Abstract: To provide a light-emitting element having high luminous efficiency and to provide a light-emitting device and an electronic device which consumes low power and is driven at low voltage, a carbazole derivative represented by the general formula (1) is provided. In the formula, ?1, ?2, ?3, and ?4 each represent an arylene group having less than or equal to 13 carbon atoms; Ar1 and Ar2 each represent an aryl group having less than or equal to 13 carbon atoms; R1 represents any of a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a substituted or unsubstituted phenyl group, and a substituted or unsubstituted biphenyl group; and R2 represents any of an alkyl group having 1 to 6 carbon atoms, a substituted or unsubstituted phenyl group, and a substituted or unsubstituted biphenyl group. In addition, l, m, and n are each independently 0 or 1.

Abstract: The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof, is useful as an agent for the prophylaxis or treatment of narcolepsy.

Abstract: The present invention relates to a method for synthesizing N,N?-bis(2,2,6,6-tetramethyl-4-piperidyl)-1,3-benzenedicarboxamide as shown in the following formula (III), comprising the following steps that a compound of the following formula (I) and a compound of the following formula (II) react under stirring in an organic solvent in the presence of a solid supported catalyst, and after the completion of the reaction, a compound of the formula (III) is obtained by post-treatment, wherein R1 to R2 are each the same or different selected from C1-6 alkyl. The method can achieve good technical effects through the use of a unique catalyst and the compounding of the organic solvent, has the advantages of reduced pollution, good environment and significant improvement on yield is compared with the prior art, can provide more inexpensive functional additives for the field of plastic processing, and has good industrial production prospects and application potential.

Abstract: Treatment methods including administering a compound according to Formula (I) Meta or para or a pharmaceutically acceptable salt thereof wherein: A11-A14 are N or CR11, CR12, CR13, CR14, respectively, with the proviso that no more than two of the four positions A in A11-A14 are simultaneously N; A6, A7, A8, A9, A10 are N or CR6, CR7, CR8, CR9, CR10, respectively, with the proviso that at least one but no more than two of the five positions A in A6, A7, A8, A9, A10 is N; R1 is C(2-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, (di)C(3-6)cycloalkylamino or (di)(C(3-6)cycloalkylC(1-3)alkyl)amino; R5 is H, hydroxyethyl, methoxyethyl, C(1-6)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl, C(1-9)heteroarylC(1-3)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(2-5) heterocycloalkyl or C(2-5)heterocycloalkylC(1-3)alkyl; —SO2R1 is represented by one of R7, R8 or R9; R15 is H, C(1-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)hetero

Abstract: The present invention provides an inhibitor of Bruton's tyrosine kinase, which is a compound of formula (I), or its pharmaceutically acceptable salt, solvate, ester, acid, metabolite or prodrug. The present invention also provides a pharmaceutical composition comprising the compound. The present invention also provides a method for inhibiting the activity of tyrosine kinase activity or for treating a disease, disorder, or condition, which would benefit from the inhibition of Bruton's tyrosine kinase(s), by using the Bruton's tyrosine kinase inhibitor, as well application of the Bruton's tyrosine kinase inhibitor for the same.

Abstract: The present invention provides solid forms and compositions thereof, which are useful as an inhibitor of S-nitrosoglutathione reductase and which exhibit desirable characteristics for the same.

Abstract: Provided are a sodium salt of a uric acid transporter inhibitor and a crystalline form thereof, In particular, provided are a uric acid transporter (URAT1) inhibitor 1-((6-bromo-quinoline-4-yl)thio)cyclobutyl sodium formate (the compound of formula (I)), a crystal form I, and preparation method thereof. The obtained crystal form I of the compound of formula (I) has a good crystal form stability and chemical stability, and the crystallization solvent used has a low toxicity and low residue, and can be better used in clinical treatment.

Abstract: Disclosed are Indole and Indazole derivatives, method for preparing these compounds, and methods for treating cancers.

Abstract: The present invention is directed to aminobenzimidazole derivative compounds and compositions comprising thereof. The present invention also relates to uses of these compounds to treat or prevent several conditions including neoplasia, dysplasia metaplasia, and cancer.

Abstract: Novel compositions of matter based on homopiperazine precursor materials and forming a homopiperazine-based ligand are disclosed, along with suitable techniques and materials for the synthesis and utilization thereof. In particular various synthetic schemes and techniques for applying the disclosed compositions of matter as a decontaminating agent. The decontaminating agents include homopiperazine-based ligand-metal complexes that are particularly effective at neutralizing toxicity of nerve agents, pesticides, and other toxic organophosphorus-based compounds. In preferred approaches, the homopiperazine-based ligand-metal complexes act as catalysts to facilitate substitution of a leaving group of the organophosphorus-based compound with a functional group that does not permit the organophosphorus-based compound to inactivate acetylcholinesterase upon introduction of the organophosphorus-based compound to a living organism such as insects and mammals.

Abstract: A process for producing biguanidine salts of formula (III) and s-triazines of formula (V) is described. Therein, R1 and R2 are in each case hydrogen, halogen and alkyl, and R3 and R4 are in each case hydrogen, alkyl, cycloalkyl and aryl.

