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Synthesis and structure-activity relationship of 7-azaindole piperidine derivatives as CCR2 antagonists. 2008
Mingde Xia, and
Cuifen Hou, and
Duane DeMong, and
Scott Pollack, and
Meng Pan, and
Monica Singer, and
Michele Matheis, and
William Murray, and
Druie Cavender, and
Michael Wachter
Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 8 Clarke Drive, Cranbury, NJ 08512, USA. mxia@prdus.jnj.com
The synthesis and structure-activity relationship of a series of 7-azaindole piperidine derivatives are described. SAR studies led to the discovery of the potent CCR2 antagonists displaying IC(50) values in the nanomolar range. The representative compound 15 showed reasonable P450 and pharmacokinetics profile.
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