Abstract: The present invention provides dihydroquinolinone compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.

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 disclosure relates to compounds of formula (I), which are formyl peptide 2 (FPR2) receptor agonists and/or formyl peptide 1 (FPR1) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, and related diseases.

Abstract: Disclosed are a compound as shown in general formula I, a pharmaceutically acceptable salt, an isomer or a mixture thereof, and a solvate, a polymorph, a stable isotope derivative or a prodrug thereof. The compound of the present disclosure has comparatively strong PARP inhibitory activity and can be used for treating diseases associated with PARP, such as cancers and inflammatory diseases.

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: The present invention relates to triaminopyrimidine compound 1, or pharmaceutically acceptable salts thereof, or hydrates, or solvates, or polymorphs, or optically active forms thereof, in solid state forms. The invention also relates to a process for preparation of triaminopyrimidine compound and intermediates thereof. The present invention also relates to a pharmaceutical composition comprising pure triaminopyrimidine compound, useful for preventing or treating malaria.

Abstract: A heterocyclic compound represented by Formula 1, a composition including the same, and an organic light-emitting device including the heterocyclic compound: L1 to L4, L11, a1 to a4, a11, Ar1, Ar2, Ar11, R1 to R7, R11 to R12, b1 to b7, and b11 to b12 are described in the specification.

Abstract: The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, its salt forms, and novel polymorphic forms of these salts.

Abstract: This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases onused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.

Abstract: A diprovocim compound that corresponds in structure to structural Formula V is disclosed, wherein A, W, Z, R1, R2, R3 and R4 (when present) are defined within. A diprovocim compound has immune-adjuvant properties on human and mouse cells in culture and on in vivo immunization of mice. A composition containing a diprovocim and a method of using a compound are also disclosed. A The immunostimulatory activity of a diprovocim compound is similar to that of LPS, to which there is no apparent structural similarity. A contemplated compound bears no structural similarity to either the TLR1/TLR2 lipoprotein agonists nor to any other synthetic TLR agonist, and is remarkably easy to prepare and synthetically modify.

Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, PCSK9, or a pharmaceutically acceptable salt, solvate, prodrug or polymorph thereof, and to compositions and formulations comprising such compounds, and methods of using and making such compounds. Compounds include comprising of Formula (I): (I) wherein A, D and Q are described herein.

Abstract: Provided herein are compounds and methods for modulating abnormal repeat expansions of gene sequences. More particularly, provided are dimeric inhibitors of RNA and the uses of such inhibitors in regulating nucleotide repeat expansions, e.g., to treat Myotonic Dystrophy Type 1 (DM1), Myotonic Dystrophy Type 2 (DM2), Fuchs dystrophy, Huntington Disease, Amyotrophic Lateral Sclerosis, or Frontotemporal Dementia.

Abstract: The present invention relates to a pyrimidine derivative, a method for preparing same and use thereof in medicine. In particular, the present invention relates to a pyrimidine derivative represented by general formula (I), a method for preparing same and a pharmaceutically acceptable salt thereof as well as use thereof as a therapeutic agent, in particular as a FGFR4 kinase inhibitor, definitions of each substituent in the general formula (I) being the same as those defined in the description.

Abstract: Described herein are compounds of the formulae (I)-(III) and (Ia)-(IIIa) and pharmaceutically acceptable salts, isomers, mixture of isomers, crystalline forms, non-crystalline forms, hydrates, or solvates thereof, as well as methods using compounds of the formulae (I)-(III) and (Ia)-(IIIa) to, among other things, treat cancer.

Abstract: The present disclosure provides a class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: (insert Formula I structure) wherein variables W, X, Y, R2, R2?, R3, R4, R5, R6, and R7 of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to beta amyloid (A?) plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, and other central nervous system conditions.

Abstract: [Object] It is an object of the present invention to provide an organic EL device in which various materials for an organic EL device, which is excellent in hole injection/transport performance, electron injection/transport performance, electron blocking performance, stability in a thin film state, and durability, are combined so that properties of each of the materials can be effectively expressed, thereby achieving (1) high light emission efficiency and power efficiency, (2) a low light emission start voltage, (3) a low practical driving voltage, and particularly (4) a long lifetime.

