Abstract: Provided are isocitrate dehydrogenase 2 (IDH2) inhibitor compounds useful for treating cancer and methods of treating cancer, comprising administering to a subject in need thereof a compound described herein. Also provided are polymorphic forms of the IDH2 inhibitor compounds characterized by X Ray powder diffraction patterns, having improved physicochemical properties that influence in vivo dissolution rate for formulation purposes.

Abstract: Provided herein are antagonists of prostaglandin EP3 receptor, processes to make said antagonists, and methods comprising administering said antagonists to a mammal in need thereof.

Abstract: The present invention relates to “a method for synthesizing 2,6-bis[3?-(N-carbazolyl)phenyl]pyridine compound”, and belongs to the field of chemical synthesis. In the present invention, a pyridine ring is formed by cyclization, the intermediate product can be directly used in the next reaction without purification and thus the process is very easy; the final product I will precipitate from the mixed reaction solution after the completion of the reaction, and the product can be very conveniently extracted.

Abstract: In one aspect, the invention relates to substituted 1H-benzo[d][1,2,3]triazol-1-ol analgoues, derivatives thereof, and related compound; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders, e.g. various tumors and cancers, associated with ?-catenin/Tcf protein-protein interaction dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: Provided herein is a bridged bring compound of formula (I) or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating treat hepatitis C virus C(HCV) infection or hepatitis C disease. Furthermore provided herein are pharmaceutical compositions containing the compounds and the method of using the compounds or pharmaceutical compositions thereof in the treatment of HCV infection or hepatitis C.

Abstract: There are disclosed compounds that are inhibitors of EZH2, pharmaceutical compositions containing said compounds and methods of treating hyperproliferative, inflammatory, infectious, and immunoregulatory disorders and diseases, utilizing the compounds of the invention.

Abstract: The invention relates to the compounds of formula I and formula IA or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I and formula IA; and methods for treating or preventing neurological diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of epilepsy, bipolar disorder, trigeminal neuralgia, attention-deficit hyperactivity disorder (ADHD), schizophrenia, neuropathic pain, seizures, bipolar disorder, mania, phantom limb syndrome, complex regional pain syndrome, paroxysmal extreme pain disorder, neuromyotonia, intermittent explosive disorder, borderline personality disorder, Myotonia congenita and post-traumatic stress disorder.

Abstract: A compound of formula Ia: The present invention relates to novel indazolyl derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments.

Abstract: The invention relates generally to muscarinic agonists, which are useful for stimulating muscarine receptors, and treating cognitive disorders. Included among the muscarinic agonists disclosed herein are oxadiazole derivatives, compositions, and preparations thereof. Methods of synthesizing oxadiazole compounds also are provided. This disclosure also relates in part to compositions for enhancing cognitive function in subjects such as humans, the compositions comprising a muscarinic agonist or a pharmaceutically suitable form thereof. This disclosure relates in part to methods of treating animals such as humans by administering such compositions.

Abstract: Provided are: a heterocyclic amide compound represented by formula (1); and a herbicide containing the heterocyclic amide compound. In the formula, G represents a group represented by formula (G-1) or (G-2); each of W and W1 independently represents an oxygen atom or the like; each of Z1 and Za1 represents a phenyl group or the like; Z2 represents an aromatic heterocycle; each of R1 and R2 independently represents a C1-C6 alkyl group or the like; R3 represents a hydrogen atom, a C1-C6 alkyl group or the like; and each of R4, Ra4, R5, Ra5, R6, Ra6 and R7 independently represents a hydrogen atom or the like.

Abstract: The present invention relates to certain heteroaryl amide compounds, pharmaceutical compositions containing them, and methods of using them, including methods for preventing, reversing, slowing, or inhibiting protein aggregation, and methods of treating diseases that are associated with protein aggregation, including neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, Lewy body disease, Parkinson's disease with dementia, fronto-temporal dementia, Huntington's Disease, amyotrophic lateral sclerosis, and multiple system atrophy, and cancer and melanoma.

Abstract: The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation.

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrrolopyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. 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: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

Abstract: The present invention provides pyrroloquinoline quinone lithium salt crystal and a preparation method and application thereof. Characteristic absorption peaks appear when the diffraction angles are 6.222±0.2°, 7.379±0.2°, 7.941±0.2°, 23.631±0.2°, 24.044±0.2°, 25.497±0.2°, 27.541±0.2°, 30.736±0.2°, and 32.306±0.2° degrees in a powder X-ray diffraction pattern of the pyrroloquinoline quinine lithium salt crystal. The maximum value of thermal absorption of the pyrroloquinoline quinine lithium salt crystal appears between 90° C. and 96° C. through differential scanning calorimetry. Peaks appear when infrared spectroscopy of the pyrroloquinoline quinine lithium salt crystal is at 3396.03 cm?1, 1652.70 cm?1, 1604.48 cm?1, 1500.35 cm?1, 1355.71 cm?1, 1243.86 cm?1, 1147.44 cm?1, 808.03 cm?1, 761.74 cm?1, and 570.83 cm?1. The pyrroloquinoline quinine lithium salt polymorphism can be applied to preparation of medicines for curing memory damage.

