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5-Aminomethyl-1H-benzimidazoles as orally active inhibitors of inducible T-cell kinase (Itk) |
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| Authors: | Winters Michael P Robinson Darius J Khine Hnin Hnin Pullen Steven S Woska Joseph R Raymond Ernest L Sellati Rosemarie Cywin Charles L Snow Roger J Kashem Mohammed A Wolak John P King Josephine Kaplita Paul V Liu Lisa H Farrell Thomas M DesJarlais Renee Roth Gregory P Takahashi Hidenori Moriarty Kevin J |
| Affiliation: | Johnson & Johnson Pharmaceutical Research and Development, 665 Stockton Drive, Exton, PA 19341, USA. |
| Abstract: | A series of novel 5-aminomethyl-1H-benzimidazole based inhibitors of Itk were prepared. Structure-activity relationships, selectivity and cell activity are reported for this series. Compound 2, a potent and selective antagonist of Itk, inhibited anti-CD3 antibody induced IL-2 production in vivo in mice. |
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