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Kinase Chemistry – Just a year and a half behind the times.

Archive for the ‘Lexicon’ Category

Lexicon’s got Limk2

Posted by kinasepro on February 18, 2009

LX-7101 in here 20090042893?

lex

Reminds of Exel

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LX1032 ?

Posted by kinasepro on February 9, 2007

While not telling us which one they had a ‘protein kinase’ application publish today.

WO/2007/016674 or US20070032501

I’m guessing AKT PH domain

O=C(N)C1=C(F)C=C(C2=CC(C3=CC=CC(C4CCN(C(C)=O)CC4)=C3)=CN=C2N)C=C1F

13 examples, 7 authors.

I don’t know enough about the biology to know if AKT inhibition leads to reduced peripheral serotonin levels. If so, I’d say a few puzzle pieces are falling together.

Posted in Lexicon | 3 Comments »

Better Chemistry = Better Drugs

Posted by kinasepro on December 29, 2006

Wull Duh? But in this case it’s a webcast on medchem from some mostly non-chemists: David Snitman, Paul Goddard, Arthur Sands, and Jim Mahoney of Array, ARYx, Lexicon, and Surface Logix respectively.

Read the rest of this entry »

Posted in Array, biotech, Lexicon, MEK | 5 Comments »

WO2006091450

Posted by kinasepro on October 22, 2006

Hi again Lexicon,

Kinasepro must admit that he missed your application from this passed August. Your press release bugged him though, so he wouldn’t let it go. If its not too late, I’d like to change the guess about LG293 from the last post.

LG293 = JAK3

Probably not my final answer, and of course I’ll be waiting with the rest of the peanut gallery to see what the story is over the next couple years. Heck, as far as Kinasepro knows LG293 isn’t even a kinase in which case it’s LG267 which is JAK3 (that actually kinda makes more sense) . So why does Kinasepro have this crazy idea? It’s because of WO2006091450 and the fact tha Rigel nominated R348 for JAK3 on the very same day.

While your application, like all your other body of matter patent applications, doesn’t list a single biochemical assay it does incorporate matter which bears a striking resemblance to Pfizers early JAK3 stuff. After a little digging it appears a number of companies have been poking around the azaindole / pyrrolopyrimidine motif, so today I’d say you’ve got some stiff competition.


There’s plenty of others. Pfizer hit this scene first back in ’99 (WO199965909) and Vertex and AZ have tons of applications around different chemotypes, There seems to be something special about the saturated ring – Neet – o. Presumably noone has been able to dial in pk / selectivity / etc. till recently.

Posted in biotech, JAK, Lexicon | Leave a Comment »