Abstract: Disclosed are benzonaphthyridinyl derivative compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to kinase signal transduction inhibition, regulation or modulation.

Abstract: Disclosed is a compound of formula (I) and salts thereof. Also disclosed are methods of making the compound of formula (I) and the use of the compound as an intermediate for making pharmaceutically active compounds such as 11-?-hydroxysteroid hydrogenase type 1 (11-?-HSD1) inhibitors.

Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct copper catalyzed regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.

Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; and R1, R2, R3, Q and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.

Abstract: The present invention relates to a process for preparing naratriptan or a salt thereof, the process comprising: (a) reacting a compound of formula (3) with a compound of the formula HCCR wherein Z is a protecting group, Y is a leaving group and R is a trialkyl silyl group, a trialkylstannyl group or a zinc (II) halide, to obtain the compound of formula (4); (b) converting the compound of formula (4) to a compound of formula (5) wherein Z? is hydrogen or a benzyl group; (c) converting the compound of formula (5) to naratriptan; and (d) optionally converting naratriptan to a salt thereof. The present invention also provides novel compounds (3) and (4) and processes for their preparation.

Abstract: The present invention provides bicyclo-heptan-2-amines that selectively bind to the sigma-2 receptor and are useful in the treatment of diseases related to the sigma-2 receptor, for example, cancer and neurological disorders.

Abstract: An organic amine dimmer and a method for synthesizing the same are disclosed. The method comprises the following steps: (A) mixing an iron-containing compound (e.g., Fe2O3, FeCl3), a nitrate-containing compound, oxalate acid, 4,4?-trimethylenedipiperidine (TMDP), H3PO4, and 2 to 8 ml of water to form a mixture; (B) heating the mixture and maintaining the mixture at 160° C. or above for a first predetermined time; (C) cooling the mixture; and (D) placing the mixture at room temperature for a second predetermined time, to obtain an organic amine dimmer, wherein Fe(NO3)3 can serve as the iron-containing compound as well as the nitrate-containing compound.

Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.

Abstract: The present invention is directed towards proposing ligands of formula: and is also directed towards a substrate at the surface of which is immobilized at least one unit of formula:

Abstract: The present invention relates to compounds of formula (I) which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type II diabetes, obesity, atherosclerosis and cardiovascular diseases in humans.

Abstract: Disclosed is a process for producing A-form crystals of 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazolecarboxylic acid, comprising: a step of dissolving by heating 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazolecarboxylic acid in one or a plurality of solvents as a good solvent, selected from the group consisting of 1-propanol, 2-propanol, ethanol, and acetone; a step of cooling the solution; and a step of adding to the solution a hydrocarbon solvent as a poor solvent.

Abstract: Disclosed is a novel benzoxazole derivative which has high excitation energy, particularly high triplet excitation energy, and is a bipolar substance. A benzoxazole derivative represented by the following General Formula (G1) is provided. In the formula, R1 and R2 independently represent a hydrogen atom, an alkyl group with 1 to 4 carbon atoms, or a substituted or unsubstituted aryl group with 6 to 13 carbon atoms, substituents of the substituted aryl group may be bonded to form a ring which may form a spiro ring structure, R11 to R14 independently represent a hydrogen atom, a halogen, an alkyl group with 1 to 4 carbon atoms, or an unsubstituted aryl group with 6 to 10 carbon atoms, a bond formed between any two of ?, ?, and ? forms a carbazole skeleton, and n is 0 to 3.

Abstract: The present invention provides a method for producing a 1-biphenylmethylimidazole compound having superior angiotensin II receptor antagonistic activity, or an intermediate thereof. The present invention provides a method for producing a compound having the formula (5) (R1, Ra: H, an alkyl group) by oxidizing a compound having the formula (1) (Ra: H, an alkyl group) using an oxidizing agent in the presence of a radical initiation reagent, and then reacting with an ammonia-generating reagent and a compound having the formula R1CHO(R1: H, an alkyl group) or a compound having the formula R1C(ORb)3 (R1: H, an alkyl group; Rb: an alkyl group).

