KinasePro

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

Archive for March, 2009

INCB018424

Posted by kinasepro on March 28, 2009

Incyte’s Ph2 Jak 1, 2 inhibitor: Org Lett; see also: WO/2008/157208

N#CC[C@H](C1CCCC1)N2N=CC(C3=NC=NC4=C3C=CN4)=C2

Keeping pace with CP-690550

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Posted in JAK | 9 Comments »

The History of Gleevec

Posted by kinasepro on March 28, 2009

chemistry @ 22:30

It’d be great if someone were to crystallize the first hit with Abl or Kit and compare this with 1IEP.  I suspect this would put the paradigm of structure based design in perspective.

Posted in gleevec | Leave a Comment »

SCH-727965

Posted by kinasepro on March 27, 2009

Schering-Plough’s CDK1,2,5,9 inhibitor in Ph2 for lung cancer:

O=N1=CC=CC(CNC2=CC(N3CCCC[C@H]3CCO)=NC4=C(CC)C=NN42)=C1

WO/2009/038701 has quite a bit to say about the clinical protocol including human PK and a very clean dose response measuring BrdU incorporation.

Posted in CDK, Schering-Plough | 5 Comments »

BMS-777607

Posted by kinasepro on March 26, 2009

BMS homegrown Ph1 c-Met / AXL / Ron Inhibitor.  As of now PDB 3F82 has not yet been released.

O=C(C1=C(OCC)C=CN(C2=CC=C(F)C=C2)C1=O)NC3=CC=C(OC4=C(Cl)C(N)=NC=C4)C(F)=C3

The N-Oxide is a major metabolite, and from the trial notes its either toxic, potent, or prevalent… The J Med Chem doesn’t mention it.

Posted in BMS, c-Met | 1 Comment »

AC-220

Posted by kinasepro on March 26, 2009

Is the screening company’s Ph1 FLT-3 compound:

O=C(NC1=CC=C(C2=CN3C(SC4=CC(OCCN5CCOCC5)=CC=C34)=N2)C=C1)NC6=NOC(C(C)(C)C)=C6

polymorph app: WO/2009/038757

Posted in Ambit, Flt3 | Leave a Comment »

R-343

Posted by kinasepro on March 24, 2009

Structure’s a guess from process app: WO/2009/031011

FC(C=N1)=C(NC2=CC3=C(OC(F)(C(N3)=O)F)C=C2)N=C1NC4=CC(OCC(NC)=O)=CC=C4.OC5=C(C(O)=O)C=CC6=CC=CC=C65

Posted in Pfizer, Rigel, SYK | 2 Comments »

E-7080

Posted by kinasepro on March 24, 2009

Eisai’s Ph1 VEGF inhibitor

O=C(N)C1=CC2=C(C=CN=C2C=C1OC)OC3=CC=C(C(Cl)=C3)NC(NC4CC4)=O

Posted in Eisai, VEGF | Leave a Comment »

AV-951

Posted by kinasepro on March 23, 2009

Aveo’s Vegf inhibitor; currently Ph ii in RCC & NSCLC;

O=C(NC1=CC=C(C=C1Cl)OC2=C3C=C(C(OC)=CC3=NC=C2)OC)NC4=NOC(C)=C4

Formerly KRN-951 & pM against 1, 2, & 3

Posted in VEGF | 5 Comments »

GSK’s got C-Met

Posted by kinasepro on March 19, 2009

WO/2008/049855 bears a certain resemblance to XL-184.

O=C(C1(C(NC2=CC=C(F)C=C2)=O)CC1)NC(C=C3)=CC=C3OC4=CC=NC5=C4C=C(C(NCCN6CCOCC6)=O)N5

btw: XL-880 is now going by GSK-1363089

Posted in biotech, c-Met, GSK | Leave a Comment »

AMG-458

Posted by kinasepro on March 18, 2009

Here’s one where they do tell us why its off the pipeline:

COC1=CC2=C(C(OC3=CC=C(N=C3)NC(C4=C(C)N(N(C4=O)C5=CC=CC=C5)CC(O)(C)C)=O)=CC=N2)C=C1

J Med Chem -> Chem Res Tox

Read the rest of this entry »

Posted in Amgen, c-Met | Leave a Comment »