- Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors
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On the basis of a crystal structure of a phenylpyrrolidine lead and subsequent molecular modeling results, we designed and synthesized a novel series of macrocyclic FVIIa inhibitors. The optimal 16-membered macrocycle was 60-fold more potent than an acycl
- Priestley, E. Scott,Cheney, Daniel L.,DeLucca, Indawati,Wei, Anzhi,Luettgen, Joseph M.,Rendina, Alan R.,Wong, Pancras C.,Wexler, Ruth R.
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p. 6225 - 6236
(2015/08/24)
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- MACROCYCLIC FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS
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The present invention relates generally to novel macrocycles of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, thereof, wherein the variables A, B, L, M, W, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein. These compounds are selective inhibitors of the serine protease coagulation factor VIIa which can be used as medicaments.
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Page/Page column 75-76
(2008/06/13)
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