Abstract: Triphenylethylene compounds of formula (I) are provided. The compounds are particularly useful for selective estrogen receptor modulation.

Abstract: Drug substances comprising a pharmaceutically acceptable organic acid addition salt 6f amine containing pharmaceutically active compounds useful for the treatment of a therapeutic ailment administration and exhibiting prophylactic properties when employed in non-therapeutic administration.

Abstract: A compound of the general formula (I): (wherein the symbols are as defined in the description), or a non-toxic salt thereof.

Abstract: Compounds having a formula: or a pharmaceutically acceptable salt or prodrug thereof, are provided, and are useful for the treatment of metabolic disorders.

Abstract: Disclosed are novel compound of formula I, As defined herein and their use as pharmaceutically active compounds for reducing blood glucose, and/or treating one or more of type II diabetes, disturbances of lipid and carbohydrate metabolism, arteriosclerotic manifestations, and insulin resistance.

Abstract: The present disclosure relates to novel cocrystals and novel methods for cocrystallization. In particular, the disclosure includes cocrystals comprising a salt of an active agent, such as a chloride salt of an active pharmaceutical ingredient. The present disclosure also relates to methods of preparing cocrystals and methods for screening for solid state phases.

Abstract: A compound represented by the following general formula (I) or a salt thereof, or a hydrate thereof or a solvate thereof having an inhibitory action against plasminogen activator inhibitor-1 (PAI-1): wherein R1 represents a C6-10 aryl group; or a substituted C6-10 aryl group, R2 represents a C6-10 aryl group; or a C6-10 aryl group substituted with a group or groups selected from the group consisting of a halogen atom, nitro group, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a C1-6 alkoxy group, a halogenated C1-6 alkoxy group, a phenyl group and carboxy group, X represents —CH2—, —CH2CH2—, —CH?CH— or —N(R3)—C(?O)—, Y represents carboxy group or a bioisostere of carboxy group, R3 represents hydrogen atom, a C1-4 alkyl group or a C7-12 aralkyl group, m represents 0 or 1.

Abstract: The present invention is directed to novel phenytoin derivative compounds and the use of such compounds as sodium channel blockers. Such compositions have utility as anti-cancer agents and can be used to limit or prevent PCa growth and/or metastasis.

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

Abstract: The present invention provides a methods and compounds for producing an enantiomerically enriched ?-(phenoxy)phenylacetic acid compound of the formula: from a mixture of its enantiomers, where R1 is alkyl or haloalkyl and X is halide.

Abstract: The present invention relates to a process for preparing enantiomerically enriched, optionally substituted 2-alkoxy-3-phenylpropionic acids by asymmetrically hydrogenating alkoxycinnamic acids.

Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.

Abstract: The present invention provides a production method including reacting a diphenylmethylene halide compound represented by the following formula (1) with a malonic acid diester compound represented by the following formula (2) in an organic solvent selected from N-methyl-2-pyrrolidone, N-ethyl-2-pyrrolidone and N,N-dimethylformamide, in the presence of a base selected from an alkali metal hydride and an alkali metal t-butoxide to give a diester compound represented by the following formula (3), and then subjecting the diester compound to hydrolysis and decarboxylation to give a diphenylalanine compound represented by the following formula (4). According to the present invention, diphenylalanine compound (4) can be obtained industrially advantageously in a high yield. wherein each symbol is as defined in the specification.

Abstract: Therapeutic compounds according to one of the structures below are disclosed herein.

Abstract: The invention relates to a combination which comprises (a) a cyclooxygenase-2 inhibitor (“COX-2 inhibitor”) and (b) a histone deacetylase inhibitor (“HDAI”) for simultaneous, concurrent, separate or sequential use, especially for use in the treatment of pre-malignant colon lesions or a colon cancer or other malignancies in a mammal, particularly a human. The invention also relates to pharmaceutical compositions comprising such a combination and to a method of treating pre-malignant colon lesions (e.g. polyps) and colon cancer, as well as other malignancies, in a mammal, particularly a human, with such a combination. The present invention further also relates to a commercial package or product comprising such a combination.

