, and wherein the benzene ring in the formula may be substituted, by allowing a halogenated acetaldehyde acetal derivative represented by following Formula (1): wherein R1 and R2 are as defined above; and X represents a halogen atom, to react with a benzoate represented by following Formula (2): wherein M represents an alkali metal atom and wherein the benzene ring in the formula may be substituted, in the presence of an alkali-metal halide.

Abstract: The present invention describes polymers containing 1,2-dithiolanes capable of acting as scavengers of free radicals, metals and reactive oxygen species. Also described are methods of synthesizing the antioxidant 1,2-dithiolane derivatives and polymerization thereof to produce biodegradable antioxidant polymers. The antioxidant polymers of the present invention may be used to treat diseases or conditions caused by oxidative stress and other free radical mediated conditions. The antioxidant polymers may also be used for the preparation of antioxidant particulate delivery devices of therapeutic agents.

Abstract: A novel spiroquinone derivative having a high ABCA1 stabilization effect and being useful for prophylactic and/or therapeutic agents for various diseases developing hypo-high density lipoproteinemia is obtained. The novel spiroquinone derivative is a compound represented by the following formula: wherein R1a, R1b, R1c and R1d each represents a hydrogen atom, a halogen atom, an alkyl group which may have a substituent, or an alkoxy group which may have a substituent, and R2a and R2b each represents a hydrogen atom, or an alkyl group which may have a substituent (e.g.

Abstract: The present invention provides novel methylenedioxy phenolic compounds and their derivatives, methods of making them and methods of using them to treat or prevent cardiovascular disease, vascular disease and/or inflammatory disease, as well as Type I and Type II Diabetes and Dyslipidemia patients at risk for hypertension, stroke, cardiovascular and renal disease.

Abstract: The present invention relates to oral nutritional and therapeutic products which are useful for providing vitamins and minerals required for bone health. The present invention is an oral nutritional and therapeutic composition of calcium succinate, magnesium R-(+)-alpha-lipoate, and Vitamin D for use in the maintenance of bone health, the optimization of bone growth, reducing the risk of bone fracture, and the prevention and treatment of osteoporosis. The pharmaceutical products and methods of the present invention are particularly useful in building bone mass, quality, and density during growth, maintaining bone mass, quality, and density over time, reducing bone fracture risk, and treating osteoporosis in men and women.

Abstract: The invention includes novel compounds, including but not limited to formula A and formula B, and an improved delivery method. These compounds and methods are useful in preventing or treating diseases or conditions associated with or caused by the presence of free radicals, and are useful for increasing cellular metabolism while simultaneously alleviating the resultant increase in oxidative stress. Specifically, a carnitine is bound to a lipoic acid derivative or to dihydrolipoic acid or its derivatives using a hydrolysable linker to form a single compound.

Abstract: The invention relates to derivatives of dihydroxyphenylalanine, to their synthesis and to pharmaceutical compositions containing said derivatives of dihydroxyphenylalanine. Furthermore, the invention relates to the use of said derivatives of dihydroxyphenylalanine and said pharmaceutical compositions for the treatment and prophylaxis of movement disorders, neurodegenerative diseases, Alzheimer's disease, Parkinson's disease, hemiparkinson-hemiatrophy, parkinsonian syndrome, Lewy body disease, frontotemporal dementia, Lytico-Bodig disease (parkinsonism/dementia/amyotrophic lateral sclerosis), striatonigral degeneration, Shy-Drager syndrome, sporadic olivopontocerebellar degeneration, progressive atrophy of the globus pallidus, progressive supranuclear palsy, Hallervorden-Spatz disease, Huntington's disease, X-linked dystonia-parkinsonism (Lubag), mitochondrial cytopathy with striatal necrosis, neuroacanthocytosis, restless legs syndrome, Wilson's disease.

