Abstract: The present invention relates to compounds of formula (I): wherein Q is selected from O or S; R1 is a saturated or unsaturated, optionally substituted C1-C15 hydrocarbyl group, wherein the atom of R1 which is attached to the sulfur atom of the sulfonylurea group is not a ring atom of a cyclic group; and R2 is a cyclic group substituted at the ?-position, wherein R may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

Abstract: The present invention relates to a process for the preparation of (1-alkylindo-3-ylmethyl) benzoic acid derivatives, in particular Zafirlukast and analogs thereof. Further, this process is based on protection group free and C—H bond activation strategy involving all step catalytic transformation sequence and comprises the following steps: Sonogashira coupling, indole formation by Sp3 C—H activation, reductive hydrogenation and amidation.

Abstract: The present invention relates to a composition which comprises an electron-transporting host and a hole-transporting host, to the use thereof in electronic devices and to electronic devices containing this composition. The electron-transporting host is particularly preferably selected from the class of the lactams. The hole-transporting host is preferably selected from the class of the biscarbazoles.

Abstract: The present disclosure relates to a plurality of host materials comprising a compound represented by formula 1 and a compound represented by formula 2, and an organic electroluminescent device comprising the same. The organic electroluminescent device according to the present disclosure can exhibit excellent lifespan characteristic, while maintaining low driving voltage and high luminous efficiency, by comprising a plurality of host compounds in a specific combination. wherein the substituents are as defined in the specification.

Abstract: The present invention relates to a process for the preparation of migalastat of formula (I) and intermediates useful in the synthesis thereof. The process comprises the reductive amination reaction of a compound of formula (VI).

Abstract: Newly synthesized derivatives of BAS00127538 have been discovered to possess antibiotic activity and to combat resistant bacterial strains. Compounds and pharmaceutical compositions containing these compounds are described, and are based on a generic scaffold structure. Synthetic methods and methods of using the compounds also are described. Preferred compounds bind to Lipid II with high affinity, have markedly reduced cytotoxicity compared to BAS00127538, and retain activity against drug-resistant strains of Enterococci. They are stable in plasma, have dramatically improved pharmacokinetic and pharmacodynamics properties, and possess in vivo efficacy in a mouse model of sepsis.

Abstract: A method for producing a drug substance of crystalline pitavastatin calcium excellent in stability, is presented. In the production of a compound (pitavastatin calcium) represented by the formula (1): The water content is adjusted to a level of from 5 to 15%, and the crystal form is controlled to be crystal form A, thereby to obtain a drug substance excellent in stability.

Abstract: Disclosed herein are deuterated forms of 2-ethylamino-8-fluoro-3-methyl-1-oxo-1,2-dihydro-isoquinoline-4-carboxylic acid ((S)-cyclopropyl-phenyl-methyl)-amide (also referred to herein as SJB-01) and pharmaceutical compositions comprising such compounds.

Abstract: The present invention discloses compounds according to Formula I: Wherein R1, R2, R3a, R3b, and Cy are as defined herein. The present invention relates to compounds inhibiting ADAMTS, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory conditions, and/or diseases involving degradation of cartilage and/or disruption of cartilage homeostasis by administering a compound of the invention.

Abstract: A compound of the general formula (I). The compounds of formula I are useful for treatment of a cardiac disease, disorder or condition in a mammal.

Abstract: The present disclosure relates to crystalline form CS1 and CS9 of a hypoxia-inducible factor prolyl hydroxylase inhibitor compound (I) GSK1278863, processes for preparation, and uses for preparing drugs treating and/or preventing anemia thereof.

Abstract: The present invention relates to compositions and methods for the treatment of cancer and other diseases associated with mitochondrial dysfunction, including but not limited to, neurodegenerative disease, brain injuries, and certain non-neurological disorders, using a novel compound CPT-2008 and derivatives thereof.

Abstract: The present invention provides, in certain aspects, novel syringolin analogues, In certain embodiments, the compounds of the invention are proteasome inhibitors, In other embodiments, the compounds treat or prevent a cancer such as, but not limited to, leukemia in a subject,

Abstract: Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.