Abstract: The invention relates to the use of substituted benzamide derivatives of Formula I: Wherein: A1 and A2 are —N or —CH, so that if A1 is —N, then A2 is —CH and If A2 is —N, then A1 is —CH; R is a hydrogen atom, or represents branched or unbranched —(C1-C3)-alkyl, —(C1-C3)-alkyl, wherein one, two or three hydrogen atoms may be substituted by a halogen or hydroxyl, —(C1-C3)—O—(C1-C3), —(C1-C3)—O—(C1-C3), wherein one, two or three hydrogen atoms may be substituted by a halogen, or R is a group wherein R3 and R4 both together or independently are halogen, hydroxyl, —(C1-C3)alkyl, wherein one, two or three hydrogen atoms may be substituted by a halogen or hydroxyl, —O—(C1-C3)-alkyl, —O—(C1-C3)-alkyl, wherein one, two or three hydrogen atoms may be substituted by a halogen, —O—(C1-C3)—O—(C1-C3), —O—(C1-C3)—O—(C1-C3), wherein one, two or three hydrogen atoms may be substituted by a halogen; R1 and R2 both together or independently are halogen, hydroxyl, —(C1-C3)-alkyl, —(C1-C3C)-alkyl, wherein one, two or three hydrog

Abstract: The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein A, B, W, X and Y are as defined herein.

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds modulate the mGluR2 receptor and may be useful for the treatment of various disorders of the central nervous system.

Abstract: Described herein are substituted indazoles that may selectively bind to Hsp90, methods of using the compounds, and kits including the compounds. The compounds may include detection moieties such as fluorophores that may allow for selective detection of Hsp90 in a sample.

Abstract: Substituted isoquinolinone compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.

Abstract: The present invention provides crystalline forms, solvates and hydrates of 4-amino-2-butoxy-8-(3-(pyrrolidin-1-ylmethyl)benzyl)-7,8-dihydropteridin-6(5H)-one, and methods of making.

Abstract: The present invention provides methods for the synthesis of polycyclic guanidine compounds. In certain embodiments, provided methods include the step of contacting a described reagent with a triamine compound to provide a polycyclic guanidine compound.

Abstract: The present invention relates to pyridine, pyrimidine, and pyrazine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.

Abstract: Certain tetrahydro-pyrimidoazepine compounds are described, which are useful as TRPV1 modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by TRPV1. Thus, the compounds may be administered to treat, e.g., pain, itch, cough, asthma, or inflammatory bowel disease.

Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.

Abstract: Provided herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, R1, R1a, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is a 6-membered monocyclic heteroaryl ring system of Formula (II) wherein L2, R13, G8, G10, G11, and G12 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.

Abstract: The invention concerns novel substituted spiro urea azetidinyl or piperidinyl compounds of formula (I) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns the preparation of such novel compounds, compositions comprising these compounds, and the compounds for use in the treatment of respiratory syncytial virus infection.

Abstract: The disclosure provides compounds of formula I or II, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

Abstract: The problem of the present invention is to provide a production method for safely synthesizing a nitrogen-containing heterocyclic N-oxide compound in high yield. Another problem of the present invention is to provide a novel N-oxide compound. There is provided a method for producing a nitrogen-containing heterocyclic N-oxide compound of Formula (2), such as 2,2,7,9-tetramethyl-2H-pyrano[2,3-g]quinoline N-oxide, by oxidizing a nitrogen-containing heterocyclic compound of Formula (1), such as 2,2,7,9-tetramethyl-2H-pyrano[2,3-g]quinoline with a persulfate.

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: Compounds represented by formulae (I) to (XXII) or pharmaceutically acceptable salts thereof:

Abstract: The invention relates to compounds of general formula (I) wherein X is C?O or SO2, M is NR2 or O, and Q1 and Q2 are nitroxide-containing radicals, and their use as a Dynamic Nuclear Polarization (DNP) agent for polarizing an NMR-active spin of a nucleus of an analyte in Nuclear Magnetic Resonance (NMR) spectroscopy.

