Abstract: The present invention is directed to novel quinoline compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.

Abstract: The present invention relates to compounds which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.

Abstract: Ivabradine hemipamoate of formula (I): and its hydrates. Medicinal products containing the same which are useful in the treatment or prevention of the various clinical situations of myocardial ischaemia such as angina pectoris, myocardial infarction and the associated rhythm disturbances, as well as in the various pathologies involving rhythm disturbances, especially supraventricular rhythm disturbances, and in systolic or diastolic heart failure.

Abstract: Process for preparing 3,5-bis(haloalkyl)pyrazole derivatives of the formula (I), via acylation of Hydrazones.

Abstract: The present invention provides compounds of any one of Formulae (A), (I-11), (II), and (V) (e.g., compounds of Formula (A-1)-(A-18)), and methods for treating Waldenström's macroglobulinemia (WM) and other B cell neoplasm in a subject using the compounds. The methods comprise administering to a subject in need thereof an effective amount of the compounds. Also provided are methods to treat B cell neoplasms using the compounds in combination with inhibitors of Bruton's tyrosine kinase (BTK), interleukin-1 receptor-associated kinase 1 (IRAK1), interleukin-1 receptor-associated kinase 4 (IRAK4), bone marrow on X chromosome kinase (BMX), phosphoinositide 3-kinase (PI3K), transforming growth factor b-activated kinase-1 (TAK1), and/or a Src family kinase.

Abstract: A very stable, selective and renally safe sodium channel blocker represented by the formula: The invention also includes a variety of compositions, combinations and methods of treatment using this inventive sodium channel blocker.

Abstract: The present invention provides novel phenazine derivatives, such as compounds of Formula (I) and (II), and pharmaceutically acceptable salts thereof. The compounds of the invention are expected to be antimicrobial agents and may act by a microbial warfare strategy (e.g., a reactive oxygen species (ROS)-based competition strategy). The present invention also provides pharmaceutical compositions, kits, uses, and methods that involve the compounds of the invention and may be useful in preventing or treating a microbial infection (e.g., a bacterial infection) in a subject, inhibiting the growth and/or reproduction of a microorganism (e.g., a bacterium), killing a microorganism (e.g., a bacterium), inhibiting the formation and/or growth of a biofilm, or reducing or clearing a biofilm.

Abstract: A method for the production of ethylene oxide wherein the partial pressure of water vapor at the inlet of the reactor is at least about 8 kPa using a high purity carrier comprising alpha-alumina, a promoting amount of at least one Group IA metal, and a promoting amount of rhenium.

Abstract: The invention relates to compounds of Formula (I) and their use as selective dipeptidyl peptidase I inhibitors, as well as pharmaceutical compositions comprising said compounds, and methods of treatment involving said compounds.

Abstract: Provided is a method for producing a cyclic carbonate obtained by reacting epoxide and carbon dioxide in the presence of a quaternary onium salt as a counter ion or a quaternary phosphonium salt having a halogenated anion as a counter ion, or in the presence of a solid catalyst obtained by immobilizing the quaternary onium salt onto a carrier, wherein an organohalogen compound containing at least one halogen atom in one molecule is added to the reaction system.

Abstract: The present subject matter relates generally to compounds having the formula (I): wherein each of X, Y, R1, R2, R3, R4, and n are as defined herein. Compounds of formula (I) may act as inhibitors of the thioredoxin reductase enzyme system. The subject matter also relates to use, formulation and preparation of the compounds. The compounds may be useful in the treatment of inflammatory and oxidative diseases and conditions. The compounds may also provide useful anti-proliferative and anti-apoptotic effects.

Abstract: Tetrahydrothiophene and related heterocyclic analogs and related methods for GABA aminotransferase inactivation.

