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Imidazo-pyrazine derivatives as potent CXCR3 antagonists. 2009
Xiaohui Du, and
Darin J Gustin, and
Xiaoqi Chen, and
Jason Duquette, and
Lawrence R McGee, and
Zhulun Wang, and
Karen Ebsworth, and
Kirk Henne, and
Bryan Lemon, and
Ji Ma, and
Shichang Miao, and
Emmanuel Sabalan, and
Timothy J Sullivan, and
George Tonn, and
Tassie L Collins, and
Julio C Medina
Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. xdu@amgen.com
A general way of improving the potency of CXCR3 antagonists with fused hetero-bicyclic cores was identified. Optimization efforts led to the discovery of a series of imidazo-pyrazine derivatives with improved pharmacokinetic properties in addition to increased potency. The efficacy of the lead compound 21 is evaluated in a mouse lung inflammation model.
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Darin J Gustin, and
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Kirk Henne, and
Bryan Lemon, and
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