Abstract: Certain pyrimidine-containing compounds are serotonin receptor modulators useful in the treatment of serotonin-mediated diseases.

Abstract: Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O)t; Ra is O or S.

Abstract: The invention relates to HSP90 inhibiting compounds consisting of the formula: wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

Abstract: This invention relates to a process for preparing 4-[(1,6-dihydro-6-oxo-2-pyrimidinyl)-amino]benzonitrile (I) starting from a 4-oxo-1,6-dihydro-pyrimidinylcarboxylic acid ester (II) or starting from a guanidine derivative which is reacted with an alkoxy-methylene malonic acid ester to an ester (II) which is converted to (I), which reaction sequence may be a one-pot procedure.

Abstract: Compounds represented by the following structure (II) are disclosed: as are methods for making such compounds. Compositions and methods for treating various disease conditions including cancer and non-cancer diseases associated with vascular proliferation are also disclosed.

Abstract: The present invention relates to ruthenium and osmium complexes of Formula [M(A)w(B)x(C)y]m(Xz)n, per se and the use of ruthenium and osmium complexes of Formula I as redox mediators in electrochemical biosensors.

Abstract: A dye for dye-sensitized solar cells includes an organometallic complex represented by M(L)pX2:(Z)q. In the organometallic complex, M is a Group 8 through Group 10 metallic element, L is a bidentate ligand, X is a co-ligand, and Z is a counter-ion. The ratio of the bidentate ligand (L) to the counter-ion (Z) is about 1.1 to about 1.4. A method of preparing an exemplary dye includes mixing the organometallic complex with tetrabutylammonium thiocyanate and tetrabutylammonium hydroxide to prepare a solution, and purifying the solution at a pH of about 3.8 to about 4.1. A dye-sensitized solar cell includes a first electrode with a light absorbing layer, a second electrode and an electrolyte between the first and second electrodes. The light absorbing layer includes the dye.

Abstract: Synthetic processes for preparing luminescent iridium complexes and precursors thereof are provided. The method employs water as the reaction solvent to prepare luminescent iridium complexes in two different ways. In the first way, a precursor [Ir2(C11NR8)4I2] (Formula I) is prepared from one of IrCl3, M3IrCl6 (M=Li, Na, K) and [Ir2(C11NR8)4Cl2], and then the precursor [Ir2(C11NR8)4I2] is converted into one of the two luminescent iridium isomeric complexes [Ir(C11NR8)2(C11NR?8)] (Formula II). In the second way, a metal complex IrCl3 or M3IrCl6 (M=Li, Na, K), HC11NR8 and a base are converted selectively into one of the two iridium isomeric complexes [Ir(C11NR8)3] (Formula VIII). Herein, R and R? are defined the same as the specification.

Abstract: The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2?, R3, R3?, R4, R4?, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).

Abstract: Novel mono-azide substituted rylene-imide derivatives, their use in methods for the detection of analytes and reagents kits for the detection of analytes comprising said novel mono-azide substituted rylene-imide derivatives.

Abstract: The compounds of the present invention are represented by the following formula (I): wherein M is represented by the following formula: with R1, R2, R3, R4, R5, R6, R7, R8, R10, R11, X1, X2, X3, L, a, b, c, d, e, x, y, and z defined herein.

Abstract: MCH-1 receptor antagonists are disclosed having the general formula These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.

Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salt thereof, wherein X1 to X4, R1 to R4, A, B, D and m are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Abstract: The present invention relates to compounds of formula (I).

Abstract: Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.

Abstract: The invention provides compounds of formula wherein R1, R2, R3, R4, R5, and R6 are as defined herein or a pharmaceutically suitable acid addition salt thereof. The present compounds are high potential NK-3 receptor antagonists useful for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are pharmaceutically active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

Abstract: The present invention provides dimethyl sulphoxide solvate of 4-(4-{3-[4-chloro-3 -(trifluoromethyl)phenyl]ureido}phenoxy)-N2-methylpyridine-2-carboxamide, process for its preparation, pharmaceutical composition comprising it and its use for the treatment of cancer. The present invention also provides a novel HPLC method for the identification, quantification and isolation of related substances of sorafenib.

Abstract: Disclosed are an intermediate compound of N-(1,1,1-trideuterated methyl)phthalimide, and its use in the preparation of deuterated diphenylurea derivative.

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.

Abstract: The present invention discloses a process for obtaining 4-(1-hydroxy-1-methylethyl)-2-propyl-imidazole-5-carboxylate by the reaction of 4,4-dimethyl-2-propyl-4,6-dihydrofuro[3,4-d]imidazole, or its hydrolysis product, or its ring-opening product, with alcohol under appropriate catalytic conditions. Furthermore, the present invention also provides a process for obtaining high purity 4,4-dimethyl-2-propyl-4,6-dihydrofuro[3,4-d]imidazole.

Abstract: Process for the preparation of sunitinib malate form I via sunitinib acetate and polymorphs of said intermediate.

