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

Archive for the ‘GSK’ Category

GSK’s got C-Met

Posted by kinasepro on March 19, 2009

WO/2008/049855 bears a certain resemblance to XL-184.


btw: XL-880 is now going by GSK-1363089

Posted in biotech, c-Met, GSK | Leave a Comment »


Posted by kinasepro on March 18, 2009

It’s an AKT inhibitor, and its been Terminated & WithdrawnWonder why.

CC(C)(C#CC1=NC=C(C2=C1N=C(N2CC)C3=NON=C3N)OC[C@@H]4CNCCC4)OCancer Res, Blood, J Med Chem, Dartmouth?

Posted in AKT, GSK | 3 Comments »


Posted by kinasepro on August 23, 2008

GSK’s AKT Alkynes?

Yah, you heard it here first. So Technically these are at least 3 years behind the times…



Posted in AKT, GSK | Leave a Comment »

Some highlights…

Posted by kinasepro on November 28, 2007

GSK’s been looking at Plk1 for quite a while. Sure the structure was in an earlier application (March), but here it is better late then never. See: WO/2004/074244, WO/2004/087652, WO/2005/019193, WO/2007/030361, US20070010668, & US20070270437

AP-24534 In here? Earlier Ariad had a double bond wiggling around T315I, in WO/2007/133560 & WO/2007/133562 it’s a triple bond.

And Vertex has an interesting series of series of Rock inhibitors in WO/2007/133622. Ki is reported to be <100 nM and clean across the cyps.

Oh yah, and if your curious about Cyclacel’s Aurora inhibitor CYC-116, they’ve narrowed it down to 1 of 3 for you and they also give an in vitro panel in WO/2007/132220, WO/2007/132221, WO/2007/132228. The claims make it look like the morpholine.

Posted in Ariad, bcr abl, Cyclacel, GSK, Plk1, Rho, Vertex | 4 Comments »


Posted by kinasepro on June 19, 2007

aka GW-786034 is GSK’s ‘pan Vegfr’ inhibitor:


salt: hydrochloride
some chemistry here.
clinic: ph iii: RCC, WO/2002/05911

Posted in GSK, Phase III, VEGF | Leave a Comment »


Posted by kinasepro on May 13, 2007

aka GW-786034 is GSK’s ‘pan Vegfr’ / TIE2 inhibitor:


salt: hydrochloride
some chemistry here.
clinic: ph ii, WO/2002/059110

Posted in GSK, TIE2, VEGF | 2 Comments »

Tykerb ®

Posted by kinasepro on April 8, 2007

Tykerb ®, lapatinib, GW-572016


Discovery: Glaxo UK: WO/1999/35146
US Approval: March 2007

wiki; fda; PDB: 1XKK; Nature Reviews Drug Discovery

Posted in Approved, GSK | 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.


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


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 »

Tykerb: a go

Posted by kinasepro on March 14, 2007

After announcement of the positive Ph3 it seemed like just a matter of time, and that time has come. Tykerb gets FDA approval in combination with Xeloda for treatement of advanced metatatic breast cancer where the cancer overexpresses Her2 as a second line therapy. And yes that is a mouthful… a 1.25g/d mouthful, worth eventually an estimated 1b/y.


Posted in EGF, GSK | 1 Comment »

GSK – More Aurora Active Pyrimidines

Posted by kinasepro on February 16, 2007

Here’s another Aurora application: WO/2007/018941


sensing a pattern?

Posted in Aurora, GSK | 4 Comments »