Abstract: The present invention relates to new methods of manufacturing benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), and intermediates thereof.

Abstract: Provided are compounds and compositions thereof that are useful as antioxidants in personal care formulations. The compounds are of the Formula I: wherein R1, R2, R3, R4, and R5 are independently H, —OH, C1-C6 alkoxy, —COOH, —COO?M+ or —O31 M+ where M+ is a sodium, potassium, or ammonium ion, wherein at least two of R1, R2, R3, R4, or R5 are —OH, and R6, R7, R8, R9, and R10, are independently H, —OH, C1-C6 alkoxy, —COOH, —COO?M+ or —O31 M+ where M+ is a sodium, potassium, or ammonium ion, or a substituent of Formula II: wherein R11, R12, R13, R14,and R15are independently H, —OH, C1-C6 alkoxy, —COOH, —COO?M+ or —O31 M+ where M+ is a sodium, potassium, or ammonium ion, provided that one of R6, R7, R8, R9, and R10 is a substituent of Formula II.

Abstract: The present invention pertains to the field of pharmaceutical chemicals, and relates to a substituted acethydrazide derivative, preparation method and use thereof; preferably, relates to a compound of Formula I or a pharmaceutically acceptable salt thereof. The compound of the present invention or a pharmaceutically acceptable salt thereof can effectively inhibit proline hydroxylase, stabilize HIF-?, particularly HIF-1?, and has potency in the manufacture of a medicament for treatment and/or prophylaxis and/or adjuvant therapy of anemia, acute ischemic reperfusion injury.

Abstract: The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.

Abstract: Provided herein is technology relating to imaging agents and particularly, but not exclusively, to methods of manufacturing fluorine-18-labeled phenethylguanidines and uses thereof.

Abstract: The invention provides benzenesulfonamido and related compounds, pharmaceutical compositions, methods of promoting ROR? activity, increasing the amount of IL-17 in a subject, and treating cancer using such benzenesulfonamido and related compounds.

Abstract: A family of covalent kinetic stabilizer compounds that selectively and covalently react with the prominent plasma protein transthyretin in preference to more than 4000 other human plasma proteins is disclosed. A contemplated compound corresponds in structure to Formula I, below, where the various substituents are defined within, and reacts chemoselectively with one or two of four Lys-15 ?-amino groups within the transthyretin tetramer. The crystal structure confirms the binding orientation of the compound substructure and the conjugating amide bond. A covalent transthyretin kinetic stabilizer exhibits superior amyloid inhibition potency, compared to a non-covalent counterpart, and inhibits cytotoxicity associated with amyloidogenesis.

Abstract: What is described is a compound of formula I wherein X is an ethene, or an unsubstituted or substituted arene or heteroarene; Y is a bond, an ethene, or an unsubstituted or substituted arene or heteroarene; Z is S or O; L is a linear or branched alkylene of 1 to 6 carbons; R1 and R2 are independently a linear or branched alkyl or alkenyl of 1 to 18 carbons; R3 and R4 are independently a linear or branched alkyl of 1 to 6 carbons; n is 0 to 6; and m, p, q, and r are independently 1-18; or a pharmaceutically acceptable salt thereof.

Abstract: The invention provides compounds having the general Formula (I); and pharmaceutically acceptable salts thereof; wherein the variables RA, RAA, subscript n, subscript q, ring A, X2, L, subscript m, X1, R1, R2, R3, R4, R5, D and E have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

Abstract: Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.

Abstract: Described are deuterium-substituted tetrahydrocarbazole compounds of Formulae I, II, or III which are inhibitors of sirtuin 1 (SIRT1). Also described are pharmaceutical compositions comprising the deuterium-substituted tetrahydrocarbazole compounds, and methods of use thereof.

Abstract: Described herein are modified sugar, iminosugar and azasugar compounds and methods of making same. One or more of these modified compounds contain sulfates, sulfites, sulfamates and/or sulfonamides. Also described are pharmaceutical compositions/formulations comprising these compounds, as well as methods using these modified sugar compounds for the treatment of MPS IIIC (also known as Sanfilippo Type C).

