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

Archive for the ‘p38’ Category

p38: Not dead?

Posted by kinasepro on August 13, 2009

Well.. maybe this compound will kill it: Polymorphic Forms / WO/2009/098612 & its from Pfizer no less –

pfizerp38

Part Axitinib, part Birb, Part SGX… All MW: 700

Thanks for the email PN.

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Posted in p38, Pfizer | 8 Comments »

PH-797804

Posted by kinasepro on June 9, 2009

In Ph2 for COPD & it’s an atropisomer…(biochem)

pha-797804

Who wants to guess if its R or S

Process App: 20080177077
Backup: 20080269264

Posted in p38, Pfizer | 6 Comments »

Nilotinib & P38ß

Posted by kinasepro on April 6, 2009

If you’ve got an IC50 comment here or email me:  SGC’s got a new pre-release.

 O=C(C1=CC=C(C(NC2=NC=CC(C3=CC=CN=C3)=N2)=C1)C)NC4=CC(C(F)(F)F)=CC(N5C=C(N=C5)C)=C4

p38ß = MAPK11 (not to be confused w/ p38α) 3GP0

Posted in p38, PDB | 1 Comment »

Plethora ‘o’ PDB’s

Posted by kinasepro on October 14, 2008

GSK’s AKT stuff: 3d0e, 3E8D, 3E87, 3E88; J Med Chem, KP

SGX: Jak2 3E64, 3E63, 3E62, BMCL

Shokat: SRC, SRC, SRC, SRC, PI3K-Gamma, PI3K-Gamma

reminds me of OSI-906 or vice versa

Astrazeneca: CDK2 BMCL: 2W05

Amgen: P38 J Med Chem; 3DT1

LCK: 2ZM4, 2ZM1

Posted in AKT, CDK2, JAK, Lck, p38, PDB, pi3k | 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 »

ARRY-797 goes to the dentist…

Posted by kinasepro on November 20, 2007

Promoted to ph2:

to evaluate the efficacy of ARRY-797 in the management of postoperative dental pain…

CC(F)(CN1C2=C(C=N1)C=C(C(C(N[C@](CCNC)(C(N)=O)CCC3CC3)=O)=C2)OC4=C(C=C(C=C4)F)F)C

still no structure disclosed afaik, but likely a cousin of the above.

Posted in Array, p38 | 5 Comments »

PDB Update

Posted by kinasepro on October 16, 2007

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:

 

Posted in Jnk, p38, PDB | 6 Comments »

VX-702

Posted by kinasepro on September 15, 2007

Vertex’s Ph2 p38 inhibitor:

FC1=CC=CC(F)=C1N(C(N([H])[H])=O)C2=CC=C(C(N)=O)C(C3=CC=C(F)C=C3F)=N2

is described in WO/2007/103468; model below

Read the rest of this entry »

Posted in p38, Vertex | 24 Comments »

PDB Update

Posted by kinasepro on August 21, 2007

BMS has a p38 BMCL with a PDB publishing today as well: 2QD9

O=C(N1C[C@@H](O)CC1)C(C2=CNC3=C2C=C(C(N4CC5=CN=C(C6=CC=C(F)C=C6F)N5CC4)=O)C(OC)=N3)=O

This one gives a little pespective to SCIO-469 and the related Scripps stuff: WO/2007/082079,

Posted in p38, PDB | Leave a Comment »

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

Posted in GSK, p38 | 4 Comments »