Astex’s unpartnered JAK/Aur/Abl Ph1b nib
Archive for the ‘bcr abl’ Category
Posted by kinasepro on March 18, 2009
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
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 by kinasepro on October 30, 2007
Posted by kinasepro on September 18, 2007
(compounds from SGX)
Posted by kinasepro on August 9, 2007
The news today is that LS-104 is in Ph1 and now owned by Aegera from Lymphosign who in turn licsensed it from HSC. Their portfolio of patent applications suggests the compound is likely a tyrphostin derivative.
LS104 is a novel small molecule tyrosine kinase inhibitor of therapeutically significant kinases including Jak2 and Bcr-Abl…In contrast to marketed kinase inhibitor drugs, LS104 inhibits its targets in a non-ATP-competitive manner
I don’ t know about you but I needed a history lesson to get a handle on these…
Posted by kinasepro on July 13, 2007
wt Abl 1.5 nM
T315I 18 nM
So you like pictures?
Posted by kinasepro on February 26, 2007
Wyeth talks Src/Abl: SKI-606 (American Cyanamid: WO/2000/018740)
Roche talks P38: R1487
And a former Abbot guy is talkinig LCK: A-770041
all great compounds and yadda yadda, just having a hard time seeing anything new here.
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 by kinasepro on January 5, 2007