Abstract: Disclosed are a method for preparing a dabigatran etexilate intermediate, and an intermediate compound. The method for preparing a dabigatran etexilate intermediate 4 comprises; reacting a compound 3 with a C1-C3 alkyl alcohol solution of methylamine in an organic solvent, wherein, X=chlorine, bromine, or iodine. Also disclosed are an intermediate compound 3 and a preparation method thereof. The method for preparing a dabigatran etexilate intermediate of the present invention has the advantages of simple process, easy operation, high yield, and easy purification, thus being suitable for industrial production.

Abstract: The present disclosure relates to crystalline solid forms of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, the process of preparing the forms, and pharmaceutical compositions and methods of use thereof.

Abstract: A process for preparing (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide or (R)-(?)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide, by reduction of oxcarbazepine in the presence of a catalyst and a hydride source is disclosed. The catalyst is prepared from a combination of [RuX2(L)]2 wherein X is chlorine, bromine or iodine, and L is an aryl or aryl-aliphatic ligand, with a ligand of formula (A) or formula (B): wherein R1 is chosen from C1-6 alkoxy and C1-6 alkyl, n is a number from 0 to 5, and when n is a number from 2 to 5, R1 can be the same or different, and R2 is alkyl, substituted alkyl, aryl, substituted aryl, alkaryl or substituted alkaryl. The hydride source is either NR3R4R5 and formic acid, [R3R4R5NH][OOCH] and optionally formic acid, or [M][OOCH]x and formic acid, wherein R3, R4 and R5 are C1-6 alkyl, M is an alkali metal or alkaline earth metal and x is 1 or 2. A pH from 6.5 to 8 is maintained during the process.

Abstract: Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of one or more of MAGL, ABHD6, and FAAH. Furthermore, the subject compounds and compositions are useful for the treatment of, for example, pain, solid tumors and/or obesity.

Abstract: The present application relates to an improved process for preparation of Enzalutamide (I). The present application also relates to an improved process for the preparation of substantially pure Enzalutamide (I) having purity of greater than 99.5%. The present application also relates to a novel process for the preparation of Enzalutamide intermediate useful in the industrially viable synthesis of Enzalutamide.

Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein A, R1 R5 and R6 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.

Abstract: Methods for preparing compounds having the following structure (I): or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, wherein R1, R2a, R2b, R3a, R3b, R4a, R4b and R4c, are as defined herein are provided. Related compounds and methods for making the same are also provided.

Abstract: The present invention relates to oxopiperazines that mimic helix ?B of the C-terminal transactivation domain of HIF1?. Also disclosed are pharmaceutical compositions containing these oxopiperazines and methods of using these oxopiperazines (e.g., to reduce gene transcription, treat or prevent disorders mediated by interaction of HIF1a with CREB-binding protein and/or p300, reduce or prevent angiogenesis in a tissue, induce apoptosis, and decrease cell survival and/or proliferation).

Abstract: Synthesis of novel and unique PAMAM (poly-amidoamine) polymers. PAMAM polymers can be grown by systematic alternation between ethylenediamine (EDA) and methacrylate. By taking advantage of the alternating terminal ends, successive generations G1 and G0.5 were combined under acidic conditions with Pluronic P123 as a liquid-crystal template. The resulting polymer was imaged with TEM and the product was circular and amorphous of no characteristic size ranging between about 5 nm to about 600 nm, with remarkable electrochemical activity unseen in any of the generations of PAMAM. Applications of this electroactive poly-amidoamine organic polymer include use as a new electron transfer reagent for amperometric biosensors.

Abstract: Compounds and pharmaceutical compositions that down-regulate immune checkpoints such as PD-1, PD-L1 and CTLA-4 are provided. Also provided are methods of treating a disease by down-regulating immune checkpoints such as PD-1, PD-L1 and CTLA-4. The methods are useful for treating cancer and viral infection in a subject.

Abstract: The present disclosure provides substituted isoxazole carboxamide compounds having Formula (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, A, X, and Z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.

