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Discovery of hydroxy pyrimidine Factor IXa inhibitors
Institution:1. Department of Discovery Chemistry, Merck & Co., Inc., Kenilworth, NJ 07033, USA;2. Department of Biology, Merck & Co., Inc., Kenilworth, NJ 07033, USA;1. Department of Pharmacognosy, Faculty of Pharmacy, Ain-Shams University, Cairo 11566, Egypt;2. Graduate Institute of Natural Products, Center for Natural Product Research and Development, College of Pharmacy, Drug Development and Value Creation Research Center, Kaohsiung Medical University, Kaohsiung 80708, Taiwan;3. Graduate Institute of Natural Products, College of Medicine, Chang Gung University, Taoyuan 33302, Taiwan;4. Research Center for Chinese Herbal Medicine, Research Center for Food and Cosmetic Safety, and Graduate Institute of Health Industry Technology, College of Human Ecology, Chang Gung University of Science and Technology, Taoyuan 33302, Taiwan;5. Department of Anesthesiology, Chang Gung Memorial Hospital, Taoyuan 33302, Taiwan;6. Chinese Herbal Medicine Research Team, Healthy Aging Research Center, Chang Gung University, Taoyuan 33302, Taiwan;7. Department of Biotechnology, College of Life Science, Kaohsiung Medical University, Kaohsiung 80708, Taiwan;8. Department of Marine Biotechnology and Resources, National Sun Yat-sen University, Kaohsiung 80424, Taiwan;9. Department of Medical Research, Kaohsiung Medical University Hospital, Kaohsiung 80708, Taiwan;1. Department of Chemistry, Yale University, New Haven, CT 06520, United States;2. Department of Pharmacology, Yale School of Medicine, New Haven, CT 06520, United States;3. Chemical Biology Institute, Yale University, West Haven, CT 06516, United States;4. Department of Microbial Pathogenesis, Yale School of Medicine, New Haven, CT 06536, United States;1. Key Laboratory of Natural Pharmaceutical and Chemical Biology of Yunnan Province, School of Science, Honghe University, Mengzi, Yunnan 661100, PR China;2. Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, PR China;3. State Key Laboratory for Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Science, Kunming 650204, PR China;4. Department of Soil and Water Science, University of Florida, 2181 McCarty Hall A, Gainesville, FL 32611-0290, USA
Abstract:The synthesis and structure activity relationship development of a pyrimidine series of heterocyclic Factor IXa inhibitors is described. Increased selectivity over Factor Xa inhibition was achieved through SAR expansion of the P1 element. Select compounds were evaluated in vivo to assess their plasma levels in rat.
Keywords:Factor IXa inhibition  Factor IXa  Pyrimidine  Thrombosis
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