Chemical descriptors of clinical stage kinase inhibitors

- pretty pictures – no data -

Rule of 5

>> Update: Here.

Obligatory Scivee Post

looks neet-o

More Her

‘nother ErbB 1,2,4 crystal forms app from BMS in US20070191375:

…

PDB Update

BMS has a p38 BMCL with a PDB publishing today as well: 2QD9

This one gives a little pespective to SCIO-469 and the related Scripps stuff: WO/2007/082079,

Hey C&EN

Nice cover story on c-Met and thanks for link. Have a look around and don’t miss the perennial favorites:

The Kinaverse – Kinase drugs & the Phase III compounds

Nerviano ‘n CDK

>> Update >> its really PHA-848125

WO/2007/90794 is a CDK inhibitor in combination with yada yada… from Nerviano.  The single compound claimed is pictured and potentially the phase one compound: PHA-793887.

Discovery: Pharmacia IT WO/2004/104007

BI’s PLK1 compound

WO/2007/90844 is a salt form application of a compound that we’ve seen before ’round here.

discovery: WO/2003/020722, WO/2004/076454

Don’t abuse inventorship: Scientist

So a guy named Brian Druker wrote this piece on how Gleevec is overpriced, eh? Who is he? Well he appears to have written his own byline in case you hadn’t heard:

THE?

A quick googlification suggests he has plenty of nice things to say about Brian Druker and his role in Gleevec’s discovery… To his credit he does list Jürg Zimmermann (the named inventor on a series of patents starting with EP564409) as one of the ‘unsung heroes‘ in a history of Gleevec essay.

According to Zimmermann the discovery went something like this:

etc.

ht: spicy ip, via pharmalot

WO/2007/089768

27 Authors, 586 pages, a whole bunch of examples, and 20 MB of Jak-2 goodness.

Seems likely that XL-019 came out of this series.