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New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site |
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| Authors: | Moss Neil Breitfelder Steffen Betageri Raj Cirillo Pier F Fadra Tazmeen Hickey Eugene R Kirrane Thomas Kroe Rachel R Madwed Jeffrey Nelson Richard M Pargellis Christopher A Qian Kevin C Regan John Swinamer Alan Torcellini Carol |
| Institution: | Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceutical, Inc., 900 Ridgebury Road, Ridgefield, CT 0687, USA. nmoss@rdg.boehringeringleheim.com |
| Abstract: | Discovery of the pyrazole-naphthyl urea class of p38 MAP kinase inhibitors typified by the clinical candidate BIRB 796 has encouraged further exploration of this particular scaffold. Modification to the part of the inhibitor that occupies the adenine/ATP binding site has resulted in a new way to obtain potent inhibitors that possess favorable in vitro and in vivo properties. |
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