Abstract: Processes for preparing 3-substituted phenylalkylamines comprising reacting a phenyl boronic compound with an ?-? unsaturated carbonyl-containing compound via an asymmetric 1,4-addition reaction, followed by reductive alkylation. The processes may be useful in the synthesis of tapentadol.

Abstract: The present invention provides a one-pot method for synthesizing clomiphene (a mixture of the isomers cis-clomiphene and trans-clomiphene) utilizing a single solvent. In a preferred embodiment, the single solvent is dichloromethane (DCM, also known as methylene chloride). The present invention provides an improved method for synthesizing clomiphene and purifying clomiphene isomers.

Abstract: Different polymorphs of bromfenac sodium may be prepared and interconverted using crystallization/recrystallization, drying and/or hydration techniques.

Abstract: A stearoyl amino acid salt having a structural formula of the general formula (I), wherein R1 is H or an aromatic base capable of being substituted by one or more substituents, or a C1-4 straight chain or an alkyl with a branched chain, the substituent being an alcoholic hydroxyl group or a phenolic hydroxyl group; and R2 is a C11-25 saturated or unsaturated aliphatic group. Also provided are methods of preparing the stearoyl amino acid salt, and methods of using the stearoyl amino acid salt. Compared to a prototype drug stearoyl amino acid, the stearoyl amino acid salt described herein has excellent physicochemical properties, good stability, high relative bioavailability, a strong drug effect and a high safety factor. It is thus expected to become a candidate for clinical treatment of neurodegenerative diseases and acute brain injury, and a clinical drug for weight loss, thus having broad application prospects.

Abstract: The present invention relates to the production of acrolein, acrylic acid or methacrylic acid by dehydration reaction of renewable raw material such as glycerin or hydroxycarboxylic acids, in the presence of a novel catalyst system supported on a carrier having a bimodal structure and a high pore volume and distribution. The dehydration reactions can be carried out for longer operation duration, so that acrolein, acrylic acid or methacrylic acid can be produced at higher productivity and for longer running time.

Abstract: Disclosed herein are methods for recovering phosphorus-containing ligand from mixtures comprising organic mononitriles and organic dinitriles, using liquid-liquid extraction. Also disclosed are treatments to enhance extractability of the phosphorus-containing ligand.

Abstract: The present invention generally relates to compounds and methods for inhibiting the radical polymerization of unsaturated compounds, particularly vinyl monomers. More particularly, it relates to the use of stable hydroxyl amines to inhibit the polymerization of unsaturated compounds (e.g., vinyl monomers) wherein said stable hydroxylamine is soluble in organic solvents, particularly hydrocarbon solvents consisting of unsaturated and, therefore, polymerizable constituents.

Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.

Abstract: Pyridone derivatives, methods of preparing the pyridone derivatives, and methods of using the pyridone derivatives are provided. In particular, pyridone derivatives of formula (I), and pharmaceutical salts thereof are provided. The pyridone derivatives are useful as mitogen-activated protein kinase kinase (MEK) inhibitors, and can be used as therapeutic agents for treating cancer.

Abstract: The present invention relates to a novel process for preparing 3,5-bis(haloalkyl)pyrazole derivatives of the formula (Ia) and (Ib), via acylation of ketimines.

Abstract: The invention relates to the use of a group of sigma receptor ligands of formula (I) for the potentiation of the analgesic effect of opioids and opiates and at the same time for decreasing the dependency induced by them.

Abstract: The invention provides pyrazolyl guanidine compounds that inhibit F1F0-ATPase, and methods of using pyrazolyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.

Abstract: The present invention relates to a naphthylamide compound of the structure as represented by formula (I), medicinal salts, prodrugs and hydrates or solvates thereof, and also relates to a method of preparing the compounds, pharmaceutical compositions comprising the compounds and the uses thereof as protein tyrosine kinase inhibitors, particularly as VEGFR-2 inhibitors, in preparing drugs for preventing and treating diseases related to abnormal angiogenesis.

Abstract: Optionally substituted benzoimidazol-1,2-yl amides, such as compounds of Formula 1 or Formula 2, can be used to treat disorders associated with a Kv7 potassium channel activator. Compositions, medicaments, and dosage forms related to the treatment are also disclosed herein.

Abstract: The present invention includes novel compositions useful for preventing or treating an HIV-1 infection in a subject in need thereof. The present invention further includes a novel method of preventing or treating an HIV-1 infection in a subject in need thereof, the method comprising administering to the subject an effective amount of a compound of the invention. In one embodiment, the subject is further administered at least one additional therapeutic agent.

Abstract: Bicyclic arylcarboxamides of the general formula (I) are described as herbicides. In this formula (I), Z1, Z2, Z3, Z4 and Z5 are a bond, O, S(O)n or a substituted carbon atom. X is a radical such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is a substituted heterocycle.

