KinasePro

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

Archive for December 16th, 2006

Worlds first Kinase Podcast?

Posted by kinasepro on December 16, 2006

Michael Morrissey of Exelixis’ fame is talking Kinases and drug discovery on Thursday’s GenCast. Its not terribly exciting, but they are eliciting feedback over here.

hat tip: Xcovery for turning me on the show.

>> update: XL-880, the c-Met inhibitor he talks about likely comes from one of three pct’s: WO2006108059, WO2006014325, WO2005030140

CN1CC2C(CC(COC3=CC4=NC=CC(OC5=CC=C(NC(C6(C(NC7=CC=C(F)C=C7)=O)CC6)=O)C=C5F)=C4C=C3OC)C2)C1

Was the structure divulged in Prague?

Posted in c-Met, Exelixis | 1 Comment »

US20060281764

Posted by kinasepro on December 16, 2006

WTF J&J, Oxime-aldehydes? FLT3, TRKb, cKit inhibitors… Shinogi has some related EGF compounds: WO2006106721, and there’s a Biorg Med Chem Lett with the motif in CDK so its not unheard of. Quinazoline isosteres… Cool.

O=C(NC1=CC=C(C(C)C)C=C1)CC2CN(C3=NC=NC(N([H])[H])=C3/C=N/OC)CC2

Update >> There’s a couple other relatives that make this a family of applications which all published last Thursday:

 

O=C(N(CC1)CCC1C2=C(C=CC(N(C)C)=C3)C3=NC=N2)NC4=CC=C(OC(C)C)C=C4

This looks like the primary series, and the aniline appears to dial in TRKB – albeit not all that dramatically: US20060281772

O=C(OC1CN(C2=C3C(C=CS3)=NC=N2)CC1)NC4=CC=C(N5CCCC5)N=C4

US20060281768

 

Hmm… is LG293 TRKb?

 

Posted in c-Kit, Flt3, J&J | 2 Comments »