- Quinolone-based oxazolidinone compound as well as preparation method and application thereof
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The invention discloses a quinolone-based oxazolidinone compound with a formula (HB), a solvate thereof, a stereoisomer of the compound, or a pharmaceutically acceptable salt of the compound, a preparation method of the compound and application of the com
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Paragraph 0099-0101
(2021/07/31)
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- SILICONE ATOMS CONTAINING IVACAFTOR ANALOGUES
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The present disclosure is directed to disclosed compounds that modulate e.g., address underlying defects in cellular processing of CFTR activity.
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Paragraph 0109
(2017/11/06)
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- Discovery of N -(2,4-Di- tert -butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide (VX-770, Ivacaftor), a potent and orally bioavailable CFTR potentiator
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Quinolinone-3-carboxamide 1, a novel CFTR potentiator, was discovered using high-throughput screening in NIH-3T3 cells expressing the F508del-CFTR mutation. Extensive medicinal chemistry and iterative structure-activity relationship (SAR) studies to evaluate potency, selectivity, and pharmacokinetic properties resulted in the identification of N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide (VX-770, 48, ivacaftor), an investigational drug candidate approved by the FDA for the treatment of CF patients 6 years of age and older carrying the G551D mutation.
- Hadida, Sabine,Van Goor, Fredrick,Zhou, Jinglan,Arumugam, Vijayalaksmi,McCartney, Jason,Hazlewood, Anna,Decker, Caroline,Negulescu, Paul,Grootenhuis, Peter D. J.
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p. 9776 - 9795
(2015/01/16)
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- Syntheses and Reactions of Diazepinoquinolines
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Three routes for the preparation of diazepinoquinolines (1) have been studied.The best yields resulted by starting from the amides of N-(3-quinolylcarbonyl)-N-alkyl-amino acids (5).Quaternization to 9, intramolecular cyclization under the influence of base to 10, oxidation to 11 and debenzylation by catalytic hydrogenation gave 1. - Keywords: Quinolinium Salts, Cyclization Reaction
- Guendel, Wolf-H.,Bohnert, Sabine
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p. 769 - 777
(2007/10/02)
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