698394-73-9Relevant articles and documents
Evaluation of tert-butyl isosteres: Case studies of physicochemical and pharmacokinetic properties, efficacies, and activities
Westphal, Matthias V.,Wolfst?dter, Bernd T.,Plancher, Jean-Marc,Gatfield, John,Carreira, Erick M.
, p. 461 - 469 (2015/03/13)
The tert-butyl group is a common motif in medicinal chemistry. Its incorporation into bioactive compounds is often accompanied by unwanted property modulation, such as increased lipophilicity and decreased metabolic stability. Several alternative substituents are available for the drug discovery process. Herein, physicochemical data of two series of drug analogues of bosentan and vercirnon are documented as part of a comparative study of tert-butyl, pentafluorosulfanyl, trifluoromethyl, bicyclo[1.1.1]pentanyl, and cyclopropyl-trifluoromethyl substituents.
A CRYSTALLINE FORM OF THE SODIUM SALT OF 4-TERT-BUTYL-N-[4-CHLORO-2-(1-OXY-PYRIDINE-4-CARBONYL)-PHENYL]-BENZENE SULFONAMIDE
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Page/Page column 13; 14, (2013/03/26)
A novel crystalline form of the sodium salt of 4-tert-butyl-N-[4-chloro-2-(1- oxy-pyridine-4-carbonyl)-phenyl]-benzenesulfonamide and pharmaceutical compositions containing the same are disclosed. Processes for the preparation thereof and methods for use
ARYL SULFONAMIDES
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Page 63-64, (2008/06/13)
Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