Abstract: Compounds of formula (I) are active as dopaminergic compounds or as compounds which or as compounds which diminish the symptoms of dopamine deficiency: wherein: R1 and R2 are independently selected from —C(?O)R5 or —C(?O)OR5; or one of R1 and R2 is hydrogen and the other is —C(?O)R5 or —C(?O)OR5; R3 and R4 are independently selected from hydrogen, optionally substituted C1-C6 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, or C2-C6 alkynyl, —CH2Q, —C(?O)R5, —C(?O)OR5, —C(?O)NR5R6, or R5 is hydrogen or optionally substituted C1-C6 alkyl or —CH2Q; R6 is hydrogen or optionally substituted C1-C6 alkyl Or —CH2Q; and Q is an optionally substituted monocyclic carbocyclic or heterocyclyl ring of 3 to 6 ring atoms.

Abstract: Compounds of formula I, process for making same, and cosmetic compositions and methods of skin lightening using compounds of formula I as skin lightening agents: Where each A1 and/or A2 independently is ?H or COR, CO2R, CONHR, the latter three having the following formula A: where R?C1-C18 saturated or unsaturated, linear or branched, hydrocarbon; and each Y1 and/or Y2 independently is H; C1-C18 saturated or unsaturated hydrocarbon; or OZ, where Z=H or COR1, CO2R1, CONHR1 of formula B: and where R1?C1-C18 saturated or unsaturated, linear or branched, hydrocarbon; X is Carbon, Nitrogen, Sulfur, or Oxygen; and N is in integer between 0 and 2.

Abstract: Process for purifying thioctic acid in water comprising the following steps: a) dissolving the thioctic acid in an aqueous alkaline solution or alternatively dissolving a thioctic acid salt, if necessary adjusting the pH to alkaline values, b) acidifying the solution from step (a) with an acid chosen from the class consisting of sulfuric acid, phosphoric acid, methanesulfonic acid to a pH between 5.4 and 5.8. c) isolating the thioctic acid precipitated in step (b) by conventional methods.

Abstract: The invention provides compositions and methods of use thereof for labeling peptide and proteins in vitro or in vivo. The methods described herein employ lipoic acid ligase or mutants thereof, and lipoic acid analogs recognized by lipoic acid ligase and lipoic acid ligase mutants.

Abstract: Novel mercaptan compounds, particularly those including a photolabile protecting group, are described as well as methods of using the compounds for the prevention and treatment of ocular damage and disease.

Abstract: Compounds of general formula: wherein R?, R, x and z have the meaning reported in the specification, are useful for treating inflammatory diseases including metabolic syndrome, diabetes, obesity, dyslipidemia, and insulin resistance.

Abstract: The invention relates to a medicament containing an effector of the glutathione metabolism together with ?-lipoic acid for treating diabetes mellitus. This medicament enables disturbances of the thiol-disulfide status or those that occur, for example, in diabetes mellitus to be treated simultaneously, separately or in a temporally graduated manner.

Abstract: Process for purifying thioctic acid in water comprising the following steps: a) dissolving the thioctic acid in an aqueous alkaline solution or alternatively dissolving a thioctic acid salt, if necessary adjusting the pH to alkaline values, b) acidifying the solution from step (a) with an acid chosen from the class consisting of sulfuric acid, phosphoric acid, methanesulfonic acid to a pH between 5.4 and 5.8. c) isolating the thioctic acid precipitated in step (b) by conventional methods.

Abstract: The invention relates to a process for the preparation of compounds containing at least one —CF2—O— bridge in the molecule, in which a) an acid is added onto at least one ketene dithioketal, b) the resultant bis(alkylthio)carbenium salt is reacted with at least one compound having at least one hydroxyl group in the presence of a base, c) and subsequently, preferably in situ, the resultant dithioorthoester is subjected to oxidative fluorodesulfurisation using a fluorinating agent and an oxidant to give the compound containing at least one —CF2—O— bridge in the molecule.

