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Biotech / Medical : ARIAD Pharmaceuticals -- Ignore unavailable to you. Want to Upgrade?

To: mulanoon2007 who wrote (3993)	11/24/2015 8:46:52 PM
From: jaybe	Respond to of 4474

Could be, but then compare with patent language below for pona or briga. Why specifically mention 1pM for EGFR, Her2, and Exon 20 for both, when less than 1nM would cover all cases? I say if you discovered less than 1pM you better describe it in the patent. But as biomaven said since we still don't know which compound made it through pre-clinical and IND-enabling studies, we don't which mutations are testing at this rather unprecedented level of potency, if any. Ponatinib Patent Compounds of this invention of particular interest include those with one or more of the following characteristics...inhibitory activity against a wild type or mutant (especially a clinically relevant mutant) kinase, especially a Src family kinase such as Src, Yes, Lyn or Lck; a VEGF-R such as VEGF-R1 (Flt-1), VEGF-R2 (kdr), or VEGF- R3; a PDGF-R; an Abl kinase or another kinase of interest with an IC50 value of 1 uM or less (as determined using any scientifically acceptable kinase inhibition assay), preferably with an IC50 of 500 nM or better, and optimally with an IC50 value of 250 nM or better... Brigatinib Patent A wide variety of compounds of this invention were found to potently inhibit a number of important kinase targets. Many exhibited IC50's under 100 nM, and in many cases under 10 nM, and in some cases under 1 nM, when tested as inhibitors of the kinase, ALK, for instance.