Abstract: The invention relates to novel mTOR inhibitor compounds having the formula (I) or a pharmaceutically acceptable salt thereof, compositions comprising the mTOR inhibitor compounds, methods for producing the same, and the use thereof.

Abstract: Described herein are compounds, for example, 1,2,4-triazole-substituted N-heteroaryl amines, that are useful in treating a TYK2-mediated disorder. In some embodiments, the TY-K2-mediated disorder is an autoimmune disorder, an inflammatory disorder, a proliferative disorder, an endocrine disorder, a neurological disorder, or a disorder associated with transplantation.

Abstract: The present invention is directed to 3-(ethoxydifluoromethyl)-6-(5-fluoro-6-(2,2,2-trofluoroethoxy)pyridine-3-yl)-[1,2,4]triazolo[4,3-a]pyridine, or a pharmaceutically acceptable salt thereof, or a composition thereof, which is useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. 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 is directed to 3-(ethoxydifluoromethyl)-6-(5-fluoro-6-(2,2,2-trofluoroethoxy)pyridine-3-yl)-[1,2,4]triazolo[4,3-?]pyridine, or a pharmaceutically acceptable salt thereof, or a composition thereof, which is useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. 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: Provided herein are imidazopyrimidine compounds, such as compounds of Formula (I), for use in enhancing human immune response and/or as adjuvants in vaccines.

Abstract: This disclosure relates generally to VMAT2 inhibitor compounds of Formula (Ia): and pharmaceutically acceptable salts thereof, as well as compositions and methods related thereto.

Abstract: The invention concerns compounds of formula (I) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns pharmaceutical compositions comprising these compounds and the compounds for use in the treatment of respiratory syncytial virus infection.

Abstract: The present invention provides a crystalline form of a benzodiazepine derivative hydrochloride of Formula I or its ethanolate, wherein R is methyl or ethyl. The present invention also provides a method of preparing the crystal form of the compound of Formula I and a pharmaceutical composition comprising the crystal form.

Abstract: Solid forms of Compound (I): are disclosed. Pharmaceutical compositions comprising the same, methods of treating disorders and conditions mediated by BTK activity using the same, and methods for making Compound (I) and solid forms thereof are also disclosed.

Abstract: The disclosure provides compounds of Formula (I-A) and (I-B) and the pharmaceutically acceptable salts thereof. The variables, R, R2, R3, X1, X2, X3, Y1, Y, and Z are defined herein. Certain compounds of Formula (I-A) and (I-B) act as selective mitochondrial protonophore uncouplers that do not affect plasma membrane potential. These compounds are useful for treating or decreasing the risk of conditions responsive to mitochondrial uncoupling, such as cancer, obesity, type II diabetes, fatty liver disease, insulin resistance, Parkinson's disease, ischemia reperfusion injury, heart failure, non-alcoholic fatty liver disease (NALFD), and non-alcoholic steatohepatitis (NASH), Because mitochondrial uncouplers decrease the production of reactive oxygen species (ROS), which are known to contribute to age-related cell damage, the compounds are useful for increasing lifespan. Compounds and salts of Formulae (I-A) and (I-B) are also useful for regulating glucose homeostasis or insulin action in a patient.

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: Disclosed herein are heterocyclic compounds according to formula (I) having the structure that inhibit the binding of menin and MLL or MLL fusion proteins. Also described are specific irreversible inhibitors of menin-HLL interaction. Also disclosed are pharmaceutical compositions that include compounds according to formula (I). Methods of using the menin-HLL irreversible inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, leukemia and other diseases or conditions dependent on menin-MLL interaction.

Abstract: The present invention provides a compound that have excellent harmful arthropod controlling effects, the compounds being represented by formula (I) [wherein Q represents a group represented by formula Q1 or the like, Z represents an oxygen atom or a sulfur atom, A1 represents a nitrogen atom or CR6a, A2 represents a nitrogen atom or CR6b, A3 represents a nitrogen atom or CR6c, A4 represents CR1a or the like, A5 represents a nitrogen atom or CR6e or the like, A6 represents a nitrogen atom or CR6f, R6a represents a hydrogen atom or the like, R6b represents a C1-C6 chain hydrocarbon group or the like, R6c, R6e, R6f are identical to or different from each other, and each represents a C1-C6 chain hydrocarbon group or the like, R1a represents a C1-C6 chain hydrocarbon group or the like, R2 represents a C1-C6 chain hydrocarbon group or the like, R3 represents a C1-C6 chain hydrocarbon group or the like, and n is 0, 1 or 2] or its N oxide compound.

Abstract: The invention provides various novel compositions of berberine in combination with pharmacologically active organic acids, and related methods of their use in treating various diseases or disorders. The invention further provides various novel compounds prepared from berberine and pharmacologically active organic acids and prepared from ursodeoxycholic acid and pharmacologically active organic bases, and pharmaceutical compositions thereof, and methods of their preparation and therapeutic use in treating and/or preventing various diseases or disorders.

Abstract: The invention relates to pharmaceutical compositions comprising, compounds of Formula Q: wherein W is —N(H)—, or —N(CH3)—, and Y is —C(?O)— or —O—, in free base or pharmaceutically acceptable salt form, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) pathway and/or the dopamine D2 receptor pathway, and methods of treating conditions of the central nervous system therewith.

Abstract: The invention provides compounds of Formula (A) that may inhibit ENPP1, and that are accordingly useful for treatment of disorders related to ENPP1. The invention further provides pharmaceutical compositions containing these compounds and methods of using these compounds to treat or prevent disorders related to ENPP1.

Abstract: Crystalline forms of Compound (I): are disclosed. Pharmaceutical compositions comprising the same, methods of inhibiting BTK using the same, and methods for making crystalline forms of Compound (I) are also disclosed.

Abstract: The present invention provides phenyl-2-hydroxy-acetylamino-2-methyl-phenyl compounds, such as compounds of formula I: pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat physiological disorders such as pancreatic cancer.

Abstract: Provided are heteroaryl heterocyclic compounds of formula (I), pharmaceutical compositions comprising same, methods for preparing same, and uses thereof, wherein the variables are as defined in the description. The compounds are Btk inhibitors.

Abstract: Disclosed in the present invention are a crystal form of a [1,2,4]triazolo[1,5-c]pyrimidine compound and a preparation method thereof. Further disclosed is a use of the crystal form in the preparation of a medicament for treating A2A receptor related diseases.