Abstract: Spirotetrathiocarbamates (STOCs) or oxa substituted compounds (SOTOCs) of Formula I: Formula (I) or bisSTOC or bisSOTOC compounds of Formula II: Formula (II) wherein X1, X2, X3, X4, X5, X6, X7, and X8, are independently O or S; and preferably at least two and up to all four of X1, X2, X3 and X4, and at least two and up to all four of X5, X6, X7, and X8 are sulfur; Z is —CmR22m wherein m=1 to 4; —C(R2)2SC(R2)2—, C(R2)2SSC(R2)2—, or —C(R2)OC(R2)2; n is from 0 to 4; M is selected from CH2Cl, CH2SC(O)R1, CH2SC(S)R1, CH2S(CH2CH2S)qH wherein q is 0, 1 or 2; —CR2?CH2, —CH2OC(O)CR2?CH2, CH2N?C?S, CH2N?C?O, CH2NR2H, CH2OH, CH2SCH2CH2CR2?CH2, phenyl, C(R2)phenyl, furan, thiophene, halogen, C3-C6 cycloalkyl, C3-C6 heretocyclics, thiol, H, (III) or (IV) wherein A is S, O or phenyl; x is 0 or 1; R1 is C1-C22 alkyl; and R2 is H or C1-C22 alkyl have excellent optical properties. Methods for preparing these compositions and optical lenses prepared from the compounds are also provided.

Abstract: A compound having a formula selected from the group consisting of wherein the substituents are as defined in the specification. The compounds are useful as intermediates in the preparation of compounds of formula (I), which are useful for inhibiting NO synthase and regenerate antioxidants.

Abstract: Salt of thioctic acid with L-carnitine with the formula: AY(X)x where A is where Y is the cation of an alkaline metal, of an alkaline earth metal or is a quaternary ammonium group, X is A or OH?, x is equal to 0 when Y is the cation of an alkaline metal or a quaternary ammonium group and equal to 1 when Y is an alkaline earth metal.

Abstract: An improved process for the preparation of cis-1,3-diols is described where a beta hydroxy ketone is treated with a trialkylborane or dialkylalkoxyborane or a mixture of a trialkylborane and a dialkylalkoxyborane followed by recovery and reuse of the alkylborane species to convert additional beta hydroxy ketone to the cis-1,3-diol.

Abstract: The invention relates to a method for producing pure racemic, R- or S-thioctic acid or mixtures thereof by reacting 6,8-disubstituted octanoic acid or their salts or esters with sulfides, sulfur or sulfites.

Abstract: A process for the manufacture of new crystalline salts of N-[2-(dimethylamino)ethyl]-1,2-dithiolane-3-pentanamide (racemic and chiral forms) is described. Such salts are stable, crystalline and have very good solubility in water. The salts exhibit antioxidant properties. They inhibit collagenase and elastase enzymes. They have excellent anti acne activity in addition tyrosinase inhibition. They are, by themselves and in combination with other known agents, important cosmetic ingredients.

Abstract: 1?-substituted cannabinoid derivatives of delta-8-tetrahydrocannabinol, delta-9-tetrahydrocannabinol, and delta-6a-10a-tetrahydrocannabinol that have affinity for the cannabinoid receptor type-1 (CB-1) and/or cannabinoid receptor type-2 (CB-2). Compounds having activity as either agonists or antagonists of the CB-1 and/or CB-2 receptors can be used for treating CB-1 or CB-2 mediated conditions.

Abstract: Disclosed herein are a gelling agent composed of a functional amino acid compound having a tetrathiafulvalenyl group, and a production method of a gelling agent, comprising reacting a tetrathiafulvalene derivative with an amino acid derivative in the presence of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride and 4-(N,N-dimethylamino)pyridine to obtain a functional amino acid compound having a tetrathiafulvalenyl group.

