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Archive for the ‘BMS’ 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 »

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 »

More Her

Posted by kinasepro on August 21, 2007

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

COC1=CC=CC(NC2=NC=NN3C2=C(CN4C[C@@H](O)[C@H](N)CC4)C=C3)=C1

Posted in BMS, EGF | 2 Comments »

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 »

‘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.

CC(C(OC[C@@H](C)OC([C@@H](C)N)=O)=C1)=C2N1N=CN=C2OC3=C(F)C(C=C(C)N4)=C4C=C3

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

CC1=NC(NC2=NC=C(C(NC3=C(Cl)C=CC=C3C)=O)S2)=CC(N4CCN(CCO)CC4)=N1

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 »

WO2006135796

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,

CC(C(NC(OC[C@@H]1COCCN1)=O)=C2)=C3N2N=CN=C3NC4=CC(C=NN5CC6=CC(F)=CC=C6)=C5C=C4

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 »