942316-74-7Relevant academic research and scientific papers
The discovery of new human coagulation factor XIa (FXIa) inhibitors by synthesis, biological evaluation, and structure-based modeling
Lee, Myeong Hwi,Song, Ho Young,Kim, Hyoungrae,Park, Kyung Eun,Kim, Jinyeong,Park, Tae Kyo,Kim, Yong Ju,Kang, Nam Sook
, p. 1105 - 1113 (2016)
Factor XIa (FXIa) is an enzyme that is activated during the earliest stage of initiation of the intrinsic pathway of the blood coagulation mechanism. In this study, we attempted to discover a new FXIa inhibitor based on structure-based molecular modeling. We found that compound 16 exhibits satisfactory predicted properties while maintaining important binding interactions with FX1a.
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).
New Compound Having Inhibition Activity to Factor XIa
-
Paragraph 0152-0156, (2021/05/17)
The present invention relates to a pharmacologically active amount of a novel compound, represented by chemical formula 1, having inhibition activity against factor XIa, a producing method thereof, and a pharmaceutical composition comprising: a pharmaceut
FACTOR XIA INHIBITORS
-
Page/Page column 25, (2015/12/17)
The present invention provides a compound of Formula I(The chemical formula should be inserted here.) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS
-
Page/Page column 60, (2010/02/17)
The present invention provides compounds of Formula (I) or (II): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, R3, R4, R8a, R11 and M are as defined herein. The compounds of Formula (I) or (II) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
PYRIDAZINE DERIVATIVES AS FACTOR XIA INHIBITORS
-
Page/Page column 109, (2009/10/22)
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein the variables A, L1, L2, R2, R11, and M are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS
-
Page/Page column 119, (2008/12/06)
The present invention provides compounds of Formula (I) or (II): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, R3, R4, R8a, R11 and M are as defined herein. The compounds of Formula (I) or (II) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
DIPEPTIDE ANALOGS AS COAGULATION FACTOR INHIBITORS
-
Page/Page column 147, (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.
