Abstract: A five-membered-fused six-membered compound, a preparation method, a pharmaceutical composition, and the use. The penta-fused hexa-heterocyclic compound is a compound represented by formula (II) or (III). The compound has an inhibition or/and degradation effect on IRAK4.

Abstract: Cosmetic and pharmaceutical formulations comprising specific amino acid combinations are described herein. Such formulations strengthen and enhance skin epithelial cell barrier function, thereby reducing moisture loss from the skin and restoring skin's structural integrity, epithelial differentiation, intercellular adhesion, and intracellular signaling and/or promoting maintenance of these features. Formulations described here comprise a therapeutically effective amount of free amino acids or a peptide combination of amino acids and either a therapeutically effective amount of a plant extract for skin barrier repair or a therapeutically effective amount of a retinoid for improving skin moisture. Also provided are injectable formulations described here for treating a subject suffering from osteoarthritis or symptoms thereof.

Abstract: Novel 7H-pyrido[4?,3?:4,5]pyrrolo[2,3-c][1,7]naphthyridine compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The 7H-pyrido[4?,3?:4,5]pyrrolo[2,3-c][1,7]naphthyridine compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.

Abstract: Novel pyrrolo[3,2-c]isoquinoline-2,3-diones, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrrolo[3,2-c]isoquinoline-2,3-dione compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.

Abstract: Silicon-substituted rhodamine compounds are disclosed herein. Also described herein are SiR dyes comprising at least one vinyl group attached to the Si atom (10 position) of the SiR dye. Derivatives, functionalized versions, conjugates, kits, related synthetic methods and uses of SiR compounds also are provided. Silicon-rhodamine (SiR) dyes can provide bright fluorescence at far red wavelengths and exhibit good photostability. The compounds described herein can be useful for fluorescent labeling and detection of biological samples.

Abstract: Methods, compositions, and medical kits are useful for treating and preventing multiple sclerosis using 1-(4-(((6-amino-5-(4-phenoxyphenyl)pyrimidin-4-yl)amino)methyl)piperidin-1-yl)prop-2-en-1-one, or a pharmaceutically acceptable salt thereof, according to preferred dosing regimens.

Abstract: Provided herein are methods for treating nonalcoholic steatohepatitis (NASH) in a subject, comprising administering to a subject having NASH an effective amount of a CCK receptor inhibitor.

Abstract: Provided is a compound of formula I or II, a stereoisomer, a tautomer, a geometrical isomer, a solvate, an active metabolite, a hydrate, a prodrug or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof, and the medical uses thereof in treating diseases benefiting from the capsid protein assembly inhibitor, particularly diseases caused by hepatitis B virus infection.

Abstract: The compounds of the invention, as described herein, are novel serotonin 5-HT2B antagonists useful for the treatment of myxomatous mitral valve degeneration (MMVD), congestive heart failure (CHF), and/or asymptomatic heart failure in animals, preferably canine.

Abstract: A compound of formula (I) given below or a pharmaceutically acceptable salt of the compound is useful as an IDO/TDO inhibitor.

Abstract: The present invention provides a compound or a salt thereof having a calcium-sensing receptor antagonistic activity, and being expected to be useful as an agent for preventing or treating heart failure, pulmonary hypertension, or the like. The compounds represented by formula (I) or a salt thereof has a calcium-sensing receptor antagonistic activity, and is expected to be useful as an agent for preventing or treating heart failure, pulmonary hypertension, or the like, wherein each symbol is as described in the specification.

Abstract: Biomarkers are provided that are predictive of a subject's responsiveness to a JAK inhibitor. The biomarkers, compositions, and methods described herein are useful in selecting appropriate treatment modalities for a subject having, suspected of having, or at risk of developing Graft-Versus-Host Disease.

Abstract: The present disclosure relates to pharmaceutical compositions suitable for oral administration, and more particularly to pharmaceutical compositions, including pharmaceutical tablet compositions, containing (2S)-N-{(1S)-1-cyano-2-[4-(3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-5-yl)phenyl]ethyl}-1,4-oxazepane-2-carboxamide (Compound A) or a pharmaceutically acceptable salt thereof.

Abstract: An 6-(4,5-bis(4-bromophenyl)-2-(4-methoxyphenyl)-1H-imidazol-1-yl)hexanoic acid compound, its synthesis, and its use as an antimicrobial agent.

Abstract: The invention described herein relates to compositions and methods for treating pain with wogonin. In particular, described herein are compositions and methods for treating musculoskeletal pain and arthritis with wogonin.

Abstract: A method of treating an oxidative stress disease includes orally or intragastrically administering, to a subject in need thereof, a pharmaceutical composition including edaravone with a time interval from a consumption of a meal by the subject in need thereof to an administration of the pharmaceutical composition to the subject in need thereof. The time interval is 8 hours or longer after the consumption of a high-fat meal, the time interval is 4 hours or longer after the consumption of a standard meal, or the time interval is 2 hours or longer after the consumption of a light meal.

Abstract: Liquid pharmaceutical compositions of apixaban or pharmaceutically acceptable salts thereof are described. More specifically, stable oral liquid pharmaceutical compositions of apixaban for oral administration are provided, wherein the composition is stable for extended periods of time. More specifically, stable liquid pharmaceutical compositions of apixaban at concentrations of 0.4 mg/mL or more are provided. Stable oral liquid compositions of apixaban, methods for their administration, processes for their production, and use of these compositions for treatment of diseases treatable by apixaban are disclosed.

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 defined 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 present invention regards specific IBAT inhibitors useful in the prophylaxis and/or treatment of a liver disease. It also relates to compositions comprising these IBAT inhibitors, a method for treatment of the disorders and a kit comprising the substances or the compositions.

Abstract: The invention relates to a compound of formula (I) wherein A1 and R1-R4 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.