Abstract: Adenosine receptor (e.g., A2A and/or A1 receptor) antagonist compounds and compositions including said compounds are disclosed. The present disclosure also provides methods of using said compounds and compositions for modulating (e.g., inhibiting or antagonizing) A2A and/or A1 receptor in a biological system. The compounds and compositions find use in various therapeutic applications including the treatment of central nervous system or neurodegenerative diseases, such as Parkinson's disease. The compounds and compositions may also find use in various therapeutic applications including the treatment of cancer and in immuno-oncology.

Abstract: A method of treating Parkinson's Disease, Huntington's Disease and the like, diseases with abnormal dopamine-neuro-transmission, using small molecules administered systemically that penetrate into the central nervous system to inhibit the rate-limiting step of dopamine synthesis in the central nervous system, the conversion of L-tyrosine to L-3, 4-dihydroxyphenylalanine (L-DOPA) by tyrosine hydroxylase along with its cofactors tetrahydrobiopterin and iron (Fe+).

Abstract: The invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3 and R4 are as defined herein. The invention further relates to pharmaceutical compositions comprising such compounds and salts, and to methods and uses of such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer, in a subject in need thereof. The invention further relates to solid forms of 8-((2-fluoro-4-(methylthio)phenyl)amino)-2-(2-hydroxyethoxy)-7-methyl-3,4-dihydro-2,7-naphthyridine-1,6(2H,7H)-dione.

Abstract: Compounds of Formula (I): salts thereof and methods of making and use as Janus kinase inhibitors are described herein.

Abstract: The present invention provides photosensitizer compounds for use in detecting beta-lactamase activity. Methods and kits that utilize the photosensitizer compounds of the invention for the detection of, quantitation of, and classification or typing of microbial beta-lactamases.

Abstract: The invention provides methods of treatment of heart failure with preserved ejection fraction (HFpEF) using modified forms of trimetazidine, such as CV-8972 and CV-8814.

Abstract: The present invention provides methods and compositions for treating advanced stage non-small cell lung cancer by cyclohexenone compounds.

Abstract: Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.

Abstract: The present invention provides new methods and kits for treating IBS; treating IBS in females; treating IBS in older subjects; and treating IBS in non-white subjects.

Abstract: Physicochemically stable oral pharmaceutical solution comprising fludrocortisone acetate and a non-aqueous liquid carrier comprising one or more medium-chain fatty acid triglycerides.

Abstract: Substituted imidazole and substituted pyrazole compounds and compositions derived therefrom can be useful in controlling insect pests. Suitable imidazole compounds can be analogues of 2,4,5-triphenyl-1H-imidazole, wherein the C-2 phenyl group bears at least one substitution, the C-4 and C-5 phenyl groups are optionally substituted, and N-1 is unsubstituted. Suitable pyrazole compounds can bear a 1,3,4-substitution pattern, with an optionally substituted aryl or optionally substituted alkyl group being present at N-1, an optionally substituted aryl or optionally substituted heteroaryl group being present at C-3, and a secondary amide group being present at C-4. These compounds and compositions derived therefrom can be administered to a plant, seed, soil or insect to control a variety of insect pests.

Abstract: The present invention provides a novel compound represented by Chemical Formula 2, or a pharmaceutically acceptable salt thereof. The novel compound according to the present invention exhibits an excellent acid secretion inhibitory effect.

Abstract: A process is described for the preparation of freeze-dried pharmaceutical compositions of mitomycin C, which are characterized by high stability and can be rapidly reconstituted to form solutions.

Abstract: The present invention is directed to bi-functional compounds which find use as pharmaceutical agents in the treatment of disease states and/or conditions which are mediated through macrophage migration inhibitory factor (MIF) or immunoglubin G (IgG). The present invention is also directed to pharmaceutical compositions which comprise these bi-functional compounds as well as methods for treating disease states and/or conditions which are mediated through MIF/IgG or where MIF/IgG is a contributing factor to the development and perpetuation of diseases and/or conditions, especially including autoimmune diseases and cancer, among others. The purpose of the present invention is to provide a molecular strategy to lower plasma MIF/IgG level in patients with autoimmune diseases or certain types of cancers.

Abstract: The present invention provides compounds useful for the treatment of narcolepsy or cataplexy in a subject in need thereof. Related pharmaceutical compositions and methods are also provided herein.

Abstract: Provided herein are methods of treating glaucoma in a patient, comprising: obtaining a biological sample from the patient; testing the biological sample for presence of a mutation in Kir6.2 protein or KCNJ11 gene and a mutation in the Aquaporin-9 protein or AQP-9 gene; and provided that the biological sample tests positive for the presence of a mutation in Kir6.2 protein or KCNJ11 gene and a mutation in the AQP-9 gene or aquaporin-9 protein, administering to the patient a therapeutically effective amount of a sulfonylurea such as tolbutamide or a physiologically equivalent salt or solvate thereof and a pharmaceutically acceptable carrier. Also provided herein are methods of maintaining and/or improving eye health in a subject, comprising: administering to the patient a therapeutically effective amount of tolbutamide or a physiologically equivalent salt or solvate thereof, and a pharmaceutically acceptable carrier.

Abstract: The present disclosure relates to compositions of N-acetylcysteine for use in treating aortic stenosis. Methods of treating aortic stenosis in a subject comprising administering to said subject an effective amount of N-acetylecysteine (NAC) or other thiol-reactive compound, or agents that inhibit TGF-Beta activation and/or signaling.

Abstract: The present invention relates to methods for the treatment of metastatic cancer. Methods of treating metastatic cancer by administration of a set of drugs overcome multiple mechanisms of melphalan resistance and hypersensitize cancer cells to melphalan are described. The methods involve the administration of drug(s) that induce oxidative stress in cancer cells, in conjunction with melphalan on a defined schedule.

Abstract: The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor.

Abstract: The present invention is directed towards new chemical entities which primarily inhibit the human T-type calcium channels and differentially modulate other key ion channels to control cell excitability, and abnormal neuronal activity, particularly involved in hypersensitive cough or itching.