Abstract: The present invention relates to the synthesis of a novel compound, in which liquid hydrazine and the derivatives thereof react with excess carbon dioxide to enable the carbon dioxide to chemically bond to the hydrazine and the derivatives thereof. To this end, high-pressure carbon dioxide is used to synthesize hydrazine and the derivatives thereof to which the carbon dioxide is bonded in a pure form with no water and no by-product. Furthermore, the present invention provides a method for utilizing the above-described compounds by reacting the compounds with carbonyl compounds.

Abstract: Provided is a sulfonium salt manufacturing method which can reduce the production of a monosulfonium salt. A method of manufacturing a sulfonium salt includes preparing a first sulfonium salt containing a sulfonium cation and a first anion, preparing a second sulfonium salt by exchanging the first anion for a halide ion, and preparing a third sulfonium salt by exchanging the halide ion for a second anion.

Abstract: This invention relates to the use of bis- and tris-dihydroxyaryl compounds as well as sulfonamides, heteroaryls, tricycloalkyl and their analogs and pharmaceutically acceptable salts, for modulating tau aggregation and alleviating tauopathies, such as Alzheimer's disease (AD), Pick's disease (PiD), progressive supranuclear palsy (PSP), corticobasal degeneration (CBD) and familial frontotemporal dementia/Parkinsonism linked to chromosome 17 (FTDP-17), amyotrophic lateral sclerosis/Parkinsonism-dementia complex, argyrophilic grain dementia, dementia pugilistic, diffuse neurofibrillary tangles with calcification, progressive subcortical gliosis and tangle only dementia.

Abstract: This disclosure relates to inhibitors of the Wni pathway, and compositions comprising the same, as well as to their use in the treatment of disorders characterized by the activation of Writ pathway signaling (e.g., cancer), as well as to the modulation of cellular events mediated by VVnt pathway signaling.

Abstract: The present invention discloses polythiol compositions containing sulfur-containing compounds with carbamate groups, and to methods for producing such polythiol compositions. These polythiol compositions can be synthesized via the reaction of an isocyanate with an allyl ether alcohol, followed by thiolation with H2S, and these polythiol compositions are often used in formulations for adhesives, paints, and coatings.

Abstract: Compounds of the invention, which may be useful in inhibiting thrombin and associated thrombotic occlusions, have the following structure: or a pharmaceutically acceptable salt thereof, wherein m is 0 or 1; R is a heterocycle, —(CR8R9)1-2NH2, or —(CR8R9)1-2OH, wherein R8and R9, each time in which they occur, are independently H, C1-6alkyl, —CH2F, —CHF2, CF3or —CH2OH; W is a) —CHR1R2, where R1is —C(CH3)3, and R2is —(CH2)1-2OH, b) a 5- or 6-membered unsubstituted or substituted heterocycle having 1 or 2 heteroatoms selected from N and O, wherein substituted heterocycle is substituted with R3, c) a 9- or 10-membered unsubstituted or substituted heterocycle having 1 or 2 heteroatoms selected from N, O and S, wherein substituted heterocycle is mono-substituted with R3, or disubstituted with R3and R4, or d) a 3-, 4-, or 5-membered carbocyclic ring which is unsubstituted, mono-substituted with R3, di-substituted with R3and R4, or tri-substituted with R3, R4and R5; R3is —CF3, —COOH, —COOR7, —C(O)R6, —CH(OH)R6,

Abstract: Provided are methods for the preparation of certain substituted pyrrolidine compounds, forms of (2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid hydrochloride, and methods for preparing and using these forms.

Abstract: Novel methods for the production of enantiomerically pure (EP) ?-lactams by decomposition of ?-diazo-?-ketoamides.

Abstract: The present invention relates to the use of substituted dihydroimidazolones, particularly [1-(4-Chlorophenyl)-4-(4-morpholinyl)-2,5-dihydro-1H-imidazol-2-one] (AWD 131-138) or a physiologically acceptable salt thereof for the treatment of epilepsy in dogs.

Abstract: A polyether compound containing oxirane monomer units in an average number per molecule of 10 to 100, wherein the polyether compound contains repeating units which are represented by the general formula (2) as at least part of the oxirane monomer units is provided. According to the present invention, it is possible to provide a polymer material which has suitable fluidity and is excellent in ion conductivity. (R1 to R4 respectively independently indicate a hydrogen atom or C1 to C3 alkyl group, and R2 and R3 may be bonded with each other. Further, X? is an anion which is comprised of 2 to 25 atoms.

Abstract: The present invention relates to stable novel salt forms of N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide that are suitable for the preparation of pharmaceutical formulations thereof, and their therapeutic use.