Abstract: A dihydropyrimidinone derivative includes a compound having a chemical structure according to Formula 1: wherein Z is selected from CH2O, O, and N; X is selected from O and S; and R represents aryl, substituted aryl, heteroaryl, or substituted heteroaryl, wherein the substituted aryl or substituted heteroaryl have one or more substituents selected from the group consisting of halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, nitro, hydroxyl, alkylthio, alkylamino, heteroaryl, aryloxy, haloaryloxy, arylthio, arylamino, and pharmaceutically acceptable salts thereof. The present subject matter also relates to a method of making a dihydropyrimidinone derivative, a method of treating a gastrointestinal disease, a method of treating an ulcer, a pharmaceutical composition, and a method of making a pharmaceutical composition.

Abstract: The described invention provides small molecule anti-cancer compounds that selectively target and inhibit measurable biological activity of truncated APC proteins, an immortalized Human Colonic Epithelial Cell (HCEC) model, and pharmaceutical compositions comprising at least one of the small molecule anti-cancer compounds and a pharmaceutically acceptable carrier.

Abstract: The present invention relates to a heterocyclic compound of the general formula (I) and their use and preparation, methods of making the compounds, compositions containing at least one of said compounds, and methods of treatment using at least one compound. In particular, compounds of the general formula (I) are useful for inhibiting glycogen synthase kinase 3 (GSK-3).

Abstract: The invention relates to new quinoxaline derivative compounds of formula (I), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

Abstract: Provided is a novel pyrazine derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof, or a solvate thereof which is useful for treating or preventing diseases in which URAT1 is involved, including gout, hyperuricemia, hypertension, renal diseases such as interstitial nephritis and the like, diabetes, arteriosclerosis, Lesch-Nyhan syndrome, and the like.

Abstract: Disclosed are compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, Ra, R1, R2, R3, R4, R6, w and n1 are defined and described herein; compositions thereof; and methods of use thereof. These compounds are useful for treating a variety of neurological and psychiatric disorders, such as those described herein.

Abstract: The present invention relates to the technical field of medicine, and specifically relates to the carboxylic acid compound represented by the chemical formula I or chemical formula II, and a pharmaceutically acceptable salt, a prodrug, and a solvate thereof, and a method for preparation thereof, as well as a pharmaceutical composition containing the described substances, and a use thereof.

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.

Abstract: The invention generally relates to substituted benzofuranyl and substituted benzoxazolyl compounds, and more particularly to a compound represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula (A), or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders.

Abstract: The present invention relates to 5-fluoro-N-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfone group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).

Abstract: Provided are a condensed cyclic compound of Formula 1 and an organic light-emitting device including the same

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.

Abstract: Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (III) as follows: wherein R1C, R2C, R4C, WC, YC, ZC, and GC, are defined herein.

Abstract: The invention relates to compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (TRPM8), and having formula: 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: The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5, M and X are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: The present invention relates to modulators of cystic fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating CFTR mediated diseases using such modulators.

Abstract: The present invention is directed to compounds encompassed by the Formula (I), pharmaceutical compositions thereof, methods for inhibiting LTA-4 hydrolase, and methods for the treatment of a disease and disorder which is ameliorated by the inhibition of LTA4-h activity. Non-limiting examples of such diseases and conditions include inflammatory and autoimmune diseases and disorders.

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: The present invention provides processes for the synthesis of substituted berbine compounds. Also provided are intermediates used in the synthesis of substituted berbine compounds.

Abstract: Substituted benzimidazole and 3H-imidazo[4,5-b]pyridines or formula I: where X and Y respectively are selected from: (i) N and N; and (ii) N and CR4; A2 is selected from: a C5 heteroarylene group, containing 2 or 3 ring heteroatoms, where the bonds to L1 and the core are ? to one another; L1 is selected from: (i) A1—O—CH2—A2; (ii) A1—CH2—O—A2; (iii) A1—C(?O)—NH—A2; (iv) A1—CH(OH)—A2; (v) A1—CH2—NH—C(?O)—A2; (vi) A1—S—CH2—A2; (vii) A1—CH2—S—A2; (viii) A1—CH2—A2; and (ix) A1—CH(CH3)—O—A2; A1 is phenyl, optionally substituted by F or CF3; their use as pharmaceuticals, and in particular, in treating cancer and hemoglobinopathies.

