Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 5, Issue 8, Pages 857-862Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml500117c
Keywords
NOP receptor agonists; MOP receptor agonists; cebranopadol; analgesics
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In a previous communication, our efforts leading from 1 to the identification of spiro[cyclohexane-dihydropyrano[3,4-b]indole]-amine 2a as analgesic NOP and opioid receptor agonist were disclosed and their favorable in vitro and in vivo pharmacological properties revealed. We herein report our efforts to further optimize lead 2a, toward trans-6'-fluoro-4',9'-dihydro-N,N-dimethyl-4-phenyl-spiro[cyclohexane-1,1'(3'H)-pyrano[3,4-indol]-4-amine (cebranopadol, 3a), which is currently in clinical development for the treatment of severe chronic nociceptive and neuropathic pain.
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