Abstract: Compounds are described that are active on at least one of PPAR?, PPAR?, and PPAR?, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPAR?, PPAR?, and PPAR?.

Abstract: The invention provides compounds of formula (I), wherein the substituents are as defined in the specification, to processes for their preparation and their use as pharmaceuticals.

Abstract: The present invention provides a method for forming compounds of Formula HO—C(?O)R1—X—R2—X—R1—C(?O)—O—H wherein compound (I) can be polymerized to provide a polymer that contains therapeutically active compounds. In the compounds of the invention, each R1 is group that will provide the therapeutically active compound upon hydrolysis of the polymer; each X is independently an ester linkage or an amide linkage; and R2 is a linking group.

Abstract: Novel amino acid derivatives are provided that are useful for management of disorders such as obesity and immunological diseases. The derivatives are also useful in lowering blood glucose levels in hyperglycemic disorders and for treating related disorders such as body weight gain, elevated free fatty acid, cholesterol and triglyceride levels and other disorder exacerbated by obesity.

Abstract: Hydroxy aromatic acids are produced in high yields and high purity (>95%) from halogenated aromatic acids in a reaction mixture containing a copper source and a ligand that coordinates to copper.

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

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: Terephthalic acid is prepared by reacting a 2,5-furandicarboxylate with ethylene in the presence of a solvent to produce a bicyclic ether; and then dehydrating the bicyclic ether. The process of the present invention effectively produces terephthalic acid, while reducing or eliminating the impurities, color bodies and carbon oxides produced in commercial practice by the liquid-phase oxidation of methyl-substituted benzene feedstocks.

Abstract: Disclosed is an optimized process and apparatus for more efficiently and economically carrying out the liquid-phase oxidation of an oxidizable compound. Such liquid-phase oxidation is carried out in a bubble column reactor that provides for a highly efficient reaction at relatively low temperatures. When the oxidized compound is para-xylene and the product from the oxidation reaction is crude terephthalic acid (CTA), such CTA product can be purified and separated by more economical techniques than could be employed if the CTA were formed by a conventional high-temperature oxidation process.

Abstract: The present invention relates to derivatives of succinic and glutaric acids and analogues thereof, having the following general formula: useful as inhibitors of PHEX. These derivatives are useful for promoting generation of bone mass and treating or preventing diseases or conditions associated with a phosphate metabolism defect. Methods for preparation and intermediates are also disclosed.

Abstract: Hydroxy aromatic acids are produced in high yields and high purity (>95%) from halogenated aromatic acids in a reaction mixture containing a copper source and a ligand that coordinates to copper.

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: 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: The present invention is aimed at a process for the preparation of enantiomerically enriched compounds of general formula (I). These are obtained by classical resolution of the corresponding acid using a chiral amino base in organic solvents.

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: Hydroxy aromatic acids are produced in high yields and high purity (>95%) from halogenated aromatic acids in a reaction mixture containing a copper source and a ligand that coordinates to copper.

Abstract: The present invention discloses a dibenzocycloheptene compound represented by the formula (I): wherein R1: hydrogen atom, halogen atom, etc., R2: hydrogen atom, halogen atom, etc., A: 5-membered or 6-membered heteroaromatic ring group containing 1 to 3 hetero atom(s) selected from the group consisting of nitrogen atom, oxygen atom and sulfur atom, and the heteroaromatic ring group, etc. may have halogen atom, nitrogen atom, etc. as substituent(s), B: formula; —CH?CH—, formula; —CH2O—, etc., Y: C1-C10 alkylene group which may have halogen atom, etc. as substituent(s), etc., Z: carboxyl group which may be protected, etc.

Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) in which X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, Z represents hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, CKE represents one of the groups in which A, B, D, G and Q1 to Q6 are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.

