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The search for novel TRPV1-antagonists: from carboxamides to benzimidazoles and indazolones |
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| Authors: | Fletcher Stephen Robert McIver Edward Lewis Stephen Burkamp Frank Leech Clare Mason Glenn Boyce Susan Morrison Denise Richards Gillian Sutton Kathy Jones Anthony Brian |
| Institution: | Merck Sharp & Dohme, The Neuroscience Research Centre, Terlings Park, Harlow, Essex CM20 2QR, UK. stephen_fletcher@merck.com |
| Abstract: | Based on a series of diaryl amides the corresponding inverse amides have been found to be potent TRPV1 receptor antagonists. Benzimidazole and indazolone derivatives prepared retained good potency in vitro and indazolone 4a was identified as a novel TRPV1 receptor antagonist suitable for evaluating orally in animal models of analgesia. |
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