Abstract: The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds.

Abstract: The present invention relates to improvements in processes towards the production 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid, which is a useful intermediate in fungicide production. In particular, the invention relates to a process for treating a compound of formula III, wherein R1 is C1-C6 alkyl and R2 is CF3, CF2H or CFH2, comprising the steps of a) contacting a compound of formula III with base, and b) separating the compound of formula III and the base.

Abstract: A pentamethine cyanine fluorescent dye with N-substituting at ?-position of conjugated chain is disclosed. The dye reacts with biosubstrate including protein, liposome and DNA, and shows excellent selectivity. It has good living cell membrane permeability and shows good selectivity in living cell staining In addition, the dye has good stability and low background fluorescence, and can be used together with other fluorescent dyes having consistent wavelengths for single-channel excitation and multi-channel detection. The dye can be used in the fields of protein labeling and detecting, fluorescence immunoassay and living cell selective imaging and the like.

Abstract: The present invention relates to pharmaceutically acceptable crystalline and amorphous salts of D-isoglutamyl-D-tryptophan as well as processes for their manufacture, pharmaceutical compositions comprising them, and their uses in the preparation of pharmaceutical compositions for the treatment of various conditions and/or diseases. In particular, the present invention relates to D-isoglutamyl-D-tryptophan potassium salt (1:1), D-isoglutamyl-D-tryptophan lithium salt (1:1), D-isoglutamyl-D-tryptophan calcium salt (2:1), D-isoglutamyl-D-tryptophan magnesium salt (2:1), and D-isoglutamyl-D-tryptophan organic ammonium salts (1:1).

Abstract: This invention relates to compounds useful as ionic liquids that are based on an N-substituted pyrrolidinone and incorporate a pendant ammonium cation that is spaced from the pyrrolidone ring by a variable length linker.

Abstract: The present invention relates to compounds of the general formula: (I) wherein ring B, R1, R2, R3, Z, and L1 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.

Abstract: A heterocyclic quinoid thiophene organic photoelectric material, which comprises a compound represented by formula (1), in which R1, R2, R5 and R6, which may be identical or different, are H or C1-C20 alkyl or alkoxyl; R3 and R4, which may be identical or different, are C1-C20 alkyl or alkoxyl; a and b, which may be identical or different, are integer of 1-12; X is Si or C. A preparation method of said heterocyclic quinoid thiophene organic photoelectric material and the use thereof are also disclosed.

Abstract: Selective neuronal nitric oxide synthase (nNOS) inhibitor compounds designed with one or more thiophene-2-carboximidamide substituents for improved bioavailability.

Abstract: The invention relates to a process for the production of an alkylene carbonate by the reaction of an alkylene oxide with carbon dioxide in the presence of a phosphonium catalyst in which process (a) the alkylene oxide, carbon dioxide and phosphonium catalyst are continuously introduced into a reaction zone from which a product stream containing alkylene carbonate and phosphonium catalyst is withdrawn; (b) alkylene carbonate and a stream containing phosphoniura catalyst are separated from the product stream; (c) the alkylene carbonate, separated in step (b), is recovered as product; and (d) the stream containing phosphoniura catalyst, separated in step (b), is recycled to the reaction zone, in which process a treatment of alkylene carbonate and/or catalyst with a sorption agent comprising carbon is carried out.

Abstract: A method of forming a cyclic carbonate product is carried out by reacting an alkylene oxide, such as ethylene oxide, with carbon dioxide in the presence of a metal organic framework (MOF) catalyst with less than 0.5 mol % of any potassium or quaternary ammonium salts present based on moles of alkylene oxide feed in a reaction zone under reaction conditions to form a cyclic carbonate product. The cyclic carbonate product may be optionally fed as a crude carbonate product that does not undergo any purification or separation, other than the optional removal of any portion of unreacted alkylene oxide, carbon dioxide, and light hydrocarbon gases, to a second reaction zone containing a transesterification catalyst along with an aliphatic monohydric alcohol. The cyclic carbonate product and monohydric alcohol are allowed to react under reaction conditions to form the dialkyl carbonate and diol products.

