Abstract: Disclosed are methods of extracting and purifying capsinoids (e.g., capsiate, dihydrocapsiate) from Capsicum species fruit involving drying (e.g., freeze drying) the fruit to produce dried fruit and grinding the dried fruit to produce powdered fruit, extracting the powdered fruit at least once with a non-polar organic solvent (e.g., pentane, hexane, heptane, iso-octane, cyclohexane) to produce an organic solvent extract, subjecting the organic solvent extract at least once to liquid/liquid extraction (partitioning; no drying involved) using a polar solvent (e.g., acetonitrile, methanol) to form a capsinoid enriched polar solvent partition, and optionally purifying the capsinoid enriched polar solvent partition (e.g., via HPLC using acetonitrile as a carrier) to yield capsinoids. The non-polar organic solvent is not miscible with the polar solvent.

Abstract: A process for producing a polyetheramine by reacting a polyether alcohol, previously synthesized in the presence of a basic potassium or sodium compound as catalyst, with ammonia in the presence of hydrogen and a catalyst in one reactor or a plurality of reactors, wherein the employed polyether alcohol when previously synthesized in the presence of a basic potassium compound as catalyst has a content of potassium ions of less than 50 wppm and when previously synthesized in the presence of a basic sodium compound as catalyst has a content of sodium ions of less than 50 wppm.

Abstract: Disclosed is a process for preparing ?-agonist, 1-(4-amino-3,5-dichlorophenyl)-2-(tert-butylamino) ethanol, of Formula I. The process comprises refluxing 1-(4-amino-3,5-dichlorophenyl) ethanone of Formula II and selenium dioxide in the presence of 1,4-dioxane to form compound of Formula III. Further, compound of Formula III is heated at a temperature below 30° C. in the presence of t-butyl amine to form compound of Formula IV. The compound of Formula IV is treated with sodium borohydride to form compound of Formula I.

Abstract: Disclosed in the present disclosure is a Dezocine analog, and particularly disclosed are compounds represented by formula (I), (II) and (III), a pharmaceutically acceptable salt or tautomer thereof.

Abstract: This invention relates to etheramines based on dialcohols, wherein the etheramines comprise at least three linear or branched C4-alkylene groups and a process for the manufacture of these etheramines.

Abstract: The present invention relates to an improved process for the synthesis of (R)-Lacosamide in which free base of O-methyl-N-benzyl-D-Serinamide is not isolated before acylation. The process avoids the use of column chromatography and chiral resolution for the preparation of different stages of Lacosamide.

Abstract: Provided is a highly potent and selective endocannabioid cellular reuptake inhibitor represented by formula (I): or a pharmaceutically acceptable solvate or co-crystal thereof as well as to a formulation comprising this inhibitor, and to methods of treatment in which this inhibitor is used.

Abstract: The present description provides oligourea catalysts, a polar helical oligomeric strands, and methods for catalyzing reactions with polar helical oligomeric strands and oligourea catalysts. In particular, the invention relates to a polar helical oligomeric strand of at least 4 residues selected from the formula (I) and which can be used as a catalyst.

Abstract: Process for converting a carboxamide to a thiocarboxamide includes reacting (a) a substrate that comprises a heteroatom-containing moiety and a carboxamide moiety with (b) a dialkyl dithiophosphate and/or a salt thereof. The heteroatom-containing moiety includes a heteroatom selected from the group consisting of N, O, and S. Processes for preparing piperidine-4-thiocarboxamide are described.

Abstract: Provided is a photochemical reaction device wherein two partitions formed from an optically transparent material are arranged apart from each other between a light source and a reaction liquid, and an optically transparent fluid introduction/discharge means for introducing an optically transparent fluid between the partitions and discharging the fluid and a state change detection means for detecting a change in the state of the optically transparent fluid at the discharge side of the optically transparent fluid introduction/discharge means are provided. Also provided are a photochemical reaction method that uses the photochemical reaction device and a lactam production method that uses the photochemical reaction method. The present invention prevents decreases in the performance of the light source even when the optically transparent material in the photochemical reaction device is damaged, and makes it possible to reliably prevent ignition even if the reaction liquid is a flammable liquid.

