Abstract: The invention is directed to compounds and methods of synthesizing hydroxyethlamino amides and their use in treatment of aspartyl protease mediated diseases and conditions.

Abstract: Provided are compounds of formula I or II that are useful for the treatment of diseases related to the adenosine receptor. Also included are methods oftreating patients suffering from or susceptible to at least one symptom of abuse of dependence on, or withdrawal from at least one substance.

Abstract: Compounds of the general formula (I): in which inter alia Q1 represents —NR1R3, —OR1 or —SR1 and Q2 represents —NR2R4, —OR2 or —SR2, and A represents the point of attachment to a support matrix, are useful as protein binding ligands when (a) at least one of R1, R2, R3 and R4 includes an alkyl group —CnH2n+1 in which n is greater than or equal to 7; (b) at least two of R1, R2, R3 and R4 independently include an alkyl group —CnH2n+1 or a cycloalkyl group —CnH2n?1 in which n is greater than or equal to 4; or (c) at least three of R1, R2, R3 and R4 independently include a C1-12 alkyl group substituted by —NR5R6 or aryl.

Abstract: Provided herein are compounds of formula (I): as well as pharmaceutically acceptable salts and esters thereof, which are useful as pharmaceutical compositions for the treatment of metabolic diseases and disorders.

Abstract: The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents. Also provided are processes for the preparation of the compounds and their intermediates.

Abstract: A monomer of formula (1) is provided wherein R1 is hydrogen or a monovalent C1-C6 hydrocarbon group, and R2 is a group having polymerization functionality. Using the monomer, crosslinking units can be incorporated into a polymer chain. A chemically amplified negative resist composition comprising a base polymer having crosslinking units incorporated therein has a high sensitivity and forms a resist pattern with minimized LER.

Abstract: The present disclosure is directed to the sodium salt of 5-cyclopropyl-2-{[2-(2,6-difluorophenyl)pyrimidin-5-yl]amino}benzoic acid, pharmaceutically acceptable solvates thereof, pharmaceutical combinations thereof, and methods of treatment.

Abstract: The present invention is directed to a compound of the formula: and pharmaceutically acceptable tautomers, or salts thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to pharmaceutical compositions containing such a compound.

Abstract: The present invention relates to processes for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate, i.e. the compound of the formula (I) and to a process for purifying the crude product of the formula (I) for use as pharmaceutically active compound, where, for purification, methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate sulphinyldimethane (1:2) of the formula (II) is isolated as intermediate or is generated as intermediate in this purification process, if appropriate present in a mixture.

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein A is hydrogen, C1-4alkyl, C3-6cycloalkyl, C1-3alkoxy, C1-3alkoxy C1-4alkyl, C1-2fluoroalkyl, halogen, NR6R7, optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis, osteoarthritis or neurodegenerative disorders.

Abstract: The present invention relates to a process for the manufacture of 4-((1R,3S)-6-Chloro-3-phenyl-indan-1-yl)-1,2,2-trimethyl-piperazine or a pharmaceutically acceptable salt thereof and a process for the manufacture of 1-((1R,3S)-6-Chloro-3-phenyl-indan-1-yl)-3,3-dimethyl-piperazine or a pharmaceutically acceptable salt thereof.

Abstract: A rylene-based polychromophore of the general formula I in which the variables are each defined as follows: rylene is a radical of the formula which has been functionalized by at least one imide group, ester group or amide group and which may additionally be substituted by aryloxy, arylthio, hetaryloxy and/or hetarylthio; X is a rylenedicarboximide radical which absorbs at a different wavelength from the rylene radical, is bonded to the X radical in the peri-position via Y via a moiety —Y?-A-Y—, is bonded to the rylene radical and may likewise be substituted by aryloxy, arylthio, hetaryloxy and/or hetarylthio; A is a bridging member having at least one aromatic or heteroaromatic radical, the Y or Y and Y? groups being bonded to the aromatic or heteroaromatic radical; Y is a moiety Y? is a moiety where the moieties (i) and (ii) may be part of the ester groups of the rylene radical and the moieties (iii) are part of the imide groups of the rylene radical and the moieties (iv) ar

Abstract: The present invention provides a tetomilast crystal that is industrially easily produced in a large volume. (1) a tetomilast hydrate crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in FIG. 2; (2) an anhydrous tetomilast type A crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in FIG. 4; (3) an anhydrous tetomilast type C crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in FIG. 8; (4) a tetomilast acetonitrile solvate crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in FIG. 10; and (5) a mixture consisting of the above anhydrous tetomilast type A crystal and an anhydrous tetomilast type B crystal.

Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula (I) can be used as agrochemical active ingredients and can be prepared in a manner known per se.

Abstract: The present invention is directed to a fluorosilane represented by (L)3-Si—(CH2)n—N(-Q3-Rf)-Q1-Rf where each n is independently an integer from 1 to 12; L is independently chosen from a hydrolysable or non-hydrolysable monovalent group Rf is chosen from a C2-C12 perfluoroalkyl provided that: i) one fluorine atom of the perfluoroalkyl can be optionally replaced by hydrogen, and/or ii) the perfluoroalkyl can be optionally interrupted by at least one oxygen, methylene, or ethylene; Q1 is chosen from the group consisting of a C2-C12 hydrocarbylene optionally interrupted by at least one divalent organic group; X1 is chosen from O or S; and b) Q1 and Q3 are independently chosen from the group consisting of a C2-C12 hydrocarbylene interrupted by at least one of —C(O)—O— or —O—C(O)—, and optionally further interrupted by at least one divalent organic group.

Abstract: Compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are pharmaceutical compositions comprising the compounds, and methods of using the compounds in the treatment of cancer.

Abstract: The invention provides two process for synthesizing substituted aminothiazolone compounds as inhibitors of 11-?-hydroxy steroid dehydrogenase type 1. The processes allow the stereoselective synthesis of the desired compounds without the use of stoichiometric amounts of chiral catalysts.

Abstract: Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.

Abstract: Provided are compounds having Formula VIIIa-1: wherein Z, X5, R2, R2a and R10 are as defined herein. Compounds of Formula VIIIa-1 can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.

Abstract: Benzimidazole compounds of formula (I): wherein R1, R2, R3, R4, R5, X, Y, Z1, and Z2 are defined herein. Also disclosed is a method for treating cancer with benzimidazole compounds.

Abstract: A compound for absorbing sunlight and converting the sunlight into electrical energy, which is formed by coupling a fullerene with at least one or more triarylamine derivatives. The fullerene is selected from among those having carbon numbers C60, C70, C78, C82 and C84, and the triarylamine derivatives are coupled with at least one or more aliphatic or aromatic hydrocarbons and are also coupled with a dopant. A method of manufacturing the compound includes steps of synthesizing a fullerene derivative, synthesizing fullerene-triarylamine, wherein a fullerene-triarylamine adduct is prepared by coupling the fullerene derivative with a triarylamine derivative, preparing an adduct solution by dissolving the fullerene-triarylamine adduct in an organic solvent, and conducting a doping reaction by adding an acid dropwise slowly to the adduct solution.

Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.

Abstract: The invention provides Saxagliptin Schiff bases, polymorphs of Saxagliptin and (1S,3S,5S)-2-[(2S)-2-propan-2-ylideneamino-2-(3-hydroxy-1-adamantyl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile, processes for preparing Saxagliptin hydrates, and pharmaceutical compositions thereof.

Abstract: Compounds that inhibit proteolytic enzymes of Human Immunodeficiency Virus (HIV) are described. Preparation of the inhibitors, pharmaceutical compositions containing them, and uses of the compounds or compositions for the treatment of HIV infections are also described.

Abstract: The present invention relates to an improved process for the preparation of N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidine)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide—Sunitinib base of formula (I) and its pharmaceutically acceptable malate salt of formula (I(a)).

Abstract: The invention includes methods of processing an initial di-carbonyl compound by conversion to a cyclic compound. The cyclic compound is reacted with an alkylating agent to form a derivative having an alkylated ring nitrogen. The invention encompasses a method of producing an N-alkyl product. Ammonia content of a solution is adjusted to produce a ratio of ammonia to di-carboxylate compound of from about 1:1 to about 1.5:1. An alkylating agent is added and the initial compound is alkylated and cyclized. The invention includes methods of making N-methyl pyrrolidinone (NMP). Aqueous ammonia and succinate is introduced into a vessel and ammonia is adjusted to provide a ratio of ammonia to succinate of less than 2:1. A methylating agent is reacted with succinate at a temperature of from greater than 100° C. to about 400° C. to produce N-methyl succinimide which is purified and hydrogenated to form NMP.

