KinasePro

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

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?

 

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2 Responses to “US20060281764”

  1. I think the oxime ether is just a carbonyl isostere, or used to block metabolism, although its possible they are doing something else here.

    See
    Drug Disc Today, 2004, Vol.9, p 1020-1028 on page 1024

    or
    Current Medicinal Chemistry, 2005, Vol 12, 23-49 on page 44.

  2. kinasepro said

    just found a J&J BMCL on the motif in VEGF.

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