Abstract: This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, genetic (Type 1, Type 5 hyperlipidemia) and acquired forms of hypertriglyceridemia or hyperlipoproteinemia-related disorders, caused by but not limited to lipodystrophy, hypothyroidism, medications (beta blockers, thiazides, estrogen, glucocorticoids, transplant) and other factors (pregnancy, alcohol intake), hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, cardiovascular outcomes, angina, exce

Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.

Abstract: The present invention provides a compound of formula (I) or the salt thereof: wherein R is at least one selected from the group consisting of unsubstituted C1-4 alkyl, C1-4 alkyl substituted by C6-18 aryl or —OR1, and —C(?O)Z. The compound is a type-S protein kinase inhibitor, which binds to an ATP-binding site and a substrate-recognition site of a protein kinase simultaneously. The present invention further provides a pharmaceutical composition, which includes a compound of formula (I) or a salt and a pharmaceutically acceptable carrier thereof. The present invention further provides a use of a compound of formula (I) or a salt thereof, which is for the manufacture of a protein kinase inhibitor as a drug.

Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

Abstract: This invention provides processes for forming halomagnesium tetrakis(Faryl)borates, which processes comprise bringing together, in an anhydrous liquid organic medium, at least one boron trihalide; at least one Faryl Grignard reagent; and at least one copper compound. Also provided are processes for forming halomagnesium tetrakis(Faryl)borates, which processes comprise bringing together, in an anhydrous liquid organic medium, at least one boron trihalide; at least one copper compound; magnesium metal; and at least one polyhaloaromatic compound.

Abstract: The present invention relates to a process for the preparation of aminoaryl- and aminoheteroaryl boronic acids and esters thereof of formula (I) in high yield. The claimed process uses diarylketal formula (V) to generate an arylbromide of formula (III) in which the amino-group is protected as bisarylmethylidenimino-group, which is then transformed into a formula (I) compound.

Abstract: Protease inhibitors, particularly aspartyl protease inhibitors, and more particularly HIV protease inhibitors which are boronated to enhance activity or to enhance entry into cells. Compounds, prodrugs and salts thereof of this invention contain phenylboronate groups, in particular p -B(OH)2-phenyl groups, benzoxaborole groups or borono-pyridyl groups or analogous groups in which the boronate group is protected. Methods for treating AIDS and ARC as well as providing a method for treating or preventing HIV infection.

Abstract: Porous metal-organic frameworks (MOFs) and metallated porous MOFs are provided. Also provided are methods of metallating porous MOFs using atomic layer deposition and methods of using the metallated MOFs as catalysts and in remediation applications.

Abstract: Provided is an electrolyte salt comprising a quaternary ammonium cation indicated by formula (1) and a trimethylsilyl alkanesulfonate anion indicated by formula (2). (In the formula, R1-R4 each independently indicate a C1-4 alkyl group or an alkoxyalkyl group indicated by —(CH2)n—OR. Any two among R1-R4 can mutually bond and form a ring together with a nitrogen atom to which same have bonded. The remaining two can mutually bond and form a spiro ring having a nitrogen atom as the spiro atom therefor. R indicates a methyl group or an ethyl group. n indicates 1 or 2 and m indicates 2 or 3.

Abstract: Provided is a novel phosphorus-containing compound represented by general formula (I). The compound has reactivity with a glycidyl group and is therefore capable of providing a curing epoxy resin composition that is expected to achieve flame retardation and reduction of dielectric constant. wherein m is a number of 1 to 10; R1, R2, R3, and R4 are each hydrogen, alkyl, or aryl; R5 is alkyl, alkanediyl, alkanetriyl, alkanetetrayl, or an aromatic group; X is oxygen or sulfur; Y is oxygen, sulfur, or ?NR?; and R? is hydrogen, alkyl, or aryl.

Abstract: Benzothiazole phosphonate analogs and methods of using the same to inhibit the activity of Amyloid Binding Alcohol Dehydrogenase and in the amelioration or treatment of Alzheimer's disease are provided.

Abstract: Aspects of the present disclosure relate to compounds which have enhanced oral bioavailability. A transition metal complex includes a transition metal coordinated by a macrocycle comprising the pentaaza 15-membered macrocyclic ring corresponding to Formula A and two axial ligands having the formula —OC(O)X1. each of the two axial ligands has the formula —OC(?O)X1 wherein each X1 is independently substituted or unsubstituted phenyl or —C(—X2)(—X3)(—X4); each X2 is independently substituted or unsubstituted phenyl, or substituted or unsubstituted alkyl; each X3 is independently hydrogen, hydroxyl, alkyl, amino, —X5C(?O)R13 where X5 is NH or O, and R13 is C1-C18 alkyl, substituted or unsubstituted aryl or C1-C18 aralkyl, or —OR14, where R14 is C1-C18 alkyl, substituted or unsubstituted aryl or C1-C18 aralkyl, or together with X4 is (?O); and each X4 is independently hydrogen or together with X3 is (?O).

