1094103-75-9Relevant academic research and scientific papers
Novel phenylalanine derived diamides as Factor XIa inhibitors
Smith, Leon M.,Orwat, Michael J.,Hu, Zilun,Han, Wei,Wang, Cailan,Rossi, Karen A.,Gilligan, Paul J.,Pabbisetty, Kumar B.,Osuna, Honey,Corte, James R.,Rendina, Alan R.,Luettgen, Joseph M.,Wong, Pancras C.,Narayanan, Ranga,Harper, Timothy W.,Bozarth, Jeffrey M.,Crain, Earl J.,Wei, Anzhi,Ramamurthy, Vidhyashankar,Morin, Paul E.,Xin, Baomin,Zheng, Joanna,Seiffert, Dietmar A.,Quan, Mimi L.,Lam, Patrick Y.S.,Wexler, Ruth R.,Pinto, Donald J.P.
, p. 472 - 478 (2016/01/09)
The synthesis, structural activity relationships (SAR), and selectivity profile of a potent series of phenylalanine diamide FXIa inhibitors will be discussed. Exploration of P1 prime and P2 prime groups led to the discovery of compounds with high FXIa affinity, good potency in our clotting assay (aPPT), and high selectivity against a panel of relevant serine proteases as exemplified by compound 21. Compound 21 demonstrated good in vivo efficacy (EC50 = 2.8 μM) in the rabbit electrically induced carotid arterial thrombosis model (ECAT).
DIPEPTIDE ANALOGS AS COAGULATION FACTOR INHIBITORS
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Page/Page column 159-160, (2009/01/23)
Disclosed are novel dipeptide analogs compounds of Formula (I), (II) or (III) or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate, or a prodrug thereof, which are inhibitors of factor XIa and/or plasma kallikrein, compositions containing them, and methods of using them, for example, for the treatment or prophylaxis of thrombotic diseases.