Abstract: Biologically active compounds related to the bryostatin family of compounds, having simplified spacer domains and/or improved recognition domains are disclosed, including methods of preparing and utilizing the same.

Abstract: Disclosed are electroluminescent devices that comprise organic layers that contain dibenzofuran compounds. The compounds are suitable components of, for example, blue-emitting, durable, organo-electroluminescent layers. The electroluminescent devices may be employed for full color display panels in, for example, mobile phones, televisions and personal computer screens.

Abstract: The present invention provides crystalline forms, including an anhydrate form, of cabazitaxel and processes for the preparation of these forms, designated as Forms C1, C2, C3, C4, C5, C6, C7, C8, C8b, C9 and C9p.

Abstract: A pretreated titanium silicalite with MFI structure (TS-1) catalyst which has been pretreated with methanol, and then optionally filtered and optionally air-dried to form a pretreated activated TS-1 catalyst. The activated TS-1 may be used in an epoxidation reaction with no additional methanol added and has equivalent activity to TS-1 used with large excesses of methanol. By removing the need for additional methanol during the reaction, the losses of epichlorohydrin from solvolysis are minimized significantly.

Abstract: A process for the manufacture of propylene oxide (“PO”) by catalytic oxidation of propylene with an oxidant wherein the catalytic oxidation is performed in an aqueous reaction medium, comprising water with less than 10% by volume of cosolvents, wherein a water-soluble manganese complex is used as oxidation catalyst, characterized in that the water-soluble manganese complex is a mononuclear species of the general formula (I): [LMnX3]Y ??(I) or a binuclear species of the general formula (II): [LMn(?-X)3MnL]Y2 ??(II) wherein Mn is a manganese; L or each L independently is a polydentate ligand, each X independently is a coordinating species and each ?-X independently is a bridging coordinating species, whereas Y is an non-coordinating counterion, and wherein the catalytic oxidation is carried out at a pH in the range of from 1.5 to 6.0.

Abstract: Process for the manufacture of 1,2-epoxy-3-chloropropane by reaction between allyl chloride and hydrogen peroxide in the presence of a solid catalyst and in the possible presence of at least one solvent in an epoxidation medium comprising at least two liquid phases under the conditions of reaction, wherein the catalyst exhibits an external surface to volume ratio lower than to 2.4 104 m?1.

Abstract: A method for extracting an unsaponifiable fraction from a renewable raw material selected among oilfruits, oleaginous seeds, oleoproteaginous seeds, seed husks, oil-yielding almonds, sprouts, stones and cuticles of fruits, high-fat raw materials from animals, algae, fungus or yeast, includes the following steps: a) dehydrating and packaging the renewable raw material, not resulting in any extraction of the fat; b) reactive crushing of the fatty packaged raw material in the presence of a light alcohol and a catalyst; c) evaporating the light alcohol; d) concentrating the liquid phase such as to obtain a concentrate including the unsaponifiable fraction diluted in fatty acid alkyl esters; e) saponifying the unsaponifiable concentrate; f) extracting the unsaponifiable fraction from the saponified mixture. The use of an unsaponifiable fraction or co-products obtained by implementing the method for preparing a composition such as a cosmetic, drug, food, or food additive or supplement is also described.

Abstract: Steps in the processing of oils derived from plants or vegetables include the degumming, deodorizing and bleaching of the oil before it can be used for further applications. By eliminating one or more of these steps from the processing of the oil, followed by hydrogenating the oil to a specified degree of hydrogenation, the resulting upgraded oils can be incorporated into products having commercial applications. The process uses a high shear mixing device and a hydrogenation catalyst. The process can utilize a single or multiple high shear devices, and utilize renewable oils instead of increasingly scarce petroleum based products. The resulting hydrogenated products may then be utilized in a variety of other commercial applications, such as to render cellulosic products water resistant, provide a coating for numerous cellulosic products, adhesive compositions, ink compositions, firelog compositions, drilling muds or asphalt modifiers.

