CH-4987655

Some have walked a country mile to get away from the hydroxamate, others think nothing of tacking ‘nother one on:  Its Chugai’s ‘ATP-Collaborative’  Ph1 MEK inhibitor: Ro-4987655 / CH-4987655.  More potent, stable, and soluble…

Reduced signs of hydrolysis to the inactive acid and no BBB penetration.(preclinically)

WO/2009/047163

WO/2009/047163 show’s a series of minimalist designed CK1 inhibitors:

Compound A

Roche’s JNK

An awful lot like Takeda’s JNK

Roche: WO/2008/138920; WO/2009/015917
Takeda:  BMCL; WO/2003/068750; WO/2002/062764

I  detect some similarity to SP-600125 within this class, but a cross screen of the older DPPIV inhibitors seem like a more likely origin.

R-406

3FQS is Roche dropping the dime on R-406

currently in Ph2 as R-788

\ : still no BMCL, eh Rigel? : /

Jnk Science

Roche Palo Alto just published 3E7O: JNK2 (7x mutant) bound to an indazole:

Which brings up that nearly two years ago I suggested CC-401 may be from an ’06 Celgene application.  Right flavor wrong compound, the drawn compound is CG-930 (IND filed Dec 18, 2007 – claimed in Ph1 for fibrotic diseases).  As NCI suggests CC-401 is an SP-600125 analog which incidentally is no longer on the CG pipeline.  

That’s life on the edge for yah.

Who cares about the Roche p38 inhibitors?

Probably a few less people in PA then a few months ago, eh?  But this one’s been getting press recently:

WO/2008/104473

WO/2007/96259

Roche has a 2nd gen series of hydantoins as MEK inhibitors with WO/2007/96259:

 > hydroxamates?

More kinase-blogging…

…over at Het.Chem. Check 2uv2 for the binding mode. WO/2007/071348

(Rumors of my imperfection are greatly exaggerated.)

Roche ‘n Raf

US20070060607 is ‘nother thienopyridine application from Roche. The listed in vitro assay uses c-Raf, but selectivity isn’t described.

WO/2007/019884

Roche’s got a Vegf/FGF app in WO/2007/019884

They’ve been around since ’05 though