Abstract: Aspects of the present disclosure relate to compounds which have enhanced oral bioavailability. A transition metal complex includes a transition metal coordinated by a macrocycle comprising the pentaaza 15-membered macrocyclic ring corresponding to Formula A and two axial ligands having the formula —OC(O)X1. each of the two axial ligands has the formula —OC(?O)X1 wherein each X1 is independently substituted or unsubstituted phenyl or —C(—X2)(—X3)(—X4); each X2 is independently substituted or unsubstituted phenyl, or substituted or unsubstituted alkyl; each X3 is independently hydrogen, hydroxyl, alkyl, amino, —X5C(?O)R13 where X5 is NH or O, and R13 is C1-C18 alkyl, substituted or unsubstituted aryl or C1-C18 aralkyl, or —OR14, where R14 is C1-C18 alkyl, substituted or unsubstituted aryl or C1-C18 aralkyl, or together with X4 is (?O); and each X4 is independently hydrogen or together with X3 is (?O).

Abstract: The present invention provides stable, cyclic bent allene metal complexes and methods of conducting chemical processes, preferably olefin hydrogenation, comprising contacting an olefin substrate, preferably an unsaturated polymer, with a cyclic bent allene metal complex as described herein, under hydrogenation conditions.

Abstract: The present teachings relate to compounds and compositions for treatment of cancers. In some embodiments, the composition comprises a platinum (IV) complex having at least one polar moiety as a ligand.

Abstract: The present invention relates to the ferrocene derivative represented by formula (IA) or formula (IB), or to the pharmaceutically acceptable salt or solvate thereof and to the pharmaceutical composition thereof. Wherein, R is independently selected from H, halogen, cyano, nitro, C1-C6 alkyl, C1-C6 alkoxy, hydroxy-C1-C6 alkyl, halo-C1-C6 alkyl, halo-C1-C6 alkoxy or C1-C6 alkoxy-C1-C6 alkoxy; Z is selected from O, S or NR1, wherein R1 is independently H or C1-C6 alkyl; n is an integer from 0 to 5. The present invention also provides a method and the pharmaceutical application thereof for preparing the compounds represented by formula (IA) or formula (IB) or the pharmaceutically acceptable salts thereof. The compounds have a strong inhibitory activity against human lung cancer cell line A549, colorectal cancer cell line HCT116 and/or breast cancer cell line MCF-7.

Abstract: A process for enabling the production of a particulate composition containing crystalline trehalose dihydrate is provided. Including allowing an ?-glycosyltrehalose-forming enzyme to act on liquefied starch derived from a microorganism of the genus Arthrobacter and a trehalose-releasing enzyme derived from a microorganism of the genus Arthrobacter along with a starch debranching enzyme and a cyclomaltodextrin glucanotransferase; allowing glucoamylase to act on the resulting mixture to obtain a saccharide solution containing ?,?-trehalose; precipitating crystalline ?,?-trehalose dihydrate from the above saccharide solution; collecting the precipitated crystalline ?,?-trehalose dihydrate by a centrifuge; and ageing and drying the collected crystals. Cyclomaltodextrin glucanotransferase derived from a microorganism of the genus Paenibacillus or a mutant enzyme thereof is used to increase the ?,?-trehalose content in the saccharide solution to over 86.

Abstract: A diarylethene compound represented by formula (I) wherein, Sg is a monovalent sugar residue formed by removing one hydroxyl group from a sugar compound or a monovalent protected sugar residue formed by removing one hydroxyl group from a sugar compound in which one or more other hydroxyl groups are protected, and wherein the sugar is selected from the group consisting of a six-membered ring sugar, a five-membered ring sugar, cyclitol, and oligosaccharides containing a six-membered ring sugar, a five-membered ring sugar, or cyclitol; U is —(CH2)n—, —CH2—U?—, or —C(?O)— wherein n is an integer of 1 to 5, U? is a C2-C10 branched alkylene group binding to Ar); and Ar is a group represented by formula (A1) or (A2); wherein, X is S, SO2, NR3 in which R3 is a C1-C3 alkyl group, or O, R is C1-C4 alkyl group, R1 and R2 are independently a C1-C3 alkyl group, a is 0 or 1, b is an integer of 0-3, and * represents a bond with U; Y is a hydrogen atom or a halogen atom; and m is an integer of 3 to 5.