Schering’s Macrocycles

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

Related series, complete w/ a Chem Med Chem.

Subtle… Interesting… and thoroughly Swiss

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

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.

ENMD-981693

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

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

PLX4032: burried in here?

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.