Pi3k @ Bayer

This one hones in on the sulphonamides: (from the former site in CT)

WO/2009/091550; They stuck morpholines out there previously: WO/2008/070150

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.

RDEA-119

Its Ardeas’s $35 million non-hydroxamate MEK inhibitor in Ph1.  The pictured structure is one of three claimed in the ‘combination w/ Nexavar’ app: WO/2009/018238.

“Ardea will grant Bayer a worldwide, exclusive license to develop and commercialize Ardea’s MEK inhibitors for all indications”

DAST (BAY 73-4506)

It’s Bayer’s Ph2 follow-on to Sorafenib.  VEGF / RAF yadda yadda… Don’t have the structure, but maybe it’s one of these:

from polymorph apps:

WO/2008/058644 –            WO/2008/079968
WO/2008/043446 –            WO/2008/079972

& yeh, that is Fluoro-Nexavar…

Bayer ‘n Egf

Set of covalent ErbB inhibitors from Bayer:

WO/2007/109279

Bayer US: We used to work on IGF-1R

The ontology of WO/2007/056170 seems pretty clear, and given the lack of a BMCL even though everybody got laid off they’re probably moving a compound forward.

Oh yah, and Derek: Welcome to the dark side.

Nexavar ®

Nexavar ®, sorafenib tosylate, BAY-439006

Discovery: Bayer WO/2000/042012
US Approval: December 2005

wiki; Org.Proc.Res.Dev. ’02, 777

PDB: 1UWH; 1UWJ; 2HZN

News of the day…

In case you’ve been under a rock today, Bayer is closing both its West Haven, CT site and Schering’s Richmond, CA site. They claim the number is 800, but estimates put the Richmond site at 380, and the CT site at 1,100. They either plan on relocating 600 people or they are lieing.

This is an unhappy day in KinaseLand.