Abstract: Disclosed herein are compounds of formula (I), and methods of inhibiting histone deacetylase (“HDAC”) enzymes (e.g.

Abstract: In the method, a trione compound represented by the following formula (1) is (i) reduced by NaAlH2(OCH2CH2OCH3)2 and subsequently further reduced by a metal borohydride salt, or (ii) reduced by calcium borohydride, thereby producing an amide alcohol compound represented by the following formula (3) (wherein, R1 and R2 may be the same or different and each represents a hydrogen atom or a protecting group of an ureylene group; R4 represents an alkyl group, an aralkyl group, or an aryl group; and each of R5, R6, and R7 represents a hydrogen atom, an alkyl group, an alkoxy group, or a halogen atom).

Abstract: Provided herein are imidazolium polymers having steric hindrance at the 4-position of the imidazole moieties in the polymeric chain. The sterically-protected, N-methylated imidazolium polymers exhibit hydroxide stability in concentrated caustic solutions at elevated temperatures, such as at 100° C. and higher.

Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, Ra, Rb, Q1, and Q2 are defined in the specification. The invention also comprises a method of treating or ameliorating a ROR-?-t mediated syndrome, disorder or disease, including wherein the syndrome, disorder or disease is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, and psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.

Abstract: The invention relates to 1,3-diaza-spiro-[3.4]-octane derivatives, their preparation and use in medicine, particularly in various neurological disorders, including but not limited to pain, neurodegenerative disorders, neuroinflammatory disorders, neuropsychiatric disorders, substance abuse/dependence.

Abstract: The present invention relates to a vinylarene deriv. which modulates or inhibits the enzymic activity of indoleamine 2,3-dioxygenase 1 (IDO-1), and the use thereof, and further relates to a vinylarene deriv. and the use thereof. The vinylarene deriv. and its stereoisomer, cis- or trans-isomer, or tautomer thereof and pharmaceutically acceptable salt thereof, has an IDO-1 enzyme inhibitory activity, and is expected to provide brand new therapeutic methods and schemes for related diseases caused by IDO enzymes.

Abstract: A process for preparing a tetra-substituted aminobiphenol macrocyclic ligand having the structure (I), comprising the step of treating a precursor compound having the structure (II) with a compound having the structure R6-L where L represents a leaving group (hereinafter compound (III)) in the presence of a base.

Abstract: The present application relates to thiadiazole compounds of formula (I) in which A, B, E, and Q have the meanings provided in the specification, compositions containing such compounds, their use for controlling animal pests including arthropods, insects and nematodes, and to processes and intermediates for the preparation of the thiadiazole compounds.

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 MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, traumatic brain injury, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.

Abstract: This disclosure relates to anti-agglomerant low dosage hydrate inhibitors that can inhibit the formation of hydrate agglomerants and/or plugs. Thus, provided herein are carboxy alkyl ester compounds that can be used in hydrate inhibitor compositions and methods of inhibiting formation of hydrate agglomerants in a fluid comprising water, a gas, and optionally a liquid hydrocarbon. Also provided herein are methods of making the carboxy alkyl ester compound.

Abstract: A method is for the preparation of furoic acid or of one of its derivatives of formula (I): in which R1, R2, R3 and R4 represent, independently of each other, a hydrogen atom, a linear or branched C1-C6 alkyl group, a —C(?O)—H group or a —COOH group, by heterogeneous catalytic oxidation of furfural or a derivative thereof of formula (II). The oxidation is carried out in the presence of a supported catalyst based on gold nanoparticles, and in a non-alkaline aqueous medium. A composition useful in the method includes at least furfural and supported gold nanoparticles.

Abstract: The present invention relates to a process for preparing benzylic amides of formula I wherein the variables have the meaning as defined in the description, by reductive amidation of a nitrile of formula II wherein the variables have the meanings given for formula I, with an activated carbonyl compound of formula III, and which nitrile is obtained by reaction of a compound of formula IV with a halogen compound of formula V, wherein X is a halogen atom, preferably bromo, which halogen compound V in turn is obtained by Sandmeyer reaction of an aniline derivative of formula VI novel compounds of formula I, and processes for preparing compounds of formula XII wherein the variables have the meaning as defined in the description by condensing compounds of formula I with compounds of formula X and subjecting the resulting ?,?-unsaturated ketone of formula XI to a reaction with hydroxylamine to yield compounds of formula XII.

Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatohepatitis, metabolic syndrome, atherosclerosis, and cancer.

Abstract: The disclosures herein provide compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, enantiomers, stereoisomers, solvates, and hydrates thereof. These compounds may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral administration, intravenous, spray, parenteral, lozenge, solution, syrup, sachet, transdermal administration, or injection. Such compositions may be used to treatment of inflammation or its associated complications.

Abstract: Compounds that may selectively inhibit Oplophorus luciferase-derived bioluminescent complexes, e.g., NanoBiT® bioluminescent complex, are disclosed as well as compositions and kits comprising the compounds, and methods of using the compounds.

Abstract: A compound represented by Formula (1): The compound can be used as insecticides.

Abstract: Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity.

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: Provided herein is a process for the preparation of 4-((6-(2-(2,4-difluorophenyl)-1, 1-difluoro-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)pyridin-3-yl)oxy)benzonitrile.

Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders, or symptoms thereof mediated by such metalloenzymes.

Abstract: The aryl sulfonamide compounds of this invention have powerful and cell-type specific Bcl inhibitory activity. Selected compounds in this class promote apoptosis in senescent cells, and are being developed for treating senescent-related conditions. Selected compounds in this class promote apoptosis in cancer cells, and can be developed as chemotherapeutic agents.

Abstract: To provide an industrial method for producing a 5-alkynyl pyridine compound at a high yield. A method for producing a compound represented by the formula (3), which comprises reacting a 5-chloropyridine compound represented by the formula (1) and an alkyne compound represented by the formula (2) by using sodium carbonate or sodium hydrogen carbonate in the presence of a palladium catalyst having phosphine ligands: (in the formula (2), R is a hydrogen atom, a C1-C6 alkyl or a C3-C7 cycloalkyl).

Abstract: The present invention comprises compounds of Formula I. wherein: R1, Q, R3, R4, R5, R6, A1, and A2 are defined in the specification. The invention also comprises a method of treating or ameliorating a ROR-?-t mediated syndrome, disorder or disease, including wherein the syndrome, disorder or disease is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, and psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.

Abstract: Provided are a (hetero)arylamide compound as shown in formula (I) having an inhibitory effect on protein kinase activity, a pharmaceutically acceptable salt, a stereoisomer, a solvate or hydrate thereof, a pharmaceutical composition comprising the compound or a derivative thereof, and a method for preparing the compound. The compound can be used as an irreversible inhibitor for protein kinase for preparing a plurality of drugs comprising an anti-tumour drug.

Abstract: The present disclosure provides a triazole antibacterial derivative and a pharmaceutical composition thereof and a use thereof and in particular relates to a compound represented by the following formula (I), and a racemate, a stereoisomer, a tautomer, an oxynitride or a pharmaceutically acceptable salt thereof: The compound of the present disclosure has a desirable water solubility and can be formulated into an injection for use without adding a cosolvent having a potential safety risk (such as hydroxypropyl-?-cyclodextrin, sulfobutylether-?-cyclodextrin, and the like), facilitating drug administration for patients, and greatly improving clinical safety. The drug can be used even by patients with moderate or severe renal impairment, thereby expanding the application scope of the drug.

Abstract: Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, and Formula IV or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

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, isotopic form or stereoisomer thereof, wherein A is a five-membered heteroaryl comprising 1 or 2 non-adjacent heteroatoms, inclusive of X and Y; W, X, Y, Z, L, L1, E, R1, R2bR2c and the dotted circle are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and compounds for use in methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided. Preferred compounds are e.g. 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and related compounds such as e.g. the corresponding derivatives with e.g. a benzoimidazole, indole, benzooxazole, imidazopyridine or imidazole core structure, substituted on ring A by e.g.

Abstract: The present invention provides compounds of Formula (I): (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 invention relates to HPK1 inhibitors useful in the treatment of cancers, and other serine-threonine kinase mediated diseases, having the Formula: where A, R1, R2, R3, R4, R5, R6, R16, R17, X1, X2, X3, X4, m, and n are described herein.

Abstract: Disclosed are compounds of Formula (I?) methods of using the compounds for inhibiting HPK1 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer.

Abstract: The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of diseases and conditions mediated by the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.