Abstract: The invention provides ?-amino esters of a hydroxypropylthiazolidine carboxamide derivative, (2S)-3-([1,1?-biphenyl]-4-ylsulfonyl)-N-[(1S)-3-hydroxy-1-phenylpropyl]-1,3-thiazolidine-2-carboxamide, as well as salts and crystal polymorph s thereof, that can be used to inhibit prostaglandin F receptor. The invention further encompasses methods of treating disorders such as pre-term labor at the early gestational stage by the administration of these substances to a patient in need of treatment.

Abstract: The invention relates to compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (TRPM8), and having formula (I). Said compounds are useful in the treatment of diseases associated with activity of TRPM8 such as pain, inflammation, ischaemia, neurodegeneration, stroke, psychiatric disorders, itch, irritable bowel diseases, cold induced and/or exacerbated respiratory disorders and urological disorders.

Abstract: Provided is a method for producing a polymerizable compound represented by a formula (I) comprising: a step (1) that reacts a compound represented by a formula (II) with 2,5-dihydroxybenzaldehyde in an organic solvent in the presence of a base to obtain a reaction mixture including a compound represented by a formula (III); and a step (2) that adds a compound represented by a formula (IV) and an acidic aqueous solution to the reaction mixture obtained by the step (1) to effect a reaction, wherein A represents a hydrogen atom, a methyl group or the like, L represents a leaving group, n represents an integer from 1 to 20, X represents an oxygen atom, a sulfur atom, —C(R1)(R2)— or the like, R represents a hydrogen atom, an organic group or the like, and each of RX represents a hydrogen atom, a halogen atom or the like. According to the present invention, provided is a method for producing a polymerizable compound represented by a formula (I) at high purity and at high yield.

Abstract: The present disclosure relates to cyclopropyl compounds of general formula (I), wherein R1, and R2 are as defined in the specification. The present application also relates to pharmaceutical compositions containing such compounds and to their use in therapy.

Abstract: The invention relates to 1-(3-sulfonylphenyl)-3-(cyclopent-2-en-1-yl)urea derivatives, and their use in treating or preventing diseases and conditions mediated by the CXCR2 receptor In addition, the invention relates to compositions containing the derivatives and processes for their preparation

Abstract: In some variations, the invention provides a process for producing furfural, 5-hydroxymethylfurfural, and/or levulinic acid from cellulosic biomass, comprising: fractionating the feedstock in the presence of a solvent for lignin, sulfur dioxide, and water, to produce a liquor containing hemicellulose, cellulose-rich solids, and lignin; hydrolyzing the hemicellulose contained in the liquor, to produce hemicellulosic monomers; dehydrating the hemicellulose to convert at least a portion of C5 hemicelluloses to furfural and to convert at least a portion of C6 hemicelluloses to 5-hydroxymethylfurfural; converting at least some of the 5-hydroxymethylfurfural to levulinic acid and formic acid; and recovering at least one of the furfural, the 5-hydroxymethylfurfural, or the levulinic acid. Other embodiments provide a process for dehydrating hemicellulose to convert oligomeric C5 hemicelluloses to furfural and to convert oligomeric C6 hemicelluloses to 5-hydroxymethylfurfural.

Abstract: A process for preparing a batch of highly purified, pharmaceutical grade tasimelteon comprises analyzing a batch of tasimelteon synthesized under GMP conditions for the presence of one or more identified impurities.

Abstract: The present invention relates to a preparation method for a chiral intermediate for use in statins, acquired with chloroacetic acid and benzyl alcohol as starting materials via a series of reactions, namely etherification, condensation, substitution, and asymmetric reduction. The preparation method provided in the present invention has a novel route of synthesis, allows an intermediate compound to be introduced conveniently into the chiral center of a glycol via enzyme reduction, and not only is low in costs, but also is reliable in quality. The route of synthesis provided in the present invention uses raw materials of low costs, has an easy to operate process, and provides a final product of great purity and high yield.