Abstract: The present invention is concerned with a process for preparing compounds of the general formula (I). These compounds can preferably be used to prepare bioactive agents. The reaction of the invention starts from the corresponding hydroxy compounds which are oxidized, with Ru catalysis, in a one-phase aqueous system.

Abstract: This invention is directed to stereoselective synthesis of compounds of formula (I) or formula (II): or a pharmaceutically acceptable salt, ester, amide, complex, chelate, clathrate, solvate, polymorph, stereoisomer, metabolite or prodrug thereof; wherein R3, R4 and R5 are defined herein. Compounds of formula (I) and formula (II) are known to be useful in treating arrhythmias.

Abstract: Production of a bicyclo[3.1.0]hexane derivative, useful as a metabotropic glutamate receptor modulator, becomes possible by a production method that includes converting a compound represented by Formula (II) into a compound represented by Formula (III) by reaction with an acyl group donor in the presence of a microorganism-derived enzyme, without using an expensive optically active trans hydroxy ester as a starting material and without employing a fluorination reaction requiring an ultralow temperature reaction. Furthermore, since asymmetric synthesis can be carried out in a stage closer to the final product, the production method is useful as a production method that can mass produce a bicyclo[3.1.0]hexane derivative.

Abstract: Intermediates and methods of their use in the synthesis of analogs of halichondrin B are provided.

Abstract: This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center.

Abstract: The present invention relates to a process for the preparation of 2-substituted 4-hydroxy-4-methyltetrahydropyranols by reacting 3-methylbut-3-en-1-ol (isoprenol) with the corresponding aldehydes in the presence of a strongly acidic cation exchanger. Specifically, the present invention relates to a corresponding process for the preparation of 2-isobutyl-4-hydroxy-4-methyltetrahydropyran by reacting isoprenol with isovaleraldehyde.

Abstract: Esterquats (reaction products of a fatty acid source and a trialkanolamine) having a desirable distribution of mono-, di-, and tri-quat esters, such as at least 55 wt. % of the diester and at most 25% of the triester, can be produced by heating a trialkanolamine and a fatty acid source at a temperature ramp rate of 0.4° C. per minute or less. This result can be achieved, for example, by reducing the amount of catalyst to a suboptimal amount for rapid formation of the quat diester.

Abstract: The present invention relates to organic electroluminescence devices containing metal complexes having the formula (1) and metal complexes for use in organic electroluminescence devices.

Abstract: The present invention provides a process for the preparation of a complex of formula (I) comprising the steps of: (a) mixing Pd(diolefin)Br2 and tBu3P in a solvent; and (b) adding an alkali hydroxide to form the complex of formula (I).

Abstract: A novel catalyst component for producing a crystalline ?-olefin polymer or ?-olefin/(meth)acrylate copolymer having few branches, especially a polymer having a high molecular weight, and a method for producing an ?-olefin polymer or an ?-olefin/(meth)acrylate copolymer using the catalyst component. A metal complex represented by the following general formula (D), as well as a method for producing an ?-olefin polymer and a method for producing an ?-olefin/(meth)acrylate copolymer using the metal complex.

Abstract: A practical and efficient method for halogenation of activated carbon atoms using readily available N-haloimides and a Lewis acid catalyst has been disclosed. This methodology is applicable to a range of compounds and any halogen atom can be directly introduced to the substrate. The mild reaction conditions, easy workup procedure and simple operation make this method valuable from both an environmental and preparative point of view.

Abstract: New types of derivatives of tris(2-hydroxyphenyl)methanes which have, as functional groups, polyalkoxy groups or polyalkoxy groups modified with terminal hydrophilic groups, preparation of such compounds and their use, especially as surfactants and thickeners.

Abstract: The invention relates to a process for the preparation of an alkanediol and a dialkyl carbonate comprising: reacting an alkylene carbonate and an alkanol in the presence of a transesterification catalyst to obtain a reaction mixture comprising dialkyl carbonate, unconverted alkanol, alkanediol and unconverted alkylene carbonate; and then subjecting the mixture to separation in three distillation columns.

Abstract: A composition comprising a polymer backbone and at least one side group, wherein the side group comprises a benzene ring-based chromophore comprising a ketone at the 1-position, a substituted or unsubstituted amino group at the 2-position, and an oxygen atom at the 3-position of the benzene ring. The chromophore is a kynurenine-based compound. Methods of making and using the composition are also provided. The composition can be used in an ophthalmic lens or device for protecting the retina by blocking UV rays and filtering violet rays.

Abstract: The present invention includes compound compositions and methods of making compounds that include an oligo-benzamide compound having at least two optionally substituted benzamides.

