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Archive for the ‘multi-target’ Category

Schering’s Macrocycles

Posted by kinasepro on July 20, 2007

Aurora Eh? What can I say, I like’m: WO/2007/079982

BrC(C=N1)=C2N=C1NC3=CC=C(S(C)(=O)=NC(NCC)=O)C(NCCCCN2)=C3

Related series, complete w/ a Chem Med Chem.

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Posted in Aurora, multi-target, Schering AG, VEGF | 12 Comments »

Subtle… Interesting… and thoroughly Swiss

Posted by kinasepro on June 13, 2007

WO/2007/062805 is a ‘multi-target’ application from Novartis that tags the earlier WO/2006/050946 with the Gleevec H1.

O=C(NC1=CC=C(C)C(NC2=C3C(N(C4=CC=C(N5CCOCC5)C=C4)N=C3)=NC=N2)=C1)C6=CC=CC(C(F)(F)F)=C6

Claim 11 suggests a few targets on their minds in addition to the titled Vegf / Ephb4:

11. The use according to claim 10, where the protein kinase modulation responsive disease is one or more diseases selected from the group consisting of diseases, that respond to the inhibition of one or more protein tyrosine kinases selected from abl kinase, especially v-abl or c-abl kinase, kinases from the family of the src kinases, especially c-src kinase, b-raf (V599E) and/or especially RET-receptor kinase or Ephrin receptor kinases, or mutated forms thereof.

Posted in multi-target, Novartis, VEGF | 1 Comment »

ENMD-981693

Posted by kinasepro on June 1, 2007

So Entremed is over in Boston stumping for their Aurora inhibitor and they happened to drop the MW and cLogP:

CC1=CC(NC2=NC(/C=C/C3=CC=CC=C3)=NC(N4CCN(CC4)C)=C2)=NN1

Only two compounds from WO/2007/041358 fit that bill. That one, and the Z isomer.

Posted in Aurora, biotech, Flt3, multi-target | 4 Comments »

PLX4032: burried in here?

Posted by kinasepro on January 8, 2007

So you know that kinase your working on. Yah, yah that one. Turns out that Plexxikon has compounds that inhibit it too. No, really. Between their two most recent applications to publish: WO/2007/002325, and WO/2007/002433 they claim <10 uM inhibition on no less then 36 kinases (+ n isoforms) with 22 authors. It’s an impressive body of matter, if pyrrolopyridines are your thing, and 1200+ pages of patent apps don’t scare you, check it out.

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Posted in multi-target, Plexxikon, RAF | 7 Comments »