KinasePro

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

Archive for the ‘IGF’ Category

OSI-906

Posted by kinasepro on March 16, 2009

It’s OSI‘s ph1 IGF1R inhibitor

O[C@]1(C[C@H](C1)C2=NC(C3=CC=C4C=CC(C5=CC=CC=C5)=NC4=C3)=C6C(N)=NC=CN62)C

and it’s synergistic with Tarceva

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Posted in IGF, OSI | Leave a Comment »

AEW-541

Posted by kinasepro on March 16, 2009

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

NC1=C2C(N([C@H]3C[C@H](CN4CCC4)C3)C=C2C5=CC=C(OCC6=CC=CC=C6)C=C5)=NC=N1

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

Posted in IGF, Novartis | Leave a Comment »

Astra’s got IGF1R

Posted by kinasepro on October 2, 2008

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

CC1=CC(NC2=NC(N3CCC[C@H]3C4=NOC(C5=NC=CC=N5)=C4)=NC(OC)=C2)=NN1

10x enough?

‘o’; mode

Posted in Astra, IGF | 1 Comment »

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 »

PDB Update

Posted by kinasepro on May 1, 2007

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

O=C(C1=CC=C(C2=NC(NC)=NC=C2)S1)N[C@@H](CC3=CC=C(Cl)C=C3Cl)CN

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

O=C1C(C2=NC3=CC(N4C=CN=C4)=CC(C)=C3N2)=C(NCC5=NC=CC=C5)C=CN1

Posted in AKT, BMS, Chiron, IGF, PDB | 1 Comment »

US20060276514

Posted by kinasepro on December 10, 2006

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.

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Posted in IGF, Merck & Co. | 2 Comments »

WO2006109026

Posted by kinasepro on November 2, 2006

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

Posted in Astra, IGF | 1 Comment »