Abstract: The present invention relates to novel 5-(hydroxyalkyl)-1-heteroaryl-1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.

Abstract: The present invention relates to the field of pharmaceutical chemistry, and specifically relates to a fused heterocyclic compound derivative and an application thereof. The fused heterocyclic compound derivative has the structure of general formula (I), and can be used to treat neuropsychiatric diseases.

Abstract: The present invention is concerned with indolin-2-one derivatives of general formula wherein the substituents are defined in claim 1. The compounds may be used in the treatment of CNS diseases related to positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, neurodegenerative disease, sleep disturbances, chronic fatigue syndrome, stiffness, inflammatory disease, asthma, Huntington's disease, ADHD, amyotrophic lateral sclerosis, effects in arthritis, autoimmune disease, viral and fungal infections, cardiovascular diseases, ophthalmology and inflammatory retinal diseases and balance problems, epilepsy and neurodevelopmental disorders with co-morbid epilepsy.

Abstract: Embodiments described herein provide a compound that may be used in a variety of applications such as corrosion inhibition, additives for metalworking, mining reagents, epoxy curatives, emulsifiers, fuel or lubricant additives, surfactant manufacture, acid scavengers and asphalt additives. The compound has the following structure: where R1 is a methoxy group, R2, R3, R4 and R5 are independently a hydrogen atom or an alkyl group, and R6 is an aminomethyl group.

Abstract: Inhibitors of HBV replication of Formula (IA) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein X and R1 to R6 have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.

Abstract: Phthalate derivatives that are aspartate-P-semialdehyde dehydrogenase (ASADH) inhibitor compounds, aspartate N-acetyltransferase (ANAT) inhibitor compounds, or both, are described, as well as methods of making the same, and methods of using the same.

Abstract: The present invention provides a heterocyclic compound having a HDAC inhibitory action, and useful for the treatment of central nervous system diseases including neurodegenerative disease, and the like, and a medicament comprising the compound. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

Abstract: Provided are 4?-arylmethoxy isoindoline compounds, e.g., 3-(1-oxo-4-((4-((3-oxomorpholino)methyl)benzyl)oxy)isoindolin-2-yl)piperidine-2,6-dione, or an isotopologue thereof, or an enantiomer or a mixture of enantiomers thereof. Pharmaceutical compositions comprising and methods for using the compounds are also disclosed.

Abstract: Disclosed in the present invention are a salt type and crystal type of 4H-pyrazolo[1,5-alpha]benzimidazole compound and a preparation method and intermediate thereof.

Abstract: The present disclosure provides compounds and nanostructures having one or more quaternary ammonium salts, compositions including the compounds and nanostructures, and methods useful for treating conditions using the compounds, nanostructures, and compositions. In at least one aspect, a compound is represented by formula (I): or a pharmaceutically acceptable salt thereof, wherein: Q is fluoro, chloro, bromo, or iodo; each of s, b, and n is independently an integer from about 10 to about 100; and each of v, j, p, z, q, x and m is independently an integer from 1 to about 20.

Abstract: Polymorphic forms of tetrahydro-N,N-dimethyl-2,2-diphenyl-3 -furanmethanamine hydrochloride (ANAVEX2-73) and a metabolite of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine hydrochloride (ANAVEX2-73) are disclosed and characterized. Compositions and method for treatment of Alzheimer's disease that includes the polymorphic forms and metabolite of tetrahydro-N,N-dimethyl-2,2 -diphenyl-3-furanmethanamine hydrochloride (ANAVEX2-73).

Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, and R6 are as described herein. The compounds of Formula I are agonists of the kappa opioid receptor and relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology, organic chemistry and polymer chemistry.

Abstract: Crystalline forms of brigatinib, pharmaceutical compositions comprising the same, and methods of their preparation and use of the same are disclosed herein.

Abstract: Compounds of Formula (I), which are activators of long form cyclic nucleotide phosphodiesterase-4 (PDE4) enzymes, are provided. Methods and uses of these compounds for the treatment or prevention of disorders requiring a reduction of second messenger responses mediated by cyclic 3?,5?-adenosine monophosphate (cAMP) are also described.

Abstract: The present invention discloses a process for recovery of a boronic acid of formula R3—B(OH)2, wherein R3 is selected from the group consisting of C1-C6 linear or branched alkyl, C3-C6 cycloalkyl, and C6 aryl, optionally substituted with a group selected from the group consisting of methyl, ethyl, n-propyl, i-propyl, n-butyl, sec-butyl, t-butyl, and phenyl, comprising admixing the boronic acid with a water-immiscible organic solvent in a weight ratio between the boronic acid and the water-immiscible organic solvent from 1:10 to 1:20, adding an aqueous solution to a final pH of neutral, and partitioning the boronic acid into an organic water-immiscible phase and recovery of the organic water-immiscible phase.

Abstract: The present disclosure relates to indole derivatives of the formula (I) which are cannabinoid type 1 receptor modulators and which are useful in the treatment of diseases in which modulation of the receptor is beneficial; to processes for their preparation; to pharmaceutical compositions comprising them; and to methods of using them.

Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatohepatitis, metabolic syndrome, atherosclerosis, and cancer.

Abstract: The invention relates to novel chemical entities that act as thromboxane (TX) A2 receptor, or T prostanoid receptor (TP), antagonists and to their use in the treatment of human diseases in which thromboxane (TX) A and of all other agents that act as incidental ligands of TP, including the endoperoxide prostaglandin (PG)G2/PGH2, 20-hydroxyeicosatetraenoic acid (20-HETE) and the free-radical derived isoprostanes (e.g., 8-iso-prostaglandin (PG)F2?), play a role. Compounds of the invention preferably include a benzenesulfonyl urea in which the benzene is substituted by a substituted biphenylyloxy group (e.g., at the 2 position) and by a nitrile group (e.g., at the 5 position), which compounds show promising results as TP-isoform selective TP antagonists.

Abstract: Provided is a compound having formula (I): wherein R2 is selected from —C1, —Br and —CN; R1 and R4 are independently selected from H and —F; R631, R632, R641 and R642 are independently selected from —H, —F and substituted or unsubstituted C1-C3 alkyl groups; and R651 and R652 are independently selected from H and substituted or unsubstituted C1-C3 alkyl groups and substituted or unsubstituted phenyl groups; and wherein at least one of R631, R632, R641, R642 and R652 is not —H, or wherein when all of R631, R632, R641, R642 and R652 are —H, R651 is not Me or Et.

Abstract: The present invention provides compounds useful as inhibitors of Tyrosine Kinase 2 (Tyk2), solid forms and compositions thereof, methods of producing the same, and methods of using the same in the treatment of Tyk2-mediated diseases.