- Evaluation of tert-butyl isosteres: Case studies of physicochemical and pharmacokinetic properties, efficacies, and activities
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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.
- Westphal, Matthias V.,Wolfst?dter, Bernd T.,Plancher, Jean-Marc,Gatfield, John,Carreira, Erick M.
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p. 461 - 469
(2015/03/13)
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- PROPHYLACTIC OR THERAPEUTIC METHOD FOR SJOGREN'S SYNDROME
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The present invention provides a prophylactic or therapeutic agent and a prophylactic or therapeutic method superior in the prophylaxis or treatment of Sjogren's syndrome. Provided are a prophylactic or therapeutic agent for Sjogren's syndrome, containing
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- 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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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
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Page/Page column 13; 14
(2013/03/26)
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- ARYL SULFONAMIDES
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The present invention relates to compounds that modulate various chemokine receptors. These compounds are useful for treating inflammatory and immune diseases.
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Page/Page column 158-159; 180-181
(2010/02/14)
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- ARYL SULFONAMIDES
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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.
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