原创力文档discovery of phenyl acetamides as potent and selective gpr119 agonists：（发现苯乙酰胺有效和选择性gpr119受体激动剂）.pdfVIP
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discovery of phenyl acetamides as potent and selective gpr119 agonists：（发现苯乙酰胺有效和选择性gpr119受体激动剂）
Bioorganic Medicinal Chemistry Letters 27 (2017) 1124–1128
Contents lists available at ScienceDirect
Bioorganic Medicinal Chemistry Letters
journal homepage: www.else /locate/bmcl
Discovery of phenyl acetamides as potent and selective GPR119 agonists
Cheng Zhu a,⇑, Liping Wang b, Yuping Zhu a, Zack Zhiqiang Guo b, Ping Liu a, Zhiyong Hu a,
Jason W. Szewczyk b, Ling Kang b, Gary Chicchi b, Anka Ehrhardt b, Andrea Woods b, Toru Seo b,
Morgan Woods a, Margaret van Heek a, Karen H. Dingley a, Jianmei Pang a, Gino M. Salituro b, Joyce Powell b,
Jenna L. Terebetski a, Viktor Hornak b, Louis-Charles Campeau b, Robert K. Orr b, Feroze Ujjainwalla a,
Michael Miller a, Andrew Stamford b, Harold B. Wood a, Timothy Kowalski a, Ravi P. Nargund a,
Scott D. Edmondson a
a Early Development and Discovery Sciences, Merck Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA
b Early Development and Discovery Sciences, Merck Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA
a r t i c l e i n f o a b s t r a c t
Article history: The paper describes the SAR/SPR studies that led to the discovery of phenoxy cyclopropyl phenyl aceta-
Received 9 January 2017 mide derivatives as potent and selective GPR119 agonists. Based on a cis cyclopropane scaffold discovered
Accepted 27 January 2017 previously, phenyl acetamides such as compound 17 were found to have excellent GPR119 potency and
Available online 1 February 2017
improved physicochemical properties. Pharmacokinetic data of compound 17 in rat, dog and rhesus will
be descri
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