Abstract: In one aspect, the invention relates to compounds of formula I: where Y, R1, R2, n, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

Abstract: An inexpensive and industrially advantageous method for producing optically active syn-3-(N-substituted-aminomethyl)-4-fluoropyrrolidine which may be an intermediate for producing pharmaceuticals is provided. The present invention relates a method for producing a syn-1-protected-4-fluoro-3-(N-substituted-N-nitrobenzenesulfonyl)pyrrolidine derivative or it's enantiomer, or their salts comprising the process of fluorinating a compound represented by the general formula (6) (in the formula, PG1 represents a protecting group for an amino group, R1 represents a C1 to C6 alkyl group which may be substituted or a C3 to C8 cycloalkyl group which may be substituted, and Ns represents a 2-nitrobenzenesulfonyl group or a 4-nitrobenzenesulfonyl group) or it's enantiomer using a nucleophilic fluorinating agent and an organic base having an amidine or guanidine structure.

Abstract: The present invention provides a method for producing a methylene disulfonate compound including reacting, in the presence of an acid and a dehydrating agent, a formaldehyde compound with at least one salt of alkanedisulfonic acid selected from the group consisting of alkali metal salts of alkanedisulfonic acid and alkaline earth metal salts of alkanedisulfonic acid each represented by a specific formula. According to the method of the present invention, a methylene disulfonate compound can be obtained in a simple manner at low cost.

Abstract: A process for the preparation of N-monosubstituted ?-aminoalcohol sulfonates of formula (1a), (1b): wherein R1 is C6-20-aryl or C4-12-heteroaryl, each optionally being substituted with one or more halogen atoms and/or one or more C1-4-alkyl or C1-4-alkoxy groups, R2 is C1-4-alkyl or C6-20-aryl, each aryl optionally being substituted with one or more halogen atoms and/or one or more C1-4-alkyl or C1-4-alkoxy groups, and wherein R3 is selected from the group consisting of C1-18-alkyl, C6-20-cycloalkyl, C6-20-aryl and C7-20-aralkyl residues; including a) reacting a methyl ketone, a primary amine, formaldehyde and a sulfonic acid, at a pressure above 1.5 bar, optionally in a organic solvent, said organic solvent which can include water to provide N-monosubstituted ?-aminoketone sulfonates of formula (II): wherein R1, R2 and R3 are as defined above, and b) asymmetrically hydrogenating.

Abstract: Antitumoral compounds obtained from a porifera, of the family Raspailiidae, genus Lithoplocamia, species lithistoides, and derivatives thereof are provided.

Abstract: Inhibitors of bacterial communication, such as quorum sensing, and method of use and manufacture thereof.

Abstract: The invention relates to a novel process for the preparation of C-4 coupled flavonoids, proanthocyanidins and analogues thereof. According to a specific application of the invention, there is provided a method for the preparation of proanthocyanidins and proanthocyanidin analogues.

Abstract: The subject of the present invention is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-dibutylamino)propoxy]benzoyl}-1-benzofuran-5-yl]methanesulfonamide of formula I: and the new intermediates of the preparation process.

Abstract: A solid fatty acid alkyl ester sulfonate metal salt is disclosed having an endothermic peak area between 50° C. and 130° C. of 50% or more relative to the whole endothermic peak area between 0° C. and 130° C. when determined using a differential scanning calorimter. A method for producing a fatty acid alkyl ester sulfonate metal salt powder is also disclosed, including a step of pulverizing the solid fatty acid alkyl ester sulfonate metal salt in a pulverizer, with the internal temperature of the pulverizer being adjusted to 30° C. to 50° C.

Abstract: This disclosure relates generally to olefin metathesis, and more particularly relates to the synthesis of terminal alkenes from internal alkenes using a cross-metathesis reaction catalyzed by an olefin metathesis catalyst. According to one aspect, for example, a method is provided for synthesizing a terminal olefin, the method comprising contacting, in the presence of a ruthenium alkylidene metathesis catalyst, an olefinic substrate comprised of at least one internal olefin with a cross metathesis partner comprised of an alpha olefinic reactant, under reaction conditions effective to allow cross-metathesis to occur, wherein the reaction conditions include a reaction temperature of at least 35° C. The methods, compositions, reactions and reaction systems herein disclosed have utility in the fields of catalysis, organic synthesis, and industrial chemistry.

Abstract: Disclosed is a process for producing alkyl fatty esters from fats/oils and C1 to C5 lower alcohols by a multistage reaction process, which includes feeding fats and oils to a reactor at an upper stage and then sent to a stage at the downstream side while feeding lower alcohols to a reactor at a lower stage, and simultaneously returning lower alcohols recovered from an outlet of the reactor to a stage at the upstream side, thereby repeating the reaction.

