KinasePro

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

GSK and Ranbaxy in the P38 game

Posted by kinasepro on April 5, 2007

Earlier Ranbaxy had WO/2006/082492 and now its: WO/2007/036791. Add to that GSK has 2 oral P38 inhibitors in the clinic but despite some crafty wording of a recent Ranbaxy press release, the current clinical batch wasn’t an Indian invention. It looks as though GSK has shipped finding more backups overseas.

O=C1C(C2=CC=CC=C2C)=CC3=CN=C(NC4CCN(C(C5=CC=C(F)C=C5)=O)CC4)N=C3N1[C@@H]6CN(C(C)=O)CC6

SB681323: Phii: COPD, Neuropathic pain
GW856553: Phii RA; RA; COPD;

O=C1C=CC2=C(C3=CC=C(F)C=C3F)N=C(N[C@H](C)CO)N=C2N1C4=CC=C(F)C=C4F

One of them is likely from WO/2006/134382 (compound on the left) The other? Not so obvious. There’s a number of GSK p38 applications, but my guess is it hails from the pyrimidopyridone scaffold: Something like: WO/2003/088972 (above) or WO/2006/104915

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4 Responses to “GSK and Ranbaxy in the P38 game”

  1. weirdo said

    I think it’s significant that the original player (discoverer, really) in the p38 game is still at it, despite their own multiple failures in the clinic. I wouldn’t touch this target with the proverbial ten-foot pole, but more power to them.

    Or, maybe, this is another prime example of good money following bad. Didn’t work for RA? Try COPD. Or athero. Or pain. Another adverse event? Can’t be the target, let’s try another molecule!

    You’d think after all this time one would have heard of a successful Phase 2 trial (don’t say “Vertex” unless you look at their data). How many hundreds of millions have been spent at various companies on this single target, and where has that gotten us?

  2. milkshake said

    the long-term systemic use is problematic, short-term intervention or topical use may be OK

    there is an inflammation component to necrosis/apoptosis following ischemia and the organ re-perfusion – so a mixed inhibitor that targets kinases involved in cell death can have additional effect if it also hits p38

  3. GSK have a massive inflammatory disease franchise to defend (Advair – COPD, Asthma etcetera) which an oral and/or inhaled p38 inhibitor would go along way to helping out.

  4. milkshake said

    The GSK pyridine compound is rather lovely – I think it binds exactly the same way as the older Pharmacia pyridone/pyrimidone compounds.

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