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: The invention discloses a synthesizing method of benzimidazole derivant and intermediate, which is characterized by the following: proceeding arylation among aryl halide and primary amine; adopting L-pro as additive, cuprous iodide as catalyst; proceeding molecular arylation coupling reaction for aryl iodide or aryl bromide and primary amine; adopting iodo phenylamine compound and bromophenylamine compound as starting material; synthesizing the material through several-step transformation.

Abstract: The present disclosure relates to a nitrogen-containing compound, and an organic electroluminescent device and an electronic apparatus including the same. The nitrogen-containing compound of the present disclosure includes a tetramethylcyclohexanocarbazole group and a nitrogen-containing heteroaryl group, and when the nitrogen-containing compound is used as a host material of an organic electroluminescent device, the luminous efficiency of the device can be significantly improved.

Abstract: Provided herein are compounds of formula (I?): or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein Y2, Y3, L1, L2, X1, X2, X3, X4, X5, Q1, R1, R2, Rk, Rm, and Rn are as defined elsewhere herein. Also provided herein are methods of preparing compounds of formula (I?). Also provided herein are methods of inhibiting GYS1 and methods of treating a GYS1-mediated disease, disorder, or condition in an individual in need thereof.

Abstract: The present invention relates to a heteroaryl derivative compound and a use thereof. The heteroaryl derivative of the present invention exhibits excellent inhibitory activity against HER2 and EGFR, and thus can be effectively used as a therapeutic agent for HER2- and/or EGFR-associated diseases.

Abstract: Testis-restricted melanoma antigen (MAGE) proteins are frequently hijacked in cancer and play a critical role in tumorigenesis. These proteins assemble with E3 ubiquitin ligases and function as substrate adaptors that direct the ubiquitination of novel targets, including key tumor suppressors. However, the development of MAGE-directed therapeutics heretofore has been extremely limited. In one aspect, the disclosure relates to compounds and peptides useful as inhibitors of MAGE-All: substrate interaction, methods of making same, pharmaceutical compositions comprising same, and methods of treating a disorder associated with a MAGE-All dysfunction. e.g., a cancer, using same. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

Abstract: Described herein are compounds that are kinase inhibitors. The disclosed compounds have improved properties that lead to specific targeting of kinases without inhibiting the activity of related enzymes including, making them useful for therapeutic intervention in a variety of disorders and disease in which inhibition of the kinase can be clinically useful, e.g., Alzheimer's disease and other neurodegenerative diseases. In further aspects, the disclosed compounds can be used in methods of treating a neurodegenerative disease associated with inflammation, such as Alzheimer's disease, Huntington's disease, Parkinson's disease, epilepsy, stroke, amyotrophic lateral sclerosis (ALS), spinal muscular atrophy (SMA), or a disease or disorder such as deafness, glaucoma, organ failure, or cancers, including, but not limited to, those susceptible to combination therapy with epigenetic targets such as those associated with bromodomain (BRD) proteins, histone deacetylases (HDACs), and the like.

Abstract: The instant disclosure describes compounds having IL-6 modulating activity, pharmaceutical compositions and kits thereof, and methods of treating diseases, disorders or symptoms thereof mediated by IL-6.

Abstract: Provided herein are novel compounds (e.g., Formula I or II), pharmaceutical compositions, and methods of using related to Tyrosine kinase 2 (TYK2). The compounds herein are typically TYK2 inhibitors, which can be used for treating a variety of diseases or disorders, such as an autoimmune disorder or an inflammatory disorder, e.g., psoriasis, psoriatic arthritis, Crohn's disease, ulcerative colitis, inflammatory bowel disease, and/or systemic lupus erythematosus.

Abstract: The present invention provides a compound represented by chemical formula I and a control composition comprising same.

Abstract: Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.

Abstract: The present disclosure relates to crystalline solid forms of a stimulator of soluble guanylate cyclase (sGC), Compound I. Also provided herein are methods for the preparation of these solid forms. The invention also relates to pharmaceutical formulations and dosage forms comprising these solid forms and their uses thereof, alone or in combination with one or more additional agents, for treating and/or preventing various diseases or disorders; these diseases or disorders are ones that may benefit from sGC stimulation or from an increase in the concentration of nitric oxide (NO) and/or cyclic guanosine monophosphate (cGMP).

