Biphenyl derivatives as novel dual NK(1)/NK(2)-receptor antagonists |
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Authors: | Mah Robert Gerspacher Marc von Sprecher Andreas Stutz Stefan Tschinke Vincenzo Anderson Gary P Bertrand Claude Subramanian Natarajan Ball Howard A |
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Institution: | Pharma Research, Novartis Pharma AG, CH-4002, Basel, Switzerland. robert.mah@speedelgroup.com |
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Abstract: | In a continuation of our efforts to simplify the structure of our neurokinin antagonists, a series of substituted biphenyl derivatives has been prepared. Several compounds exhibit potent affinities for both the NK(1) receptor (<10nM) and for the NK(2) receptor (<50 nM). Details on the design, synthesis, biological activities, SAR and conformational analysis of this new class of dual NK(1)/NK(2) receptor antagonists are presented. |
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