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Archive for the ‘c-Met’ Category

BMS-817378

Posted by kinasepro on August 1, 2009

A comments to BMS-777607 suggest that this structure is the backup:

O=C(NC1=CC=C(C(F)=C1)OC2=C(C(N)=NC=C2)Cl)C3=CNC=C(C3=O)C4=CC=C(C=C4)F

WO/2009/094427

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Posted in BMS, c-Met | 6 Comments »

Amgen: Us too.

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:

WO/2008/008539 / US2009012461 / 3CD8 / J Med Chem

COC1=CC2=NC=CC(OCC3=NN=C4C=CC(C5=CC=CC=C5)=NN43)=C2C=C1

amg-cmet-i

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

Sanofi’s got’m too…

Posted by kinasepro on May 13, 2009

‘Nother Triazolopyridazine c-Met app:

sanofi-cmetWO/2009/056692

Posted in c-Met, Sanofi-Aventis | Leave a Comment »

PF-04217903

Posted by kinasepro on May 12, 2009

This one snuck past me… and into the clinic.  Currently its Ph1 via: WO/2007/132308

OCCN(N=C1)C=C1C2=CN=C(N=NN3CC4=CC=C(N=CC=C5)C5=C4)C3=N2

this and PF-2341066 both still in the pipeline.

note also WO/2007/138472

Posted in c-Met, Pfizer | 1 Comment »

JNJ-38877605

Posted by kinasepro on May 8, 2009

Still in the clinic:  It’s JnJ’s ph1 c-Met inhibitor.

FC(C1=NN=C2N1N=C(C3=CN(C)N=C3)C=C2)(C4=CC5=C(N=CC=C5)C=C4)F

Posted in c-Met, J&J | 16 Comments »

2WD1

Posted by kinasepro on May 6, 2009

It’s a recent c-Met PDB published via UCB with relevance to my guess for a certain metabolite recently in the news…

O=C(C1=CN=C2C(N(S(=O)(C3=C([N+]([O-])=O)C=CC=C3)=O)C=C2)=C1)N

BMCL

Posted in c-Met | 4 Comments »

SGX-523

Posted by kinasepro on May 6, 2009

It’s SGX’s former Ph1 c-Met inhibitor & Derek‘s got a post on it.  Lilly released that the trial was halted due to a reversible acute renal failure in the 80 mg dose group brought on by a compound crystallizing in the kidney.

CN1N=CC(C2=NN3C(SC4=CC5=CC=CN=C5C=C4)=NN=C3C=C2)=C1

makes you wonder…

Posted in c-Met, SGX | 8 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 »

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 »