Abstract: Provided herein are pyrrolomycin derivatives, which can be used to modulate Mcl-1, inhibit proliferation of bacteria and pathogens, as well as to treat infectious diseases and cancers.

Abstract: A compound of formula (I) or a compound of formula (II) or pharmaceutically acceptable salts thereof, wherein R1-R7 and X are as defined in the description, and the use of these compounds in therapy, in particular in treating cancer or as an inhibitor of the interaction of the MDM2 protein with p53.

Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.

Abstract: The present invention provides a method of treating one or more sodium channel related diseases or disorders in an individual, including related symptoms. The method comprises administering to the individual a tetrahydropyridine derivative in an amount effective to treat sodium channel related diseases or disorders in individuals. These compounds are generally categorized as Ritalin related compounds. The present invention also provides compounds for use in the treatment of and also for use in the manufacture of a medicament for the treatment of sodium channel related diseases or disorders in an individual. A method is further provided for the preparation and isolation of the derivatives of the compound of the present invention.

Abstract: Dynamic nuclear polarization (DNP) agents are provided for DNP nuclear magnetic resonance of analytes. The DNP agents can have the structure A-X-L-R, where A is none or an amphiphilic group; X is a coupling group capable of site-specific binding with the analyte or, when A is an amphiphilic group, capable of site-specific binding with the amphiphilic group; L is a bond or a linker group; and R is a poly-radical group. The poly-radical can be a di-radical, a tri-radical, a tetra-radical, or a combination thereof. Methods of NMR measurement of an analyte comprising an NMR-detectable nucleus are provided. The methods can include the steps of providing a frozen sample containing the analyte and a DNP agent; applying radiation having a frequency that excites electron spin transitions in the DNP agent at an intensity to polarize the NMR-detectable nucleus; and detecting a signal from nuclear spin transitions in the NMR-detectable nucleus.

Abstract: The present invention relates to a novel catalytic hydrogenation of substituted 2-methyl cyanopyridyl derivatives, in particular 3-chloro-5-(trifluoromethyl)pyridin-2-yl]acetonitrile [=Py-CN] to substituted 2-ethylaminopyridine derivatives, in particular 2-[3-chloro-5-(trifluoromethyl)pyridin-2-yl]ethanamine [=Py-ethanamine] or salts thereof in the presence of metal catalysts, in particular palladium catalysts.

Abstract: The invention relates to substituted oxopyridine derivatives of formula (I) and to processes for preparation thereof, and also to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.

Abstract: The present invention provides freebase and salt forms, and compositions and methods thereof, useful for treating various conditions, in which aldehyde toxicity is implicated in the pathogenesis, by the administration of small molecule therapeutics acting as a scavenger for toxic aldehydes.

Abstract: The present invention relates to a process for preparing a pyrazole compound of formula V, the process including cyclizing a hydrazone substituted ?,?-unsaturated carbonyl compound of formula IV by reacting it with a suitable reagent, e.g. a reducing agent, an organometallic reagent or a nucleophilic reagent. The compounds of formula V are versatile reaction tools for the preparation of pyrazole derived fine chemicals. The present invention also relates to pyrazole compounds of formulae Va, Vb, Vc, and VI.

Abstract: The present invention relates to benzimidazol-2-amines of general formula (I) in which R1, R2, R3, R4, R5, R6 and R7 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.

Abstract: The present teachings relate to hydroxypyrimidinone derivatives of Formula IV, pharmaceutical compositions thereof, and methods of using such compounds to treat bacterial infections.

Abstract: Disclosed is a method of preparing ezetimibe, including cross-metathesis using a Grubbs 2nd catalyst and deprotection using a Pearlman's catalyst, and an intermediate thereof. The method of preparing ezetimibe is useful as an efficient ezetimibe synthesis technique in pharmaceutical fields using ezetimibe as a raw material.

