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Tricyclic aminopyrimidine histamine H4 receptor antagonists |
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| Authors: | Savall Brad M Gomez Laurent Chavez Frank Curtis Michael Meduna Steven P Kearney Aaron Dunford Paul Cowden Jeffery Thurmond Robin L Grice Cheryl Edwards James P |
| Institution: | Johnson & Johnson Pharmaceutical Research & Development, LLC 3210 Merryfield Row, San Diego, CA 92121, USA. bsavall@its.jnj.com |
| Abstract: | This report discloses the development of a series of tricyclic histamine H(4) receptor antagonists. Starting with a low nanomolar benzofuranopyrimidine HTS hit devoid of pharmaceutically acceptable properties, we navigated issues with metabolism and solubility to furnish a potent, stable and water soluble tricyclic histamine H(4) receptor antagonist with desirable physiochemical parameters which demonstrated efficacy a mouse ova model. |
| Keywords: | Histamine Histamine H4 Antagonists Benzofuran Amino pyrimidine Tricyclic |
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