Archive for the ‘Amgen’ Category
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:
Posted by kinasepro on March 18, 2009
Here’s one where they do tell us why its off the pipeline:
Posted by kinasepro on November 20, 2008
Looks like this one might be coming off the ph3 list…
Posted by kinasepro on August 2, 2007
Posted by kinasepro on June 19, 2007
Motesanib diphosphate, AMG-706 hits: Vegfr1,2,3, c-kit, Pdgfr-b, and Ret
Posted by kinasepro on March 12, 2007
They describe Tie2 and LCK assays in a number of new apps, but it wouldn’t surprise me to learn a handful of other kinases were running in fear at the site of these things.
app is US20070054916
They’ve also got a C-Met application this week with US20070054903:
Posted by kinasepro on February 20, 2007
Irak-4? Yah I never heard of it either, but the IRAKs appear to be immunology targets for which Amgen is way out in front. They’ve got a nice paper in Structure, a Biorg. Med. Chem. Lett., and 2 PDB’s: 2NRU, 2NRY.
At first look I was mesmerized by the tyrosine gatekeeper but a second glance on looking over the recent CIP: US20070037803 shows something interesting.
they suggest as much in the BMCL. Read the rest of this entry »
Posted by kinasepro on December 12, 2006
Also, Amgen released the structurally interesting IRAK-4 bound to staurosporine (2NRY), and a benzimidazole inhibitor (2NRU). The Bioorg Med Chem Lett came out in March and the Xray is featured in this Structure paper.
The tyrosine gatekeeper is certainly different
Posted by kinasepro on November 6, 2006
Update>> They named it: Motesanib diphosphate
Xcovery has the roundup on AMG706. I tend to think it’s a little apples and oranges to try and line it up against Sutent at this point. Heck it’s been nearly a year since release and noones come out and said Sutent is really any better then Nexavar.
The compound is second generation to ptk787; a VEGF inhibitor which failed to meet a Phase III endpoint.
There’s an article on the preclinical stuff: Cancer Research (2006), 66(17), 8715
Frankly KP is shocked that noone has yet published an application claiming the Bayer modification, woops scratch that, looks like Bayer has an application floating around: WO2006002383, but they don’t have the magic indoline.
ClC(C=C1)=CC=C1NC2=NN=C(C3=C2C=CC=C3)CC4=C=NC=C4 O=C(NC1=CC(NCC2(C)C)=C2C=C1)C(C=CC=N3)=C3NCC4=CC=NC=C4 O=C(C1=NC=CC(CNC2=CC=CC=C2C(NC3=CC=C(OC(F)(F)O4)C4=C3)=O)=C1)NC5CC5