872624-52-7Relevant academic research and scientific papers
Discovery of Icenticaftor (QBW251), a Cystic Fibrosis Transmembrane Conductance Regulator Potentiator with Clinical Efficacy in Cystic Fibrosis and Chronic Obstructive Pulmonary Disease
Grand, Darren Le,Gosling, Martin,Baettig, Urs,Bahra, Parmjit,Bala, Kamlesh,Brocklehurst, Cara,Budd, Emma,Butler, Rebecca,Cheung, Atwood K.,Choudhury, Hedaythul,Collingwood, Stephen P.,Cox, Brian,Danahay, Henry,Edwards, Lee,Everatt, Brian,Glaenzel, Ulrike,Glotin, Anne-Lise,Groot-Kormelink, Paul,Hall, Edward,Hatto, Julia,Howsham, Catherine,Hughes, Glyn,King, Anna,Koehler, Julia,Kulkarni, Swarupa,Lightfoot, Megan,Nicholls, Ian,Page, Christopher,Pergl-Wilson, Giles,Popa, Mariana Oana,Robinson, Richard,Rowlands, David,Sharp, Tom,Spendiff, Matthew,Stanley, Emily,Steward, Oliver,Taylor, Roger J.,Tranter, Pamela,Wagner, Trixie,Watson, Hazel,Williams, Gareth,Wright, Penny,Young, Alice,Sandham, David A.
, p. 7241 - 7260 (2021/06/28)
Mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel are established as the primary causative factor in the devastating lung disease cystic fibrosis (CF). More recently, cigarette smoke exposure has been shown to be asso
Design, synthesis and insecticidal activities of novel anthranilic diamides containing fluorinated groups as potential ryanodine receptors activitors
Wu, Chang-Chun,Wang, Bao-Lei,Liu, Jing-Bo,Wei, Wei,Li, Yu-Xin,Liu, Yang,Chen, Ming-Gui,Xiong, Li-Xia,Yang, Na,Li, Zheng-Ming
, p. 1248 - 1251 (2017/06/19)
In order to search for novel potent and environmentally benign insecticides, a series of anthranilic diamides containing various fluorinated groups were designed and synthesized. Their structures were confirmed by 1H NMR, 13C NMR, s
Design and Synthesis of Selurampanel, a Novel Orally Active and Competitive AMPA Receptor Antagonist
Orain, David,Tasdelen, Engin,Haessig, Samuel,Koller, Manuel,Picard, Anne,Dubois, Celine,Lingenhoehl, Kurt,Desrayaud, Sandrine,Floersheim, Phillip,Carcache, David,Urwyler, Stephan,Kallen, Joerg,Mattes, Henri
, p. 197 - 201 (2017/02/15)
A series of potent quinazolinedione sulfonamide antagonists of the α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptor were designed and synthesized. The structure–activity relationships (SAR) and in vivo activity of the series were investigated. In particular, compound 1 S (selurampanel; N-[7-isopropyl-6-(2-methylpyrazol-3-yl)-2,4-dioxo-1H-quinazolin-3-yl]methanesulfonamide) has shown excellent oral potency against maximal electroshock seizure (MES)-induced generalized tonic–clonic seizures in rodents as well as significant activity in patients suffering from various forms of epilepsy. The X-ray crystal structure of selurampanel bound to the AMPA receptor hGluA was also obtained.
N-SUBSTITUTED HETEROCYCLYL CARBOXAMIDES
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Page/Page column 64; 65, (2013/03/28)
A compound of Formula I and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, Ra, A, B, D and E are all as defined herein. The compounds modulate the activity of CFTR and are useful in
1H-QUINAZ0LINE-2,4-DIONES AND THEIR USE AS AMPA-RECEPTOR LIGANDS
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, (2010/11/24)
The present invention relates to l H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as AMPA-receptor ligands, in particular for the treatment of epilepsy or schizophrenia, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) and combinations comprising compounds of formula (I) are disclosed.
COMPOUNDS AND METHODS FOR TREATING DYSLIPIDEMIA
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Page/Page column 56, (2010/02/15)
Compounds of Formula (I): wherein n, m, p, q, Y, R1 R2, R3a, R3b, R4, R5, and R6 are as defined herein and their pharmaceutical compositions and methods of use are disclosed.
