Altering metabolic profiles of drugs by precision deuteration 2: Discovery of a deuterated analog of ivacaftor with differentiated pharmacokinetics for clinical development
Ivacaftor is currently used for the treatment of cystic fibrosis as both monotherapy (Kalydeco; Vertex Pharmaceuticals, Boston, MA) and combination therapy with lumacaftor (Orkambi; Vertex Pharmaceuticals). Each therapy targets specific patient population
Harbeson, Scott L.,Morgan, Adam J.,Liu, Julie F.,Aslanian, Ara M.,Nguyen, Sophia,Bridson, Gary W.,Brummel, Christopher L.,Wu, Lijun,Tung, Roger D.,Pilja, Lana,Braman, Virginia,Uttamsingh, Vinita
p. 359 - 367
(2018/11/23)
MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
This invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R is COOH or CH2OH.
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Page/Page column 14; 35; 40
(2010/10/03)
PROCESS FOR MAKING MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
The invention provides a process for the preparation of a compound of Formula 1; comprising coupling a carboxylic acid of Formula 2; with an aniline of Formula 3; in the presence of a coupling agent.
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Page/Page column 65; 70
(2010/10/03)
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