Abstract: Derivatives of relebactam, therapeutic methods of using the derivatives of relebactam, particularly in combination with ?-lactam antibiotics and pharmaceutical compositions thereof are disclosed. The derivatives of relebactam are suitable for oral administration.

Abstract: The invention provides compounds of formula (I) or salts thereof: wherein: A, B, C, D, W, X, Y and Z are as defined in the specification, and at least one of A, B, C, D, W, X, Y and Z is OR1; each R1 being independently H or C(?O)R2, and at least one R1 group being C(?O)R2; where each R2 is selected from: CHR3NHR4, where R4 is H and R3 is a group selected from CH3, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-3-(1H-indole), CH2CH2SCH3, CH2OH, CHOHCH3, CH2SH, CH2SeH and CH2PhpOH, wherein said R3 group can optionally be substituted by one or more groups selected from halogen, cyano, nitro, ORA or C1-C4 alkyl; or R3 and R4 together with the C and N atoms to which they are attached form a 5-membered heteroalkyl ring, wherein said heteroalkyl ring can optionally be substituted by one or more groups selected from halogen, cyano, nitro, ORA or C1-C3 alkyl, wherein RA is C1-C4 alkyl optionally substituted with one or more halogen, cyano or nitro groups.

Abstract: Estrane-based and androstane-based aminosteroid derivatives are described herein. More specifically, the following piperazinyl-steroid compounds of Formula I, Formula II, Formula III, and Formula IV are described. The compounds display cytotoxicity on a variety of cancer cell lines. A process for producing the compounds and their use in the manufacture of pharmaceutical formulations and/or combinations is also disclosed.

Abstract: Identified compounds demonstrate protein kinase inhibitory activity. More specifically, the compounds having the structures below (I) are demonstrated to inhibit receptor interacting kinase 2 (RIPK2) and/or Activin-like kinase 2 (ALK2). Compounds that are either dual RIPK2/ALK2 inhibitors or that preferentially inhibit RIPK2 or ALK2 could provide therapeutic benefit.

Abstract: Provided herein are compounds useful for the treatment of various parasitic diseases. These compounds, as well as pharmaceutically acceptable salts thereof may be formulated in pharmaceutical compostions, veterinary compositions and may be used in methods of treatment and/or prophylaxis of diseases spread by parasites, including malaria and cryptosporidiosis.

Abstract: The present invention addresses the problem of providing a therapeutic agent for abdominal aortic aneurysms, with which pharmacotherapy is possible. The present invention provides a therapeutic agent for an aortic aneurysm comprising, as an active component, (?)-6-[3-[3-cyclopropyl-3-[(1R,2R)-2-hydroxycyclohexyl]ureido]propoxy]-2(1H)-quinolinone or a salt thereof, or a solvate of these.

Abstract: This application relates to compounds of the following Formula: or pharmaceutically acceptable salts thereof, which are inhibitors of PI3K-? which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.

Abstract: Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.

Abstract: This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those benzodiazepine derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of a a5-containing GABAA receptor agonist (e.g.

Abstract: The present invention provides compounds and compositions which are positive allosteric modulators of GABA-A receptors that selectively target the peripheral nervous system and organs of the body, and which do not pass through the blood-brain barrier. The compounds and compositions of the present invention are useful for treatment of diseases or disorders which are mediated by GABA-A neuronal activity, such as, for example, visceral pain, gut motility, irritable bowel syndrome, functional abdominal pain, functional idiopathic diarrhea, inflammatory bowel diseases, drug induced pain, bile salt malabsorption, lactase or other carbohydrate intolerance.

Abstract: The present invention relates to polymorphic forms of marizomib (e.g., Morphic Form I). The morphic forms can be used alone and in pharmaceutical compositions for the treatment of disease.

Abstract: The present invention provides crystalline solids of 6?-((6-aminopyrimidin-4-yl)amino)-8?-methyl-2?H-spiro[cyclohexane-1,3?-imidazo[1,5-a]pyridine]-1?,5?-dione: The crystalline compounds of the present application are inhibitors of Mnk and finds utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.

Abstract: The disclosure is directed to compounds of Formula I Pharmaceutical compositions comprising compounds of Formula I as well as methods of their use and preparation, are also described.

Abstract: Disclosed are compounds of Formula (I?), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

Abstract: The present invention relates to avibactam free acid, a method for preparing avibactam free acid and a method for preparing avibactam sodium by further reacting avibactam free acid. The invention further refers to a pharmaceutical composition comprising avibactam free acid, one or more alkaline sodium salt(s) and one or more beta-lactam antibiotic(s). The pharmaceutical composition of the present invention can be used as medicament, in particular for treatment and/or prevention of bacterial infections.

Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula I or their pharmaceutically acceptable salts, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.

Abstract: The present invention relates to bisaryl heterocycle compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 activators.

Abstract: The invention describes the pyrimidine-based compounds of the general formula I. Described compounds lower the production of the prostaglandin E2. In concentrations lowering production of this factor by 50%, these compounds have no negative effect on the cell viability and they are not cytotoxic. Furthermore, the method of production of the compounds of the general formula I is provided. A pharmaceutical composition comprising the polysubstituted pyrimidines according to the invention and the use of these compounds for the treatment of the inflammatory diseases are also provided.

Abstract: A heteroaryl-pyrazole derivative, and a preparation method therefor and a medical application thereof are described. Specifically, a new heteroaryl-pyrazole derivative as shown in formula (I), a preparation method for the derivative, a pharmaceutical composition containing the derivative, and a use of the derivative as a therapeutic agent, in particular as a TLR7 agonist, are described. The substituents in formula (I) have the same definitions as in the description.

Abstract: Disclosed are 4-pyrimidin-5-ylmethyl-morpholines of formula A and pharmaceutically acceptable salts thereof, wherein R1 and R2 are defined herein. Also disclosed are processes for their preparation, pharmaceutical compositions containing the compounds, and their use in therapy, particularly in the treatment or prevention of conditions having an association with NR2B negative allosteric modulating properties.