1000771-65-2Relevant academic research and scientific papers
UROTENSIN II RECEPTOR ANTAGONISTS
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Page/Page column 57-58, (2008/06/13)
The invention is directed to Urotensin II receptor antagonists. More specifically, the present invention relates to certain novel compounds and methods for preparing compounds, compositions, intermediates and derivatives thereof. Pharmaceutical compositio
Phenylpiperidine-benzoxazinones as urotensin-II receptor antagonists: Synthesis, SAR, and in vivo assessment
Luci, Diane K.,Ghosh, Shyamali,Smith, Charles E.,Qi, Jenson,Wang, Yuanping,Haertlein, Barbara,Parry, Tom J.,Li, Jian,Almond Jr., Harold R.,Minor, Lisa K.,Damiano, Bruce P.,Kinney, William A.,Maryanoff, Bruce E.,Lawson, Edward C.
, p. 6489 - 6492 (2008/03/13)
Various 4-phenylpiperidine-benzoxazin-3-ones were synthesized and biologically evaluated as urotensin-II (U-II) receptor antagonists. Compound 12i was identified from in vitro evaluation as a low nanomolar antagonist against both rat and human U-II receptors. This compound showed in vivo efficacy in reversing the ear-flush response induced by U-II in rats.
