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Arylsulfonamide pyrimidines as VLA-4 antagonists |
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| Authors: | Ying-zi Xu Andrei W. Konradi Frederique Bard Michael Dappen Lilibeth Dofiles Mark Dreyer Ian Gallager Caroline Garrido Mike Krimm Zhenmei Liao Elizabeth Messersmith Linda Mutter Michael A. Pleiss Bhushan Samant Christopher M. Semko Jennifer Smith Frank Stappenbeck Brian Stupi Ted Yednock |
| Affiliation: | 1. Department of Chemical Sciences, Elan Pharmaceuticals, Inc., 180 Oyster Point Blvd., South San Francisco, CA 94080, USA;2. Department of Biology, Elan Pharmaceuticals, Inc., 180 Oyster Point Blvd., South San Francisco, CA 94080, USA;3. Department of Pharmacology, Elan Pharmaceuticals, Inc., 180 Oyster Point Blvd., South San Francisco, CA 94080, USA;4. Department of DMPK, Elan Pharmaceuticals, Inc., 180 Oyster Point Blvd., South San Francisco, CA 94080, USA |
| Abstract: | A series of (S)-2-(2-(diethylamino)-5-(N-alkyl-N-sulfonamido)pyrimidin-4-ylamino)-3-(4-(carbamoyloxy)phenyl)propanoic acid is discovered as orally available VLA-4 antagonists. Representative compounds 11b and 11p showed efficacy in multiple in vivo animal models. The in vitro selectivity of 11p is also described. |
| Keywords: | VLA-4 Antagonist Orally available CIA model EAE model |
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