Abstract: The present invention relates to a novel fused ring compound having urea structure that exhibits excellent NAMPT activating effect, and a method using the same for treating/preventing metabolic disorder, cardiovascular and kidney disease, mitochondrial disease, neurodegenerative disease, ocular disease, and muscle wasting disorder. The present invention provides a compound represented by following formula (I) or a pharmacologically acceptable salt: wherein A, B, R1, R2 and R3 represent the same meanings as in the claims.

Abstract: Provided are a preparation of semicarbazide-sensitive amine oxidase inhibitor and the use thereof. In particular, disclosed are a compound as shown in formula I, or a stereoisomer or racemate or pharmaceutically acceptable salt thereof. Also disclosed is that the above-mentioned compound can inhibit semicarbazide-sensitive amine oxidase.

Abstract: This invention provides a compound of formula I, their synthesis and their use for treating a SHP2 mediated disorder. More particularly, this invention provides a pharmaceutical composition comprising the said compound.

Abstract: The invention discloses herein related to synergistic combination of exogenous bioactives for activating intracellular secondary messenger (cAMP) signalling pathway. Particularly, the invention relates to synergistic compositions comprising combination of therapeutically effective amount of (3R)-3-acetyloxy-4-(trimethylazaniumyl) butanoate and N-4-aminobutylguanidine and salts thereof present in a weight ratio of 1:0.01 to 1:2 along with pharmaceutically acceptable excipients. Furthermore, the composition is useful for treating disease conditions or disorders related to depletion of secondary messenger pathway. The present invention further provides method of treating disease conditions related mental illness or disorder.

Abstract: HM30181 (shown below) can be used to improve absorption of cancer chemotherapy drugs, such as paclitaxel. Herein are described various polymorphisms of HM30181, in particular polymorphisms B, D, E, F, G, H, I, J, K, L, and M as well as their physical properties and methods for their preparation and characterization.

Abstract: This document provides methods and materials for improving arteriovenous fistula (AVF) maturation and/or maintaining AVF functionality. For example, methods and materials for using one or more senolytic agents to improve AVF maturation, to maintain AVF functionality, and/or to maintain the patency of an AVF are provided. Methods and materials for using one or more senolytic agents to maintain functionality and/or patency of a venous graft (e.g., a venous graft that bypasses an occluded artery) also are provided.

Abstract: The invention provides compounds of the formula (1): or a salt or tautomer thereof, wherein R1 is hydrogen or fluorine, pharmaceutical compositions containing the compounds and medical uses of the compounds (for example, in the treatment of inflammatory or immune disorders).

Abstract: The present invention aims to provide a compound that may be useful for the prophylaxis or treatment of constipation and the like. The present invention provides a compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof.

Abstract: Provided in the present disclosure is crystal form I of compound 1, and a preparation method thereof and the use thereof.

Abstract: Disclosed herein, inter alia, are compositions and methods for targeting E3 ligases. In an aspect is a targeted protein degrader including 1) a targeted protein binder and 2) an E3 Ubiquitin ligase binder, wherein the E3 Ubiquitin ligase is human RNF4 or human RNF114. In an aspect is provided a pharmaceutical composition including a compound as described herein, including embodiments, and a pharmaceutically acceptable excipient.

Abstract: The present invention provides a novel thiazole derivative or a pharmaceutically acceptable salt thereof, and a method for preparing the same. The thiazole derivative or pharmaceutically acceptable salt thereof according to the present invention has selective inhibitory activity against cyclin-dependent kinase (CDK) and thus can be used as a preventive or therapeutic agent for various diseases associated with CDK.

Abstract: The present disclosure relates to a method of reducing or arresting viral load in a subject infected with a coronavirus, the method comprising the step of administering to the subject a therapeutically effective amount of a viral protease inhibitor. In some embodiments, the subject is a human. In one embodiment, the coronavirus is SARS-COV-19 and the viral protease inhibitor is E)-N-(4-(3-(tert-butyl)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-methoxystyryl)phenyl)methanesulfonamide; (R)-3-((2S,3S)-2-hydroxy-3-(3-hydroxy-2-methylbenzamido)-4-phenylbutanoyl)-5,5-dimethyl-N-(2-methylbenzyl)thiazolidine-4-carboxamide; R)—N-allyl-3-((2S,3S)-2-hydroxy-3-(3-hydroxy-2-methylbenzamido)-4-phenylbutanoyl)-5,5-dimethylthiazolidine-4-carboxamide; (4-((N-(5-cyclopropyl-2-(4-fluorophenyl)-3-(methylcarbamoyl)benzofuran-6-yl)methylsulfonamido)methyl)-2-fluorophenyl)boronic acid or salts thereof.

Abstract: The embodiments of present invention provide processes for the large-scale preparation of 2,4,6-trifluoro-N-[6-(1-methylpiperidine-4-carbonyl)-2-pyridyl]benzamide hemisuccinate, and formulations and product forms, such as tablets, made by these processes. Additionally, embodiments of the present invention provide tablets including 25 mg, 50 mg, 100 mg, or 200 mg free base equivalent of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide hemisuccinate.

Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.

Abstract: This invention relates to LOX enzyme-inhibiting compounds in accordance with Formula I or Formula II, or a pharmaceutically acceptable salt or hydrate thereof: and pharmaceutical compositions comprising the compounds. Such compounds and compositions can be useful in treating a variety of conditions, diseases, and disorders including, but not limited to, fibrotic disorders, proliferative disorders, cardiovascular disorders, acute and chronic inflammatory disorders, primary and metastatic cancer, pulmonary conditions, ocular diseases, and neurological and neuropsychiatric conditions. 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: Provided herein is a method for the manufacture of a compound of obicetrapib and salts thereof, such as calcium salts thereof. Also provided herein is amorphous obicetrapib hemicalcium. New intermediates for use in the synthesis of obicetrapib, and salts thereof are also provided, including obicetrapib HCl and a mesylate salt for the use in the synthesis of obicetrapib and amorphous obicetrapib hemicalcium.

Abstract: The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, such as a compound of Formula I: or a tautomer, stereoisomer, mixture of stereoisomers, hydrate, solvate, isotopically enriched analog, or pharmaceutically acceptable salt thereof, to products containing the same, as well as to methods of their use and preparation.

Abstract: Provided are compounds of Formula (I): Formula (I), including compounds of Formulas (II), (III), (IV), (V) and (VI), wherein X, R1, R2, R3, R4 and n are as defined herein, and pharmaceutically acceptable salts thereof, and methods for their use and production. These compounds can be useful, e.g., in the treatment of disorders responsive to the inhibition of apoptosis signal-regulating kinase 1 (ASK1).

Abstract: The invention relates to nitric oxide releasing phosphodiesterase type 5 (PDE5) inhibitors of formula or a stereoisomer or a pharmaceutically acceptable salt thereof: useful for the treatment of ocular condition associated with elevated intraocular pressure such as ocular hypertension, glaucoma or retinopathies.

Abstract: Pharmaceutical compositions comprising filgotinib maleate Form I characterized by an XRPD pattern substantially the same as shown in FIG. 1 and uses thereof are described herein.