discovery of n-substituted-endo-3-(8-aza-bicyclo[3.2.1]oct-3-yl)-phenol and -phenyl carboxamide series of μ-opioid receptor antagonists：（发现n-substituted-endo-3(8-aza-bicyclo[3.2.1]oct-3-yl)苯酚和苯甲酰胺系列的）.pdfVIP

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discovery of n-substituted-endo-3-(8-aza-bicyclo[3.2.1]oct-3-yl)-phenol and -phenyl carboxamide series of μ-opioid receptor antagonists：（发现n-substituted-endo-3(8-aza-bicyclo[3.2.1]oct-3-yl)苯酚和苯甲酰胺系列的）.pdf

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discovery of n-substituted-endo-3-(8-aza-bicyclo[3.2.1]oct-3-yl)-phenol and -phenyl carboxamide series of μ-opioid receptor antagonists：（发现n-substituted-endo-3(8-aza-bicyclo[3.2.1]oct-3-yl)苯酚和苯甲酰胺系列的）

Bioorganic Medicinal Chemistry Letters 27 (2017) 2926–2930 Contents lists available at ScienceDirect Bioorganic Medicinal Chemistry Letters journal homepage: www.else /locate/bmcl Discovery of N-substituted-endo-3-(8-aza-bicyclo[3.2.1]oct-3-yl)-phenol and -phenyl carboxamide series of l-opioid receptor antagonists Lan Jiang, David T. Beattie, John R. Jacobsen, Samuel Kintz, Glenmar P. Obedencio, Daisuke Saito, Ioanna Stergiades, Ross G. Vickery, Daniel D. Long ⇑ Theravance Biopharma US, Inc, 901 Gateway Blvd, South San Francisco, CA 94080, United States a r t i c l e i n f o a b s t r a c t Article history: Gastrointestinal dysfunction as a consequence of the use of opioid analgesics is of signiﬁcant clinical con- Received 23 March 2017 cern. First generation drugs to treat these opioid-induced side-effects were limited by their negative Revised 29 April 2017 impact on opioid receptor agonist-induced analgesia. Second generation therapies target a localized, Accepted 30 April 2017 peripherally-restricted, non-CNS penetrant drug distribution of opioid receptor antagonists. Herein we Available online 3 May 2017 describe the discovery of the N-substituted-endo-3-(8-aza-bicyclo[3.2.1]oct-3-yl)-phenol and -phenyl carboxamide series of l-opioid receptor antagonists. This report highlights the discovery of the key l- Keywords: opioid receptor antagonist pharmacophore a