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Archive for the ‘Roche’ Category

CH-4987655

Posted by kinasepro on April 23, 2009

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…

O=C(NOCCO)C1=C(NC2=CC=C(I)C=C2F)C(F)=C(F)C(CN3OCCCC3=O)=C1

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

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Posted in biotech, MEK, Roche | Leave a Comment »

WO/2009/047163

Posted by kinasepro on April 22, 2009

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

O=C(N)C1=CC(C2=CC=NC=C2)=CN1

Compound A

roche-data

Posted in CK1, Roche | 2 Comments »

Roche’s JNK

Posted by kinasepro on April 11, 2009

An awful lot like Takeda’s JNK

r-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.

Posted in Jnk, Roche | 3 Comments »

R-406

Posted by kinasepro on March 10, 2009

3FQS is Roche dropping the dime on R-406

currently in Ph2 as R-788

O=C1NC2=NC(NC3=NC(NC4=CC(OC)=C(OC)C(OC)=C4)=NC=C3F)=CC=C2OC1(C)C

\ : still no BMCL, eh Rigel? : /

Posted in Rigel, Roche, SYK | Leave a Comment »

Jnk Science

Posted by kinasepro on September 9, 2008

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.   C12=C(C=C(C=C2)C3=NN=CN3)C(C4=CC(OCCN5CCCCC5)=CC=C4)=NN1

That’s life on the edge for yah.

Posted in Celgene, Jnk, Roche | Leave a Comment »

Who cares about the Roche p38 inhibitors?

Posted by kinasepro on September 5, 2008

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

CN(C(C(N1CCCCC1)=NN2)=C2C=C3C4=CC(C(NC)=O)=CC=C4C)C3=O

WO/2008/104473

Posted in p38, Roche | Leave a Comment »

WO/2007/96259

Posted by kinasepro on September 5, 2007

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

IC1=CC=C(NC([C@H](C(C)C)N2C([C@@H]([C@@]3=CC=C(OCC(N4CCCC4)=O)C=C3)NC2=O)=O)=O)C(Cl)=C1

 > hydroxamates?

Posted in MEK, Roche | Leave a Comment »

More kinase-blogging…

Posted by kinasepro on July 6, 2007

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

CC1=CC(NC2=NC(SC3=CC=CC=C3F)=C4C=CC(OC)=CC4=C2)=NN1

(Rumors of my imperfection are greatly exaggerated.)

Posted in Aurora, Roche | Leave a Comment »

Roche ‘n Raf

Posted by kinasepro on March 19, 2007

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

O=C(C1=CN=C(N)C2=C1SC=C2COC3=C(C)C=CC(NC(C4=CC=C(Cl)C=C4)=O)=C3)NCCO

Posted in RAF, Roche | Leave a Comment »

WO/2007/019884

Posted by kinasepro on February 26, 2007

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

NC1=C(C(COC2=CC=C(Br)C=C2)=CS3)C3=C(C(NCCCCN4CCCC4)=O)C=N1

They’ve been around since ’05 though

Posted in Fgf, Roche, VEGF | 1 Comment »