CG-?

A likely backup to CG-930, its a Signal discovered JNK inhibitor for which there is a solid forms app: WO/2008/057252

– no mention of stereochemistry –

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.

SR & JNK

Published the other stuff.. filed on these:

WO/2009/032861

SR-3451

Not your grandmothers diaryl urea -> aryl-amino-indazole, 3FI3, & 3FI2 snake around a methionine GK

Takeda’s got…

a Jnk3 BMCL:

2ZDT and 2ZDU …reminds of 2R9S

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.

Pfizer’s Jnk

SD’s got a series of Jnk1 inhibitors in WO/2007/125405:

First half of the compounds look about like that one, and Jnk1 data is given…
Second half appear discretely in the claims and look more like Jnk3 inhibitors to me.

PDB Update

2R9S is Jnk3 bound in an unusual fasion to a quinoline inhbitor:(Reminds me a little of Vertex’s 2ok1) (BMCL)

2NPQ is p38 bound to 2 molecules of octyl-glucoside:

 

PDB Update

Abbott’s got an anilinopyrimidine bound to Jnk1 with 2No3; BMCL. Their other JNK1 structure is 2g01

KRX-0401

Hey Keryx, Good luck with the “Akt, MAPK, and JNK” Phase ii. Don’t’ know anything about the compound other then what you tell us: “KRX-0401 (perifosine) is in-licensed by Keryx from Aeterna Zentaris”

Might take a little digging to get at this one.