INCB018424

Incyte’s Ph2 Jak 1, 2 inhibitor: Org Lett; see also: WO/2008/157208

Keeping pace with CP-690550

The History of Gleevec

chemistry @ 22:30

It’d be great if someone were to crystallize the first hit with Abl or Kit and compare this with 1IEP.  I suspect this would put the paradigm of structure based design in perspective.

SCH-727965

Schering-Plough’s CDK1,2,5,9 inhibitor in Ph2 for lung cancer:

WO/2009/038701 has quite a bit to say about the clinical protocol including human PK and a very clean dose response measuring BrdU incorporation.

BMS-777607

BMS homegrown Ph1 c-Met / AXL / Ron Inhibitor.  As of now PDB 3F82 has not yet been released.

The N-Oxide is a major metabolite, and from the trial notes its either toxic, potent, or prevalent… The J Med Chem doesn’t mention it.

AC-220

Is the screening company’s Ph1 FLT-3 compound:

polymorph app: WO/2009/038757

R-343

Structure’s a guess from process app: WO/2009/031011

E-7080

Eisai’s Ph1 VEGF inhibitor

AV-951

Aveo’s Vegf inhibitor; currently Ph ii in RCC & NSCLC;

Formerly KRN-951 & pM against 1, 2, & 3

GSK’s got C-Met

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

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

AMG-458

Here’s one where they do tell us why its off the pipeline:

J Med Chem -> Chem Res Tox