Abstract: Non-flammable, VOC-free organosilane quaternary ammonium compositions are provided in the form of pure or substantially pure water-soluble products that have bactericidal, fungicidal and viricidal activity and which are capable of bonding to various surfaces to form durable hydrophobic coatings. The resulting compositions are free of unreacted chloropropyltrialkoxysilanes, alkylamines and organic solvents that would otherwise provide flammable, corrosive, and/or toxic properties thereby inhibiting their safe and effective use in surface care, personal care and coating products.

Abstract: Processes for preparing (E)-2,4,6-(Trimethoxystyryl)-3-O-Phosphate Disodium-4-Methoxybenzyl Sulfones and uses thereof as antiproliferative agents, including, for example, anticancer agents, and as radioprotective and chemoprotective agents.

Abstract: Carbamate preparation process comprising, the reaction between at least: an amine or polyamines, an organic carbonate of formula (OR)(OR?)C?O, a catalyst which is formed by at least a support selected from at least a metal oxide, a microporous material, a mesoporous material, an anionic laminar compound of hydrotalcite type or their derivatives or an organic polymer and which may further contain a metal from groups 8, 9, 10 and 11 of the periodical system. The carbonates obtained can be transformed in their corresponding isocyanates.

Abstract: The present invention provides compounds, or derivatives or prodrugs thereof, that comprise a methyllysine mimic, and an ?-ketoglutarate mimic that are attached through a linker and methods for using and producing the same. In some embodiments, compounds of the invention are of the formula: M-L-K, or a derivative or a prodrug thereof, wherein M is a methyllysine mimic, L is a linker, and K is an ?-ketoglutarate mimic.

Abstract: The invention relates to the field of pharmaceutical chemistry, specifically to processes for preparing biologically active substances (BAS), in particular creatine amides. What is proposed is a process for preparing creatine amides which comprises treating creatine with para-toluenesulfonic acid in an organic solvent with subsequent reaction of the resultant complex with compounds comprising a primary or secondary amino group in the presence of a condensing agent and a base which are introduced subsequently. The claimed process makes it possible to increase the yield of the end product by 2-5 times in comparison with known similar processes and also to extend the range of the compounds prepared.

Abstract: The present invention relates to novel polymorphs of (2E)-1-hydroxy-2-methylpent-2-enyl-pyrophosphonate disodium (CHDMAPP-Na2), to the process for preparing them and to the pharmaceutical compositions containing them.

Abstract: The invention is directed to compounds of formula I: wherein Ar, r, R3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula I have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.

Abstract: A method of producing an aromatic amino compound using a primary or secondary amine compound and a halogenated aromatic compound as starting materials, and relying upon the Ullmann reaction, the method being capable of obtaining the highly pure aromatic amino compound in high yields and inexpensively. A primary or secondary amine compound having an aromatic ring group and a halogenated aromatic compound as starting materials, are reacted with the halogenated aromatic compound in the presence of copper catalyst and base to produce the aromatic amino compound having a structure in which an aromatic ring group derived from the halogenated aromatic compound is coupled to the amino group of the amine compound, wherein the amine compound and the halogenated aromatic compound are reacted together such that an aromatic oxycarboxylic acid having a hydroxyl group and a hydroxycarbonyl group bonded to neighboring carbon atoms, is present together with the copper catalyst and the base.

Abstract: The present invention relates to processes for the preparation of (2-Amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol hydrochloride (Fingolimod) and pharmaceutically acceptable salts thereof, and intermediates formed in such processes.

Abstract: Processes for alkylating hydroxyaryl compounds by reacting a hydroxyaryl with at least one olefin of a complex hydrocarbon stream. The complex hydrocarbon stream preferably comprises a fraction of a cracked hydrocarbon feed stream or the reaction products of a dehydrogenation of a paraffinic feedstock. The olefin of the complex hydrocarbon stream is preferably a branched olefin, e.g., isobutylene or isoamylene. The alkylated compositions are suitable for forming liquid phosphite compositions.