Abstract: A method of manufacturing ruthenium carbene complexes and novel aryl alkylidene ruthenium complexes based on the method, the complexes able to used as catalysts in metathesis reactions.

Abstract: A novel lead zirconium titanate (PZT) material having unique properties and application for PZT thin film capacitors and ferroelectric capacitor structures, e.g., FeRAMs, employing such thin film material. The PZT material is scalable, being dimensionally scalable, pulse length scalable and/or E-field scalable in character, and is useful for ferroelectric capacitors over a wide range of thicknesses, e.g., from about 20 nanometers to about 150 nanometers, and a range of lateral dimensions extending to as low as 0.15 ?m. Corresponding capacitor areas (i.e., lateral scaling) in a preferred embodiment are in the range of from about 104 to about 10?2 ?m2. The scalable PZT material of the invention may be formed by liquid delivery MOCVD, without PZT film modification techniques such as acceptor doping or use of film modifiers (e.g., Nb, Ta, La, Sr, Ca and the like).

Abstract: A new platinum complex which has strong antitumor activity and has effect with smaller doses and a pharmaceutical composition containing the same are provided. A spiro[4,4]nonane-1,6-diamineplatinum(II) complex which is represented by a following general formula (A). (In the formula, X and Y are same or different, and X and Y represent halogen atoms respectively, or X and Y cooperatively represent a divalent residue which is described by a formula (Z).) The platinum complex has a strong antitumor activity and is efficacious as a therapeutic agent for malignant tumors.

Abstract: A process for manufacturing a polyfluroalkanoyl phosphorodichloridate comprising reacting a polyfluoroalkanol having the general formula Rf—CH2—OH, wherein Rf is a linear or branched C1-C8 perfluoroalkyl group optionally interrupted by O, with at least 4 moles of POCl3 per mole of Rf—CH2—OH in the presence of 0.1 to 0.2 moles of LiCl catalyst per mole of Rf—CH2—OH at a temperature between 95° C. and 110° C. to form a phosphorodichloridate of the general formula Rf—CH2—O—P(O)Cl2.

Abstract: A process for the preparation of compounds containing nitrile functions and, more specifically, compounds containing two nitrile functions, such as succinonitrile and adiponitrile, is described. A process for preparing dintrile compounds obtained by reacting ammonia with an aqueous solution of a dicarboxyl compound in the presence of a silicon orthophosphate catalyst is also described.

Abstract: Disclosed are a process suited to large scale synthesis with high yield for producing oseltamivir phosphate, in which a preparation of oseltamivir phosphate which is highly safe as a pharmaceutical product can be produced, and an intermediate compound for producing oseltamivir phosphate. In this production process, an intermediate compound represented by general formula (V) is synthesized by employing Michael reaction/Michael reaction/Horner-Wadsworth-Emmons reaction, and oseltamivir phosphate is produced by converting the substituent groups in this intermediate compound.

Abstract: The invention relates to compounds of the formula I in which R1, R2, X, A, B, Z and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.

Abstract: Compounds that bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analyses of the GLP-1 receptor. Methods of synthesis, methods of therapeutic and/or prophylactic use, and methods of use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor of such compounds are provided.

Abstract: A monomer compound that contains at least one polymerizable functional group per molecule, and at least one bicycloheptyl-, bicycloheptenyl-, or branched (C5-C42)alkyl-polyether radical per molecule, wherein the bicycloheptyl- or bicycloheptenyl-polyether radical may optionally be substituted on one or more of the ring carbon atoms by one or two (C1-C6)alkyl groups per ring carbon atom is useful in making polymers, particularly pH responsive polymers.

Abstract: A method for preparing a palladium-gold catalyst containing a titania extrudate is disclosed. The titania extrudate is produced by using a carboxyalkyl cellulose and a hydroxyalkyl cellulose as extrusion aids. The titania extrudate has improved processibility and/or mechanical properties. After calcination, the extrudate is used as a carrier for the palladium-gold catalyst. The catalyst is useful in producing vinyl acetate by oxidizing ethylene with oxygen in the presence of acetic acid.

Abstract: The object of the present invention is the use of phosphonium salts in coupling reactions, and a method for their preparation.

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: Process for producing glycolic acid by contacting carbon monoxide and formaldehyde, optionally in the presence of a solvent, with a catalyst including a solid acid. The solid acid is an acidic polyoxometalate compound insoluble in formaldehyde, glycolic acid and the optional solvent, and has a concentration of acid sites of greater than 60 ?mol g?1 on the external surface and/or a Hammett Acidity value of less than ?12.8.