Abstract: The invention provides tricyclic heterocyclic compounds, pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variables are defined herein. The compounds of the invention may be useful for treating immunological and oncological conditions.

Abstract: Imidazoquinoline compounds with an alkoxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.

Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where R1, R2, R3, R4 and R5 have any of the meanings defined herein. The specification also relates to the use of compounds of Formula (I) and salts thereof to treat or prevent ATM mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising substituted imidazo[4,5-c]quinolin-2-one compounds and pharmaceutically acceptable salts thereof; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; and intermediates useful in such manufacture.

Abstract: The present invention relates to novel pyridino[1,2-?]pyrimidone compounds represented by formula (I) or pharmaceutically acceptable salts thereof; and a method of use thereof for treating tumors, such as colon cancer and gastric cancer.

Abstract: The invention related to pyrazolonaphthyridinone derivatives of formula (I) to their preparation and to their therapeutic use as selective inhibitors of type 2 methionine aminopeptidase (hMETAP2).

Abstract: A compound of Formula I: wherein, R1 and R2 independently are selected from the group consisting of optionally substituted (6-10C)aryl and (1-5C)heteroaryl groups. The compounds can be used in pharmaceutical compositions, in particular in the treatment of cancer.

Abstract: Heterocyclic compounds of formula (I), pharmaceutical compositions containing such a compound and their therapeutic uses.

Abstract: The present invention includes compositions that are useful in preventing or treating metastasis in a subject diagnosed with cancer. The present invention also includes methods of preventing or treating metastasis in a subject diagnosed with cancer, wherein the method comprises administering to the subject in need thereof an effective amount of a pharmaceutical formulation comprising at least one pharmaceutically acceptable carrier and at least one CX3CR1 or fractalkine antagonist.

Abstract: The present invention relates to new piperidine inhibitors of Janus kinase 3 activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Disclosed is a series of analogs of 4H-pyrazolo[1,5-?]benzimidazole compound as PARP inhibitors. In particular, disclosed in the invention is a compound as shown by formula (I) or a pharmaceutically acceptable salt thereof as a PARP inhibitor.

Abstract: The present invention provides, in part, compounds of Formula (I): and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), schizotypal personality disorder, cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, Parkinson's disease, anxiety, and depression.

Abstract: The present invention discloses a class of isoquinolinesulfonyl derivatives as RHO kinase inhibitors, and pharmaceutical compositions thereof, and relates to pharmaceutically acceptable uses thereof. Specifically, the present invention relates to a compound as represented by formula (I), or a pharmaceutically acceptable salt thereof.

Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitroge

Abstract: The invention provides compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.

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: 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: Compounds useful as kinase inhibitors are provided herein, as well as salts, pharmaceutical compositions, methods of medical treatment and methods of synthesis thereof.

Abstract: A method for producing a highly pure PMDA comprises at least the following steps: (1) a step of preparing a raw material solution by dissolving a raw material of a pyromellitic dianhydride in an acetic acid solvent, (2) a step of preparing a precursor pyromellitic dianhydride by recrystallizing the pyromellitic dianhydride in the prepared raw material solution and separating the acetic acid solvent, (3) a step of performing a degassing treatment on the precursor pyromellitic dianhydride by stirring the precursor pyromellitic dianhydride in a fluidized state while heating under reduced-pressure conditions, and (4) a step of taking out the pyromellitic dianhydride subjected to the degassing treatment.

Abstract: Dolutegravir potassium salt and solid state forms thereof are provided, as well as methods of making and interconverting these forms. The Dolutegravir potassium forms, and pharmaceutical compositions containing them, may be used to treat subjects in need of medical treatment, such as for HIV infection.