Abstract: Novel compounds, and therapeutic methods, compositions and medicament related thereto are disclosed herein.

Abstract: This invention relates to the novel use of a composition comprising benzoic acid or a derivative of benzoic. It has been found surprisingly that the long-term ingestion of benzoic acid by swine was followed by a significant increase of the bone resistance and mineralization. The benzoic acid or its derivative can be administered to the animal either in its feed composition or in its drinking water.

Abstract: The invention relates to novel 2,6-diethyl-4-methylphenyl-substituted tetramic acid derivatives of the formula (I) in which A, B, D and G are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selectively herbicidal compositions comprising, firstly, the 2,6-diethyl-4-methylphenyl-substituted tetramic acid derivatives of the formula (I) and, secondly, at least one crop plant tolerance promoter compound.

Abstract: A compound having a structure is disclosed herein. Compositions, medicaments, and therapeutic methods related thereto are also disclosed.

Abstract: The invention concerns a process for the manufacture of substituted propionic acids comprising providing a substrate of formula (I): And subjecting the substrate to enantioselective hydrogenation under enantioselective hydrogenation conditions in the presence of an enantioselective hydrogenation catalyst comprising a catalyst ligand having a metallocene group with a chiral phosphorus or arsenic substituent to provide in enantiomeric excess a product of formula (II): or its enantiomer or if applicable its diastereomer.

Abstract: The subject of the present invention is to provide a method for deuteration, which can obtain a compound having an aromatic ring and/or a heterocyclic ring at an improved deuteration ratio. The present invention relates to a method for deuteration of a compound having an aromatic ring and/or a heterocyclic ring, comprising reacting the compound having an aromatic ring and/or a heterocyclic ring with a heavy hydrogen source in the presence of an activated mixed catalyst of not less than two kinds of catalysts selected from among a palladium catalyst, a platinum catalyst, a rhodium catalyst, an iridium catalyst, a ruthenium catalyst, a nickel catalyst and a cobalt catalyst.

Abstract: Methods and reagents for photo-initiated carbonylation with carbon-isotope labeled carbon monoxide using alkyl/aryl iodides with alcohols or water treated by photosensitizers are provided. The resultant carbon-isotope labeled esters and acids, and pharmaceutical acceptable salts and solvates are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits and method for PET studies are also provided.

Abstract: Therapeutically active anthranilic acid derivatives of Formula (I) wherein R1, R2 and W, are as defined in the specification, processes for the preparation of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, particularly in the treatment of diseases in which under-activation of the HM74A receptor contributes to the disease or in which activation of the receptor will be beneficial, are disclosed.

Abstract: Methods and reagents for photo-initiated carbonylation with carbon-isotope labeled carbon monoxide using alkyl/aryl iodides with sulfoxides and triethylamine are provided. The resultant carbon-isotope labeled acids, and pharmaceutical acceptable salts and solvates are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits and method for PET studies are also provided.

Abstract: The present invention is directed to a process of maximizing the solubility of a nonelectrolyte solute in a solvent by operating within an optimal temperature range at conditions wherein the nonelectrolyte solute is not a pure liquid. In particular, the process of the present invention is directed to conversion of a carboxylic acid compound to an ester under conditions wherein the solubility of the ester in an alcoholic solvent approaches ideal solubility behavior.

Abstract: 2,5-dihydroxyterephthalic acid is produced in high yields and high purity from 2,5-dihaloterephthalic acid by contact with a copper source and a ligand that coordinates to copper under basic conditions.

Abstract: Compounds of the formula (I): in which A, R1, R2, X, Y and Z are defined in the description, the processes for the preparation of these compounds, the uses thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, and the pharmaceutical compositions comprising them.

Abstract: The invention relates to a method for producing 5-halo-2,4,6-tifluoroisophthalic acid of formula (I), wherein X represents F, Cl, Br, or I, by hydrolysis of 5-halo-2,4,6-trifluoroisophthalodinitrile of formula (II). Said invention is characterised in that in a first step, isophthalodinitrile (II) or a solution containing isophthalodinitrile (II) is reacted with a concentrated sulphuric acid at room temperature in order to form a 5-halo-2,4,6-trifluoroisophthalodiamide of general formula (III), and is, subsequently, heated and in a second step, isophthalic acid (I) is produced after additional heating and addition of water.

Abstract: Described are ortho carboxy phenol derived acetals and compositions containing ortho carboxy phenol derived acetals which are useful for delivering biologically active compounds to cells. The acetals can be used to reversibly link up to three different molecules and have rapid hydrolysis kinetics in conditions which are present in a cell as well as in vivo. Cleavage of the acetal enhances delivery of the biologically active compound.