Abstract: The invention provides compounds, compositions, and methods for the treatment of diseases, disorders, or conditions that are modulated by matrix metalloproteinases (MMPs). The compounds can be selective MMP inhibitors, for example, selective inhibitors of MMP-2, MMP-9, and/or MMP-14. The disease, disorder, or condition can include, for example, stroke, neurological disorders, ophthalmological disorders, or wounds, such as chronic wounds or diabetic wounds.

Abstract: The problem addressed by the present invention is to provide a novel method for separating and purifying pure enantiomer of lenalidomide. Pure enantiomer of lenalidomide can be separated and purified by using, as the mobile phase, an organic solvent selected from the group consisting of aprotic solvents, secondary alcohols, and mixtures thereof.

Abstract: The present invention is directed to novel compounds of formula (I), pharmaceutically acceptable salts or solvates thereof, and their use.

Abstract: Disclosed are novel crystalline salts of (S)-6-((1-acetylpiperidin-4-yl)amino)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)pyrimidine-4-carboxamide and pharmaceutical compositions containing the same. Also disclosed are processes for the preparation thereof and methods for use thereof.

Abstract: The present disclosure provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that modulate the activity of phosphoinositide 3-kinases-gamma (PI3K?) and are useful in the treatment of diseases related to the activity of PI3K? including, for example, autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.

Abstract: A new process for the preparation of 5-fluoro-1H-pyrazoles of the general formula (I) as described herein and further reactions with this compound.

Abstract: The invention relates to a compound of the 5-acylsulfanyl-histidine type and the derivatives thereof, of general formula (I), wherein R1 to R3=H, alkyl, especially CH3; R4=H, alkyl, especially CH3, alkyle(C?O), substituted alkyl (C?O), aryl (C?O); ?-alanyl (H2NCH2CH2 (C?O); ?-amino-acyl; R5=alkyl, especially methyl, phenyl. The invention also relates to the use of said compound for producing compounds of the 5-sulfanyl-histidine type and the derivatives thereof, in addition to corresponding disulfides; and to the various methods for the production thereof.

Abstract: The present disclosure relates to: (a) mandelate salts of atrasentan, (b) pharmaceutical compositions comprising an atrasentan mandelate salt, and, optionally, one or more additional therapeutic agents; (b) methods of using an atrasentan mandelate salt to treat nephropathy, chronic kidney disease, and/or other conditions; (c) kits comprising a first pharmaceutical composition comprising an atrasentan mandelate salt, and, optionally, a second pharmaceutical composition comprising one or more additional therapeutic agents; (d) methods for the preparation of an atrasentan mandelate salt; and (e) atrasentan mandelate salts prepared by such method.

Abstract: The invention provides for compounds of formula (I) wherein R1, X, Y, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, m, and R? have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sjögren's syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

Abstract: Provided is a pyridine derivative represented by formula (I), a prodrug thereof, a pharmaceutically acceptable salt of the pyridine derivative or the prodrug, or a solvate of the pyridine derivative, the prodrug or the pharmaceutically acceptable salt, which is useful for treatment or prophylaxis of diseases associated with URAT1 such as gout, hyperuricemia, hypertension, kidney diseases such as interstitial nephritis, diabetes, arteriosclerosis and Lesch-Nyhan syndrome.

Abstract: There is provided a novel agent for controlling harmful arthropods or nematodes that are parasites and hygienic pests for animals. An ecto- or endo-parasiticide for mammals or the like comprising as active ingredient, one or more selected from substituted benzamide compounds of formula (1) or salts thereof: wherein A1 is C—X3 or nitrogen atom, etc., A2 and A3 are C—H, etc., A4 is C—H or nitrogen atom, etc., G is G-2a, etc., W is oxygen atom or sulfur atom, X1 is halogen atom, trifluoromethyl, etc., X2 is hydrogen atom, halogen atom, trifluoromethyl, etc., X3 is hydrogen atom, halogen atom, etc., Y1 is hydrogen atom, halogen atom, methyl, etc., R1 is trifluoromethyl, etc., R2 is E-3a, etc., R3 is hydrogen atom, etc., p is an integer of 0 to 2.

