KinasePro

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

Archive for November 1st, 2006

Bioorg. Med. Chem. Lett. 2006, 5809

Posted by kinasepro on November 1, 2006

 

Hi Merck, Nice P38 patent BMCL describing the observed selectivity for VX-745 and related analogs. This is the companion article to: 2I0H

O=C1N(CCCN(C2=CC=C(F)C=C2Cl)C(C=C3)=NN(C4=CC=CC=C4Cl)C3=O)C(C5=C1C=CC=C5)=O

1M7Q droped the dime on this motif back in ’03

Posted in Merck & Co., p38 | Leave a Comment »

TG100801

Posted by kinasepro on November 1, 2006

Hi TargeGen. So whats with the new VEGF compound, eh?  Oh well. I also see you’ve disclosed that it’s an ester prodrug that hits VEGFR2 / PDGFR / SRC so its either a pyrimidine from WO2006101977 or a benzotriazine from the BMCL / ( US20050245524):

Using reverse logic, they’d probably publish the series that didn’t work right? Ergo, I’d put my bet down on the pyrimidines. The chloro-phenol of the above prodrug is 1.8 nM on SRC and single digit on EphB4 / PDGF / YES. I’d say these are a go for efficacy, but Tox?

>> Update 11/02 US20060247250 is a patent application which houses SRC/VEGF compounds, claims eyedrop formulations… and they’re pyrimidines.

Posted in biotech, SRC, VEGF | 1 Comment »