280771-60-0Relevant articles and documents
URETHANES, UREAS, AMIDINES AND RELATED INHIBITORS OF FACTOR XA
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Page/Page column 23, (2011/10/03)
The invention relates to a new class of compounds, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions that are effective as selective inhibitors of factor Xa, both in the isolated state and in a complex with other proteins. The compounds of the invention can be used for treating and preventing diseases, such as acute coronary syndrome, myocardial infarction, unstable angina, refractory angina, thromboses caused by post-thrombolytic therapy or coronary angioplasty, acute ischemia mediated cerebrovascular syndrome, embolic stroke, thrombotic stroke, and other diseases in humans and other mammals associated with blood coagulation problems.
Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor
Zhang, Penglie,Huang, Wenrong,Wang, Lingyan,Bao, Liang,Jia, Zhaozhong J.,Bauer, Shawn M.,Goldman, Erick A.,Probst, Gary D.,Song, Yonghong,Su, Ting,Fan, Jingmei,Wu, Yanhong,Li, Wenhao,Woolfrey, John,Sinha, Uma,Wong, Paul W.,Edwards, Susan T.,Arfsten, Ann E.,Clizbe, Lane A.,Kanter, James,Pandey, Anjali,Park, Gary,Hutchaleelaha, Athiwat,Lambing, Joseph L.,Hollenbach, Stanley J.,Scarborough, Robert M.,Zhu, Bing-Yan
scheme or table, p. 2179 - 2185 (2009/12/07)
Systematic SAR studies of in vitro factor Xa inhibitory activity around compound 1 were performed by modifying each of the three phenyl rings. A class of highly potent, selective, efficacious and orally bioavailable direct factor Xa inhibitors was discovered. These compounds were screened in hERG binding assays to examine the effects of substitution groups on the hERG channel affinity. From the leading compounds, betrixaban (compound 11, PRT054021) has been selected as the clinical candidate for development.
Anthranilamide inhibitors of factor Xa
Mendel, David,Marquart, Angela L.,Joseph, Sajan,Waid, Philip,Yee, Ying K.,Tebbe, Anne Louise,Ratz, Andrew M.,Herron, David K.,Goodson, Theodore,Masters, John J.,Franciskovich, Jeffry B.,Tinsley, Jennifer M.,Wiley, Michael R.,Weir, Leonard C.,Kyle, Jeffrey A.,Klimkowski, Valentine J.,Smith, Gerald F.,Towner, Richard D.,Froelich, Larry L.,Buben, John,Craft, Trelia J.
, p. 4832 - 4836 (2008/02/11)
SAR about the B-ring of a series of N2-aroyl anthranilamide factor Xa (fXa) inhibitors is described. B-ring o-aminoalkylether and B-ring p-amine probes of the S1′ and S4 sites, respectively, afforded picomolar fXa inhibitors that performed well in in vitro anticoagulation assays.
AROMATIC ETHER DERIVATIVES USEFUL AS THROMBIN INHIBITORS
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Page/Page column 41, (2008/06/13)
This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor. An example of a compound of formula (I) is (a).
AROMATIC AMIDES
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, (2008/06/13)
This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