Abstract: The present invention relates to a process for the preparation of R- and S-lipoic acid and R- and S-dihydrolipoic acid comprising (a) reaction of where MS is SO2—R? and R and R? independently of one another are C1–C6-alkyl, C3–C8-cycloalkyl, C3–C8-cycloalkylalkyl, aryl or aralkyl, with sodium sulfide and sulfur in methanol. The invention especially relates to processes for preparing pure R- or S-dihydrolipoic acid, which is either used directly or processed further to give R- and S-lipoic acid. The process also serves for the production of pharmaceuticals. The present invention further relates to a solution of sodium sulfide trihydrate and sulfur in methanol, the sulfur being present in a molar excess over the sodium sulfide trihydrate, and a kit which comprises the solution according to the invention.

Abstract: A method of stabilizing R-?-lipoic acid includes combining R-?-lipoic acid with nicotinamide in a weight ratio between about 10:4 to about 10:8. A composition for treating oxidative stress includes R-?-lipoic acid and nicotinamide in a weight ratio of between about 10:4 and about 10:8.

Abstract: The invention relates to new modifications of the trometamol salt of R-thioctic acid of the formula I, processes for their production, pharmaceutical preparations containing these modifications, and their medical application.

Abstract: This invention relates to the identification of a novel class of therapeutic agents which selectively target and kill tumor cells and certain other types of diseased cells, and to compositions comprising lipoic acid derivatives which poison the pyruvate dehydrogenase complex specifically in such cells. This invention also provides for methods of using therapeutically effective amounts of the lipoic acid derivatives for the treatment of cancer and other diseases. The lipoic acid derivatives described herein have a wide range of preventive and therapeutic applications.

Abstract: The present invention provides novel compounds having scavenging and anti-ROS properties and pharmaceutical composition comprising these compounds for treatment of conditions associated with oxidative stress or free radical injury. The compounds of the invention are of general formula (I).

Abstract: Process for the synthesis of R(+)?-lipoic acid comprising the following stages: a) Salifying of racemic 6,8-halo-octanoic acid with S(?)?-methylbenzylamine; b) separation by filtration of the crystallized diastereoisomeric salt of R(+)6,8-di-halo-octanoic acid-S(?)?-methylbenzylamine; c) purification by re-crystallization of the diastereoisomeric salt of R(+)6,8-di-halo-octanoic acid-S(?)?-methylbenzylamine; (d) separation of the diastereoisomeric salt to obtain R(+)6,8-di-halo-octanoic acid by reation of said salt with strong mineral acids in an aqueous solution with a dilution between 2 and 10% by weight; e) esterification of R(+)6,8-di-halo-octanoic acid to obtain the corresponding alkyl ester; f) reaction of the alkyl ester of R(+)6,8-di-halo-octanoic acid in an organic solvent with an aqueous solution of alkali disulfide in presence of a compound for phase transfer catalysis; g) hydolysis of the ester of R(+)?-lipoic acid.

Abstract: The invention relates to new modifications of the trometamol salt of R-thioctic acid of the formula I, processes for their production, pharmaceutical preparations containing these modifications, and their medical application.

Abstract: Process for the synthesis of racemic thioctic acid comprising the following stages: a) reaction of the alkyl ester of 6,8-di-halo-octanoic acid in an organic solvent with an aqueous solution of alkali disulfide in presence of a compound for phase transfer catalysis selected from the group consisting of quaternary ammonium or phosphonium salts having the following general formula: where: A is nitrogen of phosphorus, X is selected from the group consisting of Cl, Br, I, HSO4, and H2PO4 and the substitutents R1, R2, R3 and R4 are selection from the group consisting of linear or branched alkyl radicals having one to twenty carbon atoms (C1-C20), said substituents being identical or different one from the other, or only one of said substituents is selected from the group consisting of arylalkyl radicals having the following formula —(CH2)nC6H5 in which n=1-16; b) followed by the hydrolysis of the ester of racemic thiotic acid.

