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

Archive for the ‘BMS’ Category


Posted by kinasepro on August 1, 2009

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




Posted in BMS, c-Met | 6 Comments »


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.


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 »

More Her

Posted by kinasepro on August 21, 2007

‘nother ErbB 1,2,4 crystal forms app from BMS in US20070191375:



Posted in BMS, EGF | 2 Comments »

PDB Update

Posted by kinasepro on May 1, 2007

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


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



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

‘Nother “Novel” VEGF candidate

Posted by kinasepro on April 10, 2007

BMS-582664 / Brivanib alaninate

WO/2007/038648 is a development ‘crystalline forms’ application from BMS.


Discovery: WO/2004/009784. Process: WO/2006/130657. It’s a prodrug / isostere rip on AZD-2171 / Cediranib / Recentin; WO/2000/047212


Posted in BMS, VEGF | Leave a Comment »

Sprycel ®

Posted by kinasepro on April 8, 2007

Sprycel ®, dasatinib, BMS-354825


Discovery: Bristol-Myers Squibb WO/2000/062778
US Approval: June 2006

wiki; PDB: 2GQG; FDA; J Med Chem ’06 6819;

Named after its inventor?


Posted in Approved, BMS | Leave a Comment »

Takeda to BMS: pwned

Posted by kinasepro on January 6, 2007

So if your on the Aurora program at BMS you had to be a little disturbed when you saw US2006084650 with a priority date of: Oct 15, ’04 come out back in April ’06 as your earliest provisionals are from July 1 ’05. Who knows maybe there’s enough room in the sandbox for both. Takeda’s primary series appears to be the imidazopyrimidine anyways, but the pyrollo compounds are claimed and exemplified.

CC1=CC(NC2=NC(SC3=CC=C(NC(C4CC4)=O)C=C3)=CC5=NC(CN(C)C)=CN52)=NN1  CC1=CC(NC2=NC(SC3=CC=C(NC(C4CC4)=O)C=C3)=NN5C2=CC=C5)=NN1  CC1=CC(NC2=NC(SC3=CC=C(NC(C4CC4)=O)C=C3)=NC(N5CCN(C)CC5)=C2)=NN1

US20070004734; US20070004731


Posted in Aurora, BMS, Takeda | Leave a Comment »


Posted by kinasepro on December 21, 2006

‘Crystaline Forms’ of these HER1, 2, & 4 inhibitors. Interesting compounds. There’s already a BMCL on the series, and a Can J Chem on the route,


but this is the first I’ve heard of the morpholine.


Posted in BMS, EGF | 2 Comments »

Exelixis: bag of cash en route

Posted by kinasepro on December 19, 2006

While not saying what for I think its safe to assume they’ll hit a kinase or two along the way.

upfront payment of $60 million in cash. Exelixis will also receive $20 million for each of up to three different drug candidates selected by Bristol-Myers Squibb at IND…

Sweetheart oncology deal. boring webcast here.

>> update: 8k,  The check must-a-been postdated.


Posted in BMS, Exelixis | 1 Comment »

BMS-354825 vs. VX-680

Posted by kinasepro on November 24, 2006

At least the PDB gave us something to look at a few days ago. Here’s a super-cool alignment of dasatinib in Abl to VX-680 in an abl mutant.


Posted in Aurora, bcr abl, BMS, Vertex | Leave a Comment »