Abstract: The present invention relates to a benzamide derivative, a method for preparing same, and a pharmaceutical composition for the prevention or treatment of cancer, containing same as an active ingredient. The benzamide derivative according to an aspect of the present invention can be used in the prevention or treatment of cancer by suppressing EGFR mutation, and, when administered in combination with an EGFR antagonist such as cetuximab, exhibits a significantly synergistic effect on anticancer activity, and thus can be effectively used as an anticancer agent.

Abstract: The present disclosure encompasses solid state forms of Lanifibranor, in embodiments crystalline polymorphs of Lanifibranor, processes for preparation thereof, and pharmaceutical compositions thereof.

Abstract: The invention provides novel anilino-pyrazole derivatives as a cyclin-dependent kinase 2 (CDK2) inhibitors. The invention also provides pharmaceutical compositions comprising the compounds and methods thereof for treating various conditions, diseases and disorders associated with or related to CDK2 activities, or associated with abnormal cell growth, such as tumor growth and cancer.

Abstract: A compound represented by the following general formula (1) that has an activity of suppressing a virus protease and an antiviral activity and has a low toxicity to a host cell:

Abstract: Provided herein are compounds that modulate glucocerebrosidase (GCase), an enzyme whose activity is associated with neurological diseases and disorders (e.g., Gaucher's disease, Parkinson's disease). Also provided are pharmaceutical compositions and kits comprising the compounds, and methods of treating GCase-related diseases and disorders (e.g., Gaucher's disease, Parkinson's disease) with the compounds in a subject, by administering the compounds and/or compositions described herein.

Abstract: The present disclosure relates to an organic compound including at least one fused hetero aromatic moiety with at least one nitrogen atom linked to a triazine moiety directly or through a linking group and a benzothiazole moiety linked to the triazine moiety, and substituted with at least one of deuterium and a deuterium-substituted group, an organic light emitting diode and an organic light emitting device having the organic compound. The organic light emitting diode and the organic light emitting device where an emissive layer includes the organic compound have beneficial luminous efficiency and luminous lifespan.

Abstract: Provided herein are compounds of formula (I) and (II), or salts, esters, tautomers, prodrugs, zwitterionic forms, or stereoisomers thereof, as well as pharmaceutical compositions comprising the same. Also provided herein are methods of using the same in modulating (e.g., inhibiting) KRAS (e.g., KRAS having a G12D mutation) and treating diseases or disorders such as cancers in subjects in need thereof.

Abstract: Heterobifunctional compounds (e.g., bi-functional small molecule compounds) and compositions comprising one or more of the heterobifunctional compounds are provided. The heterobifunctional compounds are used for the treatment of certain disease in a subject in need thereof. Methods for identifying such heterobifunctional compounds are also presented.

Abstract: The present invention relates to bifunctional compounds, compositions, and methods for treat diseases or conditions mediated by aberrant activity of at least one class IIa histone deacetylase (HDAC4/5/7/9).

Abstract: Compounds of the formula (I) wherein R1, R2, R3, L and Y have the designations described herein, or a pharmaceutically or veterinarily acceptable salt, hydrate or solvate thereof. Further, the invention relates to processes for the preparation of compounds of the formula (I) or a pharmaceutically or veterinarily acceptable salt, hydrate or solvate thereof. The invention also relates to compounds of the formula (I) or a pharmaceutically or veterinarily acceptable salt, hydrate or solvate thereof for use as a medicament. Further, the invention relates to compounds of the formula (1) or a pharmaceutically or veterinarily acceptable salt, hydrate or solvate thereof for use in the amelioration, prevention and/or treatment of a disease caused by or related to delipidation of a neural tissue. In particular, the disease is a neurodegenerative disease.

