Abstract: The invention relates to a novel method to isolate a natural product, a flavonoid namely inoscavin A from a Sri Lankan mushroom, medicinal preparation thereof to treat rhabdomyosarcoma cancer condition. This compound was isolated from the terrestrial basidiomycete Fulviformes fastuosus for the first time. The isolation method of the inoscavin A comprises the following steps of: (1) carrying out sonication extraction of pulverized specimen by methanol; (2) partitioning in to hexane, dichloromethane and ethyl acetate respectively by liquid-liquid extraction 3) fractionation using normal phase silica gel column chromatography 4) purification using preparative high performance liquid chromatography (HPLC) to obtain flavonoid compound inoscavin A in substantially purified form (?98%). In vitro cytotoxicity experiments demonstrated that the composition comprising inoscavin A strongly induced the apoptosis of human rhabdomyosarcoma (RD) cells compared to the cytotoxicity produced on normal epithelial cells (CC-1).

Abstract: The present invention relates to heterocyclic compounds, their process of preparation, pharmaceutical compositions comprising these compounds and use thereof, optionally in combination with other antibacterial agents and/or beta-lactam compounds, for the prevention or treatment of bacterial infections. The present invention also relates to the use of these compounds as ?-lactamase inhibitors and/or as antibacterial agents.

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective Factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Abstract: Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.

Abstract: The invention relates to besylate salts of the compound of formula (I): Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.

Abstract: Provided herein are maytansinoid compounds, derivatives thereof, conjugates thereof, and methods of treating or preventing proliferative diseases with the same.

Abstract: An exemplary embodiment relates to novel protein modulators capable of altering function of the mutant CFTR protein and their use for treating diseases associated with CFTR protein malfunction. The invention provides compositions, pharmaceutical preparations and methods of correcting the cellular alteration of a mutant CFTR protein wherein the CFTR mutation is a mutation ?F508-CFTR, or another mutation of class II.

Abstract: A process can prepare a 3-glycidyloxypropylalkoxysilane of formula (I), (R?)O—(CH2)3—Si(OR)3 (I), where R groups are independently a methyl or ethyl group and R? represents an H2C(O)CHCH2— group. The process includes reacting (i) a functionalized alkene of formula (II), (R?)O—C3H5 (II), where R? represents an H2C(O)CHCH2— group, with (ii) at least one hydroalkoxysilane of formula (III), HSi(OR)3 (III), where R groups are independently a methyl or ethyl group. The reacting takes place in the presence of (iii) a Karstedt catalyst or a catalyst having hexachloroplatinic acid as a homogeneous catalyst, and (iv) 2-ethylhexanoic acid, isononanoic acid, or both. The process further includes obtaining a product of the reacting.

Abstract: The present disclosure provides methods and reagents useful for analyzing protein-protein interfaces such as interfaces between a presenter protein (e.g., a member of the FKBP family, a member of the cyclophilin family, or PIN1) and a target protein. In some embodiments, the target and/or presenter proteins are intracellular proteins. In some embodiments, the target and/or presenter proteins are mammalian proteins.

Abstract: and salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods using a compound of formula I.

Abstract: The present disclosure provides macrocyclic compounds of Formula (I). The provided compounds are able to bind protein kinases and may be useful in modulating (e.g., inhibiting) the activity of a protein kinase in a subject or cell and/or in treating or preventing a disease (e.g., proliferative disease, genetic disease, hematological disease, neurological disease, painful condition, psychiatric disorder, or metabolic disorder) in a subject in need thereof. Also provided are pharmaceutical compositions, kits, methods, and uses that include or involve a compound described herein.

Abstract: The present invention provides cyclic dimers of alpha acids and polymers derived therefrom. Also provided are processes for preparing and methods of using the cyclic dimers and the polymers derived from the cyclic dimers.

Abstract: This disclosure is directed to non-aromatic difluoro analogues of resorcylic acid lactones, pharmaceutical compositions comprising non-aromatic difluoro analogues of resorcylic acid lactones, and methods of treatment comprising non-aromatic difluoro analogues of resorcylic acid lactones.

Abstract: This invention provides for a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R3, n, p, L1 and L2 are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.

Abstract: The present invention relates to a method for producing N-substituted sulfonamide compounds including a step of reacting a sulfonamide compound of general formula (1) with a halogenated organic compound of general formula (2) in the presence of cesium carbonate or potassium carbonate in an organic solvent to produce an N-substituted sulfonamide compound of general formula (3).

Abstract: Compounds of formula (I) defined herein are useful as a dopamine D1 receptor positive allosteric modulators (D1 PAM) and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating cognitive impairment, schizophrenia negative symptom, CIAS, Parkinson's disease, Alzheimer's disease, Huntington's disease, depression, ADHD, drug dependency, or the like.

Abstract: A pharmaceutical composition comprising an ailanthone (AIL) compound or a derivative thereof, for the treatment of diseases or conditions caused by, dependent from, or associated with excessive androgen receptor activity. Ailantone compounds have been discovered to be a potent inhibitor of both full-length AR (AR-FL) and constitutively-active truncated AR splice variants (AR-Vs), and are found to possess favorable drug-like properties such as good bioavailability, high solubility, lack of CYP inhibition, and low hepatotoxicity. Methods of treatment are also provided.

Abstract: An exemplary embodiment relates to novel protein modulators capable of altering function of the mutant CFTR protein and their use for treating diseases associated with CFTR protein malfunction. The invention provides compositions, pharmaceutical preparations and methods of correcting the cellular alteration of a mutant CFTR protein wherein the CFTR mutation is a mutation ?F508-CFTR, or another mutation of class II.

Abstract: Provided are a novel compound or a salt thereof, and a pharmaceutical composition comprising the same, which selectively and strongly inhibit JAK3, exhibit an excellent activity for suppressing the growth of human peripheral blood monocytes and an excellent oral absorbability, and exhibits an activity of inhibiting IL-2-induced IFN-? production in vivo. A compound represented by formula (I) [wherein X represents —CH?CH—, —NH—, a sulfur atom or an oxygen atom; and n represents an integer of 0 to 2], or a salt thereof.

Abstract: The invention relates to a process for preparing concentrated solutions of polymerization inhibitor, that can be used for the production, purification and storage of monomer compositions. This process comprises a step in which at least one polymerization inhibitor in the molten state is mixed with a solvent.