Posted by kinasepro on November 28, 2007
GSK’s been looking at Plk1 for quite a while. Sure the structure was in an earlier application (March), but here it is better late then never. See: WO/2004/074244, WO/2004/087652, WO/2005/019193, WO/2007/030361, US20070010668, & US20070270437
AP-24534 In here? Earlier Ariad had a double bond wiggling around T315I, in WO/2007/133560 & WO/2007/133562 it’s a triple bond.
And Vertex has an interesting series of series of Rock inhibitors in WO/2007/133622. Ki is reported to be <100 nM and clean across the cyps.
Oh yah, and if your curious about Cyclacel’s Aurora inhibitor CYC-116, they’ve narrowed it down to 1 of 3 for you and they also give an in vitro panel in WO/2007/132220, WO/2007/132221, WO/2007/132228. The claims make it look like the morpholine.
Posted in Ariad, bcr abl, Cyclacel, GSK, Plk1, Rho, Vertex | 4 Comments »
Posted by kinasepro on February 25, 2007
Everyone looking at Abl these days is trying to wiggle their way around T315 and Ariad’s latest go is described in the app: WO/2007/021937 with a series of styrene-purines. They look to be a follow-on series to the earlier purine stuff described elsewhere.
Structures for their two previous SRC/ABL leads: AP23464 and AP23451 were disclosed but afaik AP24534 has not.
Posted in Ariad, bcr abl | Leave a Comment »