Abstract: The present invention provides an acrylic ester compound represented by formula (1), a polymerizable composition containing the acrylic ester compound, and a cured product and an optical component obtained by polymerizing the polymerizable composition: (wherein “a” is an integer of 0 to 4; R1 is a directly bonded single bond, an alkylene group, an aralkylene group or arylene group which may have a substituent, or a —Y3—S—R4—S—Y4— group (R4 is an alkylene group, an aralkylene group or an arylene group; and Y3 and Y4 are each an alkylene group); R2 and R3 are each a hydrogen atom or an alkyl group; X1 and X2 are each an oxygen atom or a sulfur atom; and Y1 and Y2 are each an alkylene group which may contain an oxygen atom or a sulfur atom).

Abstract: The invention relates to new modifications of the trometamol salt of R-thioctic acid of the formula I, 1

Abstract: Salt of thioctic acid with L-carnitine with the formula:

Abstract: An acrylic ester compound represented by the general formula (1): wherein, R1 and R2 represent independently a hydrogen atom, an alkyl group which may have a substituent, an aromatic alkyl group which may have a substituent or an aromatic residue which may have a substituent, respectively; R3 represents a hydrogen atom or an alkyl group; A represents a divalent organic group; and X represents a sulfur atom or an oxygen atom; provided that when X is an oxygen atom, R1 represents an aromatic residue that may have a substituent, a polymerizable composition comprising the compound, and a cured article and optical components obtained by polymerizing the polymerizable composition.

Abstract: The invention relates to a process for the preparation of compounds having at least one —CF2O— bridge in the molecule, which comprises initially reacting a bis(alkylthio)carbenium salt with a compound containing at least one hydroxyl group in the presence of a base followed by oxidative fluorination, preferably in situ, with a fluorinating agent and an oxidizing agent to form the compound having at least one —CF2O— bridge in the molecule.

Abstract: The present invention provides an acrylic ester compound represented by formula (1), a polymerizable composition containing the acrylic ester compound, and a cured product and an optical component obtained by polymerizing the polymerizable composition: 1

Abstract: Processes for the preparation of R-lipoic acid or S-lipoic acid comprising a process step selected from

Abstract: The present invention features biarsenical molecules. Target sequences that specifically react with the biarsenical molecules are also included. The present invention also features kits that include biarsenical molecules and target sequences. Tetraarsenical molecules are also featured in the invention.

Abstract: Process for the synthesis of R(+)&agr;-lipoic acid comprising the following stages: a) Salifying of racemic 6,8-halo-octanoic acid with S(−)&agr;-methylbenzylamine; b) separation by filtration of the crystallized diastereoisomeric salt of R(+)6,8-di-halo-octanoic acid-S(−)&agr;-methylbenzylamine; c) purification by re-crystallization of the diastereoisomeric salt of R(+)6,8-di-halo-octanoic acid-S(−)&agr;-methylbenzylamine; (d) separation of the diastereoisomeric salt to obtain R(+)6,8-di-halo-octanoic acid by reation of said salt with strong mineral acids in an aqueous solution with a dilution between 2 and 10% by weight; e) esterification of R(+)6,8-di-halo-octanoic acid to obtain the corresponding alkyl ester; f) reaction of the alkyl ester of R(+)6,8-di-halo-octanoic acid in an organic solvent with an aqueous solution of alkali disulfide in presence of a compound for phase transfer catalysis; g) hydolysis of the ester of R(+)&agr;-lipoic acid.

Abstract: Process for the synthesis of R(+)&agr;-lipoic acid comprising the following stages: a) Salifying of racemic thioctic acid with R(+)&agr;-methylbenzylamine; b) separation by filtration of the crystallized diastereoisomeric salt of R(+)&agr;-lipoic acid-R(+)&agr;-methylbenzylamine; c) purification by re-crystallization of the diastereoisomeric salt of R(+) &agr;-lipoic acid-R(+)&agr;-methylbenzylamine, in which the re-crystallization solvent consists of a mixture of non-polar/polar solvents; d) separation of the diastereoisomeric salt to obtain R(+)&agr;-lipoic acid by reaction of said salt with acids selected from the group consisting of aliphatic hydroxy-carboxylic acids having 3 to 6 carbon atoms and aqueous phosphoric acid.

Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.

Abstract: Process for the synthesis of R(+)&agr;-lipoic acid comprising the following stages: a) Salifying of racemic thioctic acid with R(+)&agr;-methylbenzylamine; b) separation by filtration of the crystallized diastereoisomeric salt of R(+)&agr;-lipoic acid-R(+)&agr;-methylbenzylamine; c) purification by re-crystallization of the diastereoisomeric salt of R(+)&agr;-lipoic acid-R(+)&agr;-methylbenzylamine, in which the re-crystallization solvent consists of a mixture of non-polar/polar solvents; d) separation of the diastereoisomeric salt to obtain R(+)&agr;-lipoic acid by reaction of said salt with acids selected from the group consisting of aliphatic hydroxy-carboxylic acids having 3 to 6 carbon atoms and aqueous phosphoric acid.

Abstract: A description is given of a process for preparing dihydroxycarboxylic esters and of an overall process for preparing R-(+)-&agr;-lipoic acid.

Abstract: A description is given of a process for preparing dihydroxycarboxylic esters and of an overall process for preparing R-(+)-&agr;-lipoic acid.

Abstract: This invention provides sulfur-containing (meth)acrylic ester compounds each of which is represented by the following formula (1); wherein R1 and R2 each independently represent a hydrogen atom or an alkyl group or may be fused together to form a ring, R3 represents a hydrogen atom or a methyl group, X1 represents an oxygen atom or a sulfur atom, m stands for an integer of from 0 to 3, and n stands for an integer of from 1 to 4, polymerizable compositions comprising the sulfur-containing (meth)acrylic acids, and cured products and optical parts obtained by polymerizing the polymerizable compositions. The sulfur-containing (meth)acrylic ester compounds according to the present invention are very useful, as monomers for photocurable, polymerizable compositions, in applications such as optical materials and dental materials.

Abstract: The present invention provides biotechnologically useful oligo(ethylene glycol)-terminated 1,2-dithiolane compositions and conjugates of these compositions with biological or non-biological receptor, ligand, sequestering, or reporter moieties. The invention also provides methods for the preparation of these compositions. Further, the invention provides self-assembled monolayer (SAM) compositions on a metal and methods for their preparation.

Abstract: The present invention provides a compound containing at least one sulfhydryl group and at least one NO donor group, wherein said compound is a) a compound containing one or more sulfhydryl groups linked to at least one aromatic ring or a heteroaromatic ring with a nitrogen in the ring structure, which ring is substituted by one or more substituents bearing a terminal —ONO2 group; b) a 5-membered ring heterocyclic compound containing a sulfur atom and a nitrogen atom, which ring is substituted by one or more substituents bearing a terminal —ONO2 group; c) a 5-membered ring compound containing two conjugate S-atoms, which ring is linked to one or more substituents bearing a terminal —ONO2 group; or d) a compound containing an acyclic —S—S group, linked to at least one aromatic ring or a heteroaromatic ring with a nitrogen in the ring structure, which ring is substituted by one or more substituents bearing a terminal —ONO2 group.

Abstract: The invention relates to compounds of formula: wherein R1 is selected from the group consisting of fatty acid acyl groups of 12 to 30 carbon atoms and fatty alcohol groups of 12 to 30 carbon atoms, and wherein R2 is selected from the group consisting of H, fatty acid acyl of 12 to 30 carbon atoms and fatty alcohol groups of 12 to 30 carbon atoms, the same as or different from R1, and the residue of a nutrient, drug, or other bioactive compound, and to the use of these compounds to deliver drugs and other bioactive compounds.