Aurigene’s Insights

A Big thanks to Aurigene‘s [colorblind] scientists who have been gracious enough to share with us this presentation given in India at a recent med-chem conference.

Structural Insights into Kinase Inhibition
More like this please!

Allosterism: A Diatribe

So just what is an allosteric kinase inhibitor?

BAY 73-4506

So Bayer is in Ph2 with fluoro-sorafenib aka DAST, BAY-734506… Only this time they’re in without Onyx and I gather Onyx is none too happy about this.

The distinct compound is claimed in WO/2005/009961 and the I believe the original Sorafenib app is: WO/2000/042012.  What strikes the chemist inventor about a structure like this isn’t usually about who owns it, but if it can really be considered a new invention? The claim structure in the 2000 Sorafenib application can be schematized:

So for the purpose of this discussion the only meaningful definition is the ring designated as “L” and whether or not they claim the fluoride:

Anyhow while this structure and their priority date may be vulnerable to obviousness, all of these applications are assigned to Bayer, and not Onyx, so that disagreement will more likely be resolved based on the wording of the Onyx / Bayer contract.  The Onyx press release suggests this very structure was discovered during the collaboration…  We’ll see.  Given the timing I bet someone saw the structure here on Kinasepro and told Onyx, heh.

3H9F

Normally…

an A-loop doesn’t do that! (its new SGC prerelease of  a BI-PLK1-like inhibitor bound to TTK)

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 –

Asco Abstracts

Up!

Amgen: Us too.

As a comment in another thread notes, they have a handful of these too.  The regioismer is the novelty factor:

WO/2008/008539 / US2009012461 / 3CD8 / J Med Chem

Sanofi’s got’m too…

‘Nother Triazolopyridazine c-Met app:

WO/2009/056692

Roscotivine: The Saga

mmm KinaseBlogging:

Part 1, 2, 3, & 4

BI-6727

BI’s PhII follow on to BI-2536

PDB: 3FC2; Clin Can Res