Abstract: A modular system and method for producing urea from bio-mass includes cleaning a bio-mass feedstock to remove substantially all non-organic matter; blending the cleaned bio-mass to obtain a substantially homogeneous blend; pelletizing the blended bio-mass; and gasifying the pellets in a gasifier. The bio-mass feedstock may include bio-mass materials having different processing characteristics. The gasifying step preferably includes pulverizing the pellets to a fine particle size, injecting an organic oil into the input biomass mist when needed, and controlling the feed rate to maintain a substantially constant burn temperature. The resultant syngas stream is cleaned and compressed to a high pressure of about 6,000 to 7,000 psi. The resultant ammonia stream is processed in a bypass recycling loop system at 30% conversion rate at a high pressure of about 6,000 to 7,000 psi.

Abstract: Disclosed is a method of making a 2-substituted-1,4-benzenediamine by nucleophilic aromatic substitution.

Abstract: The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use. For example, the present invention provides chalcone and cyanopyridine compounds, and derivatives thereof, exhibiting high antibacterial activities having multiple electron withdrawing group substituents, such as halogens and fluorinated alkyl groups, and optionally having hydroxyl and/or alkoxyl groups substituents.

Abstract: Disclosed herein are phosphine compounds represented by the general formula (4): and corresponding phosphonium salts represented by the general formula (4a): Also disclosed are processes for the preparation of these phosphines and phosphonium salts as well as their use as ligands in catalytic reactions.

Abstract: The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition.

Abstract: A hexafluorodimethylcarbinol terminated compound, method of making it, and a composition of matter are disclosed. The compound may have the formula (CF3)2C(OH)-L-M-R. The substructure L may be selected from an optionally substituted propenylene group (—CH2CH?CH—) and trimethylene group (—CH2CH2CH2—). The substructure M may be selected from a substituted or unsubstituted methylene chain, a substituted or unsubstituted oxyalkylene chain, and a silicon-containing chain or combination thereof. In one embodiment, M may be selected from —(CH2)n—, —(OCH2CH2)m—, and —(Si(CH3)2O)p—Si(CH3)2—(CH2)q—, wherein n is at least 1, e.g., n is up to 10, m can be at least 1, e.g., m is up to 10, p can be 0 and in one embodiment is from 1 to 10, and wherein q can be 1 and in one embodiment is from 1 to 12. The substructure R represents one of a halogen, —SH, —SZ, —S—S-M-L-C(CF3)2(OH), wherein Z represents a thiol protecting group.

Abstract: Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.

Abstract: Process for the preparation of the powdery crystalline mixtures of alpha-hydroxycarbonyl derivatives of alpha-methylstyrene dinners comprising the use of a solvent having polarity from 0 to 0.1.

Abstract: A compound of the general formula X-[Q-W—(CH?CH)n—(CH2)2-L]m (I) in which X represents a polymer; Q represents a linking group; W represents an electron-withdrawing group; n represents 0 or an integer of from 1 to 4; L represents a leaving group; and m represent an integer of from 1 to 8. The compounds find use in the conjugation of biological molecules.

Abstract: Methods for continuously preparing cyclohexanone from phenol make use of a catalyst having at least one catalytically active metal selected from platinum and palladium. The process includes enriching phenol in a distillation fraction as compared to a subsequent fraction, wherein the subsequent fraction includes phenol and side-products having a higher boiling point than phenol. Distillation is carried out in a vacuum distillation column equipped with trays in the lower part of the column. In an upper part of the column, i.e., in the part above the feed inlet, packing material is present instead of trays in at least part thereof. The packing material has a comparable or improved separating efficiency, and provides a reduction of the pressure drop by at least 30%, preferably more than 50%, as compared to the case with trays in the upper part, under otherwise similar distillation conditions.

Abstract: An object of the present invention is to provide an industrially advantageous process for preparing a benzaldehyde compound from a benzyl alcohol compound with high yield. The present invention relates to a process for preparing an aromatic aldehyde compound represented by the formula (2); which comprises reacting an aromatic methyl alcohol compound represented by the formula (1); and a peroxide under a pH value of a reaction solution being pH 0.01 or higher and less than 10 in the presence of at least one metallic compound selected from a molybdenum compound and a tungsten compound, a quaternary ammonium salt and an organic phosphonium salt.

Abstract: A process for long-term operation of a heterogeneously catalyzed partial gas phase oxidation of propene to acrolein, in which the propene present in the reaction gas input mixture is partially oxidized as this gas mixture passes through the fixed catalyst bed which is accommodated in two spatially successive temperature zones A, B, and, in long-term operation, as a measure to counteract the reduction in the quality of the fixed catalyst bed, the temperature of at least one of the two temperature zones is increased such that the difference TB?TA becomes increasingly greater, where TB is the temperature of temperature zone B, and TA the temperature of temperature zone A.

Abstract: The invention relates to a process for preparing polyether alcohols by reacting a) aromatic amines with b) alkylene oxides in the presence of c) a catalyst, wherein the alkylene oxide b) comprises at least 90% by weight, based on the weight of the component b), of propylene oxide and an amine is used as catalyst c).