Abstract: The present invention provides a compound that is highly safe and useful in the prevention, alleviation, and/or treatment of various diseases involving enteropeptidase inhibition and/or trypsin inhibition, a pharmaceutical composition containing the compound, a method for producing the compound, and the like. Specifically, the present invention provides a compound represented by the following general formula (I): [wherein: A1 and A2 each independently represent an inhibitor residue having at least one activity selected from an enteropeptidase inhibitory activity and a trypsin inhibitory activity; and Z represents a spacer that links A1 to A2] or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed herein are methods for treating solid tumors by direct injection into the tumors of chemotherapeutic particles, methods for inhibiting tumor metastasis by administering chemotherapeutic particles to a subject having a tumor, and compositions that include chemotherapeutic particles, small amounts of a polysorbate, and a carrier.

Abstract: The present invention relates to a novel compound exhibiting enteropeptidase-inhibiting activity, a pharmaceutically acceptable salt thereof, a pharmaceutical composition for preventing and treating metabolic diseases such as obesity, diabetes mellitus or hyperlipidemia, etc. comprising the compound or pharmaceutically acceptable salt, and a method for preventing or treating metabolic disease using the above novel compound. The compound of the present invention has excellent inhibitory activity against enteropeptidase, and thus is not absorbed into the body, but are excreted outside the body. However, since not only fat but also protein are discharged together, it has few side effects such as fat stools and acts only in the gastrointestinal tract, so it has few side effects such as depression, and is very useful as a therapeutic or prophylactic drug for various metabolic diseases such as obesity, diabetes mellitus, and hyperlipidemia.

Abstract: The present disclosure generally relates to methods of treating hemolytic diseases such as sickle cell anemia using kinase inhibitors, for example, compounds that inhibit the spleen tyrosine kinase (SYK). In some embodiments a method is presented to prevent thrombosis in blood vessels of patients with a hemolytic disease comprising the step of: administrating to a patient having at least one hemolytic disease a therapeutically effective amount of at least one SYK inhibitor. In some embodiments the method includes repeatedly administering the SYK kinase inhibitor to a patient.

Abstract: The present disclosure is directed to a topical composition, e.g., a physically and chemically stable topical composition of Fenoldopam comprising about 0.1% to about 5% by weight of Fenoldopam or a pharmaceutically acceptable salt thereof, at least one polyacrylamide-type gelling agent, at least one cellulose-type gelling agent, and at least one solvent, wherein the Fenoldopam is substantially solubilized in the composition, and wherein the composition is stable for at least twelve months at 25° C. and 60% relative humidity.

Abstract: Disclosed herein are new dosage regimens for deuterium-substituted benzoquinoline compounds, and methods for the treatment of abnormal muscular activity, movement disorders, and related conditions.

Abstract: The disclosure provides new, stable, pharmaceutically acceptable hydrochloride salt forms of 1-(4-fluoro-phenyl)-4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one, together with methods of making and using them, and pharmaceutical compositions comprising them.

Abstract: Compositions are provided for the liquid oral administration of topiramate and its salts. The invention further provides methods for treating diseases and disorders using the compositions.

Abstract: This invention provides methods utilizing ketamine for the treatment of motor disorders and/or side effects associated with certain medications used in the treatment of motor disorders. For example, in some embodiments, methods are provided for treating side effects associated with the administration of levodopa to a subject having Parkinson's disease, by administering a dose of ketamine or a pharmaceutically acceptable salt thereof. In particular, the invention provides methods for reducing dyskinesia associated with motor disorder (e.g., Parkinson's disease) treatments, and effective doses of ketamine or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to the compound (S)-n-hydroxy-2-(2-(4-methoxyphenyl) butanamido)thiazole-5-carboxamide, which is a novel histone deacetylase inhibitor. The invention further relates to the use of the compound for the inhibition of histone deacetylating activities of HDAC isoforms and treatment of histone deacetylase (HDAC)-associated diseases. The invention also relates to the pharmaceutical compositions and the making of the pharmaceutical compositions comprising the compound.

Abstract: Disclosed herein are methods of reprograming autologous tissues or cells into astrocytes or astroglial progenitor cells using one or more small molecule compounds only without any transgenes. Also disclosed are methods of preventing or treating neurodegenerative diseases or neurological disorders associated with dysfunction of astrocytes, such as Alzheimer's Disease, by transplanting the astrocytes or astroglial progenitor cells produced by the methods disclosed herein into the brain of a subject suffering from the neurodegenerative disease or neurological disorder.

Abstract: The use of ferric maltol compositions for the treatment or prevention of cancer and tumours is disclosed, in particular for the treatment or prevention of gastrointestinal cancers or gastrointestinal tumours, such as large bowel (colorectal), small bowel or upper gastrointestinal cancers.

Abstract: Natural cooling formulations which include one or more natural cooling compounds and are suitable for use in consumer products are provided. Natural cooling compounds include natural isopulegol, natural menthyl lactate, natural menthyl succinate, natural menthol and combinations thereof. The disclosed formulations provide enhanced cooling attributes.

Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables are as devined herein. Moreover, The compounds of this invention have formula I-A: or a pharmaceutically acceptable salt, wherein the variables are as defined herein.

Abstract: The invention relates to a method for the diagnosis of non-alcoholic steatohepatitis (NASH), for determining the activity, the stage, or the severity of NASH or for classifying a subject as a potential receiver or non receiver of a treatment of NASH using circulating miRNAs and other blood circulating markers of liver damage, e.g. alpha 2 macroglobulin, HbA1c, N-terminal pro-peptide of collagen type III, miR-34 and miR-200. It also relates to a kit for implementing the method of the invention, and the compounds for use in a method for the treatment of NASH, wherein the subject to be treated is identified, evaluated or classified according to the method of the invention.

Abstract: A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises subjecting to elevated temperature the compound of Formula I, the water-soluble polymeric carrier and the surfactant, to provide an extrudable semi-solid mixture; extruding the semi-solid mixture; and cooling the resulting extrudate to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer or an immune or autoimmune disease.

Abstract: The present invention is directed to novel prodrugs of modulators of the NMDA receptor. Separate aspects of the inventions are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat neurological disorders or neuropsychiatric disorders such as depression.

Abstract: The present invention generally relates to systems and methods for treating vitiligo. In one set of embodiments, the present invention comprises a composition comprising pyruvic acid and/or a pyruvate salt. The composition may be formulated for application to the skin of a subject, for instance, as a gel, lotion, cream, ointment, soap, or stick. In some cases, the composition may comprise a lecithin, such as phosphatidylcholine. In certain embodiments, the lecithin is present as a liquid crystal, and/or in liposomes, micelles, or other vesicles. Other aspects of the present invention are generally directed to methods of making or using such compositions, methods of promoting such compositions, kits including such compositions, or the like.

Abstract: A method for relieving menstrual pain and reducing menstrual blood loss in a female is provided. The method comprises administering to the female an oral combination drug formulation comprising a first therapeutically effective dose of a non-steroidal anti-inflammatory drug (NSAID) and a second complementary low dose of tranexamic acid, wherein the NSAID is formulated to relieve the menstrual pain and to reduce a volume of menstrual blood loss of the female, wherein the dose of tranexamic acid ranges from 50 mg to 425 mg per oral combination drug formulation.

Abstract: A SMAC mimetic and pharmaceutical compositions thereof and methods of use.