Abstract: New compounds and a method of treating a retinal disease that leads to photoreceptor loss or outer-retina degeneration, including administering compound of the formula (I) or a pharmaceutically acceptable salt, a racemic mixture, a corresponding enantiomer or, if applicable, a corresponding diastereomer thereof, wherein: A is a 5-oxazolyl residue or a pyridine-4-yl residue, R1 is selected from the group consisting of fluoro, chloro and methoxy; B is selected from the group consisting of a residue of formula (II), (III) and (IV) wherein, “*” denotes the point of attachment to the remainder of the molecule, and R2, R2?, R2?, R3, R3?, R3?, R4, R4?, R4?, R5, R5? and R5? are independently selected from the group consisting of hydrogen, a linear or branched alkyl having 1 to 4 carbon atoms, trifluoromethyl, 2,2,2-trifluoroethyl, methylsulfanyl, ethylsulfanyl, methylsulfonyl, ethylsulfonyl, difluoromethoxy, trifluoromethoxy, fluoro, bromo, chloro, methoxy, ethoxy, propoxy, butoxy, hydroxy and amino.

Abstract: The present invention provides a novel process for preparing an aminopyrimidine derivative or pharmaceutically acceptable salt thereof having a selective inhibitory activity against protein kinases, especially against the protein kinases for mutant epidermal growth factor receptors. And also, the present invention provides novel intermediates useful for said process and processes for preparing the same.

Abstract: Provided are an aminopyrimidine compound as shown in formula (I), a polymorph, a pharmaceutically acceptable salt, a prodrug, a stereoisomer, an isotopic variant, a hydrate or a solvate thereof, and a pharmaceutical composition containing the same and the use thereof. The aminopyrimidine compound and the composition containing the same have excellent inhibition to protein kinases, and at the same time have better pharmacokinetic parameter characteristics, and can improve the drug concentration of the compound in animals, and thereby improve the efficacy and safety of the drug.

Abstract: The present disclosure provides an organic electroluminescent compound represented by the formula (1): wherein each of R1 and R2 is independently an electron-donating group and each of n and m is independently an integer between 1 and 4. The present disclosure further provides an organic light-emitting device and an organic electroluminescent device each comprising the organic electroluminescent compound represented by the formula (I).

Abstract: The present specification discloses tripartite androgen receptor eliminators (AREs), pharmaceutical compositions and medicaments comprising such AREs, methods and uses for such AREs and compositions and medicaments, and methods and uses for AREs and compositions and medicaments for treating an androgen receptor signaling-mediated condition, disease or disorder.

Abstract: Provided is a heterocyclic compound of Formula 1: and an organic light emitting device comprising the same.

Abstract: Compositions containing the compound of general formula I: are disclosed. The compositions be used to prevent or treat hepatitis B virus infection.

Abstract: The present invention relates to a pyrrolopyridine derivative compound, a method for preparing the same, and a pharmaceutical composition containing the same as an active ingredient for the prevention or treatment of protein kinase-related diseases. A compound represented by chemical formula 1, an optical isomer thereof, or a pharmaceutically acceptable salt thereof, according to the present invention, has excellent inhibitory activity against various protein kinases including DYRK1A, and therefore, the pharmaceutical composition containing the same as an active ingredient can be favorably used in the treatment or prevention of protein kinase-related diseases. Particularly, the pharmaceutical composition can be effectively used in the prevention, treatment, or alleviation of Alzheimer's disease, dementia, or Alzheimer's dementia.

Abstract: A deuterated compound having structural formula I or a pharmaceutically acceptable salt thereof: Values and example values of the variable in formula (I) are disclosed herein. Also disclosed are the use of compounds of formula (I) in the methods of treating a disease selected from cancer, an autoimmune disease, and an infectious disease, and methods of enhancing an immune response to an antigen.

Abstract: The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

Abstract: The present invention relates to new compounds of general formula (I) that show dual activity towards ?2? subunit of voltage-gated calcium channels (VGCC), especially the ?2?-1 subunit, and to the noradrenallne transporter (NET). The invention is also related to the process for the preparation of said compounds as well as to compositions comprising them, and to their use as medicaments.

