KinasePro

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

Wyeth gets Jak’d up!

Posted by kinasepro on December 30, 2006

via Jak3 but of course – in an underanounced deal with Pharmacopeia:

…Wyeth will pay Pharmacopeia $5 million initially, as much as $9 million of research funding over the next three years, and as much as $175 million for reaching certain goals with the JAK3 kinase inhibitor drug.

While it’s likely they have a few which haven’t published yet, WO/2006/108103 is the most recent PCOP Jak3 application.

O=C1NC2=C(N=C(N3C4=CC(F)=CC=C4N=C3)N=C2)N1[C@H]5CCC(C6=C5C=CC=C6)=O

They’ve been at this stuff for a while – I reckon since WO/2001/047921 and have a recent Tet Lett on a related series. Check 2HK5 for a clue on how they bind.

>> update 1/25/07 >> US20070021443 Jak3 Pharmacopeia patent application

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3 Responses to “Wyeth gets Jak’d up!”

  1. medchemist said

    Selectivity is tricky in the JAKs and it doesn’t look like there is much interaction with the gatekeeper, Met902, with this ligand. I would think that going after Cys909 could payoff big too.

  2. kinasepro said

    Hey MedChemist, I agree that cystine residue is kind of dangling out there. It’s the same one a lot of groups are going after for oncology indications in kinases like EGF with irreversible inhibitors (Cys773). Jak3 being more of an immunosuppressant target, and most folks being all sissy about going after covalent inhibitors for chronically delivered compounds…

    Seen people going after that CYS reversibly?

  3. weirdo said

    “all sissy”

    Hey, I resemble that remark.

    Attacking active site cysteines with reversible covalent modifiers is a common tactic for, of all things, cysteine proteases, so this seems like a good candidate for a cyanomethyl-amide or alpha-ketoamide. But, again, covalent ligands can be a tough sell for chronic therapy . . .

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