Abstract: The present invention relates to compounds that are antagonists of the orexin-1 receptor. The compounds have the structural formula (I) defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or disorders associated with orexin-1 receptor activity.

Abstract: The present disclosure describes methods of treating pancreatic cancer and limiting over-expression of oncogenes, activating tumor suppressor genes or regulating signaling proteins in patients comprising administering compounds and pharmaceutical combinations as described herein.

Abstract: There is provided compounds of formula (I) or pharmaceutically-acceptable salts thereof, wherein W, X, Y, Z, R1, R2 and R3 have meanings provided in the description, which compounds are useful in the treatment of cancers.

Abstract: Compounds that selectivity inhibit the STAT3 pathway and not the STAT1 pathway and exhibit anti-proliferative activity are disclosed. Also disclosed are methods of treatment of cancers that are characterized by overexpression of STAT3, which are safer that other therapies.

Abstract: Provided herein are phosphodiesterase 4D (PDE4D) inhibitors, including methods of using the same. Also provided are methods of treating subjects suffering from conditions associated with aberrant PDE activity.

Abstract: The invention provides compounds of Formula (I): as further described herein, as well as pharmaceutical compositions comprising such compounds, and methods to use the compounds and pharmaceutical compositions for treatment of certain viral disorders, including influenza.

Abstract: Disclosed are adsorption complexes that include 1-methylcyclopropene (1-MCP) and a metal coordination polymer network (MCPN), wherein the MCPN is a porous material, and the 1-MCP is adsorbed into the MCPN. Also disclosed are kits for containing 1-MCP that include the adsorption complex in a 1-MCP-impermeable package. Also disclosed are methods of releasing 1-methylcyclopropene (1-MCP) from the kit that include the application of aqueous fluids, heat, and/or pressure.

Abstract: Cycloalkylamine derivatives may be used for preventing or treating diseases in humans, animals, and have demonstrated efficacy specifically in treating type 2 diabetes. In an embodiment, the cycloalkylamine derivatives can include a compound selected from the group consisting of cycloheptanamine salts, cyclohexanamine salts, cyclopentanamine salts 1-cycloheptyl-[4,4?-bipyridin]-1-ium, N1,N2-dicycloheptyloxalamide, 1-[3?,5?-bis(trifluoromethyl)phenyl]-3-cycloheptylurea, 1,1?-(4-methyl-1,3-phenylene)bis(3-cycloheptylurea), 1-(2?-aminopyrimidin-4?-yl)-3-cycloheptylurea, 4-amino-N-(cycloheptylcarbamoyl)benzenesulfonamide, 4-(3?-cycloheptylureido)-N-(5?-methylisoxazol-3?-yl)benzenesulfonamide, N-(cycloheptylcarbamoyl)-4-methylbenzenesulfonamide, 1-cycloheptylguanidine hydrochloride, (E)-amino[(amino(cycloheptylamino)methylene)amino]methaniminium chloride, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides tricyclic compounds, and pharmaceutically acceptable salts thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.

Abstract: De-ethylflavopereirine, a pharmaceutically acceptable salt thereof, a solvate or a hydrate thereof, or a pharmaceutically acceptable salt of a solvate or a hydrate thereof may be used as cancer therapy (i.e., prevention and/or treatment) in a subject in need thereof, including a pathological condition such as inflammation, especially chronic, or cancer (e.g., a carcinoma, a sarcoma, a melanoma, a leukemia, a lymphoma), especially a solid tumor and/or a metastasis thereof. In particular, systemic administration of such improved anti-cancer agents in effective amounts may selectively destroy cancer cells (including cancer stem cells) in a solid tumor and/or at a site of metastasis. They are well-tolerated by the subject, even at large systemic doses and their resulting high concentrations in the circulation, and provide safe and effective anti-cancer agents.

Abstract: The present disclosure provides improved methods for controlled cyclization of peptoid dimers to form N,N?-2,5-diketopiperazines (N,N?-2,5-DKPs) with significant selectivity. In at least some examples, selectivity is based on a serendipitous conglomeration of slow exchange of amide rotamers, steric repulsion from the degree of ?-substitution, and the geometric bulk of an amine nucleophile. By varying reaction conditions, the selectivity of the reaction and formation of a particular N,N?-2,5-DKP can be switched. The cyclization works in the presence of a variety of protection groups and diverse functionalities. The teachings herein provide techniques for synthesizing N,N?-2,5-DKPs that can be readily docked with drug candidates for shuttling across the blood brain barrier. This method provides a facile way to produce substituted DKPs containing groups ready for post-modification to include docking drug candidates.

Abstract: The invention concerns compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, X, Ring A, Ring B and Ring C have any of the meanings hereinbefore defined in the description; process for their preparation; pharmaceutical compositions containing them and their use in treating MCT4 mediated diseases.

Abstract: Provided is a new polycyclic aromatic hydrocarbon derivative. The polycyclic aromatic hydrocarbon derivative is a derivative of a polycyclic aromatic hydrocarbon having 6 or more aromatic rings and has a substituent represented by the following formula (1). (In the formula (1), R1 and R2 are carbon atoms of the aromatic rings in the polycyclic aromatic hydrocarbon, and R3 to R5 are carbon atoms of an aromatic ring or a heterocyclic ring in a group having the aromatic ring or the heterocyclic ring. n is 0 or 1, and m is the number of substituents.

Abstract: The present invention provides novel crystalline forms of Ponatinib hydrochloride. Specific crystalline forms provided by the present invention include Ponatinib hydrochloride Form APO-I, APO-III and APO-IV, each of which is obtained from acetonitrile/formic acid solutions. Additionally, Form APO-V is provided, which is obtained from concentrated hydrochloric acid.

Abstract: Described herein are compounds that are LOXL2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with LOXL2 activity.

Abstract: Monomeric bimetal hydroxycitric acid (HCA) compounds are provided. The subject compounds include a divalent metal (X) bonded to the carboxylic acids of C2 and C3 and a monovalent metal (Y) bonded to the carboxylic acid of C1. Also provided are methods of preparing the subject compounds from a dimeric starting material (e.g., X3(HCA)2) which include acidifying the dimer to produce a monomeric intermediate which is subsequently neutralized with YOH base. Methods of alleviating at least one symptom associated with a target disease or condition in a subject are provided. Also provided are compositions including the subject monomeric bimetal HCA compounds which find use in a variety of therapeutic applications.

Abstract: The present invention relates to a pyrimidine compound, a chloride salt thereof, and a manufacturing and application of same. The chloride salt of the pyrimidine compound is presented by formula (II). The chloride salt has higher solubility, good stability, higher bioavailability, and very low hygroscopicity, and has excellent inhibition against a PIM kinase.

Abstract: Disclosed are methods and compositions for the treatment of facioscapulohumeral muscular dystrophy. In some cases, the methods and compositions involve the use of kinase inhibitors include Src, Syk, Abl, Tie, Flt, ErbB, Trk, PRKDC, and Yes families to repress DUX4 expression in muscle cells. Further disclosed are methods and cell based assays for screening compounds for the treatment of facioscapulohumeral muscular dystrophy.

Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I), or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A, W, X, Y, Z, and are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, Y, X, W, m and n are as defined herein, compositions including the compounds and methods of using the compounds.