Abstract: A pyridine compound having a SF5 group on position-3 and position-4 of a pyridine ring is provided.

Abstract: The present invention is related to crystalline forms of 2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1-yl)-4-(o-tolyl)pyridin-3-yl)propanamide which is an NK-1 antagonist useful in the treatment of induced vomiting and other disorders.

Abstract: Production of pitavastatin calcium safely on an industrial scale with a high yield and high selectivity at low cost. A method of producing pitavastatin calcium including step (i) for acetalizing a compound represented by the formula (1) to give a compound represented by the formula (3), step (ii) for reacting a compound represented by the formula (3) with an acid to give a compound represented by the formula (4), and step (iii) for hydrolyzing a compound represented by the formula (4) and reacting same with a calcium compound.

Abstract: The present invention discloses a salt derivative of 1-(3-methanesulfonamidobenzyl)-6-methoxy-7-benzyloxy-1,2,3,4-tetrahydroisoquinoline. The salt derivative has a solubility in water of not less than 3.0 nmol/mL or 1.8 mg/mL. The salt derivative has a solubility in water of not less than 3.0 nmol/mL or 1.8 mg/mL.

Abstract: The invention relates to a new and improved method for preparation of (4S)-4-[4-cyano-2-(methyl sulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydro pyrimidine-5-carbonitrile of formula (I), as well as the preparation and use of the crystal form (A) of (4S)-4-[4-cyano-2-(methylsulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydro pyrimidine-5-carbonitrile of formula (I).

Abstract: Provided are novel salts and polymorphs of 5-(2,4-diamino-pyrimidin-5-yloxy)-4-isopropyl-2-methoxy-benzenesulfonamide, which are potentially useful for modulating a condition mediated by a P2X3 or P2X2/3 receptor. Also provided are pharmaceutical formulations and methods of administration and dosing of these salts and polymorphs to subjects in need thereof.

Abstract: A new azido compound, 5-amino-6-chloro-2,4-diazido-pyrimidine, and a process for synthesizing. The synthesis may include reacting 5-amino-2,4,6-trichloropyrimidine and sodium azide. There is an excess molar amount of sodium azide for each chloro fractional molar amount on the 5-amino-2,4,6-trichloropyrimidine. The synthesis is a two phase reaction that is a dispersion. The 5-amino-2,4,6-trichloropyrimidine dissolved in acetone is a liquid phase, and the sodium azide is insoluble in acetone and is a solid phase, that is present in excess of chemical equivalents. The reaction product is soluble in acetone, and the reaction by-product, sodium chloride is also insoluble in acetone, and the crude yield is about 92%. Unreacted sodium azide and formed sodium chloride are removed by filtration.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R12, R13, R14, A1, A2, A3, n and m are as described herein.

Abstract: The present invention provides a benzotriazole derivative compound represented by a general formula, (wherein R3 represents an alkyl group, and R4 represents an acryloyloxyalkyl group or a methacryloyloxyalkyl group), as a novel compound capable of being suitably used as a highly light-resistant ultraviolet absorber or resin composition that exhibits an ultraviolet-blocking function over a prolonged period of time and that strongly absorbs wavelengths in the ultraviolet light range of 400 nm or less while ensuring little coloration.

Abstract: The invention relates to a novel method for producing polyisocyanurates comprising isocyanate groups, based on 2,4- and 2,6-toluylene diisocyanate (TDI) and to the use thereof in coating compositions.

Abstract: Compounds of Formula I: wherein: R1 and R1? are independently selected from hydrogen, halogen, C1-to-C12 linear or branched hydroxyalkyl, C1-to-C12 linear or branched halo-alkyl, carboxy, carboxyalkyl, amido, N-alkylamido, N,N-dialkylamido, carbamoyloxy, N-alkylcarbamoyloxy, and N,N-dialkylcarbamoyloxy, provided that that R1 and R1? are not simultaneously hydrogen; R2 and R2? hydrogen, halogen, C1-to-C12 linear or branched hydroxyalkyl, C1-to-C12 linear or branched halo-alkyl, carboxy, carboxyalkyl, amido, N-alkylamido, N,N-dialkylamido, carbamoyloxy, N-alkylcarbamoyloxy, and N,N-dialkylcarbamoyloxy, provided that that R2 and R2? are not simultaneously hydrogen; R3 is selected from hydrogen, C1 to C12 linear or branched alkyl, and nitrogen protecting groups; X is oxygen or nitrogen; when X is oxygen, R4 is absent; and when X is nitrogen, R4 is selected from H, C1-to-C12 linear or branched alkyl, and nitrogen protecting groups.

Abstract: In a process for the epoxidation of an olefin with hydrogen peroxide in the presence of a solvent, where a mixture comprising olefin, an aqueous hydrogen peroxide solution and a solvent is continuously passed through a fixed bed of an epoxidation catalyst comprising a titanium zeolite, addition of a chelating agent to the aqueous hydrogen peroxide solution before mixing it with solvent reduces or prevents formation of deposits on the catalyst and blocking of orifices of a liquid distributor.