Abstract: The present invention relates to the field of organic synthesis and describes the synthesis of specific triazolopyrimidine compounds and intermediates thereof as well as related derivatives.

Abstract: The invention provides certain quinoxalines and aza-quinoxalines of the Formula (I), and their pharmaceutically acceptable salts, wherein J1, J2, R1, R2, R3, R22, Ra, Rb, Rc, Rd, X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.

Abstract: The present invention provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.

Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”).

Abstract: The present invention relates to new thiadiazolidinediones of formula (I), or any pharmaceutically acceptable salt, solvate or prodrug thereof, and its use in the treatment of a disease in which glycogen synthase kinase 3 (GSK-3) is involved, particularly neurodegenerative diseases, inflammatory and autoimmune diseases and cardiovascular disorders. Additionally, there is provided a process for preparing such compounds, as well as pharmaceutical compositions comprising them.

Abstract: Provided is a two-step method of producing a compound of chemical formula 1 in the presence of an alcohol solvent and a Group 3B metal catalyst or a salt thereof, comprising a first step comprising alkylation or isomerization of an aldohexose-containing substrate to obtain an intermediate, and a second step comprising dehydration of the intermediate to produce a compound of chemical formula 1. Preferably, additional solvent and/or catalyst are not added in the second step.

Abstract: The present invention concerns a process to obtain primary, secondary or tertiary amines, via a direct amination reaction of alcohols in presence of bis(perfluoroalkylsulfonimide) acid or salts thereof catalysts, and derivatives.

Abstract: A method for producing a multisubstituted biphenyl compound is represented by the following formula (2), including a step of coupling a substituted benzene compound represented by the following formula (1) in the presence of a solid catalyst with gold immobilized onto a support.

Abstract: A process for manufacturing tetrahydrofuran, tetrahydropyran and, more generally, cycloether derivatives through the cyclodehydration of 1,4- or 1,5-diols. More specifically, the process of the invention involves (i) the stereoselective cyclodehydration in water of 1,4- or 1,5-diols including at least one chiral tertiary alcohol functional group with retention of the initial chirality, and/or (ii) the cyclodehydration in water of 1,4- or 1,5-diols, said diols being non-miscible with and/or non-soluble in water, into corresponding cycloether derivatives, by bringing the reaction mixture to high temperature water (HTW) conditions and/or by mixing the aqueous reaction mixture with a solid catalyst, such as for example a smectite clay. Also, the use of the process for manufacturing ambrafuran, especially (?)-ambrafuran and other cycloether derivatives.

Abstract: An object of the present invention is to provide an optically active bicyclic ?-amino acid derivative in a high purity.

Abstract: A process for producing cyclic acetals is described. A formaldehyde source is contacted with an aprotic compound in the presence of a catalyst to produce the cyclic acetals. The aprotic compound can increase conversion rates and/or efficiency. In one embodiment, the formaldehyde source is obtained from methanol. In particular, methanol can be converted into formaldehyde which is then converted into a cyclic acetal. In one embodiment, the cyclic acetal can then be used to produce oxymethylene polymers.

Abstract: The invention relates to compounds and methods of treatment relating to nicotinic receptor antagonists. For example, the compounds and methods of treatment function block the activity of certain acetylcholine receptors and subtypes therein, and are useful treating diseases and conditions mediated by nicotinic receptor stimulation, e.g., small cell lung cancer.

Abstract: The invention provides new methods for the direct umpolung self-condensation of 5-hydroxymethylfurfural (HMF) by organocatalysis, thereby upgrading the readily available substrate into 5,5?-di(hydroxymethyl)furoin (DHMF). While many efficient catalyst systems have been developed for conversion of plant biomass resources into HMF, the invention now provides methods to convert such nonfood biomass directly into DHMF by a simple process as described herein. The invention also provides highly effective new methods for upgrading other biomass furaldehydes and related compound to liquid fuels. The methods include the organocatalytic self-condensation (umpolung) of biomass furaldehydes into (C8-C12)furoin intermediates, followed by hydrogenation, etherification or esterification into oxygenated biodiesel, or hydrodeoxygenation by metal-acid tandem catalysis into premium hydrocarbon fuels.

Abstract: This invention is directed to a compound of formula (I): wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related macular degeneration (AMD).

Abstract: Provided herein are improved, commercially viable and consistently reproducible processes for the preparation of highly pure crystal Modification I of Rivaroxaban, which is free from other polymorphs and undesired solvated forms. Provided also herein is a highly pure and stable crystal Modification I of Rivaroxaban essentially free of other solid state forms.

Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.

