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

p38: Not dead?

Posted by kinasepro on August 13, 2009

Well.. maybe this compound will kill it: Polymorphic Forms / WO/2009/098612 & its from Pfizer no less –


Part Axitinib, part Birb, Part SGX… All MW: 700

Thanks for the email PN.

8 Responses to “p38: Not dead?”

  1. milkshake said

    It’s alive! And the sole inventor on this patent is one Kenneth John Butcher – but he probably did not design it. Looks like a handywork of some small startup company that started with fragment-based design and then progressed to old-fashioned BIRB-series patent busting.

  2. viledonkey said

    Saw a Pfizer talk earlier this year about some very similar compounds….it was for p38 in the lungs & so the compounds were designed to be inhaled, have low systemic exposure, meaning they were damn ugly and broke Lipinski’s Law (which is sacrilege in Pfizer!!) This looks like another one…..

  3. Biotech said

    Am surprised this molecule got as far as it did, looks to be lots of metabolic liabilities in it does there not?

  4. petros said

    Metabolic liabilities might be good for an inhaled drug; and Pfizer currently has two phase I compounds for COPD at least one of which is inhaled

    Vile Donkey – where was that Pfizer talk>?

  5. petros said

    Ah found it, Anglo Swedish Med Chem 2009 example PF-994888 has the basic scaffold, just different aryl and fused azole substituents.

  6. ATP->ADP said

    An example of Cut-Paste chemistry to make hybrid p-38 inhibitor!

  7. spuddo said

    i love this frankenmolecule! it got it all except a non-standard element. Couldn’t the put a Boron in there somewhere?

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