OSI-906

It’s OSI‘s ph1 IGF1R inhibitor

and it’s synergistic with Tarceva

AEW-541

aka: NVP-AEW541 is Novartis’ IGF1R ‘Nib been ’round a while, but its off the pipeline?

Org Proc Res Dev; ASCO, Nature, Gist, Cancer Cell

Astra’s got IGF1R

Its not in the pipeline, but it is a candidate. WO/2008/117051 has xrpd, and lots of data.

10x enough?

‘o’; mode

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.

PDB Update

2GU8, AKT, Chiron, BMCL, 06, 4163

2OJ9, IGF-1R, BMS, BMCL, 07, 2317

US20060276514

Ok Merck, so what’s with the aldehyde? Ahhah, I see you already dropped the dime in Biochemistry back in ’05. ‘Reductive amination’ with no reducing agent. Somebody needs to break these kinds of things down for me, since I still don’t get it.

WO2006109026

Hi AstraZeneca, Nice IGFR inhibitors. They could be 20 uM for all I know, but they’ve got it all. Pyrimidine, pyrazine, and pyridines, pyrrolidine, isoxazole, and even a chiral center all on a sub-500 MW molecule! Hot Damn, strap on a morpholine and I’ll have died and gone to heaven. WO2006109026, WO2006106307, WO2006100461, WO2005040159.

Some of the points of diversity are highlighted, not entirely sure whats going on with these. Pretty cool though. The ’05 application references Vertex: WO2002022601