Abstract: The invention provides alkyne substituted quinazoline compounds, such as compounds of the formula (I), which are irreversible ErbB kinase inhibitors. The compounds are useful in the treatment of diseases and disorders where ErbB kinase activity is implicated such as a hyperproliferative disorder (e.g., cancer).

Abstract: Provided herein are compounds of formula (I) wherein R1, Y, L1, G1, X1, X2, L2, R2, R3, and R4 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, which are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising compounds of formula (I).

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 provides a tetrazolinone represented by formula (I) and a pest control agent comprising the same, and their use thereof.

Abstract: Chemical compounds that are useful as inhibitors of mechanotransduction in the treatment of pain and modulation of touch perception and topical administration of the compounds described herein in the treatment of pain and modulation of touch perception.

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: 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: Methods of preparation and purification of a compound of Formula I, intermediates thereof, a polymorph thereof, and related compounds are disclosed. Formulations and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed.

Abstract: The present invention relates to an improved method for producing a diphenylmethane derivative which is effective as a sodium-dependent glucose cotransporter (SGLT) inhibitor, the method being carried out by means of a convergent synthesis method in which each major group is separately synthesized and then coupled. As such, in comparison to a linear synthesis method disclosed in existing documents, the synthesis pathway is compact and yield can be increased, and risk factors inherent in the linear synthesis pathway can be reduced. Furthermore, the crystal form of the compound produced according to the method has superb physicochemical characteristics, and thus can be effectively utilized in fields such as pharmaceutical manufacturing.

Abstract: The present invention relates to cryptophycin compounds of formula (I). The invention also relates to cryptophycin payloads, to cryptophycin conjugates, to compositions containing them and to their therapeutic use, especially as anticancer agents. The invention also relates to the process for preparing these conjugates.

Abstract: A furazan-3-carboxylic acid derivative or pharmaceutically acceptable salt thereof for treatment of acute myeloid leukemia.

Abstract: A bis(benzoxazinyl)phthalimidine has the structure wherein R1, R2, R3, R4, j, and k are defined herein. The bis(benzoxazinyl)phthalimidine is useful as a component of a curable composition. It exhibits a high melting temperature and a high exotherm onset temperature. Also described is a composite that includes a reinforcing filler and the curing product of the bis(benzoxazinyl)phthalimidine.

Abstract: Provided are compounds of Formula (I), or pharmaceutically acceptable salts thereof, and methods for their use and production.

Abstract: Disclosed are imidazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein R1, X, Y1, Y2, Y3 and Z are as described herein. In certain embodiments, a compound disclosed herein inhibits a cellular TAM receptor, and can be used to treat disease mediated by or involving the TAM receptor family.

Abstract: Disclosed herein are new substituted bicyclo[1.1.1]pentane compounds which inhibit the kinase activity of dual leucine zipper (DLK) kinase (MAP3K12). Also disclosed herein are solid polymorph forms of these compounds. Also disclosed herein are salts of these compounds, and solid polymorph forms of these salts. Also disclosed herein are compounds, pharmaceutical compositions, and methods of treatment of DLK-mediated diseases, such as neurological diseases that result from traumatic injury to central nervous system and peripheral nervous system neurons, or that result from a chronic neurodegenerative condition, from neuropathies resulting from neurological damage and from cognitive disorders caused by pharmacological intervention.

Abstract: The invention relates to a compound comprising the following general formula (1): and said compound for use as a medicament, in particular for use in the treatment psychiatric or neurological disorders and inflammation, in particular neuroinflammation: (formula 1) wherein each of R1, R2 and R3 are selected independently from each other from alkyl, alkoxy, alkenyl, alkynyl, cycloalkyl, aryl, heterocycle, or heteroaryl.

Abstract: This invention is directed to benzenesulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of diseases or conditions associated with voltage-gated sodium channels, such as epilepsy and/or epileptic seizure disorders.

Abstract: The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.

Abstract: The present disclosure relates to the field of pharmaceutical synthesis, and more particularly, relates to a monocyclic ?-lactam-siderophore conjugate as well as a method for synthesizing same and its use in the treatment of bacterial infectious diseases. Provided are a monocyclic ?-lactam-siderophore conjugate represented by formula (I) as described herein, an optical isomer thereof or a pharmaceutically acceptable salt thereof, and a method for synthesizing same, and a use thereof in treating bacterial infectious diseases.