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: 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 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: 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.

Abstract: Compounds for treating cancer and, particularly, to compounds that are 5-(3-substituted phenyl)-pyrimido[4,5-d]pyrimidine-2,4,7(1H,3H,8H)-trione analogues and their use as anticancer agents.

Abstract: Compounds, such as compounds having Formula (I): wherein each variable is as described herein, that modulate the conversion of AMP to adenosine by 5?-nucleotidase, ecto, and compositions containing the compounds and methods for synthesizing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by 5?-nucleotidase, ecto is also provided.

Abstract: The present invention provides pyrazole pyrimidine derivatives which inhibit Casein kinase I (CKI) and/or Interleukin-1 receptor-associated kinase 1 (IRAKI) and methods of their manufacture, compositions comprising them and uses thereof in methods of treating malignant disease and disorders and methods for treating inflammatory diseases and disorders.

Abstract: Provided herein are 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 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: Formula (I) wherein A, B, R, R2 and R3 represent the same meanings as in the claims.

Abstract: Provided are a compound of the formula: (5-(2-(4-((3,5-difluoro-4-(trifluoromethoxy)benzyl)amino)butoxy)ethoxy)benzo[c][2,6]naphthyridine-8-carboxylic acid) or a pharmaceutically acceptable salt thereof and a pharmaceutical composition comprising the above compound, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.

Abstract: The present disclosure relates to a compound of Formula (0): a stereoisomer thereof, a prodrug thereof, or a pharmaceutically acceptable salt thereof. The present disclosure also relates to uses of the compound.

Abstract: The embodiments of present invention provide processes and an intermediate 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: Provided are crystal forms A, B, C and D of a compound of formula (I), and application of the crystal forms in the preparation of drugs for treating ASK1-related diseases.

Abstract: This invention provides stable, highly crystalline forms of Complement factor D inhibitors Compound 1 for advantageous therapeutic pharmaceutical efficacy and dosage form stability.