- Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties
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In an effort to identify a potential back-up to apixaban (Eliquis), we explored a series of diversified P4 moieties. Several analogs with substituted gem-dimethyl moieties replacing the terminal lactam of apixaban were identified which demonstrated potent
- Orwat, Michael J.,Qiao, Jennifer X.,He, Kan,Rendina, Alan R.,Luettgen, Joseph M.,Rossi, Karen A.,Xin, Baomin,Knabb, Robert M.,Wexler, Ruth R.,Lam, Patrick Y.S.,Pinto, Donald J.P.
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p. 3341 - 3345
(2014/07/22)
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- COMPOUNDS USEFUL AS PHOSPHOTYROSINE MIMICS
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New uses are disclosed for compositions containing compounds of formula (I) wherein A, B, C, G, Q and R are defined herein. The compositions inhibit the binding of tyrosine kinase-dependent regulatory proteins to their native phosphotyrosine-containing li
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- 1,1-DISUBSTITUTED CYCLOALKYL DERIVATIVES AS FACTOR XA INHIBITORS
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The present application describes 1,1-disubstituted cycloalkyl compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
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Page 367-368
(2010/02/05)
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- Nonpeptidic, monocharged, cell permeable ligands for the p56lck SH2 domain
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p56lck is a member of the src family of tyrosine kinases and plays a critical role in the signal transduction events that lead to T cell activation. Ligands for the p56lck SH2 domain have the potential to disrupt the interaction of p56lck with its substra
- Proudfoot,Betageri,Cardozo,Gilmore,Glynn,Hickey,Jakes,Kabcenell,Kirrane,Tibolla,Lukas,Patel,Sharma,Yazdanian,Moss,Beaulieu,Cameron,Ferland,Gauthier,Gillard,Gorys,Poirier,Rancourt,Wernic,Montse
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p. 2421 - 2431
(2007/10/03)
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- Compounds useful as phosphotyrosine mimics
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Disclosed are compositions containing compounds of the formula (I) below wherein A,B,C,G,Q and R are defined herein. The compounds are useful as phosphotyrosine mimics that, when incorporated into an appropriate molecular structure, inhibit the binding of
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