Biphenyl derivatives as novel dual NK1/NK2-receptor antagonists

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Abstract

In a continuation of our efforts to simplifly the structure of our neurokinin antagonists, a series of substituted biphenyl derivatives has been prepared. Several compounds exhibit potent affinities for both the NK1 receptor (<10 nM) and for the NK2 receptor (<50 nM). Details on the design, synthesis, biological activities, SAR and conformational analysis of this new class of dual NK1/NK2 receptor antagonists are presented.

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Acknowledgments

The authors wish to thank H. Bammerlin, E. Braun, A. Cosenti, M. Erard, C. Ferraretto, S. Fuhrer, H. Hettrich, S. Kimmel, M. Kuhn, Th. Kull, M. Modena, C. Mouzo, T. Osman, V. Pawelzik, C. Ruesch, K. Ryffel, N. Stuber, A. Widmer and D. Wyss for their excellent technical assistance.

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