Abstract: Prodrugs of itaconic acid and 1- and 4-methyl itaconic acid and their use for treating a disease, disorder, or condition associated with inflammation are disclosed.

Abstract: The present invention provides, inter alia, methods, pharmaceutical compositions, and kits for treating or ameliorating the effects of a cancer in a subject, which harbors an atypical BRAF mutation (i.e. a non-V600E/K BRAF mutation), comprising an ERK inhibitor. Also provided are methods for identifying a subject having an atypical BRAF mutant cancer who would benefit from therapy comprising an ERK inhibitor.

Abstract: Provided herein are lipids having the Formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, a, and b are as defined herein. Also provided herein are lipid nanoparticle (LNP) compositions comprising lipid having the Formula (I) and a capsid-free, non-viral vector (e.g., ceDNA). In one aspect of any of the aspects or embodiments herein, these LNPs can be used to deliver a capsid-free, non-viral DNA vector to a target site of interest (e.g., cell, tissue, organ, and the like).

Abstract: The invention relates to pharmaceutical compositions comprising one or more benzodiazepine drugs for nasal administration, methods for producing and for using such compositions.

Abstract: The present disclosure relates to an ionic liquid (IL)-based formulation comprising inhibitors of NADPH oxidases enzymes (Nox's), preferably isoforms 1 and 4, in particular the specific inhibitor 3-cyclohexyl-5-(2,4-dihydroxybenzylidene)-1-methyl-2-thiohydantoin, for the treatment, therapy or prevention of neurological diseases, in particular Parkinson's diseases.

Abstract: In one aspect, the present disclosure provides methods of treating a bacterial infection using an inhibitor of the nucleotidyltransferase superfamily enzyme. In some embodiments, the compounds have one of the following formulas (I), (II), (III), or (IV) wherein R1, R2, and R3 are as defined herein or a pharmaceutically acceptable salt thereof. The compounds may be used to treat a bacterial infection including an infection of Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter species.

Abstract: Prodrugs of itaconic acid and 1- and 4-methyl itaconic acid and their use for treating a disease, disorder, or condition associated with inflammation are disclosed.

Abstract: A method of treating includes contacting cancer cells with a bis-(organoselanyl urea)aryl agent of Formula (I).

Abstract: The hemitartrate salt of a compound represented by the following structural formula: (Formula I Hemitartrate), which may be used in pharmaceutical applications, are disclosed. Particular single crystalline forms of the Formula (I) Hemitartrate are characterized by a variety of properties and physical measurements. As well, methods of producing crystalline Formula (I) Hemitartrate, and using it to inhibit glucosylceramide synthase or lowering glycosphingolipid concentrations in subjects to treat a number of diseases, are also discussed. Pharmaceutical compositions are also described.

Abstract: A method of treating cancer including administering a bis-(organoselanyl urea)aryl agent having a Formula (I) to a subject with cancer. The method includes effective inhibition of growth of cancer cells using the compound of Formula (I) as compared to doxorubicin.

Abstract: The present invention relates to a benzamide derivative compound, a method for preparing the same, and a pharmaceutical composition for treating or preventing an inflammatory disease containing the same as an active ingredient. The benzamide derivative compound according to the present invention inhibits the expression of PDE4 and regulates the expression of an inflammatory disease-related substance such as IL-4 (interleukin-4), IL-5 (interleukin-4), IFN-? (interferon-?), IL-17 (interluekin-17), IgE (immunoglobulin E), and TNF-? (tumor necrosis factor-?), and thus may be utilized as a pharmaceutical composition for treating or preventing an inflammatory disease.

Abstract: Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods that restore DNA binding affinity of p53 mutants. The compounds of the present disclosure can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.

Abstract: Certain embodiments of the invention pertain to a method of treating an infection in a subject caused by an infectious agent other than Escherichia coli, the method comprising administering to the subject arsinothricin or a salt thereof. The infectious agent other than E. coli can be a bacterium, protozoan, helminth, archaebacterium, or a fungus. In preferred embodiments, the infectious agent is Mycobacterium tuberculosis, Mycobacterium bovis, or Enterobacter cloacae. The invention also pertains to a method of treating an infection in a subject caused by an infectious agent, comprising administering to the subject arsinothricin or a salt thereof in combination with an inhibitor of phosphinothricin N-acetyltransferase or arsinothricin N-acetyltransferase. In certain such embodiments, the infectious agent expresses phosphinothricin N-acetyltransferase or arsinothricin N-acetyltransferase.

Abstract: The group of inventions relates to medicine, pharmacology, namely to psychiatry and can be used for effective and safe treatment of mental disorders associated with dysfunction of dopamine and serotonin (5-hydroxytryptamine) neurotransmitter systems. Pharmaceutical compositions containing halogenated clozapine, in an amount effective as selective antagonists of D4 and 5NT2A receptors, and at least one pharmaceutically acceptable carrier, as well as their use and methods of treatment are offered for this purpose. The inventions make it possible to create a new drug with a well-balanced receptor profile, the intake of which will allow to treat mental disorders in an effective way without causing side effects associated with exposure to receptors that are not involved in the pathology of a mental disorder.

Abstract: Compositions capable of promoting mitofusin activation may include a mitofusin activator having a structure represented by any stereoisomer thereof, or any pharmaceutically acceptable salt thereof. G is N or CH, and A is an optionally substituted 5- or 6-membered cycloalkyl or heterocycloalkyl ring. X is (CH2)3, OCH2CH2, CH2OCH2, CH2CH2O, Cyc, CH2Cyc, NR1 (CH2)3, NR1OCH2CH2, NR1CH2OCH2, NR1CH2CH2O, or NR1Y, R1 is H or C1-C6 alkyl, and Cyc is 1,2-cyclopropyl, 1,2-cyclobutyl, 1,3-cyclobutyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 1,2-cyclohexyl, 1,3-cyclohexyl, or 1,4-cyclohexyl. Z is (CH2)n or (CH2)n1 O(CH2)n2. R2 is an optionally substituted aryl or heteroaryl group. Variable n is an integer ranging from 1 to 5, variable n1 is an integer ranging from 0 to 4, variable n2 is an integer ranging from 0 to 4, and n1+n2=n?1.

Abstract: The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure useful for the synthesis of compounds that target KRAS G12C mutations, such as

Abstract: The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure useful for the synthesis of compounds that target KRAS G12C mutations, such as

Abstract: The present invention provides 6-hydroxy-8-oxatricyclo[3.2.1.02,4]octane-2-carboxamide derivatives of Formula (1) wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds. The compounds are used for inducing chondrogenesis, in methods of treating or preventing joint damage, resulting from joint injury or arthritis, and for inducing hyaline cartilage production. The present description discloses the preparation of exemplary compounds as well as pharmacological data thereof (examples 1 to 82; tables 1 and 2). An exemplary compound is e.g. rac-(1R,2R,4S,5R,6S)-4-(2-fluoropyridin-4-yl)-6-hydroxy-N-(4-(trifluoromethyl)pyridin-2-yl)-8-oxatricyclo[3.2.1.02,4]octane-2-carboxamide (example 1).

Abstract: Various aspects of this patent document relate to beverage concentrates that comprise active ingredients, containers comprising beverage concentrates, and methods to prepare beverage formulations from beverage concentrates.

Abstract: The technology described herein is directed to methods and compositions for prognosis and treatment of respiratory disease, e.g., COPD.