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Synthesis and SAR of diazepine and thiazepine TACE and MMP inhibitors |
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| Authors: | Zask Arie Kaplan Joshua Du XueMei MacEwan Gloria Sandanayaka Vincent Eudy Nancy Levin Jeremy Jin Guixian Xu Jun Cummons Terri Barone Dauphine Ayral-Kaloustian Semiramis Skotnicki Jerauld |
| Affiliation: | Wyeth Research, 401 N. Middletown Road, Pearl River, NY 10965, USA. zaska@wyeth.com |
| Abstract: | Potent and selective TACE and MMP inhibitors utilizing the diazepine and thiazepine ring systems were synthesized and evaluated for biological activity in in vitro and in vivo models of TNF-alpha release. Oral activity in the mouse LPS model of TNF-alpha release was seen. Efficacy in the mouse collagen induced arthritis model was achieved with diazepine 20. |
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