Abstract: The present invention is related to aryl dicarboxamides of formula (I) and use thereof for the treatment and/or prevention of obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholes-terolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of aryl dicarboxamides of formula (I) to modulate, notably to inhibit the activity of PTPs.

Abstract: The compound of the formula (I): wherein R1 is alkyl substituted by fluorine(s); R2 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR3R4, in which R3, R4 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl substituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R3 and R4, taken together a saturated heterocyclic ring or amino acid residues; and non-toxic salts thereof and acid addition salts thereof.

Abstract: Novel calcilytic compounds and methods of using them are provided.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: The present invention provides a process for producing 2-halobenzoic acids of the general formula (I), characterized by reacting a benzoic acid of formula (II) with a halogenating agent in the presence of Pd catalyst: (wherein A is —OH, —OM (M is alkali metal), —N(R6)R7 (R6 and R7 are each H, C1–C6 alkyl, optionally substituted phenyl, or the like); R is H, C1–C6 alkyl, C1–C6 alkylcarbonyl, carboxyl, C1–C12 alkoxycarbonyl, optionally substituted phenylcarbonyl, or the like; n is 0 to 4; X is Cl, Br or I, or alternatively (R)n may be present on benzene-constituting carbon atoms adjacent to each other and form a C3–C4 alkylene- or C3–C4 alkenylene-fused ring).

Abstract: A process for labeling organic compounds with deuterium and tritium is described using specific catalysts.

Abstract: Compositions including a conjugate of ?-difluoromethylornithine can be applied topically to reduce hair growth.

Abstract: A process is described for preparing compounds of formula (I) where R is H, optionally halogen-substituted alkyl, cycloalkyl, aryl, alkyl-aryl or heteroaryl, and, in alkyl and cycloalkyl, one or more CH2 groups may be replaced by —O—. The compounds of the formula (I) are valuable intermediates in the synthesis of PPAR agonists.

Abstract: The present invention provides a process for preparing an aromatic bromide or aromatic iodide from an aromatic amine derivative using nitrite anion and halodimethylsulfonium halide generated in situ from hydrobromic acid/DMSO or hydriodic acid/DMSO. The process for producing compounds of the formula (1) is disclosed (1) wherein X is bromine or iodine: Y is carbon or nitrogen; R1, R2, R3, R4 and R5 which may be the same or different and are selected independently from the group consisting of a hydrogen, a hologen, a C1-C8 alkyl, a C1-C10 alkoxy, a nitro, a formyl, an aryl, a benzyl, a C2-C10 alkylcarbonyl and an arylcarbonyl, provided that adjacent groups as selected from R1, R2, R3, R4 and R5 may combine to form a ring.

Abstract: Compounds of the formula: where the variables have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effects of reducing serum thyroxine levels and transiently increasing triglyceride levels.

Abstract: A novel achiral biaryl-type compound and a circular dichroism (CD) color fixing agent are provided. Furthermore, a method for determining an absolute configuration of a chiral compound is carried out by introducing the above achiral biaryl-type compound into the chiral compound.

Abstract: A process for the preparation of 2-bromomethyl-6-methyl-benzoic acid (I) and derivatives thereof by selective bromination of 2,6-dimethylbenzoic acid (II) with sodium bromate and hydrobromic acid in the presence of light.

Abstract: The present invention refers to a process for the preparation of 2-bromomethyl-6-methyl-benzoic acid (I) and derivatives thereof by selective bromination of 2,6-dimethylbenzoic acid (II) with sodium bromate and hydrobromic acid in the presence of light.

Abstract: Metformin salts of lipophilic acids, their pharmaceutical formulations, and methods of administrating the metformin salts for the treatment of hyperglycemia.

Abstract: Venlafaxine besylate compounds provide certain advantages over venlafaxine hydrochloride and are useful in forming pharmaceutical compositions and n treating venlafaxine-treatable diseases and conditions. Venlafaxine besylate can be easily formulated into an extended release dosage form including a hydrogel tablet as well as other matrix-based tablet compositions. A preferred tablet making process involves hot melt granulation.

Abstract: Perfluoroisopropylbenzene derivatives of the general formula (I) or salts thereof, useful as intermediates or raw materials in the synthesis of various industrial materials including agricultural chemicals, drugs and surfactants, wherein X1 is H, halogeno, formyl, optionally halogenated C1-6 alkyl, —C(═O)—R1 (wherein R1 is H, halogeno, hydroxyl, C1-6 alkyl, or NR2R3, with R2 and R3 being each H, C1-6 alkyl, or the like), or the like; X3 is H, halogeno, hydroxyl, cyano, isocyanato, hydrazino, diazo, —C(═O)—R1, —SO2—R4 (wherein R4 is halogeno, hydroxyl, C1-6 alkyl, or NR5R6, with R5 and R6 being each H or C1-6 alkyl), or the like; and X4 is H, halogeno, C1-6 alkyl, or C1-6 alkoxy, with publicly known compounds being excepted.