Abstract: Disclosed is a process for purifying propylene oxide. A stream S0 containing propylene oxide, acetonitrile, water, and an organic compound containing one or more of acetone and propionaldehyde is provided. Propylene oxide is separated from S0 by subjecting S0 to distillation in a first distillation unit, obtaining a gaseous top stream S1c enriched in propylene oxide, a liquid bottom stream S1a enriched in acetonitrile and water, and a side stream S1b containing propylene oxide and enriched in the carbonyl compound; reacting the carbonyl compound in S1b with an organic compound containing an amino group to obtain a reaction product; separating propylene oxide from the reaction product in a second distillation unit, obtaining a gaseous top stream S3a enriched in propylene oxide and a liquid bottoms stream S3b enriched in the reaction product; and introducing stream S3a into the first distillation unit.

Abstract: The present invention relates to compounds for prophylaxis or treatment of organ damage by restoring endothelial function and/or inhibiting reactive oxygen species production and especially to compounds for prophylaxis or treatment of diabetic kidney damage. Specifically, the present invention relates to 6-hydroxy-2,5,7,8-tetramethylchroman-2-yl)(piperazin-1-yl)methanone or N,6-dihydroxy-2,5,7,8-tetramethylchroman-2-carboxamide or a pharmaceutically acceptable salt or base thereof for use in the prophylaxis or treatment of organ damage by restoring endothelial function and/or inhibiting reactive oxygen species production and especially diabetic kidney organ damage.

Abstract: A process to decarboxylate THCA in cannabis material while minimizing the thermal decomposition of THC and the loss of volatile components such as terpenoids consists of four steps. Prepared cannabis material is first heated to about 105° C. for 20 min. to complete the dehydration of the material. The processing temperature is then increased to about 110° C. for about 30 min. to start the decarboxylation process. Thereafter, the temperature is increased to about 115° C. for about 35 min. Finally, the temperature is increased by about 2.5° C. (but not exceeding 118° C.) for about an additional 15 min. to complete the decarboxylation.

Abstract: A process produces a (meth)acrylate ester mixture. The process includes reacting a glycerol formal isomer mixture with an alkyl (meth)acrylate in the presence of a catalyst.

Abstract: Embodiments of the invention include methods of treating, preventing, and/or reduce the risk or severity of a condition selected from the group consisting of muscle wasting, muscle weakness, cachexia, and a combination thereof in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction in the risk of muscle wasting. In at least particular cases, the small molecules are inhibitors of STAT3.

Abstract: The present invention provides a genus of polycyclic amines that are useful as opioid receptor modulators. The compounds of the invention are useful in both therapeutic and diagnostic methods, including for treating pain, neurological disorders, cardiac disorders, bowel disorders, drug and alcohol addiction, drug overdose, urinary disorders, respiratory disorders, sexual dysfunction, psoriasis, graft rejection or cancer.

Abstract: The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

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: A compound of formula I wherein A, X, Y, Z, R1 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.

Abstract: The present invention relates to N-((3S,4R)-1-((8-chloroquinoxalin-6-yl)carbonyl)-3-(4-fluorophenyl)piperidin-4-yl)-1-methyl-5-(trifluoromethyl)-1H-pyrazole-3-carboxamide, which is a compound that can be useful for the treatment or prevention of SPT-related diseases including congenital diseases associated with the storage of sphingolipids, such as cancer and Niemann-Pick disease, or a salt thereof.

Abstract: A compound represented by general formula (I) has a strong Axl inhibitory activity by introducing a distinctive bicyclic structure in which a saturated carbon ring is fused to a pyridone ring, and can be a therapeutic agent for Axl-related diseases, for example, cancer such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glioma, kidney diseases, immune system diseases, and circulatory system diseases

Abstract: There are provided a novel isocyanurate compound having a glycidyl group as a substituent to be bonded to a nitrogen atom. A monoglycidyl isocyanurate compound of the following Formula (1), (2), or (3). (wherein two R1s are each a C2-10 alkyl group, two R2s are each a C1-5 alkylene group, two R3s are each a C1-2 alkyl group, two R4s are each a C1-2 alkylene group, and two R5s are each a C1-2 alkyl group).

Abstract: Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity.

Abstract: Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, and 7-aza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.

Abstract: The present invention relates to a crystalline hydrate of the compound (2S,3R)-isopropyl 2-(((2-(1,5-dimethyl-6-oxo-1,6-dihydropyridin-3-yl)-1-((tetrahydro-2H-pyran-4-yl)methyl)-1H-benzo[d]imidazol-5-yl)methyl)amino)-3-hydroxybutanoate edisylate and to its use in the treatment of various disorders for which a BET inhibitor is indicated, in particular inflammatory and autoimmune diseases, and cancers. Processes for the manufacture of this crystalline form and pharmaceutical compositions comprising the crystalline form are also disclosed and form part of the present invention.

