1197-66-6Relevant articles and documents
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Cabani,Ceccanti
, p. 77,85 (1966)
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Discovery of N-(3-Carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-lH-pyrazole-5-carboxamide (GLPG1837), a Novel Potentiator Which Can Open Class III Mutant Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Channels to a High Extent
Van Der Plas, Steven E.,Kelgtermans, Hans,De Munck, Tom,Martina, Sébastien L. X.,Dropsit, Sébastien,Quinton, Evelyne,De Blieck, Ann,Joannesse, Caroline,Tomaskovic, Linda,Jans, Mia,Christophe, Thierry,Van Der Aar, Ellen,Borgonovi, Monica,Nelles, Luc,Gees, Maarten,Stouten, Pieter,Van Der Schueren, Jan,Mammoliti, Oscar,Conrath, Katja,Andrews, Martin
, p. 1425 - 1435 (2018)
Cystic fibrosis (CF) is caused by mutations in the gene for the cystic fibrosis transmembrane conductance regulator (CFTR). With the discovery of Ivacaftor and Orkambi, it has been shown that CFTR function can be partially restored by administering one or more small molecules. These molecules aim at either enhancing the amount of CFTR on the cell surface (correctors) or at improving the gating function of the CFTR channel (potentiators). Here we describe the discovery of a novel potentiator GLPG1837, which shows enhanced efficacy on CFTR mutants harboring class III mutations compared to Ivacaftor, the first marketed potentiator. The optimization of potency, efficacy, and pharmacokinetic profile will be described.
SUBSTITUTED IMIDAZOLES AS N-TYPE CALCIUM CHANNEL BLOCKERS
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Paragraph 0320; 0321, (2015/02/25)
Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, and G are defined herein.
THIENO[2,3-C]PYRANS AS CFTR MODULATORS
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Paragraph 00207, (2015/02/25)
The present invention discloses compounds according to Formula I: Wherein R is as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment cystic fibrosis by administering a compound of the invention.