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

Archive for May, 2009

Aurigene’s Insights

Posted by kinasepro on May 29, 2009

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.

aurigeneStructural Insights into Kinase Inhibition
More like this please!

Posted in General Interest | Leave a Comment »

Allosterism: A Diatribe

Posted by kinasepro on May 25, 2009

So just what is an allosteric kinase inhibitor?

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Posted in General Interest, gleevec | 8 Comments »

BAY 73-4506

Posted by kinasepro on May 20, 2009

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.

BAY-734506The 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:

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

L-definedAnyhow 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.

Posted in Bayer, RAF, VEGF | 5 Comments »


Posted by kinasepro on May 18, 2009



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

Posted in PDB, SGC | Leave a Comment »


Posted by kinasepro on May 15, 2009

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 –

Posted in Celgene, Jnk | Leave a Comment »

Asco Abstracts

Posted by kinasepro on May 15, 2009


Posted in clinical | Leave a Comment »

Amgen: Us too.

Posted by kinasepro on May 14, 2009

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



Posted in Amgen, c-Met | Leave a Comment »

Sanofi’s got’m too…

Posted by kinasepro on May 13, 2009

‘Nother Triazolopyridazine c-Met app:


Posted in c-Met, Sanofi-Aventis | Leave a Comment »

Roscotivine: The Saga

Posted by kinasepro on May 13, 2009

mmm KinaseBlogging:

Part 1, 2, 3, & 4

Posted in CDK | Leave a Comment »


Posted by kinasepro on May 12, 2009

BI’s PhII follow on to BI-2536


PDB: 3FC2; Clin Can Res

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Posted in BI, Plk1 | Leave a Comment »