Abstract: Among the various aspects of the present disclosure is the provision of a compositions for binding sphingosine-1-phosphate receptor 1 (S1P1), imaging of S1P1, and methods of use thereof. Provided are imaging agents for imaging S1P1 and S1P1 associated diseases, disorders, and conditions. Also provided are therapeutic compositions and methods for the treatment of S1P1 associated diseases, disorders, and conditions.

Abstract: Disclosed are novel N-(3-heteroarylaryl)-4-arylarylcarboxamides and analogs thereof, represented by the Formula I: wherein C cyclic group, D1-D4, Q1, Q2, R5 are defined herein. Compounds having Formula (I) are hedgehog pathway inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of hedgehog activity, such as cancer.

Abstract: Compounds are provided that antagonize the kappa-opioid receptor (KOR) and products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof: wherein X, Y, R1, R2, R4, R5 R6, R7, R8 and R11 are as defined herein.

Abstract: The present invention relates generally to therapeutics targeting the bacterium Porphyromonas gingivalis, including its protease Lysine gingipain (Kgp), and their use for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, as described herein, and pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein A, L, D, R1-R15, w, x, y, and z are defined herein. The novel cycloalkyl-linked diheterocycle derivatives that are useful in the treatment of abnormal cell growth, such as cancer, in mammals. The present invention also relates to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.

Abstract: The invention relates to crystalline salts of a compound having the structure of formula (I), methods for their preparation, and related pharmaceutical compositions comprising the crystalline salt. The invention further relates to methods of treating or preventing cancer or an immunological or neurological disease comprising administering a crystalline salt of the invention.

Abstract: Disclosed are chemical entities which are inhibitors of spleen tyrosine kinase (SYK), namely, chemical entities comprising 6-((1R,2S)-2-aminocyclohexylamino)-7-fluoro-4-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[3,4-c]pyridine-3(2H)-one and certain solid state forms thereof. Also disclosed are methods of using the chemical entities to treat disorders such as a cancer.

Abstract: Disclosed is a series of compounds acting as CDK4/6 inhibitors. Specifically disclosed are compounds as represented by formula (I), pharmaceutically acceptable salts or isomers thereof, pharmaceutical compositions containing same, and the use thereof in the preparation of drugs for treating cancers.

Abstract: Provided herein are compounds useful for improving mRNA splicing in a cell. Exemplary compounds provided herein are useful for improving mRNA splicing in genes comprising at least one exon ending in the nucleotide sequence CAA. Methods for preparing the compounds and methods of treating diseases of the central nervous system are also provided.

Abstract: Purine scaffold Hsp90 inhibitors are useful in therapeutic applications and as radioimaging ligands.

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 factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Abstract: The present invention relates to a 7-(thiazol-5-yl)pyrrolopyrimidine compound as a TLR7 agonist, and particularly relates to a compound shown in formula (I), pharmaceutically acceptable salt and preparation method thereof, a pharmaceutical composition containing such a compound, and usage thereof in preparing an antiviral drug.

Abstract: A compound of Formula (IA), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein A, R3, R4, R6, and R7 are as defined herein.

Abstract: Methods of inhibiting the growth or metastasis of a cancer in a subject by inhibiting a Ral GTPase in the subject, and small molecule inhibitors of Ral GTPases useful in the methods of the invention. Pharmaceutical compositions containing the compounds of the invention, and methods of using the same.

Abstract: The invention relates to methods and intermediates useful in the synthesis of eribulin.

Abstract: The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.

Abstract: A method of treating a patient having cancer is provided comprising administering a therapeutically effective amount of a tricyclic compound or a pharmaceutically acceptable salt of the tricyclic compound to a patient. A method of inhibiting the mitosis of a cancerous cell is also provided.

Abstract: The invention provides compositions, methods, and kits for the treatment of acute myeloid leukemia in a subject.

Abstract: The present disclosure provides for compounds of formula (I) wherein A2, A3, A4, A6, A7, A8, A15, RA, R5, R9, R10A, R10B, R11, R12, R13, R14, R16, W, X, and Y 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, including cancer. Also provided are pharmaceutical compositions comprising compounds of formula (I).

Abstract: The present invention relates to macrocyclic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of RIP2 and/or mutants thereof, for use in the diagnosis, prevention and/or treatment of RIP2-kinase associated diseases. Moreover, the present invention provides methods of using said compounds, for instance as a medicine or diagnostic agent.

Abstract: The present invention describes new compounds that are useful for image-guided surgery and photodynamic therapy. In particular the compounds may be targeted to the nucleus or the mitochondria after compounds were delivered to diseased tissues such as cancer using a ligand that target receptor that express on the diseased tissue and followed by receptor mediated endocytosis and provide effective activity against cancer cells as well as other disorders. Methods and compositions for use of the same are described.

Abstract: A supramolecular metal-organic framework material is a reaction product of a copper compound, a trialkylamine represented by Chemical Formula 1, and benzene substituted with 3 or more carboxyl groups.