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Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors
Authors:Shi Yan  Zhang Jing  Stein Philip D  Shi Mengxiao  O'Connor Stephen P  Bisaha Sharon N  Li Chi  Atwal Karnail S  Bisacchi Gregory S  Sitkoff Doree  Pudzianowski Andrew T  Liu Eddie C  Hartl Karen S  Seiler Steven M  Youssef Sonia  Steinbacher Thomas E  Schumacher William A  Rendina Alan R  Bozarth Jeffrey M  Peterson Tara L  Zhang Ge  Zahler Robert
Affiliation:

Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA

Abstract:N,N′-Disubstituted ketene aminals are good bioisosteres of thiourea functional groups. We report the design and synthesis of a novel class of ketene aminal-based lactam derivatives as potent and orally active FXa inhibitors.
Keywords:Serine protease   Factor Xa inhibitors   Antithrombotic agents   2-Methylbenzofuran   Thiourea   Bioisosteres   N,N′-Disubstituted ketene aminal   2,2-Dicyanoketene aminal   2-Nitroketene aminal   Orally active
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