KinasePro

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

Archive for the ‘Bayer’ Category

Pi3k @ Bayer

Posted by kinasepro on July 25, 2009

This one hones in on the sulphonamides: (from the former site in CT)O=C(C1=CC=CN=C1)NC2=NC3=C(OC)C(OCCOCCNS(C)(=O)=O)=CC=C3C4=NCCN24

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

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Posted in Bayer, pi3k | 1 Comment »

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 »

RDEA-119

Posted by kinasepro on April 29, 2009

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.

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

Posted in Bayer, MEK | 1 Comment »

DAST (BAY 73-4506)

Posted by kinasepro on April 7, 2009

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:

O=C(C1=NC=CC(OCC2=C(Cl)C(NC(NC3=CC(C(C)(C)C)=NN3C4=CC=CC(CO)=C4)=O)=CS2)=C1)NC.O=C(C5=NC=CC(OC6=CC=C(NC(NC7=CC=C(Cl)C(C(F)(F)F)=C7)=O)C(F)=C6)=C5)NC

from polymorph apps:

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

& yeh, that is Fluoro-Nexavar…

Posted in Bayer, c-Kit, PDGFR, RAF, VEGF | Leave a Comment »

Bayer ‘n Egf

Posted by kinasepro on October 2, 2007

Set of covalent ErbB inhibitors from Bayer:

O=C(/C=C/CN(CC)C)N(CC3)CC2=C3C1=C(NC4=CC(C=CN5CC6=NC=CC=C6)=C5C=C4)N=CN=C1S2

WO/2007/109279

Posted in Bayer, EGF | 3 Comments »

Bayer US: We used to work on IGF-1R

Posted by kinasepro on May 18, 2007

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.

NC1=NC=NN2C1=C(C3=CC4=NN(CC5=CC=CC=C5)C=C4C=C3)C=C2C6CCN(C7CC7)CC6

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

Posted in Bayer, IGF | 1 Comment »

Nexavar ®

Posted by kinasepro on April 8, 2007

Nexavar ®, sorafenib tosylate, BAY-439006

O=C(C1=NC=CC(OC2=CC=C(NC(NC3=CC=C(Cl)C(C(F)(F)F)=C3)=O)C=C2)=C1)NC

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

wiki; Org.Proc.Res.Dev. ’02, 777

PDB: 1UWH; 1UWJ; 2HZN

Posted in Approved, Bayer | Leave a Comment »

News of the day…

Posted by kinasepro on November 9, 2006

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.

Posted in Bayer | 7 Comments »