Abstract: Substituted piperidines as BTK inhibitors, a preparation method thereof and a pharmaceutical application thereof. The substituted piperidines is a compound represented by a general formula (I) or a stereoisomer or a pharmaceutically acceptable salt thereof, and the substituted piperidines is used to treat BTK-related diseases such as tumors or autoimmune system diseases.

Abstract: Disclosed are heterocyclic heteroaromatic macrocyclic ether compounds of Formula (I): pharmaceutically acceptable salts of the compounds and pharmaceutical compositions thereof. The disclosure further relates to methods of treating or preventing cancer using the heterocyclic heteroaromatic macrocyclic ether compounds, pharmaceutically acceptable salts of the compounds and pharmaceutical compositions thereof.

Abstract: Described herein are polymorphs comprising 2?,6-difluoro-5?-[3-(1-hydroxy-1-methylethyl)-imidazo[1,2-b][1,2,4]triazin-7-yl]biphenyl-2-carbonitrile (TPA023B) or salts thereof. In one aspect, disclosed herein is a crystalline polymorphic salt or co-crystal of TPA023B with phosphoric acid. Also described herein are methods of making and using the same.

Abstract: Some embodiments of the invention include inventive compounds (e.g., compounds of Formula (I)) and compositions (e.g., pharmaceutical compositions) which can be used for treating, for example, certain diseases. Some embodiments include methods of using the inventive compound (e.g., in compositions or in pharmaceutical compositions) for administering and treating (e.g., diseases such as head and neck squamous cell carcinoma (HNSCC), cancer, blood disorders, etc.). Additional embodiments provide synergistic combinations of a BCL2 inhibitor with an IRAK inhibiting compound, and methods of using same.

Abstract: Provided herein are compounds of Formula IV, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity.

Abstract: Provided herein are compounds, compositions and methods of using the compounds and compositions for the treatment of diseases modulated, as least in part, by AhR. The compounds are represented by formula: wherein the letters and symbols a, b, c, d, e, f, A, R1, X1, Ar1 and Ar2 have the meanings provided in the specification.

Abstract: The present disclosure relates to novel compounds of Formula (I) that degrade Bruton's tyrosine kinase (BTK), pharmaceutical compositions containing such compounds, and their use in prevention and treatment of conditions modulated by BTK.

Abstract: Cellular biological activities are tightly controlled by intracellular signaling processes initiated by extracellular signals. Protein tyrosine phosphatases, which remove phosphate groups from tyrosine phosphorylated signaling molecules, play equally important tyrosine roles as protein kinases in signal transduction. SHP-2, a cytoplasmic SH2 domain containing protein tyrosine phosphatase, is involved in the signaling pathways of a variety of growth factors and cytokines. Recent studies have clearly demonstrated that this phosphatase plays an important role in transducing signal relay from the cell surface to the nucleus, and is a critical intracellular regulator in mediating cell proliferation and differentiation.

Abstract: The disclosure is directed to compounds of Formula (I) and Formula (II). Formula (I) and Formula (II) and pharmaceutically acceptable salts or solvates thereof. Pharmaceutical compositions comprising compounds of Formula (I) or Formula (II), as well as methods of their use and preparation, are also described.

Abstract: Provided herein are compounds of the Formula I: and tautomers and pharmaceutically acceptable salts and solvates thereof, wherein R1 and R2 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.

Abstract: The present application relates to compounds of Formula I or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB, such as cancer.

Abstract: The present disclosure relates to compounds that are Syk inhibitors or pharmaceutically acceptable salts or co-crystals thereof, and pharmaceutical compositions thereof, and to their use in the treatment of various disease states, including cancer and inflammatory conditions.

Abstract: The present invention discloses phthalazine isoxazole alkoxy derivatives, a preparation method thereof, a pharmaceutical composition, and a use thereof. The present invention provides a compound represented by Formula I, cis-trans isomers thereof, enantiomers thereof, diastereoisomers thereof, racemates thereof, solvates thereof, hydrates thereof, and pharmaceutically acceptable salts or prodrugs thereof. The compound has an excellent inverse agonist effect with respect to ?5-GABAA.

Abstract: Provided, in part, are compounds of Formula I: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of conditions associated with the activity of sodium channels. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including neurological disorders (e.g., Dravet syndrome, epilepsy), pain, and neuromuscular disorders are also provided herein.

Abstract: The present invention relates to methods of making certain pyrrolopyrimidine derivatives, which are useful in the treatment of proliferation disorders and other diseases related to the dysregulation of kinase (such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, BTK, FLT3(D835Y), ITK, JAK1, JAK2, JAK3, TEC and TXK) and/or the respective pathways, salts, polymorphs, and amorphous forms of said compounds, synthetic intermediates for preparing said compounds, and pharmaceutical compositions comprising said compounds and methods for making such compositions.

Abstract: Disclosed are compounds having the structure of Formula I, or a pharmaceutically acceptable salt of any thereof: wherein: “Z” and R1 are defined herein, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.

Abstract: The disclosure includes compounds of Formula (I) wherein Q1, Q2, Q3, W, X, Y, Z1, m, n, Warhead, R1, R2, R3, R4, and R5, are defined herein. Also disclosed is a method for treating a neoplastic disease, autoimmune disease, and inflammatory disorder with these compounds.

Abstract: The present invention provides a compound substituted with an excellent control effect against a harmful arthropod, which is represented by formula (I) Het-Q??(I) wherein Q represents a group represented by Q1, etc., Het represents a group represented by Het1, etc., R2 represents a C1-C6 alkyl group, etc., G1 represents a nitrogen atom or CR3a, G2 represents a nitrogen atom or CR3b, G3 represents a nitrogen atom or CR3c, G4 represents a nitrogen atom or CR3d, R3a, R3b, R3c, and R3d are identical to or different from each other and represent a C1-C6 chain hydrocarbon group, etc., n represents 0, 1, or 2, T represents a C1-C10 chain hydrocarbon group substituted with one or more halogen atoms, etc., A2 represents a nitrogen atom or CR4a, A3 represents a nitrogen atom or CR4b, R4a and R4b are identical to or different from each other and represent a C1-C6 chain hydrocarbon group, W1 represents an oxygen atom, etc., and R6 represents a C1-C6 chain hydrocarbon group, etc.

Abstract: The present invention relates to compounds that inhibit Polycomb Repressive Complex 2 (PRC2) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.

Abstract: The disclosure includes compounds of Formula (I) wherein Q, R1, R2, and m are defined herein. Also disclosed is a method for treating a neoplastic disease with these compounds.