2-Amino-5-aryl-pyridines, exemplified by compound 1, had been identified as a synthetically tractable series of CB2 agonists from a high-throughput screen of the GlaxoSmithKline compound collection. Described herein are the results of an investigation of the structure-activity relationships (SAR) which led to the identification a number of potent and selective agonists. (C) 2009 Elsevier Ltd. All rights reserved.
机构:
Univ Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, DK-2100 Copenhagen O, DenmarkUniv Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, DK-2100 Copenhagen O, Denmark
Hansen, Martin
Phonekeo, Karina
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Univ Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, DK-2100 Copenhagen O, DenmarkUniv Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, DK-2100 Copenhagen O, Denmark
Phonekeo, Karina
Paine, James S.
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Univ Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, DK-2100 Copenhagen O, DenmarkUniv Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, DK-2100 Copenhagen O, Denmark
Paine, James S.
Leth-Petersen, Sebastian
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Univ Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, DK-2100 Copenhagen O, DenmarkUniv Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, DK-2100 Copenhagen O, Denmark
Leth-Petersen, Sebastian
Begtrup, Mikael
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Univ Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, DK-2100 Copenhagen O, DenmarkUniv Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, DK-2100 Copenhagen O, Denmark
Begtrup, Mikael
Braeuner-Osborne, Hans
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Univ Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, DK-2100 Copenhagen O, DenmarkUniv Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, DK-2100 Copenhagen O, Denmark
Braeuner-Osborne, Hans
Kristensen, Jesper L.
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Univ Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, DK-2100 Copenhagen O, DenmarkUniv Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, DK-2100 Copenhagen O, Denmark
Kristensen, Jesper L.
ACS CHEMICAL NEUROSCIENCE,
2014,
5
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249
机构:
Pfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, JapanPfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, Japan
Omura, Hirofumi
Kawai, Makoto
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Pfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, JapanPfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, Japan
Kawai, Makoto
Shima, Akiko
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Pfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, JapanPfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, Japan
Shima, Akiko
Iwata, Yasuhiro
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Pfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, JapanPfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, Japan
Iwata, Yasuhiro
Ito, Fumitaka
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Pfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, JapanPfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, Japan
Ito, Fumitaka
Masuda, Tsutomu
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Pfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, JapanPfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, Japan
Masuda, Tsutomu
Ohta, Atsuko
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Pfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, JapanPfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, Japan
Ohta, Atsuko
Makita, Naoya
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Pfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, JapanPfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, Japan
Makita, Naoya
Omoto, Kiyoyuki
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Pfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, JapanPfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, Japan
Omoto, Kiyoyuki
Sugimoto, Hiromi
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Pfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Biol Res, Aichi 4702393, JapanPfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, Japan
Sugimoto, Hiromi
Kikuchi, Akira
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Pfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Biol Res, Aichi 4702393, JapanPfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, Japan
Kikuchi, Akira
Iwata, Hiroshi
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Pfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Biol Res, Aichi 4702393, JapanPfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, Japan
Iwata, Hiroshi
Ando, Kazuo
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Pfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, JapanPfizer Japan Inc, Nagoya Labs, Pfizer Global Res & Dev, Discovery Chem Res, Aichi 4702393, Japan
机构:
Lilly Corp Ctr, Lilly Res Labs, Discovery Chem, Indianapolis, IN 46285 USALilly Corp Ctr, Lilly Res Labs, Discovery Chem, Indianapolis, IN 46285 USA
Hollinshead, Sean P.
Astles, Peter C.
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Lilly Res Labs, Erl Wood Manor, Discovery Chem, Windlesham GU20 6PH, Surrey, EnglandLilly Corp Ctr, Lilly Res Labs, Discovery Chem, Indianapolis, IN 46285 USA
Astles, Peter C.
Chambers, Mark G.
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Lilly Corp Ctr, Lilly Res Labs, Musculoskeletal Res, Indianapolis, IN 46285 USALilly Corp Ctr, Lilly Res Labs, Discovery Chem, Indianapolis, IN 46285 USA
Chambers, Mark G.
Johnson, Michael P.
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Lilly Corp Ctr, Lilly Res Labs, Discovery Biol, Indianapolis, IN 46285 USALilly Corp Ctr, Lilly Res Labs, Discovery Chem, Indianapolis, IN 46285 USA
Johnson, Michael P.
Palmer, John
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Lilly Corp Ctr, Lilly Res Labs, Discovery Chem, Indianapolis, IN 46285 USALilly Corp Ctr, Lilly Res Labs, Discovery Chem, Indianapolis, IN 46285 USA
Palmer, John
Tidwell, Michael W.
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Lilly Corp Ctr, Lilly Res Labs, Discovery Chem, Indianapolis, IN 46285 USALilly Corp Ctr, Lilly Res Labs, Discovery Chem, Indianapolis, IN 46285 USA
机构:
Univ Calif San Diego, Skaggs Sch Pharm & Pharmaceut Sci, Dept Pharmacol, La Jolla, CA 92093 USAUniv Calif San Diego, Skaggs Sch Pharm & Pharmaceut Sci, Dept Pharmacol, La Jolla, CA 92093 USA
Camacho-Hernandez, Gisela Andrea
Stokes, Clare
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Univ Florida, Dept Pharmacol & Therapeut, POB 100267, Gainesville, FL 32610 USAUniv Calif San Diego, Skaggs Sch Pharm & Pharmaceut Sci, Dept Pharmacol, La Jolla, CA 92093 USA
Stokes, Clare
Duggan, Brendan M.
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Univ Calif San Diego, Skaggs Sch Pharm & Pharmaceut Sci, Dept Pharmacol, La Jolla, CA 92093 USAUniv Calif San Diego, Skaggs Sch Pharm & Pharmaceut Sci, Dept Pharmacol, La Jolla, CA 92093 USA
Duggan, Brendan M.
Kaczanowska, Katarzyna
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Univ Calif San Diego, Skaggs Sch Pharm & Pharmaceut Sci, Dept Pharmacol, La Jolla, CA 92093 USAUniv Calif San Diego, Skaggs Sch Pharm & Pharmaceut Sci, Dept Pharmacol, La Jolla, CA 92093 USA
Kaczanowska, Katarzyna
Brandao-Araiza, Stefania
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Univ Calif San Diego, Skaggs Sch Pharm & Pharmaceut Sci, Dept Pharmacol, La Jolla, CA 92093 USAUniv Calif San Diego, Skaggs Sch Pharm & Pharmaceut Sci, Dept Pharmacol, La Jolla, CA 92093 USA
Brandao-Araiza, Stefania
Doan, Lisa
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Univ Calif San Diego, Skaggs Sch Pharm & Pharmaceut Sci, Dept Pharmacol, La Jolla, CA 92093 USAUniv Calif San Diego, Skaggs Sch Pharm & Pharmaceut Sci, Dept Pharmacol, La Jolla, CA 92093 USA
Doan, Lisa
Papke, Roger L.
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Univ Florida, Dept Pharmacol & Therapeut, POB 100267, Gainesville, FL 32610 USAUniv Calif San Diego, Skaggs Sch Pharm & Pharmaceut Sci, Dept Pharmacol, La Jolla, CA 92093 USA
Papke, Roger L.
Taylor, Palmer
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Univ Florida, Dept Pharmacol & Therapeut, POB 100267, Gainesville, FL 32610 USAUniv Calif San Diego, Skaggs Sch Pharm & Pharmaceut Sci, Dept Pharmacol, La Jolla, CA 92093 USA