Abstract: Disclosed are a novel isoindoline derivative, a pharmaceutical composition and use thereof. The compound of formula I, or the pharmaceutically acceptable salt, solvate, polymorph, co-crystal, stereoisomer, isotopic compound, metabolite or prodrug thereof disclosed in the invention can regulate the generation and/or activity of PDE4 and/or TNF-? so as to effectively treat cancer and inflammatory diseases.

Abstract: The present disclosure is concerned with thioquinolinone compounds for the treatment of disorders associated with heme oxygenase-1 (HO-1) signaling dysfunction such as, for example, kidney diseases (e.g., chronic kidney disease, acute kidney injury). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: Disclosed are a method for destroying cellular mechanical homeostasis and the use thereof, especially disclosed is a method for destroying cellular mechanical homeostasis by using a Myosin inhibitor thereby leading to cell softening and reduction of fibrosis in tissues and organs. Also disclosed are a method for promoting regeneration and repair of tissues and organs and the use thereof. The Myosin inhibitor can destroy the homeostasis of the cellular mechanical stress system, reduce the rigidity of tissues and organs in a pathological state, and stimulate stress and regeneration reactions similar to those in the regeneration processes in lower organisms; and can use the characteristics to greatly inhibit fibrosis during the organ damage and to promote the regeneration and repair of tissues and organs, and meanwhile can use stress response to greatly improve the ability of cellular genetic repair. The Myosin inhibitor is preferably (?)-Blebbistatin, or a derivative thereof (?)-Blebbistatin O-Benzoate.

Abstract: The present invention relates generally to novel rhodamine dyes which upon conjugation with another molecule form single isomeric conjugation products. These novel rhodamine dyes contain only one single functional group on the rhodomine molecule for conjugation so that their conjugation products are single isomeric conjugation products.

Abstract: The present invention relates to a compound and the application thereof in treating inflammation or inflammation-related diseases, and more specifically to a compound UTLOH combination. Said compound effectively inhibits the level of LPS-induced PGE2 and NO, while effectively treating inflammatory or inflammatory-related diseases.

Abstract: This disclosure provides pharmaceutical compositions comprising defined amino acid components, and methods for treating traumatic brain injury comprising administering an effective amount of the compositions to a subject in need thereof.

Abstract: This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteoblastic bone metastases, with a dual inhibitor of MET and VEGF.

Abstract: The present disclosure relates to solid state forms of Omecamtiv mecarbil and Omecamtiv mecarbil diHCl, processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: A quaternary ammonium salt comprising a chromophore constituent, a tertiary amine cation constituent connected to the para-position of the chromophore constituent via a methylene linkage, and a borate anion constituent, wherein chromophore constituent is a 3-ketocoumarin constituent or a benzophenone constituent. Also, a photobase-redox initiating system comprising the quaternary ammonium salt and a peroxide.

Abstract: The present invention generally relates to novel pharmaceutical formulations containing 2-[3,5-Bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-3-pyridinyl}-N,2-dimethylpropanamide, methods of preparation thereof and their use in medical therapy.

Abstract: Methods and compositions are disclosed for diagnosing a patient suspected of suffering from, and for treating a patient suffering from, a disorder such as hypercortisolemia, metabolic syndrome, pre-diabetes, diabetes, Cushing's syndrome, Cushing's Disease, hyperglycemia secondary to hypercortisolemia, a liver disease, a cardiac disorder, high blood pressure, a blood clotting disorder, a cancer, a psychological disorder, weight gain, a disorder of glucose control, a bone disorder (e.g., osteoporosis), hypogonadism, pseudoacromegaly, pituitary tumors, functional hypercortisolism, ACTH secreting tumors, peripheral neuropathy, dyslipidemia and other disorders. The methods and compositions include administration of a heteroaryl-ketone fused azadecalin glucocorticoid receptor modulator (GRM).

Abstract: Methods of improving visual endpoints related to retina-associated disease with CCR3 modulating agents are provided. An example of such an endpoint is visual acuity. Retina-associated diseases upon which visual acuity and other visual endpoints may be improved include retinopathy of prematurity, age-related macular degeneration, central retinal vein occlusion, and diabetic retinopathy.

Abstract: In various aspects and embodiments provided are compositions and methods for a disease or disorder in a patient such as a disease or disorder that affects the brain in a patient and treating such patient.

Abstract: Provided herein are inhibitors of SLC26A3, which is an anion (CV, HCO3, oxalate) exchanger expressed in intestinal epithelial cells. SLC26A3 inhibitors have potential utility for treatment of constipation including chronic idiopathic constipation (CIC), opioid-induced constipation (OIC), constipation-predominant irritable bowel syndrome (IBS-C), cystic fibrosis-associated constipation, meconium ileus, distal intestinal obstruction syndrome, calcium oxalate kidney stone disease, enteric hyperoxaluria and primary hyperoxalurias.

Abstract: Compositions for intravenous infusion of istaroxime, or a metabolite of istaroxime, in human patients suffering from heart failure are disclosed. Likewise, methods for extended infusion of istaroxime or its metabolites in individuals with heart failure are disclosed. In particular, some methods disclosed herein include the infusion of istaroxime, or a metabolite thereof, for a period of time that is greater than six hours in order to improve cardiac relaxation without triggering arrhythmogenic events in an individual suffering from heart failure. Other methods include administration of istaroxime until certain plasma concentration thresholds of istaroxime metabolites are achieved. Also disclosed are istaroxime metabolites with selective SERCA2a activation.

Abstract: The present invention relates to a method of synthesizing a compound of formula (I) also referred to as 4-(((2S,4S)-(4-ethoxy-1-(((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl))benzoic acid, or a pharmaceutically acceptable salt thereof, and/or intermediates thereof, their use as pharmaceuticals and pharmaceutical compositions and the use of intermediates for preparing a compound of formula (I), or a pharmaceutically acceptable salt thereof.

Abstract: Two crystals of (S)-(+)-hydroxychloroquine sulfate. One crystal features diffraction peaks at 12.3±0.1°, 13.1±0.1°, 17.9±0.1°, 22.8±0.1°, 23.4±0.1°, 25.1±0.1°, and 26.3±0.1° as 2? angles in a powder X-ray diffraction pattern. The other crystal features diffraction peaks at 12.8±0.1°, 14.5±0.1°, 16.7±0.1°, 17.6±0.1°, 20.2±0.1°, 21.4±0.1°, 23.8±0.1°, 25.7±0.1°, and 26.0±0.1° as 2? angles in a powder X-ray diffraction pattern. Also disclosed are methods of preparing crystals of (S)-(+)-hydroxychloroquine sulfate.

Abstract: A process for preparing a batch of highly purified, pharmaceutical grade tasimelteon comprises analyzing a batch of tasimelteon synthesized under GMP conditions for the presence of one or more identified impurities.

Abstract: Provided herein are methods for making an alpha-tocotrienol enriched tocol mixture, such as from a plant or plant-derived material. Also provided herein are simulated moving bed purification methods for tocotrienol compounds such as alpha tocotrienol.

Abstract: This application is directed to a compound of Formula II Also disclosed is a process for preparing a compound of Formula II comprising using the compounds of Formulae IV and V Also disclosed is a method for preparing a compound of Formula I comprising contacting a compound of Formula II with a compound of a compound of Formula VI wherein A1, A2 A3, R1, R2, R3a, R3b, R4, B1, B2 and B3, are as defined in the disclosure.