Abstract: The invention relates to 3-phenylisoxazoline-5-carboxamides of tetrahydro and dihydrofuran carboxamides of general formula (I) and to their agrochemically compatible salts (I) as well as to the use thereof in the field of plant protection.

Abstract: The present disclosure relates to novel crystalline forms of ozanimod and preparation method thereof. The provided crystalline forms of ozanimod comprise crystalline form CS9, crystalline form CS10 and crystalline form CS11, and can be used for treating autoimmune diseases, particularly used for preparing drugs for treating multiple sclerosis and ulcerative colitis. The crystalline forms of the present disclosure have one or more advantages in solubility, stability, hygroscopicity and processability and provide new and better choices for the preparation of ozanimod drug product, and are very valuable for drug development.

Abstract: The present disclosure encompasses crystalline polymorphs of Ponesimod, processes for preparation thereof, and pharmaceutical compositions thereof.

Abstract: This invention is a benzothiophene estrogen receptor modulator or its pharmaceutically acceptable salt or a pharmaceutically acceptable composition thereof to treat an estrogen-related medical disorder.

Abstract: Disclosed are a retinoid compound, a preparation method therefor, intermediates thereof and an application thereof. The retinoid compound I of the present invention has a good tumor growth inhibition rate.

Abstract: A method for manufacturing an insecticidal compound and insecticidal compositions comprising the insecticidal compound and methods of use are presented herein. The manufacturing method presented herein allows for a high purity grade of thiocyclam hydrochloride to be synthesized. The insecticidal compositions comprising the thiocyclam hydrochloride can be used for prevention of crop destruction by insects. The use of thiocyclam hydrochloride in insecticidal compositions as described herein can achieve greater efficacy than previously known insecticides, by eliminating the insect pests more reliably and efficiently.

Abstract: A method for manufacturing an insecticidal compound and insecticidal compositions comprising the insecticidal compound and methods of use are presented herein. The manufacturing method presented herein allows for a high purity grade of thiocyclam hydrochloride to be synthesized. The insecticidal compositions comprising the thiocyclam hydrochloride can be used for prevention of crop destruction by insects. The use of thiocyclam hydrochloride in insecticidal compositions as described herein can achieve greater efficacy than previously known insecticides, by eliminating the insect pests more reliably and efficiently.

Abstract: The present technology is directed to methods of inhibiting or modulating p97 and compounds and compositions useful in such methods Diseases and conditions that can be treated with the compounds and compositions of the present technology include, but are not limited to, antibacterial infection, antiviral infection, cancer and neurodegenerative disorders susceptible to treatment by inhibition or modulation of p97.

Abstract: Provided herein are TRPC5 inhibitors and methods of using the same, e.g., to protect podocytes and/or treat kidney disease.

Abstract: Aspects of the present disclosure include compounds that activate Nrf2. Such compounds find use in the treatment of autoimmune and inflammatory diseases and disorders, such as for example psoriasis and multiple sclerosis. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Abstract: The present application relates to the use of substituted indazoles for treatment and/or prophylaxis of allergic and/or inflammatory diseases in animals, especially for treatment and/or prophylaxis of atopic dermatitis, Flea Allergy Dermatitis, inflammatory bowel disease, osteoarthritis and inflammatory pain, non-infectious recurrent airway disease, insect hypersensitivity, asthma, respiratory disease, mastitis and endometritis in animals.

Abstract: A dexrabeprazole sodium compound includes crystal forms B and C. The crystal form B has good stability and flowability. The crystal form C is an anhydrous crystal form and has good stability and low hygroscopicity. The crystal forms are suitable for preparing a dexrabeprazole sodium preparation.

Abstract: Described herein are compounds that are melanocortin subtype-2 receptor (MC2R) 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 MC2R activity.

