Abstract: Disclosed in the present invention are a macrocyclic compound serving as a Weel inhibitor, and applications thereof in the preparation of drugs for treating Weel-related diseases. The present invention specifically relates to a compound represented by formula (II), an isomer thereof, and a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to pyrrolo-aromatic heterocyclic compounds, a preparation method therefor and medical use thereof. Particularly, the present invention relates to a compound represented by formula I, a preparation method therefor, a pharmaceutical composition comprising the compound, and use of the compound as a BTK kinase inhibitor. The compound and the pharmaceutical composition comprising same can be used for the treating diseases associated with BTK kinase activity, such as inflammations, autoimmune disorders, and cancers. The definition of each substituent in formula I is the same as that in the description.

Abstract: Compounds of the formula (I), in which R1, R3, Het1 and HET have the meanings given in claim 1, are ATM kinase inhibitors and can be employed, inter alia, for the treatment of cancer.

Abstract: Described herein are NLRP3 modulators and methods of utilizing NLRP3 modulators in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.

Abstract: The present invention relates to compounds suitable for treating, ameliorating and/or preventing neuromuscular disorders, including the reversal of drug-induced neuromuscular blockade. The compounds as defined herein preferably inhibit the CIC-1 ion channel. The compounds include phenoxy propanoic acid, phenoxy propanoate, and phenoxy butanoate compounds.

Abstract: The present disclosure relates to Near-infrared fluorescent indicators for lysosomes and application thereof. These indicators are composed of lipophilic NIR BODIPY derivatives and ionizable bis-tertiary amine moiety, which enable the formation of a transient amphiphilic state in acidic environments specifically. This structural feature affords accurate lysosomal membrane targeting ability at nanomole staining concentration.

Abstract: There are disclosed, inter alia, methods of inhibiting an E1 enzyme, and compounds useful for inhibiting an E1 enzyme.

Abstract: The present disclosure is concerned with xanthine analogs, methods of making xanthine analogs, and methods of treating West Nile virus using these analogs. 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 invention.

Abstract: This invention provides substituted bicyclic pyrimidine compounds of the following formula: or a pharmaceutically acceptable salt thereof, wherein R is selected from the group consisting of a straight or a branched chain alkyl group having from 1 to 10 carbon atoms, wherein the alkyl group is partially or completely saturated. Methods of treating a patient diagnosed with cancer are disclosed comprising administering to the patient a therapeutically effective amount of the substituted bicyclic pyrimidine compounds, or a pharmaceutically acceptable salt thereof.

Abstract: Certain pyrazolo[1,5-a]pyrimidine-5,7-diamine compounds that inhibit cycline dependent kinase (CDK) (e.g., CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8, CDK9, CDK10, CDK11, CDK12, CDK13, etc.) are disclosed. Pharmaceutical compositions comprising these compounds, and the use of these compounds and compositions to inhibit CDK; to treat disorders associated with CDK such as those arising from an inappropriate activity, mutation, overexpression, or upstream pathway activation of CDK; or disorders that are ameliorated by the inhibition of CDK; proliferative disorders; cancer; viral infections; neurodegenerative disorders; ischaemia; renal diseases; and cardiovascular disorders are also disclosed. Optionally, the treatment further comprises simultaneous or sequential treatment with a further active agent, e.g., an aromatase inhibitor, an anti-estrogen, a Her2 blocker, a cytotoxic chemotherapeutic agent, etc.

Abstract: The invention provides novel morpholinylpyridone compounds of formula (I), pharmaceutical compositions containing such compounds, and methods for using such compounds in treatment of diseases including cancer, type II diabetes, inflammatory diseases, autoimmune diseases, neurodegenerative disorders, cardiovascular disorders and viral infections; Formula (I) wherein R1, R2 and A are as defined in the specification.

Abstract: The present invention is directed to kinase inhibitor compounds having the following structure: or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof, where R1, R2, X, n, R3, Y, Z, R4, R5, R6, and = are as defined herein. The present invention also relates to compositions containing the kinase inhibitor compounds, methods of inhibiting activity of a kinase in a cell, methods of increasing cell proliferation in a population of pancreatic beta cells, methods of treating a subject for a condition associated with insufficient insulin secretion, and methods of treating a subject for a neurological disorder.

Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the heterocyclic entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.

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, wherein R1, R2, L, W1, W2, X, Y, and Z are as defined herein. Methods associated with the preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: Provided herein are crystalline forms of a triazolopyrimidine compound, which is useful for treating a PRC2-mediated disease or disorder.

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 invention provides methods utilizing Prins reaction in the preparation of compounds that may be useful as intermediates in the synthesis of halichondrin macrolides and analogs thereof. The invention also provides compounds that may be useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.

Abstract: The present invention relates to bicyclic heterocycles, 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: The present invention relates to compounds of formula (I) and their use for treating or preventing a bacterial infection or as an antibacterial agent and/or as a ?-lactamase inhibitor.

Abstract: The invention relates to novel mTOR inhibitor compounds having the general formula (I), to compositions comprising said mTOR inhibitor compounds, methods for producing same, and the use thereof in compositions as a drug.