Abstract: The present invention provides a process for producing 2-halobenzoic acids of the general formula (I), characterized by reacting a benzoic acid of formula (II) with a halogenating agent in the presence of Pd catalyst: 1

Abstract: A method for synthesizing compounds of Formula I in which R is alkyl or aryl and X is any halogen is described.

Abstract: Compounds of the formula (I) and also process for preparing them 1

Abstract: The present invention provides an inexpensive process for the preparation of lithium salts of formula LiX having a desired or required level of purity using lithium chloride and lithium sulfate. In the process of the invention, a lithium salt selected from lithium chloride, lithium sulfate, and combinations thereof is reacted with NaX or KX in a aqueous, semiaqueous, or organic solution and the precipitated salts are removed to obtain the LiX solution of desired purity. Preferably, a semiaqueous solution containing water and an organic solvent is used at some point in the reaction. The process of the invention eliminates the use of highly acidic materials and thus reduces the cost of raw materials and the need for specialized equipment.

Abstract: The present invention is concerned with a novel process for the preparation of 3,5-bis(trifluoromethyl)benzoic acid (CAS 725-89-3). This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity, in particular, as substance P (neurokinin-1) receptor antagonists.

Abstract: The invention relates to substituted cinnamic acids and cinnamic acid esters of formula (I), wherein X represents F, Cl or J and R1 and R2 are the same or different and represent hydrogen, an optionally substituted C1-C10-alkyl radical or an optionally substituted benzyl radical. Substituted indanone carboxylic acid esters are produced using said substituted cinnamic acid and cinnamic acid ester in a technically simple and non-dangerous manner as far as safety is concerned.

Abstract: 3,5-Bis(trifluoromethyl)benzoyl chlorides optionally substituted with fluorine or chlorine are advantageously prepared by converting 3,5-dimethylbenzoic acids optionally substituted with fluorine or chlorine into the corresponding acid chlorides; completely free-radically chlorinating said chlorides in the side chains, giving 3,5-bis(trichloromethyl)benzoyl chlorides optionally substituted by fluorine or chlorine; fluorinating the latter with anhydrous hydrogen fluoride and/or antimony pentafluoride, giving 3,5-bis(trifluoromethyl)benzoyl fluorides optionally substituted with fluorine or chlorine; and then reacting the 3,5-bis(trifluoromethyl)benzoyl fluorides with silicon tetrachloride in the presence of a further Lewis acid. Some of the 3,5-bis(trihalogenomethyl) and 3,5-dimethylbenzoyl halides which arise as intermediates are novel compounds.

Abstract: A method for preparing chloromethylphenylacetic acids represented by formula (II): wherein a methylphenylacetic acid represented by formula (I): is reacted with a chlorine gas, in an inert solvent, under the irradiation with light or in the presence of a radical initiator, is disclosed. According to the preparation method, high purity chloromethylphenylacetic acids can be prepared at a high yield, without using toxic sulfuryl chloride as a chlorinating agent, by chlorinating the methyl group of the methylphenylacetic acids at a high selectivity while suppressing by-production of a dichloro form or &agr;-chloro form.

Abstract: The present invention is a method of producing dry, alkali metal or ammonium carboxylic acid salt particles. In accordance with the invention, a molten carboxylic acid is mixed with a solution of an alkali metal-containing or ammonium-containing alkaline compound and the carboxylic acid and alkaline compound are reacted to form the carboxylic acid salt. Water is then removed from the carboxylic acid salt to produce dry, carboxylic acid salt particles. The feed ratio of the molten carboxylic acid and the alkaline compound is controlled to neutralize the carboxylic acid in the process.

Abstract: A method for the production of an aromatic fluorine compound is provided which is capable of preventing the occurrence of benzoic acid fluorides during the course of a halogenation exchange reaction or allowing removal of the benzoic acid fluorides formed at all. A method for the production of an organic fluorine compound is disclosed which comprises preventing the occurrence of acid fluorides of an aromatic compound during the production of the organic fluorine compound by the reaction of an organic chlorine or bromine compound with a fluorinating agent in benzonitrile as a solvent or allowing removal of the acid fluorides formed.

Abstract: A process for separating a compound from a mixture of different compounds is disclosed for compounds comprising at least two negatively charged groups connected by a linker group. The process comprises treating the mixture with a material comprising layers containing at least two different types of cation disposed in an ordered arrangement within each layer, such as layers of formula LiAl2(OH)6+, in order to separate the compound from the mixture by selective intercalation of the compound into the material.