Abstract: A compound of the general formula (I) (wherein the symbols are as defined in the description), or a prodrug or a salt thereof.

Abstract: Preparation of (S)-2-[[3-[N-[4-[(4-fluorophenoxy)phenyl]methyl]carbamoyl]-4-methoxyphenyl]methyl]butanoic acid (referred to as compound (I)) on an industrial scale lies in the finding of crystals homogeneous and excellent in the stability and the establishment of a preparative process thereof. Novel crystals of compound (I) homogeneous and excellent in the stability characterized by exhibiting the diffraction angles (2?) at at least 17.7°, 19.0° and 24.1° in the X-ray powder diffraction are provided by recrystallizing from an alcoholic solvent and purifying by acid-base treatment.

Abstract: It is presently accepted that the mechanism of action for all anti-tumor tubulin ligands involves the perturbation of microtubule dynamics during the G2/M phase of cell division and subsequent entry into apoptosis (1). In this invention, we report a novel tubulin ligands which have a unique mechanism of action. These compounds, halogenated derivatives of acetamido benzoyl ethyl ester (HAABE), arrest cancer cells in S-phase and cause cell death by a combination of apoptosis (DNA ladder) and necrosis (DNA degradation) type mechanisms. Normal cells are not affected at the same concentrations of compound. The ligands bind covalently to tubulin in vitro and in vivo and shows potent cancericidal activity in tissue culture assays and in animal tumor models. These compounds target early S-phase at the G1/S transition rather than the G2/M phase and mitotic arrest.

Abstract: The present invention provides a medicament comprising a benzene compound useful as an insulin sensitizer, a salt thereof or a hydrate of them and a derivative of them as the active ingredient. Specifically, it provides a benzene compound represented by the following formula, a salt thereof or a hydrate of them. In the formula, X represents 1) a C6-10 aryl group which may have one or more substituents or 2) a 5- to 10-membered heteroaryl group which may have one or more substituents; Y represents a group represented by the formula: (in the above formulae, Ry1, Ry2 and Ry3 are the same as or different from one another and each represents a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, or a C3-7 cycloalkyl group) etc.

Abstract: Arylcycloalkyl derivatives having branched side chains, processes for their preparation and their use as pharmaceuticals The invention relates to arylcycloalkyl derivatives having branched side chains and to their physiologically acceptable salts and physiologically functional derivatives. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistence is involved.

Abstract: The invention relates to a multimeric compound or a pharmaceutically acceptable salt or derivative thereof which comprises three or more neuraminidase-binding groups attached to a spacer or linking group, in which the neuraminidase-binding group is a compound which binds to the active site of influenza virus neuraminidase, but is not cleaved by the neuraminidase. The invention also relates to processes for the preparation of the multimeric compound defined above, pharmaceutical compositions containing them or methods for the treatment and/or prophylaxis of a viral infection involving them.

Abstract: A process for preparing alkynecarboxylic acids includes the oxidation of an alkyne alcohol with a hypohalite in the presence of a nitroxyl compound at a pH of greater than 7 with continual addition of the alkyne alcohol and of the hypohalite to the reaction mixture.

Abstract: This patent discloses a substituted fullerenes, compositions comprising the same, and their use as antioxidants. The substituted fullerenes comprise a fullerene core (Cn) and at least one of: (i) from 1 to 6 (>CX1X2) groups bonded to the fullerene core; (ii) from 1 to 18 —X3 groups bonded to the fullerene core; (iii) from 1 to 6 —X4— groups bonded to the fullerene core; or (iv) from 1 to 6 dendrons bonded to the fullerene core.

Abstract: A method for making an integrated circuit is disclosed as comprising depositing alternating regions of electrically conductive and dielectric materials on a substrate, wherein an area of dielectric material is formed by: a silane precursor having a fully or partially fluorinated first organic group comprising an unsaturated carbon-carbon double bond, the fully or partially fluorinated organic group bound to silicon in the silane precursor; forming from the silane precursor a hybrid organic-inorganic material having a molecular weight of at least 500 on a substrate; and increasing the molecular weight of the hybrid material by exposure to heat, electromagnetic radiation or electron beam so as to break the unsaturated carbon-carbon double bond and cross link via the fully or partially fluorinated organic group.