Abstract: The invention relates to a compound of formula I, and a preparation method and use thereof. The compound has a bacterial quorum-sensing regulatory effect, and can be used for prevention and/or treatment of a disease caused by a bacterial infection.

Abstract: Compounds of general formula (I): wherein R1, R11, Y, R2, n and A are as defined herein are useful as inhibitors or metallo-?-lactamase (MBL) enzymes and can be used for reducing or removing antibiotic resistance in bacteria.

Abstract: The production of organic acids in low-cost, high-efficiency fermentation system makes available a new route to chemical production from biomass. A process for producing a hydrogenation product involving carboxylic acid esters recovered directly from a fermentation process is described.

Abstract: A process is disclosed for converting levulinic acid to gammavalerolactone with increased selectivity. The process is based on the recognition of the reaction intermediate, 4-hydroxyvaleric acid, and improved conversion thereof.

Abstract: The present invention provides a process for the production of furan, said process comprising the steps of: i) contacting furfural with a decarbonylation catalyst in a decarbonylation reactor to produce a gaseous decarbonylation reaction product stream comprising furan and carbon monoxide; ii) contacting said gaseous decarbonylation reaction product stream with a solvent stream comprising furfural; iii) absorbing at least a portion of the furan present in the gaseous decarbonylation reaction product stream into the solvent stream to provide a furan-containing solvent stream and a gaseous stream comprising carbon monoxide; iv) separating the furan from the furan containing solvent stream by distillation to provide a first furan stream; and v) using at least a portion of the remaining solvent stream comprising furfural as at least a portion of the furfural provided to the decarbonylation reactor.

Abstract: The present invention relates to a catalyst system for oxidation of o-xylene and/or naphthalene to phthalic anhydride (PA), comprising a plurality of catalyst zones arranged in succession in the reaction tube, which has been produced using antimony trioxide consisting predominantly of the senarmontite modification of which all primary crystallites have a size of less than 200 nm. The present invention further relates to a process for gas phase oxidation, in which a gas stream comprising at least one hydrocarbon and molecular oxygen is passed through a catalyst system which comprises a plurality of catalyst zones arranged in succession in the reaction tube and which has been produced using an antimony trioxide consisting predominantly of the senarmontite modification with a median primary crystallite size of less than 200 nm.

Abstract: The present invention provides compounds of formula (I) or a pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein W, X, n, s, t, and Ra are as described herein. The present invention relates generally to selective inhibitors of histone deacetylase and to methods of making and using them.

Abstract: An anhydrous crystalline form of S-equol has been discovered. Form I, the anhydrous crystalline form of S-equol has been isolated and characterized for the first time. As compared to other forms of S-equol, such as the known hydrate or other solvate forms, the anhydrous crystalline form of S-equol has improved properties.

Abstract: The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.

Abstract: The invention relates to crystalline forms of (S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone, processes for the preparation thereof, pharmaceutical compositions containing such crystalline forms, pharmaceutical compositions prepared from such crystalline forms, and their use as a medicament, especially as orexin receptor antagonists.

Abstract: The present invention relates to compounds of the formula (I) wherein Ar1 and Ar2 are as described in the description and to their use as pharmaceuticals for the treatment of sundown syndrome. The invention also relates to the preparation of such compounds and of pharmaceutically acceptable salts thereof.

Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy.

Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a [(1-Piperazinyl)-4-pyridinylmethyl]-Naphtho[1,2-b]furan structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.

Abstract: This invention relates to a kind of C- aryl glycoside derivatives, its pharmaceutical compositions, preparation methods, and uses thereof. The preparation method comprises: method 1: in a solvent, deprotecting the acetyl protecting groups of compound 1-f in the presence of a base; method 2: 1) compound 2-g reacts with via Mitsunobu reaction; 2) deprotecting the acetyl protecting groups of compound 2-f obtained from step 1; method 3: 1) compound 2-g reacts with via nucleophilic substitution reaction; 2) deprotecting the acetyl protecting groups of compound 3-f obtained from step 1. The pharmaceutical composition comprises a kind of C- aryl glycoside derivatives; it's pharmaceutically acceptable salts and/or prodrugs thereof and excipient thereof. This invention relates to a kind of C- aryl glycoside derivatives, it's pharmaceutically acceptable salts or compositions thereof for preparing a SGLT inhibitor. The C- aryl glycoside derivatives of this invention provides a new direction for SGLT inhibitors.

Abstract: The present invention relates to processes and intermediates for preparing compounds of formula (IA), wherein R1, R4, R5, R6, and L1 are as defined herein. Compounds of formula (IA) have been found useful as EP4 receptor agonists useful in the treatment of glaucoma, osteoporosis, neuropathic pain, and related disorders.