Abstract: An organic compound, an organic light emitting diode including the compound, and an organic light emitting device including the organic light emitting diode are disclosed. The organic compound may include a fused hetero aromatic moiety having a p-type property and an aza-acridine moiety having an n-type property bonded to the fused hetero aromatic moiety via an aromatic or a hetero aromatic linker. The organic compound has relatively high energy level since it includes plural fused hetero aromatic rings. Holes and electrons can be recombined in an emitting material layer in a balanced manner since the organic compound has a bipolar property. The organic light emitting diode and the organic light emitting device including the organic compound have enhanced luminous efficiency and luminous lifetime.

Abstract: The present invention provides a novel crystalline form of Valbenazine dibesylate, Valbenazine dibesylate Form APO-I, compositions and processes for the preparation thereof, and the use of this crystalline form in the treatment of hyperkinetic disorders, including tardive dyskinesia.

Abstract: The present invention provides, in part, compounds of Formula I: or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: R1, R2, L, A, and E are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M4-mediated (or M4-associated) disorders including, e.g., Alzheimer's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.

Abstract: The disclosure includes compounds of Formula (I) wherein A, W, m, R5, R6, R7, and R8, are defined herein. Also disclosed is a method for treating a neoplastic disease with these compounds.

Abstract: The present invention provides selected dihydrobenzimidazolones which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.

Abstract: A method of preparing Compound (1) or a pharmaceutically acceptable salt thereof: comprises: (a) reacting Compound (X): or a pharmaceutically acceptable salt thereof with Compound (Y): in the presence of a palladium catalyst and a carbonate or phosphate base to form compound (Z): or a pharmaceutically acceptable salt thereof; and (b) deprotecting the Ts group of Compound (Z) to form Compound (1) or a pharmaceutically acceptable salt thereof.

Abstract: Provided herein are methods of using KRAS G12C inhibitors. These methods of using the inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

Abstract: The present disclosure provides an azapyrene compound, a display panel and a display apparatus. The compound has a structure represented by Chemical Formula 1, in which X1-X4 are each a nitrogen atom or C—Ra, one or two of X1-X4 are a nitrogen atom; only one of X1 and X2 is a nitrogen atom; only one of X3 and X4 is N; Ra is mainly hydrogen, deuterium, or C1-C10 alkyl; Ar1 and Ar2 are each C6-C30 aryl or C3-C30 heteroaryl; m and n are 0, 1, 2, or 3, and when one of m and n is 0, the other one of m and n is not 0; and L1 and L2 are a single bond, C6-C30 arylene, or C3-C30 heteroarylene; p and q are 0, 1, or 2. The compound can be used as a CPL material to improve external quantum efficiency (EQE) of an organic light-emitting device and light-emitting efficiency.

Abstract: Disclosed is a class of new aryl-phosphorus-oxygen compounds as shown in formula (I) as EGFR kinase inhibitors, and pharmaceutically acceptable salts thereof.

Abstract: Compounds having the general formula (I) wherein R1, R2, Y and W are as described herein, compositions including the compounds and methods of using the compounds as autotaxin inhibitors.

Abstract: The invention provides a new convergent approach for the synthesis of 2?-fluoro-6?-methylene-carbocyclic adenosine (FMCA) and 2?-fluoro-6?-methylene-carbocyclic guanosine (FMCG) from a readily available starting material in eight steps. An efficient and practical methodology for stereospecific preparation of a versatile carbocyclic key intermediate, (1S,3R, 4R)-3-tert-butoxy -4-(tert-butoxymethyl)-2-fluoro-5-methylenecyclopentanol (compound 8 of scheme 1A or a) in only six (6) steps is also provided. Prodrugs of these compounds are also prepared.

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: Disclosed are a class of isoquinoline compounds acting as RHO protein kinase inhibitors, and the use thereof in the preparation of a drug for treating diseases associated with RHO protein kinase. Particularly disclosed are compounds as shown in formula (I) and pharmaceutically acceptable salts thereof.

Abstract: Provided is a FGFR inhibitor, designating a compound represented by formula (I) or a pharmaceutically acceptable salt thereof. Also provided is the application of a drug for treating solid tumors, such as FGFR related diseases.

