Substituted acrylamides as factor Xa inhibitors: improving bioavailability by P1 modification |
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Authors: | Song Yonghong Clizbe Lane Bhakta Chhaya Teng Willy Li Wenhao Wong Paul Huang Brian Sinha Uma Park Gary Reed Andrea Scarborough Robert M Zhu Bing-Yan |
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Institution: | Millennium Pharmaceuticals, Inc., South San Francisco, CA 94080, USA. yonghong.song@mpi.com |
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Abstract: | To overcome the low bioavailability of our substituted acrylamide P1 benzamidine factor Xa inhibitors reported previously, neutral and less basic groups were used to replace the benzamidine. As a result, a series of P1 aminoisoquinoline substituted acrylamide Xa inhibitors was identified to be potent, selective, and orally bioavailable. Modification of P4 moiety of these compounds further improved their pharmacokinetic properties. |
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