Abstract: The present invention relates to a composition comprising N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethylene-butyl]-(1?R,2?S,3?R,4?S)-2,3-bicyclo[2,2,1]heptanedicarboximide or a pharmaceutically acceptable acid addition salt thereof. In detail, the composition relates to a sustained release formulation for injection which maintains an effective blood level of the above-mentioned compound.

Abstract: The present invention relates to compounds of general formula (I), wherein R1, LP, LQ, (Het)Ar, m and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR1 19 receptor and modulate its activity.

Abstract: A TARP ?8 dependant AMPA receptor antagonist of the formula: wherein X is CH or N; A is and R1 is as defined herein; its pharmaceutically acceptable salts, uses, and methods for its preparation are described.

Abstract: The present invention relates to processes for the enantio-selective preparation of spyrrolidine derivatives useful in the manufacture of pesticidally active compounds, as well as to intermediates in the processes. The processes include those comprising (a-i) reacting a compound of formula Ia wherein P is alkyl, aryl or heteroaryl, each optionally substituted, wherein the heteroaryl is connected at P via a ring carbon atom; R1 is chlorodifluoromethyl or trifluoromethyl; R2 is aryl or heteroaryl, each optionally substituted; with a source of cyanide in the presence a chiral catalyst to give a compound of formula IIa wherein P, R1 and R2 are as defined for the compound of formula Ia; and (a-ii) oxidizing the compound of formula IIa with a peroxy acid, or peroxide in the presence of an acid to give a compound of formula VI wherein R1 and R2 are as defined for the compound of formula Ia.

Abstract: Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein R1, R2, RE, L, M and Z are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract: Methods of preparing substantially pure SNS-595 substance are disclosed. Also provided are compositions comprising SNS-595 substance that are substantially pure and essentially free of visible particles.

Abstract: The present invention provides a compound having a PDE2A selective inhibitory action, which is useful as an agent for the prophylaxis or treatment of schizophrenia, Alzheimer's disease and the like. The present invention is a compound represented by the formula (1): wherein each symbol is as described in the specification, or a salt thereof.

Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.

Abstract: The present invention relates to naphthylurea derivatives. Such substances can significantly inhibit VEGFR2 and PDGFR-? receptor tyrosine kinase phosphorylation at nanomolar concentration levels. It is a novel type of tyrosine kinase inhibitors which can be used in the treatment of tyrosine kinase-mediated diseases or symptoms such as malignancies and ocular diseases accompanied with pathologic neovascularization.

Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.

Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Compounds of formula (F) are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

Abstract: Polymorphs of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one, compositions thereof, methods for their preparation, and methods for their use are disclosed.

Abstract: This application discloses compounds according to generic Formula (I) wherein all variables are defined as described herein, which inhibit BTK. The compounds disclosed herein are useful to modulate the activity of BTK and treat diseases associated with excessive BTK activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.

Abstract: The invention provides a class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria.

Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.

Abstract: The present invention relates to acid addition salt and salt crystals of (6aR,9aS)-5,6a,7,8,9,9a-hexahydro-5-methyl-3-(phenylamino)-2-((4-(6-fluoropyridin-2-yl)phenyl)methyl)-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one, composition comprising the same and the method of making and using such salt and crystal.

Abstract: Provided are methods for reversing the effects of agents used for muscular immobilization and/or loss of consciousness and/or loss of pain perception. The method comprises administering a composition comprising acyclic CB[n]-type compounds to an individual in need of reversal of the effects of neuromuscular blocking agents and/or anesthetic agents such that the effects of the agent(s) are partially fully reversed.

Abstract: Synthetic voacangine, including in substantially enantiomerically enriched forms, and derivatives thereof are provided.

Abstract: The present disclosure provides derivatives of melampomagnolide B (MMB), including carbonates, carbamates, and thiocarbamates. The derivatives may be synthesized via an MMB triazole intermediate. These derivatives are useful for treating cancer in humans.

Abstract: The invention includes halichondrin B analogs having pharmaceutical activity; in some cases, crystalline forms thereof, and in some cases, halichondrin B analogs having a further utility as synthetic intermediates.

Abstract: The present invention provides thieno[2,3-c]pyrrol-4-one compounds that inhibit activity of extracellular-signal-regulated kinase (ERK) and may be useful in the treatment of cancer.

Abstract: A pharmaceutical composition for preventing or treating a degenerative brain disease, and a method of screening a material for preventing or treating a degenerative brain disease. The method may effectively screen a prophylactic or therapeutic candidate material for preventing or treating a degenerative brain disease. A variety of degenerative brain diseases may be effectively prevented or treated using the pharmaceutical composition including a screened material for preventing or treating a degenerative brain disease.