Abstract: A process for the conversion of a tertiary phosphine oxide to the corresponding tertiary phosphine includes reacting the tertiary phosphine oxide with a reducing tertiary phosphine, in the presence of a catalyst that catalyzes the conversion.

Abstract: One aspect of the present invention relates to ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in various transition-metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition-metal-catalyzed reactions, including the range of suitable substrates, number of catalyst turnovers, reaction conditions, and efficiency. For example, improvements have been realized in transition metal-catalyzed: aryl amination reactions; aryl amidation reactions; Suzuki couplings; and Sonogashira couplings. In certain embodiments, the invention relates to catalysts and methods of using them that operate in aqueous solvent systems.

Abstract: The present invention relates to a method for manufacturing methylmercaptopropionaldehyde (MMP) including at least the following steps: (a) dehydrating glycerol to acrolein from an aqueous solution of glycerol in the presence of an acid catalyst; (b) purifying the aqueous flux from step (a) to obtain a flux of acrolein containing at least 15 wt % of water relative to the acrolein; (c) causing a reaction of the acrolein flux obtained in step (b) with methylmercaptan in the presence of a catalyst; (d) optionally purifying the product obtained in step (c). The method of the invention can also include a reaction of the product obtained in step (c) or (d) with hydrocyanic acid, or sodium cyanide during a step (e) followed by a subsequent transformation to produce methionine or methionine hydroxyanalogue, which can then optionally be purified.

Abstract: The invention relates to novel polyglycerol based UV-filters as well as to topical compositions comprising such novel polyglycerol based UV-filters. Furthermore, the invention relates to the use of such novel polyglycerol based UV-filters to enhance the solubility of butyl methoxydibenzoylmethane or bis-ethylhexyloxyphenol methoxyphenyl triazine in cosmetic oils.

Abstract: A method comprising reacting glycerol with acetaldehyde or 1,1-diethoxyethane to produce 1,3-dihydroxyacetone (DHA), without using fermentation or direct oxidation of the glycerol is provided. DHA is useful in various products, including as a sunless tanning agent.

Abstract: Methods for performing a condensation reaction are disclosed. Specifically, various methods for the production of highly-pure bisphenol-A are disclosed in which an attached promoter ion exchange resin catalyst system is combined with a solvent crystallization step.

Abstract: This invention is a process for making 1,2-propane diol from glycerol. The process comprises subjecting a glycerol stream to hydrogenation conditions in the presence of a transition metal promoted skeletal copper catalyst to enhance selective production of 1,2-propane diol product. Chromium promoted catalyst is preferred for this invention, and moreover, it is preferred that the skeletal copper catalyst is prepared from copper aluminum alloys that have been subjected to leaching conditions selected to achieve at least 40% leaching of aluminum from the alloy. This process is particularly conducive to conducting the hydrogenation with reactant mixture in the liquid phase. The catalysts used in this invention are particularly suitable for use in a fixed catalyst bed, but can be activated and sized so that the catalyst is also suitable for use in slurry based reactions.

Abstract: The invention relates to a process for separating monochloro-trifluoropropenes such as HCFC-1233 from azeotrope or azeotrope like combinations with HF. The process employs a cold, liquid phase separations and multiple azeotropic distillation trains.

Abstract: A method for converting crude tall oil into high quality diesel fuels include the steps of (a) removal of non-oil contaminants present in the crude tall oil and recovery of valuable organic, (b) heating and removing the volatile fractions of the refined tall oil stream from step (a) and forming a volatiles free oil stream comprising organic components with boiling points of 170° C. and higher, (c) vacuum distilling the volatiles free oil stream of from step (b) to produce a first and second stream the first stream including components with boiling points between 170-400° C. and the second stream comprising components having boiling points greater than 400° C. and (d) passing the first stream into a catalytic reactor wherein hydrogenation and deoxygenation take place to produce a diesel range fuel depleted in oxygen.