Abstract: Provided is a pharmaceutical composition for treating melanoma, including a benzenesulfonamide derivative and a pharmaceutically acceptable carrier thereof. Also provided is a method for treating melanoma by administering the composition to a subject in need thereof. Further provided is a use of the pharmaceutical composition in the manufacture of a medicament for treating melanoma.

Abstract: The present invention is directed to inhibitors of tyrosinase, pharmaceutical compositions comprising such tyrosinase inhibitors, and methods of making and using the same. Specifically, included in the present invention are compositions of matter comprised of at least one 2,4-dihydroxybenzene analog, which inhibit the activity of tyrosinase and which inhibit the overproduction of melanin.

Abstract: The disclosure provides for small molecules inhibitory compounds of ubiquitin specific protease 1 (USP1) and compositions comprising the same. The disclosure further provides methods for targeting ubiquitin specific protease 1 (USP1) and methods of treating diseases or disorders related to USP1, such as cancer.

Abstract: Conjugates of topoisomerase I inhibitors linked to a macromolecule through a linkage that undergo beta elimination in situ in combination with one or more of an assessed defect in DNA damage response (DDR) in a subject bearing cancer, a cell cycle checkpoint inhibitor and/or a DDR inhibitor provides improved outcomes for cancer-bearing subjects.

Abstract: The present disclosure reports solid forms of ((S)-5-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile.

Abstract: The present disclosure addresses this need by providing crystalline fine particle forms of PRX-3140 potassium salt, methods for preparation and the treatment for Alzheimer's disease (AD) and other dementias affecting the cholinergic and/or serotonergic systems including post-traumatic stress disorder (PTSD). In certain aspects, the present disclosure provides novel methods of preparing the compound of Formula I thereof, or PRX-3140 potassium salts, crystalline fine particle forms of PRX-3140 potassium salt, and compositions comprising them. In certain aspects, the present disclosure provides novel crystalline fine particle form of PRX-3140 potassium salt which may provide advantages including improved bioavailability and stability relative to other crystalline or amorphous forms. In other aspects, the present disclosure provides oral dosage forms of crystalline fine particle form of PRX-3140 potassium salt and excipients with improved stability.

Abstract: The invention relates to the combined use and to a combination of either a microtubule targeting agent or a Src kinase inhibitor, a Raf-MEK-ERK pathway inhibitor and an EGFR and/or ERBB2 inhibitor for use in the treatment of RAS-mutant cancer. The invention further relates to a method of treating RAS-mutant cancers and to a method of testing a combination comprising of a either microtubule targeting agent or a Src inhibitor, a Raf-MEK-ERK pathway inhibitor and an EGFR and/or ERBB2 inhibitor on a tumor organoid. In particular, the invention relates to the combined use of either a microtubule targeting agent or a Src kinase inhibitor with: an inhibitor of the Raf-MEK-ERK pathway and at least one of an inhibitor of both EGFR and ERBB2 and a combination of an EGFR inhibitor and an ERBB2 inhibitor in the treatment of RAS mutant cancer.

Abstract: 5-substituted difluoropiperidine compounds having a capacity to cross the blood-brain barrier are provided. The compound has the structural formula represented by formula (I): The 5-substituted difluoropiperidine compounds, derivatives and pharmaceutically acceptable salts thereof of the present invention have the ability to cross the blood-brain barrier and are capable of acting as a drug characteristic of a protein kinase inhibitor, in particular for the expression of a protein through a vascular endothelial growth factor receptor 2 or SRC kinase family (FYN) and can be used to treat or prevent disorders associated with abnormal protein kinase activity, such as cancer, cancer with brain metastases, primary brain cancer (glioma), glioblastoma, cancer with meningeal metastases, Alzheimer's disease and central nervous system diseases, and the like.

Abstract: Described herein are 1,4-substituted piperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds, and methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the compounds described, including the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses.

Abstract: Compounds and methods of scavenging bifunctional electrophiles and reducing the occurrence of lysyl-levuglandin adducts in a subject in need thereof by administering a levuglandin adduct formation inhibiting amount of a compound of the following formula: wherein the variables are defined herein.

Abstract: The present disclosure provides methods of preventing HIV in a subject, comprising administering to the subject a therapeutically effective amount of a compounds of Formula (Ia) or (Ib): or a pharmaceutically acceptable salt thereof, optionally in combination with one or more additional therapeutic agents. Methods of reducing the risk of acquiring HIV (e.g., HIV-1 and/or HIV-2) are also provided.

Abstract: Provided herein are methods of treating tuberous sclerosis complex in a subject in need thereof by administering to the subject compositions comprising an mGlu5 negative allosteric modulator (NAM), having the structure of Formula I:

Abstract: The invention relates to method of treating chronic inflammatory diseases in subjects in need thereof by administering calcium lactate as an active agent. The calcium lactate can be provided in a pharmaceutical, food, or nutrient composition.

Abstract: An object of a first aspect of the present invention is to provide a radical generating catalyst that can generate (produce) radicals under mild conditions. In order to achieve the above object, a first radical generating catalyst according to the first aspect of the present invention is characterized in that it includes ammonium and/or a salt thereof. A second radical generating catalyst according to the first aspect of the present invention is characterized in that it includes an organic compound having Lewis acidic properties and/or Brønsted acidic properties.

Abstract: Provided herein are oxazolidinone derivatives that can exhibit anti-microbial activity and/or activity as biofilm modulating agents (e.g., activity as biofilm inhibitors and/or activity as biofilm dispersal agents). The compounds can exhibit potent activity anti-microbial activity (e.g., potent activity against Gram-positive positive bacteria including methicillin-resistant Staphylococcus aureus). The compounds can exhibit potent activity against biofilms. In some cases, the compounds can exhibit both anti-microbial activity and biofilm modulation properties.

Abstract: Provided herein are methods of using 2-(2,6-dioxopiperidin-3-yl)-4-((2-fluoro-4-((3-morpholinoazetidin-1-yl)methyl)benzyl)amino)isoindoline-1,3-dione, or an enantiomer, a mixture of enantiomers, a tautomer, an isotopolog, or a pharmaceutically acceptable salt thereof, for treating, preventing or managing hematological malignancies.

Abstract: Disclosed are (i) compounds of formula I, or pharmaceutically acceptable salts thereof, and (ii) lipidoid nanoparticles comprising compound of formula I or pharmaceutically acceptable salts thereof, as well as their use as vehicles for drug delivery across the blood-brain barrier.

Abstract: The invention provides compounds and methods of inhibiting a cyclin-dependent kinase, comprising contacting the cyclin-dependent kinase and an effective amount or concentration of a compound of formula (I) wherein variables are as defined herein. Compounds of formula (I) can be highly selective inhibitors of cyclin-dependent kinases such as CDK12/13, relative to other kinases such as casein kinases, such as CK1?/?. Compounds can be used in treatment of cancers, such as breast cancer, brain cancer and ovarian cancer.

Abstract: Compositions and methods for inhibiting histone lysine demethylases are provided. Several new DFP-based KDM inhibitors which alter the velocity of HP1-mediated heterochromatin gene repression are provided.

Abstract: Provided herein are compounds of the Formula I: or pharmaceutically acceptable salt or solvate thereof, wherein A, B, X1, X2, X3, X4, Ring D, E, Ra, Rb, n and m 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.