Abstract: One aspect of the present invention relates to polypharmacophoric compounds. In certain embodiments, the polyphamacophore compounds comprise individual pharmacophore units selected from the group consisting of D-1 agonists, D-2 agonists, D-3 agonists, D-4 agonists, irreversible monoamine inhibitors, reversible monoamine inhibitors, monoamine transporter inhibitors, COMT inhibitors, MAO inhibitors, and dopamine transporter inhibitors. Moreover, the present invention also relates to combinatorial libraries of polypharmacophoric compounds. Another aspect of the present invention relates to the use of a polypharmacophoric compound in a method of treating a mammal in need thereof. For example, a polypharmacophoric compound of the present invention may be used in a method of treating a mammal afflicted with Alzheimer's Disease, Huntington's Disease, depression, attention deficit disorder, autism, obesity, or inflammation.

Abstract: A supported gold catalyst is used for selective oxidation. In particular, an alcohol or ketone is oxidized to produce the corresponding carboxylic acid, an alcohol is oxidized to produce the corresponding ketone, and xylene is oxidized to produce the corresponding mono-alcohol or di-alcohol.

Abstract: A catalyst of the invention includes an imide compound having a N-substituted cyclic imide skeleton represented by following Formula (I): wherein R is a hydroxyl-protecting group. Preferred R is a hydrolyzable protecting group. R may be a group obtained from an acid by eliminating an OH group therefrom. Such acids include, for example, carboxylic acids, sulfonic acids, carbonic acid, carbamic acid, sulfuric acid, nitric acid, phosphoric acids and boric acids. The catalyst may include the imide compound and a metallic compound in combination. In the presence of the catalyst, (A) a compound capable of forming a radical is allowed to react with (B) a radical scavenging compound and thereby yields an addition or substitution reaction product of the compound (A) and the compound (B) or a derivative thereof. This catalyst can produce an organic compound with a high selectivity in a high yield as a result of, for example, an addition or substitution reaction under mild conditions.

Abstract: A process is described for preparing ammonium salts of aromatic carboxylic acids by reacting an aromatic carboxylic acid with ammonia in an aprotic solvent, which comprises carrying out the reaction in a closed vessel by continuously introducing a solution of the aromatic carboxylic acid in the aprotic solvent and passing in gaseous ammonia so that an ammonia partial pressure in the range from 0.1 to 3 bar is maintained in the gas space of the vessel, and discharging a suspension of the ammonium salt in the aprotic solvent. The process allows the preparation of ammonium salts of defined crystal size having a narrow size distribution.

Abstract: Compounds of the general formula (I) wherein R1 represents halogen, R2 and R3 represent H or halogen, and R4 represents C3-8-cycloalkyl or optionally substituted phenyl, pharamceutical compositions containing such materials, and methods of using such materials in the treatment of various diseases are disclosed and claimed.

Abstract: Novel compounds of general formula (I), the use of these compounds as medicaments, pharmaceuticaly compositions comprising the compounds and methods of treatment employing these compounds and compostiones. The present compounds may be useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR). The compounds exert their effects by modulating the PPAR? response in a partial agonist manner.

Abstract: The invention provides novel substituted phenylpropionic acid derivatives that bind to the receptor as ligands of human peroxisome proliferator-activated receptor ? (PPAR?) to activate and exhibit potent lipid-decreasing action, and processes for preparing them.

Abstract: A novel antibiotic thiobutacin, obtainable from Lechevalieria aerocolonigenes strain VK-A9, and antifungal and antioomycete compositions comprising thiobutacin as an active ingredient for control of plant diseases, e.g., those attributable to pathogens such as Phytophthora capsici and Botrytis cinerea.