Kinase Chemistry – Just a year and a half behind the times.


Posted by kinasepro on August 1, 2009

A comments to BMS-777607 suggest that this structure is the backup:



6 Responses to “BMS-817378”

  1. sks said

    any comments on the 4-pyridone like moiety instead of the 4-hydroxy pyridine???

  2. Ed said

    Better (intramolecular) h-bond acceptor for formation of a pseudo-ring?

  3. milkshake said

    4-pyridone = 4-hydroxypyridine, depending on the solvent you use to take NMR. These things are tautomers, you know

  4. kinasepro said

    Perhaps Sks meant 4 pyridone vs 2 pyridone… as is in 777607, and I have not idea. They’ve made a large number of the various permutations, and via trial and error it looks as though these two were the ones that worked out…

  5. petros said

    But the phase I trial (NCT00792558) was withdrawn before it started!

    BMS-817378 is the prodrug of BMS-794833

  6. sks said

    thanks guys!!

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