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New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck |
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| Authors: | Nina Gommermann Peter Buehlmayer Anette von Matt Werner Breitenstein Keiichi Masuya Bernard Pirard Pascal Furet Sandra W Cowan-Jacob Gisbert Weckbecker |
| Institution: | Novartis Institute of Biomedical Research, Forum 1, Novartis Campus, 4056 Basel, Switzerland |
| Abstract: | A novel series of pyrazolo1,5a]pyrimidines was optimized to target lymphocyte-specific kinase (Lck). An efficient synthetic route was developed and SAR studies toward activity and selectivity are described, leading to Lck inhibitors with enzymatic, cellular and in vivo potency. |
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