909186-04-5Relevant articles and documents
Practical synthesis of a p38 MAP kinase inhibitor
Achmatowicz, Michal,Thiel, Oliver R.,Wheeler, Philip,Bernard, Charles,Huang, Jinkun,Larsen, Robert D.,Faul, Margaret M.
scheme or table, p. 795 - 809 (2009/06/20)
p38 MAP kinase inhibitors have attracted considerable interest as potential agents for the treatment of inflammatory diseases. Herein, we describe a concise and efficient synthesis of inhibitor 1 that is based on a phthalazine scaffold. Highlights of our approach include a practical synthesis of a 1,6-disubstituted phthalazine building block 24 as well as the one-pot formation of boronic acid 27. Significant synthetic work to understand the reactivity principles of the intermediates helped in selection of the final synthetic route. Subsequent optimization of the individual steps of the final sequence led to a practical synthesisof 1.
Phthalazine, aza- and diaza-phthalazine compounds and methods of use
-
Page/Page column 28; 33; 56, (2008/06/13)
The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.