KinasePro

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

US20070049622

Posted by kinasepro on March 6, 2007

Novartis has a RAF entry in US20070049622 which looks to combine a few twists to with a familiar theme:

CN1C2=CC=C(OC3=CC(C4=NC=C(C(F)(F)F)N4)=NC=C3)C=C2N=C1NC5=CC=C(Cl)C(C(F)(F)F)=C5

not too many new twists though…

O=C(NC1=NC=CC(OC2=CC=C3C(N=C(NC4=CC(C(F)(F)F)=CC=C4F)N3C)=C2)=C1)CN(CC)CC

WO/2005/037273
WO/2003/082272

O=C(C1=NC=CC(OC2=CC=C3C(N=C(NC4=CC=C(Cl)C(CN5CCN(C)CC5)=C4)N3C)=C2)=C1)NC

WO/2004/085425

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3 Responses to “US20070049622”

  1. Setanta said

    Isn’t that CHIR-265? Belongs to NVS since they bought Chiron.

  2. kinasepro said

    Good call – as usual KP is little behind the curve. The authors on this application indeed appear to be from Chiron. Has Chir-265 beed described? They’ve been stumping for CHIR-258 for a while, but mum on the RAF series, far as I know.

  3. Setanta said

    Yup. They disclosed it last year’s AACR. Sorafenib rip off basically – urea isostere for the DFG-out and amide isostere off the pyridine. Except that it actually has P-Mek and P-Erk inhibition in cells at nM potencies. P-Kdr too. But of course.

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