Abstract: According to the invention there is provided a compound of formula I, wherein R1 and R2 have meanings given in the description, which compounds are useful in the treatment of skin disorders and other diseases.

Abstract: The present application relates to functionalized 1,2,4,5-tetrazine compounds. The compounds are useful in compositions and methods using bioorthogonal inverse electron demand Diels-Alder cycloaddition reactions for the rapid and specific covalent delivery of a “payload” to a ligand bound to a biological target.

Abstract: The present invention provides a prophylactic or therapeutic agent for an autism spectrum disorder containing compound (I) having melatonin receptor affinity. A compound represented by the formula: wherein each symbol is as described in the specification, or a salt thereof.

Abstract: Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of HIV; including the prevention of the progression of AIDS and general immunosuppression.

Abstract: An acyclic fluorinated compound of formula (I) is amine-containing acyclic hydrofluoroethers. The acyclic fluorinated compound is useful as heat transfer, solvent cleaning, fire extinguishing agents and electrolyte solvents and additives.

Abstract: The present invention relates to an indoleamine 2,3-dioxygenase inhibitor having the structure of formula (I), a preparation method therefor, and an application. The IDO inhibitor is an N?-hydroxyl-N-phenylformamidine derivative, which has a high inhibitory activity on IDO, effectively inhibits IDO activity, and may also be used to inhibit patient immunosuppression. The inhibitor may be widely applied to treat or prevent cancers or tumors, viral infections, depression, neurodegenerative disorders, trauma, age-related cataracts, organ transplant rejection or autoimmune diseases, and has the potential to be developed into a new generation of immunosuppressors.

Abstract: Prodrugs of tizoxanide, an analogue or salt thereof are disclosed. The prodrugs have an ester moiety comprising an amino acid moiety, and increase the bioavailability of the tizoxanide, an analogue or salt thereof. Compositions and methods of treating an intracellular protozoan infection, a viral infection or a cancer are also disclosed.

Abstract: The invention relates to a method for synthesis of 1-[2-(2,4-Dimethyl-phenylsulfanyl)-phenyl]piperazine in the presence of a strong base.

Abstract: The invention relates to a method for arylation of amines, such as aliphatic amines by reaction of aryl-halogens, e.g. chloro- or fluorobenzene derivatives without strongly electron withdrawing substituents in the presence of a strong base.

Abstract: The present invention relates to a type of aryl benzofuran amidated derivatives, the medical use thereof, and the preparation method; said derivatives have antioxidation activity, and xanthine oxidase inhibitory activity, and can be used for antioxidation and for preparing compositions, drugs and health products and treating gout and hyperuricemia.

Abstract: The inventive subject matter provides compounds, compositions and methods for lowering serum acid (sUA) for the treatment of gout, and having reduced liver toxicity, associated with CYP2C9 metabolic pathway.

Abstract: A urolithin-containing aqueous solution containing urolithin and collagen, a dried solid composition thereof, methods for producing these, and a stabilization method for urolithin.

Abstract: The present invention provides a new compound of formula (I): extracted from a seaweed, and its use for inhibiting the growth of cancer cells, as well as methods for its extraction and isolation.

Abstract: The present invention relates to novel compounds, comprising an 8- or 9-membered cyclic structure, wherein an (E)-1,4-dioxo-but-2-ene moiety is embedded in said cyclic structure and to pharmaceutical compositions comprising these compounds. The compounds may be used as medicaments, in particular as medicaments for treating and preventing microbial infections, such as infections by multidrug resistant and/or Gram-positive bacteria. The invention further relates to fermentation processes wherein fungi of the genus Ulocladium are used for producing the novel compounds.

Abstract: The present application relates to compounds of a formula (I), to the use thereof in electronic devices, and to processes for preparing the compounds.

Abstract: The present invention can provide a method for producing 1,2,3,5,6-pentathiepane, comprising Steps A and B: Step A: a step of synthesizing a tetrathiocarbonate in a protic solvent; and Step B: a step of carrying out reaction between the tetrathiocarbonate and a dihalogenated methane in a mixed solvent (where the mass ratio of a protic solvent and an aprotic solvent is 13:87-38:62).

Abstract: Described herein are hypervalent iodine reagents.

Abstract: The object of the invention relates to a novel group of compounds of general formula 20 that may be used as an intermediate for the production of the pharmaceutical active substance pomalidomide. The object of the invention also relates to a novel, cost-effective, productive method for the production of pomalidomide that can also be implemented on industrial scales via the novel compound of formula 20 according to the invention.

Abstract: A compound represented by formula (I) or an N-oxide compound thereof is provided with excellent control efficacies against harmful arthropods, wherein A1 represents a nitrogen atom or a CR4; R4 represents a hydrogen atom, a OR27, a NR27R28, a cyano group, a nitro group, or a halogen atom; hereinafter referred to as “Het”, represents Het-1, Het-2, Het-3, or Het-4: wherein #1 represents the binding position of Het and T, and #2 represents the binding position of Het and T represents T-1, T-2, T-3, T-4, T-5, T-6, or T-7: R1 represents a C1-C10 chain hydrocarbon group having one or more halogen atoms or the like; and R2 represents a C1-C6 alkyl group optionally having one or more halogen atoms or the like.