Abstract: Provided herein are compounds of the Formula I: or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, R1, R2, R3, R4, R5, R6 and R7 are as defined herein, which are inhibitors of one or more TAM kinases and/or c-Met kinase, and are useful in the treatment and prevention of diseases which can be treated with a TAM kinase inhibitor and/or a c-Met kinase inhibitor.

Abstract: Compounds and compositions for modulating fibroblast activation protein (FAP) are described. The compounds and compositions may find use as therapeutic agents for the treatment of diseases, including hyperproliferative diseases.

Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to salts of and solid forms comprising free base or salts of (S)-4-(4-(4-(((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)oxy)methyl)benzyl)piperazin-1-yl)-3-fluorobenzonitrile.

Abstract: Provided herein are methods for treating, preventing, or ameliorating one or more symptoms of a condition, disorder, or disease mediated by a lipid kinase or a protein kinase with benzimidazoles, for example, of Formula I or II, and pharmaceutical compositions thereof. Also provided herein are benzimidazoles, and pharmaceutical compositions thereof; and methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.

Abstract: The present embodiments provide for substituted triazolylpyridine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for modulating the activity of histone demethylase enzymes. Additionally, the subject compounds and compositions are useful for the treatment of cancer or other neoplastic diseases, or maladies associated with abnormal histone demethylase activity. Accordingly, the substituted triazolylpyridine derivative compounds described herein are useful in methods and medicaments for treating cancer.

Abstract: This application discloses novel substituted 2-anilinopyrimidine derivatives, and pharmaceutically acceptable salts, solvates, prodrugs, and compositions thereof, which are useful for the treatment or prevention of diseases or medical conditions mediated by epidermal growth factor receptors (EGFRs), including but not limited to a variety of cancers.

Abstract: The present invention relates to a crystalline form of N-((s)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)prop-2-yl)-5-(1-hydroxylethyl)-1H-pyrazole-3-carboxamide (namely, ODM-201). The ODM-201 crystalline form of the present invention has one or more improved properties compared to known ODM-201. The present invention further relates to a method for preparing the ODM-201 crystalline form, a pharmaceutical composition thereof, and a use thereof in the preparation of a medicament for the treatment of nuclear receptor, specifically steroid receptor, and more specifically androgen receptor (AR)-dependent diseases and conditions.

Abstract: The invention provides compounds of formula (I): or a pharmaceutically-acceptable salt thereof, wherein the variables are defined in the specification, that are inhibitors of JAK kinases, particularly JAK3. The invention also provides crystalline forms, pharmaceutical compositions comprising such compounds, methods of using such compounds to treat gastrointestinal and other inflammatory diseases, and processes and intermediates useful for preparing such compounds.

Abstract: The present invention relates to a surface cover for a body which can be brought into contact with a liquid, comprising: a layer which at least partly contains gas and which is designed and arranged such that at least some sections of a layer face facing the liquid contacts the liquid; a gas-permeable layer which is arranged on the gas-containing layer on a face that faces the body and is opposite the face facing the liquid or which is integrally formed with the gas-containing layer; and a gas-supplying device which is connected to the gas-permeable layer such that gas can flow from the gas-supplying device to the gas-containing layer through the gas-permeable layer. The invention also relates to an arrangement and a use.

Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.

Abstract: A method for treating a neurodegenerative disease or an inflammatory disorder in a subject, comprising administering to the subject in need thereof, a compound, or a pharmaceutically acceptable salt thereof, of formula II: wherein each of R3-R7 is independently H, halogen, optionally-substituted alkyl, amino, alkoxy or hydroxy; R8 is an optionally-substituted heterocycloalkyl; and a is 0 to 3.

Abstract: The present disclosure relates to solid state forms of Entrectinib, processes for the preparation thereof, pharmaceutical formulations/compositions thereof, and methods of use thereof.

Abstract: A novel compound is provided. In addition, a light-emitting element with high emission efficiency and a long lifetime is provided. An organic compound represented by General Formula (G0), including a dibenzocarbazole skeleton and two amine skeletons. In General Formula (G0), A represents a substituted or unsubstituted dibenzocarbazole skeleton. The dibenzocarbazole skeleton and the amine skeletons may be bonded to each other through or not through an arylene group. In addition, a light-emitting element including the compound is provided.