Abstract: Provided herein are 2-(2,4-difluorophenyl)-1,1-difluoro-1-(5-substituted-pyridin-2-yl)-3-(1H-tetrazol-1-yl)propan-2-ols and processes for their preparation.

Abstract: The present invention provides compounds of Formula (I) and pharmaceutical compositions comprising compounds of Formula I, and methods for using compounds of Formula I for treating or preventing thromboses, embolisms, hypercoaguability or fibrotic changes.

Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols A, X, Y, L1, L2, G, Q, p, R1, R2 and R10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).

Abstract: The invention relates to novel amides of acetic and propionic acids, methods for production and use thereof for the production of medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning ability and memory.

Abstract: The present application provides azaquinazoline compounds as defined herein. This application further describes compositions comprising the same. These azaquinazoline compounds and their salts have atypical protein kinase C (“aPKC”) inhibitory activity, and may be used to treat proliferative disorders.

Abstract: The invention is directed to pyrazolo[1,5-a]pyridine derivatives and their use as AXL and c-MET kinase inhibitors.

Abstract: The present invention relates to diazabicyclo[4.3.1]decane derivatives, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said diazabicyclo[4.3.1]decane derivatives can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.

Abstract: The instant invention describes biisoquinoline compounds having therapeutic activity, and methods of treating disorders such as cancer, tumors and cell proliferation related disorders, or affect cell differentiation, dedifferentiation or transdifferentiation.

Abstract: Propellant compositions containing cyclic nitramines that are susceptible to unintentional detonation are desensitized by the incorporation of a linear nitramine having a backbone containing one to three ethylene groups and one or two nitramine groups.

Abstract: The invention relates to new substituted heteroaryls of formula (1), wherein A is selected from the group consisting of N and CH, D is CH, E is selected from the group consisting of C and N, T is C, G is selected from the group consisting of C and N, and wherein each of the broken (dotted) double bonds in ring 1 are selected from either a single bond or a double bond under the proviso that all single and double bonds of ring 1 are arranged in such a way that they all form together with ring 2 an aromatic ring system, and wherein R1, M and R3 are defined according to claim 1, and to the above compounds for the treatment of a disease selected from the group consisting of asthma, COPD, allergic rhinitis, allergic dermatitis, lupus erythematodes, lupus nephritis and rheumatoid arthritis.

Abstract: The present invention is directed to substituted five membered heteroaryl benzamide compounds of formula (I) (Formula (I)) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.

Abstract: The present invention relates to a novel triazolopyrimidinone or triazolopyridinone derivative, a tautomer thereof, a stereoisomer thereof and their mixture, or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition for preventing or treating a tankyrase-related disease, which contains the same as an active ingredient.

Abstract: The invention relates to besylate salts of the compound of formula (I): Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.

Abstract: Compounds of Formula I, including their salts, as well as compositions and methods of using the compounds are set forth. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.

Abstract: Novel tetrahydroisoquinoline derivative compounds are disclosed herein that may be used as an active ingredient for a pharmaceutical composition, and in particular, for a pharmaceutical composition useful for preventing or treating a disease or condition responsive to modulation of the contractility of the skeletal sarcomere. This may be accomplished, for example, by modulation of the troponin complex of the fast skeletal muscle sarcomere through one or more of fast skeletal myosin, actin, tropomyosin, troponin C, troponin I, and troponin T, and fragments and isoforms thereof. The tetrahydroisoquinoline derivative compounds can thus be used as an agent for preventing or treating 1) neuromuscular disorders, 2) disorders of voluntary muscle, 3) CNS disorders in which muscle weakness, atrophy, and fatigue are prominent symptoms, 4) muscle symptoms stemming from systemic disorders, and 5) dysfunctions of pelvic floor and urethral/anal sphincter muscle.

Abstract: The present invention relates compounds comprising a tetra-heteroaryl indacenodithiophene-based structural unit, the synthesis of such compounds as well as their use in organic electronic devices. The invention further relates to organic electronic devices comprising such compounds.

Abstract: Provided herein is a method for preparing a silver complex. The method includes reacting a silver oxide with a mixture of ammonium carbamate and isopropyl amine at room temperature in the presence of methanol.

Abstract: Carbamatoorganosilanes are produced in exceptionally high yield with a high degree of purity, by reacting an aminoorganosilane with a dialkylcarbonate in the presence of a basic catalyst, wherein a first reaction period proceeds at a temperature in the range of 35-65° C., followed by a later reaction period at a temperature at least 10° C. higher. A low level of catalyst allows its removal by simple exit filtration, without a separate filtration step.