Abstract: Disclosed are fused imidazole derivatives, preparation methods therefor and medical uses thereof. Specifically, the present disclosure relates to a fused imidazole derivative as shown in general formula (IM), a preparation method therefor, a pharmaceutical composition containing the derivative, and the use of same as a therapeutic agent, in particular the use thereof as a GLP-1 receptor agonist, and the use thereof in the preparation of drugs for the treatment and/or prevention of diabetes.

Abstract: Disclosed are a compound of formula (I), a preparation method therefor, and a medical application thereof. In particular, provided are the compound of formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof. These compounds are agonists of a glucagon-like peptide-1 receptor (GLP-1R). The present invention also relates to a pharmaceutical composition containing these compounds and use of the compound in a drug for treating diseases such as diabetes.

Abstract: The present disclosure provides compounds and methods for inhibiting DNA-dependent protein kinase (DNA-PK). Aspects of the present disclosure also include methods of using the compounds to treat diseases, including, but not limited to, cancer. In certain embodiments, the compounds inhibit DNA-PK and thus sensitize cancers to therapies such as chemotherapy and radiotherapy. Certain compounds of the present disclosure are in the form of prodrugs that release the DNA-PK inhibitor in hypoxic tissue such as is known to occur in cancers. Aspects of the present disclosure also include methods of using the compounds for repairing a DNA break in a target genomic region or for modifying expression of one or more genes or proteins. Compounds provided are of formula.

Abstract: The present disclosure provides autotaxin (ATX) inhibitor compounds and compositions including said compounds. The present disclosure also provides methods of using said compounds and compositions for inhibiting ATX. Also provided are methods of preparing said compounds and compositions, and synthetic precursors of said compounds.

Abstract: This disclosure relates to GLP-1 agonists of Formula (I), including pharmaceutically acceptable salts and solvates thereof, and pharmaceutical compositions including the same.

Abstract: The disclosure relates to bifunctional KRAS-modulating compounds having the structure K-L-T, where K is a targeting group that binds specifically to a KRAS protein (mutant or wild-type), T is an E3-ligase binding group, and L is absent or is a bivalent linking group that connects K and T together via a covalent linkage. Compounds and pharmaceutical compositions thereof can promote degradation of KRAS protein (mutant or wild-type) in a cell and are thus useful for treating, inhibiting, and preventing KRAS-associated diseases, disorders and conditions, including cancers.

Abstract: The present disclosure includes substituted 1-aryl-1?-heteroaryl compounds, substituted 1,1?-biheteroaryl compounds, analogues thereof, and compositions comprising the same. Such compounds and analogues comprises compounds of formula (I). In one aspect, the compounds contemplated in the disclosure can be used to treat, ameliorate, and/or prevent hepatitis B virus (HBV) and/or hepatitis D virus (HDV) infections in a patient. In another aspect, the compounds contemplated in the disclosure can be used to treat, ameliorate, and/or prevent cancer in a patient.

Abstract: The present invention relates compounds of general formula (I) and stereoisomers and pharmaceutically acceptable salts thereof; wherein R1, R2, R7, Ra, Rb, Rc, and the dotted line is as defined in the claims. The invention also relates to pharmaceutical compositions comprising a compound of formula (I) and to said compounds for use as a medicament and particularly in the treatment or prevention of drug addiction and CNS related diseases and conditions. Further, the invention relates to methods for the preparation of a compound of formula (I), or pharmaceutically acceptable salt or a stereoisomer thereof.

Abstract: The present invention relates to new compounds of formula (I?): as sigma ligands having a great affinity for sigma receptors, sigma-1 receptor (?1) and/or sigma-2 receptor (?2). The present invention also refers to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.

Abstract: Compounds of Formula I that inhibit AXL, and compositions containing the compound(s) and methods for synthesizing the compounds, are described herein. Also described are the use of such compounds and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by AXL.

Abstract: Compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds disclosed herein or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.

Abstract: The present invention relates generally to compositions and methods for treating cancer, e.g. by using the compounds of formula (I). Provided herein are substituted bicyclic heteroaryl derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of Calcium/calmodulin-dependent protein kinase kinase 2. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.