Abstract: The present invention relates to novel compounds of the formula (I) in which Het represents one of the groups  in which A, B, D, G, V, W, X, Y and Z are as defined in the description, processes and intermediates for their preparation, and to their use as pesticides and herbicides.

Abstract: The present invention relates to (+)− and (−)-2-cyclododecylpropanol and (+)− and (−)-2-cyclododecylpropionic acid, to salts thereof, and to the preparation and use thereof.

Abstract: The present invention relates to a process for preparing trifluorobenzoic acids of the formula in which R is a straight-chain or branched alkyl radical having 1 to 6 C-atoms, an unsubstituted phenyl radical, a substituted phenyl radical which contains one or two alkyl or alkoxy groups having in each case 1 to 4 C atoms, or an araliphatic radical having 7 to 12 C atoms, which comprises reacting a compound of the formula in which R1 and R2 are identical or different and are —CN, —COOR3, where R3 is H, Li, Na, K, MgCl, MgBr, MgI, ½Mg, ½Ca or an alkyl radical having 1 to 6 C atoms, or —CONR4R5, where R4 and R5 are identical or different and are an alkyl radical having 1 to 6 C atoms, with at least one organometallic compound of the formula CuR, CuLiR2, MgXR, ZnR3, LiR, AlX2R, AlXR2AlR3 Al2Cl3R3, where R is as defined in formula (1) and X is Cl, Br or I, in the presence of an inert solvent at from −80 to +150° C.

Abstract: A process for the halogenation of activated methylene and methine compounds with at least equimolar amounts of an electrophilic halogenation reagent, which comprises reacting said activated methylene and methine compounds in the presence of catalytic amounts of a titanium compound of the formula I or of a titanium compound of the formula II

Abstract: The subject invention involves processes for making 2,4-difluoro-3-Q1-benzoic acid, wherein Q1 is derived from an electrophilic reagent, comprising the steps of: (a) treating 1-bromo-2,4-difluorobenzene with a strong, non-nucleophilic base; then treating with an electrophilic reagent which provides Q1, or a functional moiety which is then transformed to Q1, producing 1-bromo-2,4-difluoro-3-Q1-benzene; (b) treating the 1-bromo-2,4-difluoro-3-Q1-benzene with an alkali or alkaline earth metal or organometallic reagent; then treating with carbon dioxide, or with a formylating agent followed by oxidation, to produce 2,4-difluoro-3-Q1-benzoic acid. The subject invention also involves optional additional steps to further modify Q1, or to substitute a non-hydrogen moiety at the 5-position, at the 6-position, or at both, of the phenyl ring of the 2,4-difluoro-3-Q1-benzoic acid.

Abstract: An object of the present invention is to provide a commercially advantageous process for preparing a fluoro benzoic acid. The process according to the present invention comprises either alkylating a fluoro benzoic acid of the formula wherein R1 is halogen, or reducing a fluoro benzoic acid of the formula wherein R1 is as defined above and R2 is lower alkyl to thereby produce a fluoro benzoic acid represented by the formula wherein R1 and R2 are as defined above.

Abstract: The present invention is to provided a trifluoro-substituted benzoic acid, an ester thereof, particularly 2,3,4-trifluoro-5-iodobenzonic acid, 2,3,4-trifluoro-5-trifluoromethylbenzonic acid, esters thereof, which are useful as a starting material for synthesizeing a quinolonecarboxylic acid compound useful as a medicine, an anti-bacterial agent or an antiviral agent, and processes for preparing these compounds and 2,4,5-trifluoro-3-iodobenzonic acid, 2,4,5-trifluoro-3-trifluoromethylbenzoic acid and esters thereof.

Abstract: Disclosed is a method of isolating the aromatic product formed when a substrate having the general formula is dehalogenated, forming a product mixture of copper salts and aromatic product, where X is the halogen removed from the substrate to form the aromatic product, R′ is COOH, COOR, COR, CN, COH(R)2, or SO3H, each R″ is independently selected from halogen, R, or OR or two vicinal R″ groups form one or more fused aromatic rings, R is alkyl from C1 to C18 or aryl from C6 to C18, and n is 1 to 4. Water in an amount about 1 to about 5 times the amount of the substrate is added to the product mixture, forming an organic phase that contains the aromatic product and an aqueous phase that contains the copper salts. If the density of the organic phase differs from the density of said aqueous phase by less than 0.1 g/cc, a suitable solvent is added to the product mixture in an amount sufficient to increase the differences between the organic and aqueous phases to at least 0.

Abstract: Neurotrophic and antiproliferative compounds related to the antiepileptic drug valproate are provided. These compounds are useful for promoting neuronal function as in neurodegenerative disorders and for treating neoplastic disease.