25813-24-5Relevant academic research and scientific papers
PHARMACEUTICALS COMPRISING BIARYL DERIVATIVES OR SALTS THEREOF
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Paragraph 0633; 0634; 635, (2018/10/24)
PROBLEM TO BE SOLVED: To provide compounds with excellent antimycotic activity against Trichophyton. SOLUTION: The invention provides pharmaceuticals comprising biaryl derivatives represented by general formula (I) or salts thereof, where ring A is optionally substituted phenyl or the like; Q is CH2 or the like; X1, X2 and X3 are CR1 or the like; and Y is CH or N. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
BIARYL DERIVATIVE AND MEDICINE CONTAINING SAME
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Paragraph 0676; 0678, (2018/08/07)
Provided is a compound showing excellent antifungal activity against Trichophyton fungus, which is a major causative microorganism of superficial mycosis, and high effectiveness on diseases caused by Trichophyton fungi. A biaryl derivative represented by the formula (I) or a salt thereof: wherein ring A is an optionally substituted phenyl, or an optionally substituted 5- or 6-membered ring heteroaryl (ring A may be further condensed to form an optionally substituted fused ring); Q is CH2, C=O, NH, O, S or the like; X1, X2 and X3 are CR1 or N; Y is CH or N; Z is CR2b or N; R2a and R2b are each a hydrogen atom, a halogen atom, an optionally substituted C1-C6 alkyl group, a C1-C6 haloalkyl group or the like; R2a and R2b may form, together with carbon atoms bonded thereto, an optionally substituted carbocycle, or an optionally substituted heterocycle.
Discovery of 2,4-dimethoxypyridines as novel autophagy inhibitors
Robke, Lucas,Rodrigues, Tiago,Schr?der, Peter,Foley, Daniel J.,Bernardes, Gon?alo J.L.,Laraia, Luca,Waldmann, Herbert
supporting information, p. 4531 - 4537 (2018/07/30)
Autophagy is a catabolic process, which mediates degradation of cellular components and has important roles in health and disease. Therefore, small molecule modulators of autophagy are in great demand. Herein, we describe a phenotypic high-content screen for autophagy inhibitors, which led to the discovery of a dimethoxypyridine-based class of autophagy inhibitors, which derive from previously reported, natural product-inspired MAP4K4 inhibitors. Comprehensive structure-activity relationship studies led to a potent compound, and biological validation experiments indicated that the mode of action was upstream or independent of mTOR.
COUMARIN DERIVATIVES AND METHODS OF USE IN TREATING CYSTIC FIBROSIS, CHRONIC OBSTRUCTIVE PULMONARY DISEASE, AND MISFOLDED PROTEIN DISORDERS
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Page/Page column 57, (2014/10/04)
Novel CFTR corrector compounds that are effective in rescuing halide efflux, delF508-CFTR protein processing, and apical functional chloride ion transport in a cell are provided. Also provided are methods for treating protein folding disorders (e.g., cyst
COUMARIN DERIVATIVES AND METHODS OF USE IN TREATING HYPERPROLIFERATIVE DISEASES
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Page/Page column 56, (2014/10/04)
Coumarin derivative compounds and methods for the treatment of hyperproliferative diseases, such as cancer, polycystic kidney disease, and fibrosis of different tissues (e.g., idiopathic pulmonary fibrosis), are provided. The methods include administering
SULFONAMIDE COMPOUNDS USEFUL AS CYP17 INHIBITORS
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Page/Page column 93, (2012/02/13)
Disclosed are sulfonamide compounds of Formula (I): or stereoisomers, N-oxides, prodrugs, or pharmaceutically acceptable salts thereof, wherein ring A, R1, R2, R3, R4 and R5 are defined herein. Also disclosed are methods of using such compounds in the treatment of conditions related to CYP17 enzyme, such as cancer, and pharmaceutical compositions comprising such compounds.