Abstract: In one aspect, the disclosure relates to a scaffold for a class of small molecules that selectively inhibit the ?3?4 nicotinic acetylcholine receptor (nAChR) subtype, as well as molecules constructed using the scaffold and syntheses thereof. In some aspects, the scaffold can be used as a basis for synthesizing additional molecules capable of selectively inhibiting other nAChR subtypes. In a further aspect, the disclosed small molecules can be used as molecular probes to investigate the function of different nAChR subtypes and as potential treatments for addiction and other diseases.

Abstract: The present invention provides a compound having the basic structure shown by Formula (I) in which the indole ring and the pyrazolopyridine structure is bound through a substituent, a salt thereof or a solvate of either the compound or a salt of the compound, as well as a preventative agent or a therapeutic agent for non-insulin-dependent diabetes mellitus (Type 2 diabetes) or obesity containing such compound, salt or solvate as an active ingredient.

Abstract: This invention provides rho-associated protein kinase (ROCK) inhibiting compounds for therapeutic applications as described further herein.

Abstract: Compounds, such as cathinone derivatives, and pharmaceutical formulations that include the compounds. The compounds may have a first selectivity for a first receptor subtype that is at least 10 times greater than a second selectivity for a second receptor subtype from the same class of receptors. Methods of treating patients, which may include administering to a patient a pharmaceutical formulation that includes a compound, such as a cathinone derivative.

Abstract: The present invention relates to tricyclic compounds, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.

Abstract: Compounds for use in treating or preventing human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof. Methods associated with the preparation and use of the disclosed compounds, as well as pharmaceutical compositions comprising such compounds are also disclosed.

Abstract: The application relates to pyrazolo[1,5-a]pyrimidine derivatives of formula (IV) as Trk kinase inhibitors for treating cancer and inflammatory diseases.

Abstract: Disclosed herein are novel bifunctional compounds formed by conjugating BTK inhibitor moieties with E3 ligase Ligand moieties, which function to recruit targeted proteins to E3 ubiquitin ligase for degradation, and methods of preparation and uses thereof.

Abstract: A phenyldihydropyrimidine compound as represented by formula I, a tautomer or a pharmaceutically acceptable salt thereof. The phenyldihydropyrimidine compound has a good anti-HBV activity and can be used for preparing drugs for treating and/or preventing HBV infections.

Abstract: The present invention relates to novel cGAS inhibitor compounds, having a formula of: to pharmaceutical compositions comprising the compounds, and to methods of using the compounds and compositions to treat certain pathological conditions such as immune-mediated diseases.

Abstract: Methods are provided for modulating MRGPRD generally, or for treating a MRGPRD dependent condition more specifically, by contacting the MRGPRD or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I): or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein A, B, C, D, L, R1, R2, R3, R4, m, n, and p are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.

Abstract: The present disclosure provides certain phenylpiperidine derivatives, and pharmaceutically acceptable salts thereof, that are inhibitors of Glutaminyl-peptide cyclotransferase (QPCT) and glutaminyl-peptide cyclotransferase-like protein (QPCTL), and are therefore useful for the treatment of diseases treatable by inhibition of QPCT/L. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.

Abstract: The present invention is related to processes for preparing itacitinib, or a salt thereof, and related synthetic intermediates related thereto.

Abstract: The present invention relates to nitrogen-containing heterocyclic compounds suitable for use in electronic devices, and to electronic devices, especially organic electroluminescent devices, comprising these compounds.

Abstract: A heterocyclic compound as a Janus kinase (JAK) inhibitor or a pharmaceutically acceptable salt thereof are provided, including a compound as represented by general formula (I) or a pharmaceutically acceptable salt thereof. A process for preparing the compound or a pharmaceutically acceptable salt thereof is provided. The compounds can be used for treating and/or preventing JAK-mediated related diseases, in particular inflammatory diseases, autoimmune diseases, and cancers.

Abstract: Provided are a crystal form of a triazolopyridine-substituted indazole compound and a preparation method therefor; and specifically disclosed are a crystal form of a compound as represented by formula (I) and a preparation method therefor.