KinasePro

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

US20060247262

Posted by kinasepro on November 6, 2006

Hello Novartis, I see the title of your recent offering is ‘blablabla as inhibitors of Zap70 and / or Syk Kinase.’  The discerning Kinasefan will recognize at least 1/2 of the following molecule which is incidentally makes the highlight reel as example 1. Sure it looks the like the Rigel stuff, but thats really just the part of the game eh? (you guessed it, the 4-halo pyrimidyl’s are part of the table)

COC1=C(OC)C(OC)=CC(NC2=NC(NC3=CC=C(OCCO4)C4=C3S(=O)(N)=O)=CC=N2)=C1

Looking passed the abstract one can learn that yah, sure, some of these examples are going to have some SYK activity (100nM – 10 uM), but primary target is clearly Zap70 and compounds are also tested against ALK.

CNC1=CC(NC2=NC(NC3=CC=C(OCCO4)C4=C3S(=O)(N)=O)=CC=N2)=CC=C1C

I see in the experimental you guys made 1.2 grams of compound 140, and reported the ic50 of 10nM for the compound. I’m not sure why, I mean I’m not entirely sure why you’d drop the dime on that, but clearly it was a lead compound.
CNC1=CC(NC2=NC(NC3=CC=C(OCCO4)C4=C3S(=O)(N)=O)=CC=N2)=CC=C1C CNC1=CC(NC2=NC(NC3=CC=C(OCCO4)C4=C3S(=O)(N)=O)=CC=N2)=CC=C1C

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