325457-63-4Relevant academic research and scientific papers
Design, synthesis and structure-activity relationships of benzoxazinone-based factor Xa inhibitors
Huang, Wenrong,Zhang, Penglie,Zuckett, Jingmei F.,Wang, Lingyan,Woolfrey, John,Song, Yonghong,Jia, Zhaozhong J.,Clizbe, Lane A.,Su, Ting,Tran, Katherine,Huang, Brian,Wong, Paul,Sinha, Uma,Park, Gary,Reed, Andrea,Malinowski, John,Hollenbach, Stanley J.,Scarborough, Robert M.,Zhu, Bing-Yan
, p. 561 - 566 (2007/10/03)
A series of benzoxazinone derivatives was designed and synthesized as factor Xa inhibitors. We demonstrated that the naphthyl moiety in the aniline-based compounds 1 and 2 can be replaced with benzene-fused heterobicycles and biaryls to give factor Xa inh
BIPHENYL DERIVATIVES
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, (2008/06/13)
Novel compounds of the formula I in which X, R 1, R 2, R 3, R 4 and R 5 have the meaning indicated in Patent Claim 1, are inhibitors of the coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders.
Benzimidazole-Based fXa inhibitors with improved thrombin and trypsin selectivity
Shaw, Kenneth J.,Guilford, William J.,Griedel, Brian D.,Sakata, Steve,Trinh, Lan,Wu, Shung,Xu, Wei,Zhao, Zuchun,Morrissey, Michael M.
, p. 1311 - 1314 (2007/10/03)
Optimization of the benzimidazole-based fXa inhibitors for selectivity versus thrombin and trypsin was achieved by substitution on the benzimidazole ring and replacement of the naphthylamidine group. Substitution of a nitro group at the 4-position on the benzimidazole improves both potency against fXa and selectivity versus thrombin. Alternatively, replacement of the naphthylamidine with either a biphenylamidine or propenylbenzamidine not only improves fXa potency and selectivity versus thrombin, but selectivity versus trypsin as well.
Benzenamine derivatives as anti-coagulants
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Page column 40, (2010/02/05)
This invention is directed to benzenamine derivatives of formula (I): wherein A, W, m, n, R1, R2, R3, R4, R5and R6are defined herein. These compounds are useful as anti-coagulants.
