期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 52, 期 14, 页码 4091-4094出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm900581g
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Our efforts to optimize prototype opioid receptor-like I (ORL1) antagonist 1 led to the discovery of 4-{3-[(2R)-2, 3-dihydroxypropyl]-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl}-1-[(1S,3S,4R)-spiro[bicyclo[2.2.1]heptane-2,1'-cyclopropan]-3-ylmethyl]piperidine 10. 10 showed potent ORL1 antagonistic activity, excellent selectivity over other opioid receptors, and in vivo efficacy after oral dosing. Currently clinical trials of 10 are underway.
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