Abstract: Disclosed is a compound of Formula (I), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions comprising thereof. Also disclosed is a method of treating PI3K? related disorders or diseases by using the compound disclosed herein.

Abstract: The present disclosure relates to compounds that bind to at least one of ACAT1/2 and OXCT1/2 and inhibit mitochondrial ATP production, referred to herein as mitoketoscins. Methods of screening compounds for mitochondrial inhibition and anti-cancer properties are disclosed. Also described are methods of using mitoketoscins to prevent or treat cancer, bacterial infections, and pathogenic yeast, as well as methods of using mitoketoscins to provide anti-aging benefits. Specific mitoketoscin compounds are also disclosed.

Abstract: Disclosed herein are spirocyclic compounds, together with pharmaceutical compositions and methods of ameliorating and/or treating a cancer described herein with one or more of the compounds described herein.

Abstract: Provided is a new polycyclic aromatic hydrocarbon derivative. The polycyclic aromatic hydrocarbon derivative is a derivative of a polycyclic aromatic hydrocarbon having 6 or more aromatic rings and has a substituent represented by the following formula (1). (In the formula (1), R1 and R2 are carbon atoms of the aromatic rings in the polycyclic aromatic hydrocarbon, and R3 to R5 are carbon atoms of an aromatic ring or a heterocyclic ring in a group having the aromatic ring or the heterocyclic ring. n is 0 or 1, and m is the number of substituents.

Abstract: The disclosure provides a delayed fluorescent compound of the Formula and an organic light emitting diode including a first electrode, a second electrode and an organic emitting layer between the first and second electrodes, where the delayed fluorescent compound is included in the organic emitting layer, and an organic light emitting display device including the organic emitting layer.

Abstract: The present invention relates to thienopyrimidine compound, preparation method thereof, pharmaceutical composition and use thereof, and in particular to a type of compounds having ALK and/or c-Met selective inhibitory activity, a method for the preparation thereof, a pharmaceutical composition comprising the same, and use of these compounds in the manufacture of a medicament for preventing or treating a disease associated with anaplastic lymphoma kinase in vivo, and in the manufacture of a medicament for preventing or treating a disease associated with angiogenesis or cancer metastasis, in particular in the manufacture of a medicament for preventing or treating tumor growth and metastasis.

Abstract: The present invention relates to compounds of formula (I): wherein Q is O or S; R1 is a cyclic group substituted with at least one group X, wherein R1 may optionally be further substituted; X is any group comprising a carbonyl group; and R2 is a cyclic group substituted at the ?-position, wherein R2 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 dual action of NLRP3 inhibition and the stimulation of insulin secretion.

Abstract: Disclosed are a crystal form II of a thienopyridine derivative bisulfate and a preparation method therefor and the use thereof. The X-ray powder diffraction pattern of the crystal form II represented by the 2? diffraction angle exhibits characteristic diffraction peaks at 12.86°, 13.58°, 15.58°, 17.64°, 18.42°, 21.56°, 22.90°, 23.70° and 24.64°. The crystal form can be used as an active ingredient for preparing a pharmaceutical composition for preventing and treating diseases caused by thrombi. Compared with the original crystal form, the crystal form II of the invention has a better stability, with denser bulk solid particles, and is less susceptible to static electricity, and has better fluidity and compressibility, and when used as an active ingredient for preparing a pharmaceutical composition, the pharmaceutical preparation prepared with the crystal form II has a stronger stability.

Abstract: The present invention addresses the problem of providing a novel chemically activated water-soluble prodrug. The present invention provides a compound represented by formula (1), or a pharmacologically acceptable salt thereof (in the formula, A represents A-0; X1 and X2 are the same as or different from each other and each independently represent a hydroxyl group or —O—C(?O)—Y—(C(R1A) (R1B))n-NH—R2, where X1 and X2 are not simultaneously hydroxyl groups, n is 2, 3, or 4, Y represents an oxygen atom or —NR4, R1A and R1B are the same as or different from each other and each independently represent a hydrogen atom, etc., and R2 represents a hydrogen atom, etc.; and Ra to Rd are optionally present, are the same as or different from each other, and each independently represent a hydrogen atom, etc.).