Abstract: Benzoxazine compounds, methods of making them, polymers made therefrom and methods of polymerizing the benzoxazines. These renewable benzoxazine monomers and polymers that utilize the variety of building blocks found in renewable plant biomass, demonstrate excellent processability and large temperature windows for processing of resin systems.

Abstract: The present disclosure relates to reagents and method for performing trifluoromethylation, difluoromethylation or alkylation of aromatic or heteroaromatic rings in a redox-neutral manner without any catalyst which are enabled by light. In addition, there are methods for synthesizing the starting reagents used in the trifluoromethylation, difluoromethylation or alkylation reactions.

Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.

Abstract: The invention relates to novel derivatives of formula (I) where R1, R2, R3, R4, R5, X and m are as defined in the specification. These compounds which have therapeutic activity, in particular, as STAT3 inhibitors and so are useful in the treatment of proliferative diseases or conditions such as cancer. Methods for producing these compounds, novel intermediates used in the methods, pharmaceutical compositions containing them and their use in therapy form further aspects of the invention.

Abstract: The present invention addresses the problem of providing a compound for prophylaxis and/or treatment of central inflammatory diseases, or a pharmacologically acceptable salt thereof. The present invention addresses a compound of a general formula (I) or a pharmacologically acceptable salt thereof as a means to solve the problem.

Abstract: The present invention relates to benzofuran ureas or carbamates of formula I and heteroaromatic analogues thereof as described below or a tautomer or a pharmaceutically acceptable salt thereof; to a pharmaceutical composition containing these compounds, and to these compounds for use in therapy, especially for use in the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularization. Formula (I) wherein X1 is CR1 or N; X2 is CR2 or N; X3 is CR3 or N; X4 is CR4 or N; with the proviso that at most two of X1, X2, X3 and X4 are N; E1 is O or NR6a; E2 is O or NR6b; with the proviso that E and E2 are not simultaneously O; L1 is a bond, optionally substituted C1-C6-alkylene or C3-C8-cycloalkylene; L2 is a bond, optionally substituted C1-C6-alkylene, C3-C8-cycloalkylene, etc.

Abstract: The present invention relates to compounds of the formula I as described below or a tautomer or a pharmaceutically acceptable salt thereof; to a pharmaceutical composition containing such compounds; and to said compounds of the formula I or a tautomer or a pharmaceutically acceptable salt thereof for use as a medicament, especially for use in the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularization, wherein X1 is CR1 or N; X2 is CR2 or N; X3 is CR3 or N; X4 is CR4 or N; Y1 is N, NR5a, S, O or CR5b; Y2 is N, NR5c, S, O or CR5d; Z is N or C; with the proviso that at most two of X1, X2, X3 and X4 are N; with the proviso that Y1 is not O if Y2 is CR5d and simultaneously Z is C; with the proviso that Y1 and Y2 are not both simultaneously O or S; with the proviso that at least one of Y1, Y2 and Z is a heteroatom or heteroatom-contai

Abstract: A compound as a GLS1 inhibitor as represented by formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: This application is directed to inhibitors of RAD51 represented by the following structural formula, and methods for their use, such as to treat cancer, autoimmune diseases, immune deficiencies, or neurodegenerative diseases.

Abstract: Provided is a production method of a thiazole derivative represented by the formula (I), which has an adenosine A2A receptor antagonistic action and is useful as a therapeutic agent for, for example, Parkinson's disease, sleep disorder, analgesic resistance to opioid, migraine, movement disorder, depression, anxiety disorder and the like. Also provided is a production method of a compound represented by the formula (C), which contains (i) a step of reacting a compound represented by the formula (A) and a compound represented by the formula (B), and the like: (wherein R1 represents furyl, R4, R5 and R6 are the same or different and each represents lower alkyl or aryl, R2 represents pyridyl or tetrahydropyranyl, and X1 represents halogen).