Abstract: Provided is a diaryl-azole compound represented by formula (1) wherein R1-3 are C1-6 chain hydrocarbon, etc.; p=0-3; q=0-4; n=0-2; X is N, CH, etc.; Ar is phenyl, or 5-6-member aromatic heterocyclic ring; G is C1-6 chain hydrocarbon, etc.; and Het is a group selected from formulas (H1) (H2) (H3) described in the specification. The diaryl-azole compound of formula (1) has an excellent controlling effect against arthropod pests. Also provided are a control agent having an excellent controlling effect against arthropod pests, and a method for controlling arthropod pests in which the control agent is used.

Abstract: The present invention relates to a novel pyrrolidine compound having melanocortin receptor agonist activity or a pharmaceutically acceptable salt thereof, and to pharmaceutical applications thereof. The present invention relates to a pyrrolidine derivative represented by formula [I], wherein ring A represents an optionally substituted aryl group or the like; R1 represents an optionally substituted alkyl group or the like; R2 represents a halogen atom or the like; and R3 is an alkyl group substituted with an optionally substituted aryl group or the like, and R4 is a hydrogen atom or the like; or R3 and R4 are terminally attached to each other, and together with the nitrogen atom to which they are attached, form an optionally substituted nitrogen-containing aliphatic heterocyclic ring that may partially contain a double bond; or to a pharmaceutically acceptable salt thereof.

Abstract: The present disclosure relates generally, but not exclusively, to compounds and their use as enzyme interacting agents, in particular, agents which interact with one or more enzymes in the sphingolipid biosynthesis pathway. The disclosure further relates to the use of such compounds as research tools, use in therapy, to compositions and agents comprising said compounds, and to methods of treatment using said compounds.

Abstract: Provided is a compound which is useful as a prophylactic or therapeutic agent for various diseases in which T-type calcium channels are involved, such as hypertension, arrhythmia, pain and cancers, the compound having antagonistic activity against T-type calcium channels, being highly stable in the body and having low risk of, for example, genotoxicity. Disclosed is a compound represented by the following general formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein R1 represents —NH(C?O)—V—R3 or —(C?O)NH—V—R3; V represents a single bond, methylene, or —C(CH3)2O—; R2 represents a optionally substituted C1-6 alkyl group; X represents a hydrogen atom, an oxygen atom, a hydroxyl group, a methyl group, or a methylene group; A represents —NR6—, —O—CH2—, or —S—CH2—; n represents the number of methylene chains and represents an integer of 0, 1 or 2; and a doublet containing a dotted line represents a single bond or a double bond.

Abstract: Compounds are provided herein which are emetine derivatives that can be used as prodrugs which selectively undergo activation to release emetine in specific cellular conditions. In one aspect, a blocking group is incorporated onto the emetine molecule by the derivization of the N2?-position with moieties that can be selectively removed by hydrolysis in the cancer/tumor microenvironment. Such compounds are less cytotoxic than emetine and are substantially inactive in non-cancerous cells. In one aspect, the compounds described herein can be used for the treatment of metastatic and non-metastatic cancers, including, for example, breast cancer, prostate cancer, lung cancer, and leukemia.

Abstract: The present invention relates to Fused Tricyclic Heterocyclic Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocyclic Compound, and methods of using the Fused Tricyclic Heterocyclic Compounds for treating or preventing HIV infection in a subject.

Abstract: In one aspect, the invention provides compounds of Formula I: (I) and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, Y, Za are defined as set forth in the disclosure. The invention also provides compounds of any one of Formulae II to VII, IA to IC, and IIA to IIC, and pharmaceutically acceptable salts and solvates thereof. Other aspects of the invention include the use of compounds of Formulae I to VII, IA to IC, and IIA to IIC, and pharmaceutically acceptable salts and solvates thereof for the treatment of disorders responsive to modulation of one or more opioid receptors. In certain embodiments, the Compounds of the Invention are useful for treating pain.

Abstract: The invention provides novel compounds, composition comprising said compounds and methods for inhibiting CK1 as well as methods of treating CK1 related disorders such as Alzheimer's disease comprising administering a therapeutically effective amount of a CK1 inhibitor to a patient in need thereof.