KinasePro

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.

O=C(C1(C(NC2=CC=C(F)C=C2)=O)CC1)NC(C=C3)=CC=C3OC4=CC=NC5=C4C=C(C(NCCN6CCOCC6)=O)N5

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

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

Gsk-690693

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 »

GSK-690693

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…

NC1=NON=C1C(N2CC)=NC3=C2C(OC[C@@H]4CNCCC4)=CN=C3C#CC(C)(C)O

neener.

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 »

Pazopanib

Posted by kinasepro on June 19, 2007

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

O=S(C1=CC(NC2=NC=CC(N(C)C3=CC4=NN(C(C)=C4C=C3)C)=N2)=CC=C1C)(N)=O

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

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

Pazopanib

Posted by kinasepro on May 13, 2007

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

O=S(C1=CC(NC2=NC=CC(N(C)C3=CC4=NN(C(C)=C4C=C3)C)=N2)=CC=C1C)(N)=O

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

ClC1=CC(NC2=NC=NC3=CC=C(C4=CC=C(CNCCS(=O)(C)=O)O4)C=C32)=CC=C1OCC5=CC(F)=CC=C5

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.

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 »

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.

ClC1=CC(NC2=NC=NC3=CC=C(C4=CC=C(CNCCS(=O)(C)=O)O4)C=C32)=CC=C1OCC5=CC(F)=CC=C5

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

smiles_O=C(NCC1=CC=C(F)C(OC)=C1)C(S2)=CC=C2C3=CC=NC(NC4=CC(N5CCN(C)CC5)=CC=C4)=N3

sensing a pattern?

Posted in Aurora, GSK | 4 Comments »

 
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