Abstract: The present invention provides compounds of formula I, compositions thereof, and methods of using the same as mTORC1 inhibitors.

Abstract: The present invention encompasses compounds of formula (1) wherein the groups R1 to R4, A and p have the meanings given in the claims and specification, their use as inhibitors of SOS1, pharmaceutical compositions which contain compounds of this kind and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

Abstract: Chromenopyridine-based compounds are provided. In one aspect, the present disclosure provides a method for treating cancer in a subject in need thereof, the method comprising administering a therapeutically effective amount of a chromenopyridine-based compound to the subject. A representative compound is 2,4-diamino-7,8-dimethoxy-5-((4-methoxyphenyl)thio)-5H-chromeno[2,3-b]pyridine-3-carbonitrile (Compound 1).

Abstract: In one aspect, the present disclosure describes new estrogen receptor-related orphan receptor (EER) inverse agonist compounds. Also described are pharmaceutical formulations, methods of synthesis and uses thereof.

Abstract: A compound of Formula (I): or a pharmaceutically acceptable salt thereof, in which Ring X is a 3 to 7 membered monocyclic ring, at least one of R1, R2, R3, and R4 is OR5 or CH2OR5 and the other R1, R2, R3, and R4 each independently are halogen, OH, OR5, CH2OR5, CO2H, OC?OR6, (C?O)R6, R6, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, H, or absent. Also provided herein are therapeutic uses of the compound of Formula (I).

Abstract: The present invention relates to compounds, compositions and methods for treating diseases or conditions mediated by proteins of the SWI/SNF chromatin-remodeling complex, including PB1.

Abstract: The invention provides deuterium-enriched isoindolinonyl-azepanediones, deuterium-enriched oxoquinazolin-3(4H)-yl-azepanediones, related compounds, pharmaceutical compositions, and methods of using such compounds and pharmaceutical compositions to treat cancer, angiogenesis disorders, immune disorders, and other medical disorders.

Abstract: Provided herein are compounds of Formula (I): and forms thereof, wherein w1, w2, w3, w4, w5, w6 and w7 are as defined herein, including compositions thereof and uses therewith for treating spinal muscular atrophy.

Abstract: The present invention relates to compounds of formula I wherein the variables are defined as given in the description and claims. The invention further relates to uses and composition for compounds of formula I.

Abstract: A series of subunit selective allosteric modulators of NMDA receptor function according to Formula (I) is provided herein. Also provided is a method of treating neurological disorders such as Alzheimer's disease Parkinson's disease, schizophrenia, depression, stroke, psychosis and the like using compounds of Formula (I), optionally in combination with one or more further active agent. Pharmaceutical compositions containing a compound of Formula (I) and optionally one or more active agent for treating such disorders may be provided in the form of a tablet, capsule, pill, gel, granules, aerosol, aqueous buffer or a nanoparticle formulation, emulsion, liposome, etc.

Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts thereof: which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: The present invention relates to a method for preparing a lyophilized solid pharmaceutical composition comprising a) a compound having the formula (I): and/or a compound having the formula (II): ?and b) two different sodium phosphate salts, wherein the two different sodium phosphate salts are NaH2PO4·2H2O and Na2HPO4·2H2O, and wherein the quantity of the NaH2PO4·2H2O and Na2HPO4·2H2O present in the composition is chosen such that the molar ratio of both NaH2PO4·2H2O and Na2HPO4·2H2O to compound (I) or compound (II) ranges from 0.02 to 0.5.

Abstract: A reagent composition for a Karl Fischer titration includes (1) sulfur dioxide or a derivative thereof, (2) a derivative of imidazole, (3) an alcohol, and (4) at least one amino acid that is present in an amount that is greater than zero and up to about 10 weight percent based on a total weight of the reagent composition. Moreover, a molar ratio of the derivative of imidazole to the sulfur dioxide or derivative thereof is greater than 1:1. Iodine is optionally included in a one-component reagent and excluded in a two-component reagent. This disclosure further provides a method for determining an amount of water in a sample via Karl Fischer titration. The method includes the step of providing the sample, providing the reagent composition, which optionally includes the iodine (I2), and titrating the sample with the reagent composition.

Abstract: Disclosed are a quinazolinone derivative, a preparation method therefor, a pharmaceutical composition, and applications. Provided are a compound represented by formula I, a pharmaceutically acceptable salt, a solvate, a crystal form, a eutectic crystal, a stereoisomer, an isotope compound, a metabolite, or a prodrug thereof. Generation or activity of a cell factor can be regulated, and accordingly, cancers and inflammatory diseases can be effectively treated.

Abstract: Described herein is a process for the preparation of a compound of Formula I, wherein R1 and R2 each have the meanings provided in the description. Also described is a process for the preparation of pharmaceutically-active compounds including the process for the preparation of compounds of Formula I.

Abstract: The present invention relates to a method of treatment for chronic pain, opioid dependence, alcohol use disorder or autism using a class of pyrimidinone compounds, an adenylyl cyclase 1 (AC1) inhibitor. The invention described herein also pertains to pharmaceutical compositions and methods for treating diseases in mammals using those compounds disclosed herein.

Abstract: The present disclosure provides pladienolide compounds, pharmaceutical compositions containing such compounds, and pladienolide compounds for use in methods of medical treatment. These compounds may be useful in the treatment of cancer, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful.

Abstract: Certain embodiments are directed to adenosine receptor antagonists that inhibit migration and growth of cancer cells.

Abstract: The present disclosure provides methods of inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins with compositions of Formula (II-A). The methods are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin. Compositions of Formula (II-A) for use in these methods are also provided.

Abstract: The present disclosure is directed to inhibitors of SHP2, such as pyrazine compounds, and their use in the treatment of disease associated with SHP2 modulation, such as Noonan Syndrome, Leopard Syndrome, juvenile myelomonocytic leukemias, neuroblastoma, melanoma, acute myeloid leukemia and cancers of the breast, lung and colon. Also disclosed are pharmaceutical compositions comprising the same.