Abstract: A process for the synthesis of quinazolinone containing compounds which may be useful for the treatment of cancer, is hereby disclosed. In addition, compound intermediates relating to these processes are also disclosed.

Abstract: The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.

Abstract: The invention relates to compounds of formula (I): wherein R1, R2, R3, R4, R5 and R6 are as defined in the description. The compounds of formula (I) are inhibitors of the YAP/TAZ-TEAD interaction.

Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.

Abstract: The present invention relates to an amorphous vortioxetine and salts thereof. In particular, the invention relates to a process for the preparation of an amorphous vortioxetine hydrobromide. Further, the invention also relates to a process for preparation of amorphous vortioxetine free base. The invention also relates to pharmaceutical compositions comprising an amorphous vortioxetine or hydrobromide salt thereof for oral administration for treatment of major depressive disorder (MDD) and generalized anxiety disorder (GAD).

Abstract: Provided herein are methods of producing dialkylfurans, such as 2,5-dimethylfuran, and other alkyl furans, such as 2-methylfuran. For example, 2,5-dimethylfuran may be produced by reducing (5-methylfuran-2-yl)methanol or 2-(chloromethyl)-5-methylfuran.

Abstract: The present invention relates to polymerizable compounds, to processes and intermediates for the preparation thereof, and to the use thereof for optical, electro-optical and electronic purposes, in particular in liquid-crystal (LC) media and LC displays, especially in LC displays of the PS (“polymer sustained”) or PSA (“polymer sustained alignment”) type.

Abstract: Provided are a 4-sulfur pentafluoride phenol compound and a preparation method therefor, and a preparation method for a sulfur pentafluoride substituted benzopyran compound. According to the present invention, sulfur pentafluoride salicylaldehyde with multiple substituent groups is synthesized through a plurality of steps by using sulfur pentafluoride phenol as a raw material, and then the sulfur pentafluoride substituted benzopyran compound is synthesized on this basis. The method is simple and convenient, and low in cost; overcomes the defects that, at present, the number of types of sulfur pentafluoride phenols is small, and the synthesis of various sulfur pentafluoride substituted benzopyran compounds cannot be met; and has wide industrial application prospects.

Abstract: The present invention relates to compounds of general formula (I) wherein R1-R8 take various meanings, pharmaceutical compositions containing them and their use in medicine, particularly for the treatment and/or prophylaxis of cancer.

Abstract: A method and an intermediate for preparing a tulathromycin. The method includes the following step: in an organic solvent, subjecting a compound represented by formula (II) and an n-propylamine to a ring-opening addition shown below to obtain a tulathromycin represented by formula (I), wherein the organic solvent is a 1,2-propandiol. Tulathromycin obtained using the method has a high purity, with an HPLC purity being 95% and above, and up to 99% and above, satisfying a required purity for preparing a tulathromycin as a pharmaceutical formulation. The method has a high yield, is simple to operate, and is more suitable for industrial production.

Abstract: Compounds of general formula (Ia), compounds of general formula (Ia?), compounds of general formula (Ib), compounds of general formula (Ib?), compounds of general formula (I), compounds of general formula (I?), and their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, R6, R8, R9, X1, X2, and X3 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds of the disclosure.

Abstract: This invention relates to a crystalline form of 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate, and to pharmaceutical compositions thereof, to intermediates and methods for the production and isolation of such crystalline forms and compositions, and to methods of using such crystalline forms and compositions in the treatment of abnormal cell growth in mammals, especially humans.

Abstract: A process for preparing 3-[(S)-7-bromo-2-((2-oxo propyl)amino)-5-pyridin-2-yl-3H-1,4,-benzodiazepin-3-yl]propionic acid methyl ester (compound (FK)), at a high conversion rate with good reproducibility by oxidizing 3-[(S)-7-bromo-2-(2-hydroxypropylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3yl]propionic acid methyl ester (compound (EM)), in the presence of an oxidation catalyst is provided by defining the ammonium ion content of the oxidation reaction mixture.

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.