Abstract: The purpose of the present invention is to provide a compound having excellent antibacterial activity against mycobacterium tuberculosis, multidrug-resistant tuberculosis bacteria, and/or non-tuberculous acid-fast bacteria. A compound represented by formula [I]: (in the formula, each symbol is as described in the attached specification), or a salt thereof can be used to diagnose, prevent, and/or treat tuberculosis.

Abstract: Pyridazine derivatives that activate the excitatory amino acid transporter 2 (EAAT2), and methods of use thereof for treating or preventing diseases, disorders, and conditions associated with glutamate excitotoxicity.

Abstract: The present invention relates to compounds that are antagonists of the orexin-1 receptor. The compounds have the structural formula (I) defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or disorders associated with orexin-1 receptor activity.

Abstract: The present invention relates to compounds of the general formula (I) in which Q, V, T, W, X, Y and A have the meanings given in the description—and to their use for controlling animal pests.

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: Provided herein are Mcl-1 antagonist compositions and methods of treating cancer using the compositions described herein.

Abstract: The present invention provides compounds having a CB1 receptor-binding moiety and a directing moiety. In related aspects, the invention provides pharmaceutical compositions containing compounds of the invention, methods for inhibiting a pathway modulated in part by the CB1 receptor activity, and methods for treating a condition or disorder mediated in part by CB1 receptor activity. In certain embodiments, the compounds are compounds of Formula I. Methods of preparing compounds of Formula I are also described. In another aspect, the invention provides methods of identifying a selective agonist of the beta-arrestin pathway over the G-protein pathway.

Abstract: Provided herein are Itraconazole analogs. Also provided herein are methods of inhibition of Hedgehog pathway, vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, angiogenesis and treatment of disease with Itraconazole analogs.

Abstract: This invention relates to compounds of general formula (I) in which R1, R2, R3, R4, L, X and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.

Abstract: A process for preparing compounds of formula (I), or a salt or solvate thereof, including Brexpiprazole, which process comprises cyclization of a compound of formula (II) or (III), or a salt or solvate thereof. The invention also refers to intermediates of said process.

Abstract: A method is provided for producing a compound represented by formula (3), wherein n is 1, 2, 3 or 4, by mixing a compound represented by formula (2), a tri(C1-C3 alkyl)silyl(C1-C4 perfluoroalkane) and a fluoride. A method for producing the compound represented by formula (3) contains a step for producing the compound represented by formula (2) by an intramolecular dehydration condensation of a compound represented by formula (1) and by a step for mixing the compound represented by formula (2), a tri(C1-C3 alkyl)silyl(C1-C4 perfluoroalkane) and a fluoride.

Abstract: The present invention relates to compounds of formula I wherein the variables are as defined in the claims and the description. The invention further relates to the use of these compounds for controlling invertebrate pests and to plant propagation material and [o an agricultural and a veterinary composition comprising said compounds. The invention also relates to novel compounds useful as intermediate compounds in the preparation of compounds I.

Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.

Abstract: The present invention relates to a synthesis process of suvorexant, novel compounds represented by formulas II, III, IV or V, or salts thereof for preparing suvorexant, and a method for preparing the intermediates. The preparation method uses a chiral starting material to synthesize chiral compounds represented by formulas II, III, IV or V, the compounds obtained being used for synthesizing the suvorexant. The preparation method has the advantages of simple operation, low cost, mild reaction conditions, simple post-treatment, easy to purify, high yield, high ee value for the product, and easy to industrialize. In the reaction route shown, R represents benzyl, allyl or 1-phenethyl, or optionally substituted benzyl at the 2 position to 6 position, such as 4-methoxybenzyl, 4-nitrobenzyl, 2-methylbenzyl, 4-chlorobenzyl or 3-fluorobenzyl.

Abstract: A series of 3-imino-5-methyl-1,2,4-thiadiazinane 1,1-dioxide derivatives of formula (I), substituted in the 5-position by a phenyl moiety NH which in turn is meta-substituted by an optionally substituted fused bicyclic heteroaromatic ring system containing at least one nitrogen atom, being selective inhibitors of plasmepsin V activity, are beneficial as pharmaceutical agents, especially in the treatment of malaria.

Abstract: The present invention provides crystalline form of (R)-propylene glycol solvate of dasatinib and crystalline form of (S)-propylene glycol solvate of dasatinib.

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: Provided are a novel organic semiconductor compound, a production method thereof, and an organic electronic device using the same, wherein the organic semiconductor compound includes a thiazolidine functional group introduced into a heteroaromatic ring to thereby remarkably improve photovoltaic characteristics of an organic electronic device including the same.

Abstract: The invention relates to novel heteroaryl carboxamides, processes for their preparation, and their use for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.

Abstract: The present invention is directed to imidazo[1,5-a]pyridine and imidazo[1,5-a]pyrazine derivatives of Formula I, or a pharmaceutically acceptable salt thereof, which are LSD1 inhibitors useful in the treatment of diseases such as cancer.