Discovery of imidazo[1,2-b]pyridazines as IKKβ inhibitors. Part 3: Exploration of effective compounds in arthritis models
2011
Shimizu, Hiroki | Yamasaki, Tomonori | Yoneda, Yoshiyuki | Muro, Fumihito | Hamada, Tomoaki | Yasukochi, Takanori | Tanaka, Shinji | Toki, Tadashi | Yokoyama, Mika | Morishita, Kaoru | Iimura, Shin
We have discovered imidazo[1,2-b]pyridazine derivatives that show suppressive activity of inflammation in arthritis models. We optimized the substructures of imidazo[1,2-b]pyridazine derivatives to combine potent IKKβ inhibitory activity, TNFα inhibitory activity invivo and excellent pharmacokinetics. The compound we have acquired, which had both potent activities and good pharmacokinetic profiles based on improved physicochemical properties, demonstrated efficacy on collagen-induced arthritis models in mice and rats.
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