Abstract: The present invention relates to polymorphic forms of compound 1 or 1a and processes for preparing compound 1 and 1a polymorphs, which are useful as antifungal agents. In particular, the invention seeks to provide a new methodology for preparing polymorphs of compound 1 and substituted derivatives thereof.

Abstract: The application relates to an inhibitor of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation disorders and cancers, having the Formula (I-13):

Abstract: Disclosed embodiments concern novel interleukin receptor associated kinases (IRAK) inhibitors and compositions comprising such inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compositions may be used to treat or prevent an IRAK-associated disease or condition.

Abstract: Compounds of formula (I) wherein Ra, Rb, Rc, Rd, T, R3, R4, R5, X, Y and Het are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.

Abstract: The present disclosure provides a compound of Formula (I?): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein R1, R2, Rx, X1, n, n1, and q are as defined herein, and methods of making and using same.

Abstract: Disclosed are a 2-(2,4,5-substituted aniline) pyrimidine derivative, a pharmaceutical composition and a use thereof. The pharmaceutical composition comprises a therapeutically effective amount of the 2-(2,4,5-substituted aniline) pyrimidine derivative, a solvate, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient. Also disclosed is a use of the 2-(2,4,5-substituted aniline) pyrimidine derivative, a solvate, or a pharmaceutically acceptable salt thereof in the preparation of drugs for treating cancers. The compounds of the present invention have a relatively high solubility in water and a relatively high permeability, and/or a relatively low binding ability to plasma proteins, and at the same time have a relatively low toxicity characteristic and a relatively high anti-tumor activity.

Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R1, R2a, R2b, R2c, R3a, R3b, R4a, R4b, R5a, R5b, R6, A, G1, G2, L1, L2, m1, m2, n, X and E are as defined herein and, wherein at least one of R3a, R3b, R4a or R4b is not H. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

Abstract: Compounds and embodiments of a method for treating and/or preventing autoimmune diseases are disclosed. The method includes administering to a subject having an autoimmune disease, such as an inflammatory bowel disease, a therapeutically effective amount of a compound according to formula I wherein X and Y independently are O or NR1; each R1 is independently H or C1-C6 alkyl; ring A is aryl; each R2 independently is H, alkyl, alkoxy, amide, cyano, halo, haloalkyl, hydroxyalkyl, heteroalkyl, heterocyclyl, sulfonyl, sulfonamide, or two R2 groups, taken together with the atom or atoms to which they are attached, combine to form a 4-10 membered ring system; p is 0, 1, 2, 3, or 4; R3 and R4 independently are H or C1-C6 alkyl; and R5 is halo, cyano, or C1-C6 alkyl.

Abstract: Series of 2-phenyl-4-methylthiazole analogs are disclosed as potential therapeutic agents for the treatment of bacterial infections, especially methicillin-resistant Straphylococcus aureus (MRSA) related infections. A method for the treatment of MRSA-related infections is also claimed.

Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.

Abstract: The present invention provides a compound having a lysine-specific demethylase-1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for schizophrenia, developmental disorders, particularly diseases having intellectual disability (e.g., autistic spectrum disorders, Rett syndrome, Down's syndrome, Kabuki syndrome, fragile X syndrome, Kleefstra syndrome, neurofibromatosis type 1, Noonan syndrome, tuberous sclerosis), neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, spinocerebellar degeneration (e.g., dentatorubural pallidoluysian atrophy) and Huntington's disease), epilepsy (e.g., Dravet syndrome) or drug dependence, and the like. A compound represented by the formula wherein each symbol is as defined in the present specification, or a salt thereof.

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 a compound of formula (I) and/or a salt thereof, wherein R1, G, and X are as defined herein. A compound of formula (I) and/or its salts have aPKC inhibitory activity, and may be used to treat proliferative disorders. Compositions comprising a compound of Formula (I) and/or a salt thereof are also provided.

Abstract: The present invention relates to a process for the preparation substantially pure propane-1-sulfonicacid-{3-[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide or Vemurafenib of Formula (I).