Abstract: DP-2 antagonists reversed PGD2-mediated human hair growth inhibition in a dose-dependent manner in vitro by reducing PGD2-triggered apoptosis and maintaining proliferation of keratinocytes. Hair follicles from approximately half of the alopecia patients exhibited little susceptibility to PGD2's effect in vitro. SNPs in the human DP-2 gene were identified that are associated with hair growth inhibition by PGD2. These findings underscore the role of DP-2 in regulating hair growth and indicate that DP-2 can be an effective approach in preventing and/or treating androgenetic alopecia in patients sensitive to PGD2. Furthermore, the SNPs identified here can be used to identify patients who will benefit from treatment.

Abstract: Disclosed herein are new compounds, pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).

Abstract: Emulsion formulations and systems for the intravenous or parenteral administration of neurokinin-1 (NK-1) receptor antagonists for treatment of emesis are provided. Methods for preparing the stable NK-1 receptor antagonist emulsions and pharmaceutical formulations are further provided. The emulsion formulations are prepared and characterized as a formulation and process that will allow an NK-1 receptor antagonist compound to be incorporated into an emulsion for intravenous injection and remain stable during the shelf life of the formulation. Specifically, emulsion formulations have an oil phase that includes oil, ethanol, egg lecithin, and the further addition of sodium oleate that is mixed with an aqueous phase and processed to form the emulsion formulation.

Abstract: The invention relates to compound of formula (I): in particular flavonoid derivatives (quercetin and catechin derivatives), for use in the prevention and/or the treatment of a disease or disorder involving both carbonyl and oxidative stresses.

Abstract: In various aspects and embodiments the invention provides a method of treating epilepsy in a subject in need thereof, the method comprising providing to the subject an effective amount of an FLNA modulator. In various embodiments, the FLNA modulator is PTI-125 or kartogenin. In various embodiments, the epilepsy is epilepsy associated with focal cortical dysplasia (FCD) type II or tuberous sclerosis complex (TSC).

Abstract: The present invention provides a novel compound having a protein kinase inhibitory activity, stereoisomers thereof or pharmaceutically acceptable salts thereof. The compound according to the present invention, stereoisomers thereof or pharmaceutically acceptable salts thereof are effective in preventing or treating protein kinase-related diseases such as cancers, autoimmune diseases, neurological diseases, metabolic diseases, infections or the like by showing a protein kinase inhibitory activity.

Abstract: Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, (I) are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.

Abstract: The present application provides a borate ester compound suitable for being used as a proteasome inhibitor, a preparation method and use thereof, and the compound has the following structure wherein, R1, R2 is asymmetric substituent in para-position, and R1 and R2 are both selected from the group consisting of halogen; and when R1 is F, R2 is not Cl; when R1 is Cl, R2 is not Br or F; and when R1 is Br, R2 is not Cl; X1, X2 is selected from the group consisting of hydroxyl, or X1 and X2 together form a substituted or unsubstituted 4 to 10 membered ring containing 1 to 4 heteroatoms being selected from the group consisting of O, N and S.

Abstract: The present invention provides a method for preparing the process intermediate 4-amino-5-methylpyridone of the formula (I), characterized in that the intermediate 4-hydroxy-5-methyl-1H-pyridin-2-one of the formula (III) is reacted with ammonia in an autoclave with addition of an ammonium bromide salt.

Abstract: Disclosed is a PD-L1 inhibitor, and specifically disclosed is a compound of formula (I) as a PD-L1 immunomodulator, a pharmaceutically acceptable salt or an isomer thereof.

Abstract: A pathological mechanism in FOP patients is further revealed, and development of a novel therapeutic drug, therapeutic method, diagnostic method, etc. utilizing an obtained finding is provided. The inventors have found a novel finding that in FOP, ectopic ossification, which occurs by an inflammation due to an injury, etc., is mediated by PAR1 to occur. From this finding, the inventors completed the present invention relating to a drug, etc. characterized by suppressing ectopic ossification in FOP by inhibiting PAR1.

Abstract: Described herein are crystalline forms of (3,5-dibromo-4-hydroxyphenyl)(2-(1-hydroxyethyl)benzofuran-3-yl-4,5,6,7-d4)methanone, and solvates thereof.

Abstract: The present disclosure provides compounds represented by Formula I: I, and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, and R13 are as defined as set forth in the specification, and the deuterium enrichment of any one or more of R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, and R13 is about 15% or more. The present disclosure also provides compounds having Formula I for use to treat or delay the progression of a lysosomal storage disorder or a neurodegenerative disease in a subject, provide neuroprotection in a subject having a lysosomal disorder, treat or prevent a migraine, and the symptoms associated therewith, in a subject, or improve mobility and/or cognitive function in a subject.

Abstract: Described herein are somatostatin subtype-2 receptor (SST2R) targeted therapeutics that target tumor cells expressing SST2R and their use in the treatment of cancer.

Abstract: The present disclosure provides a substituted pyrazolo[1,5-a]pyridine compound, a composition including the same, and a use thereof. The substituted pyrazolo[1,5-a]pyridine compounds is a compound represented by formula (I) or the tautomers, stereoisomers, prodrugs, crystal forms, pharmaceutically acceptable salts, hydrates or solvates thereof. The compound of the present disclosure and composition thereof are useful for treating RET kinase-mediated diseases or conditions and have more excellent pharmacokinetic properties.

Abstract: The present application provides heteroaryl amide compounds that activate the STING pathway to produce interferons, which are useful in the treatment of various diseases including infectious diseases and cancer.

Abstract: Disclosed are a pyrimidinyl group-containing tricyclic compound and applications thereof in preparing a cancer-treating medicament. Specifically disclosed are a compound as represented by formula (I), a pharmaceutically acceptable salt of same, or an isomer thereof.

Abstract: An object of the present invention is to provide an antifungal agent which is effective against cryptococcosis. The present invention provides an antifungal agent comprising ravuconazole as an active ingredient, wherein the agent is administered to an animal suffering from cryptococcosis. Further, the present invention provides an antifungal agent comprising ravuconazole as an active ingredient, wherein the agent is administered to an animal suffering from cryptococcus that is resistant to triazole-based antifungal agents selected from the group consisting of fluconazole, itraconazole and voriconazole.

Abstract: The present invention relates to compounds that are Nrf2 activators. The compounds have the structural formula I defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or disorders associated with Nrf2 activation.

Abstract: The invention provides a compound of formula I and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the formula I compounds, as well as methods of using such as therapeutic agents for the treatment of pain-related disorders and diseases and in combination with other therapeutic agents.