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Synthesis and structure-activity relationship of 7-azaindole piperidine derivatives as CCR2 antagonists |
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| Authors: | Xia Mingde Hou Cuifen DeMong Duane Pollack Scott Pan Meng Singer Monica Matheis Michele Murray William Cavender Druie Wachter Michael |
| Institution: | Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 8 Clarke Drive, Cranbury, NJ 08512, USA. mxia@prdus.jnj.com |
| Abstract: | 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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