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Design, synthesis and structure-activity relationships of benzoxazinone-based factor Xa inhibitors. 2003
Wenrong Huang, and
Penglie Zhang, and
Jingmei F Zuckett, and
Lingyan Wang, and
John Woolfrey, and
Yonghong Song, and
Zhaozhong J Jia, and
Lane A Clizbe, and
Ting Su, and
Katherine Tran, and
Brian Huang, and
Paul Wong, and
Uma Sinha, and
Gary Park, and
Andrea Reed, and
John Malinowski, and
Stanley J Hollenbach, and
Robert M Scarborough, and
Bing-Yan Zhu
Millennium Pharmaceuticals, Inc., 256 E. Grand Avenue, South San Francisco, CA 94080, USA.
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 inhibitors with improved trypsin selectivity. The P4 modifications lead to monoamidines which are moderately active. The benzoxazinones 41-45 are potent against factor Xa, retain the improved trypsin selectivity of the corresponding aniline-based compounds, and show strong antithrombotic effect dose responsively.
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