for Alzheimer’s & Diabetes
Posted by kinasepro on April 13, 2009
Posted by kinasepro on October 11, 2008
Posted by kinasepro on August 10, 2007
WO/2007/089192 is a use app, and WO/2007/089191 is salt forms application of the pictured GSK3 inhibitor originally from WO/2003/08285. The YM-231146 / YM-359445 series bears similarity, albeit for Vegf.
Posted by kinasepro on January 28, 2007
Mitsubishi has an app covering the intermediates for their GSK3 Sanofi-Aventis stuff. I still think the spiro compounds are sexier, but the morpholines are further explored so here we have a pretty solid looking asymmetric method to make 2-aryl morpholines via CBS reduction:
Route starts on page 79 example 1, 2 & 5 shown here.
Array might have something to say with how novel the approach is, y’know given how they sell the (rac) stuff?
Posted by kinasepro on January 22, 2007
The triazolopyrimidine series hit the street with WO2005012304 where the chemistry was from Belgium, and Jannsen was calling them GSK3 inhibitors. Ahh, ’twas a simpler time… Then in WO/2006076442 they started claiming similar compounds: ‘produce a Fak/Cak enzyme inhibitory effect.’ So a) The series aint none too selective, b) there’s some subtle change that I’m not seeing where they can turn the activity around, c) GSK3 inhibitors ‘produce a fak/cak enzyme inhibitory effect,’ or of course d) I’m way over-thinking this. (yah, there is an indan in the earlier stuff too.)
ClickClick – Beats me…
Posted by kinasepro on January 14, 2007
US20070010539 is a GSK3-beta application. This series goes back to ’01, and the pictured spiro compound hit the streets in ’05. Publications on these? Other then an expert opinion (which my library doesn’t carry) and them naming SAR502250 a preclinical development candidate (also in ‘05), I haven’t seen anything. While I don’t relish posting old news, the novel spiro architecture was enough to make KP lift an eyebrow.
Only they know if these spiro compounds are the lead structures, but it looks like a well developed chemical series with an interesting story to be told, and since they’re not talking… I will.
Posted by kinasepro on October 27, 2006
Hi again Cyclacel, Good idea to cover the pyridines too. Thanks for giving us the data. And hey, it appears you can walk around the activity wheel a little by varying the amine portion of the aminothiazole, but less then 10-fold over all the CDKs and GSK3 / Aurora? Unless your not showing us your ace, it makes Kinasepro wonder just how selective your PLK1 inhibitors are.
Posted by kinasepro on October 25, 2006
Wie Gehts Roche Penzeburg?
This doesn’t otherwise strike Kinasepro as a very crowded chemical space, but it looks as though Roche is stepping a little close to Astex toes on this one… Looks as though Astex borrowed the general idea from Aventis, so hey thats just the way it goes I guess.