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• W2034671778 endingPage "2511" @default.
• W2034671778 startingPage "2501" @default.
• W2034671778 abstract "Aiming to improve upon previously disclosed Factor Xa inhibitors, a series of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides were explored with the intent of increasing the projected human half-life versus 5 (projected human t1/2 = 6 h). A stereospecific route to compounds containing a 4-aryl-4-hydroxypyrrolidine scaffold was developed, resulting in several compounds that demonstrated an increase in the half-life as well as an increase in the in vitro potency compared to 5. Reported herein is the discovery of 26, containing a (2R,4S)-4-hydroxy-4-(2,4-difluorophenyl)-pyrrolidine scaffold, which is a selective, orally bioavailable, efficacious Factor Xa inhibitor that appears suitable for a once-daily dosing (projected human t1/2 = 23 h)." @default.
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• W2034671778 date "2009-03-01" @default.
• W2034671778 modified "2023-10-16" @default.
• W2034671778 title "Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action" @default.
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• W2034671778 doi "https://doi.org/10.1016/j.bmc.2009.01.063" @default.
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