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


Posted by kinasepro on October 7, 2006


Are you guys on to something with the whole ‘ribose pocket’ thing?

Going after c-Met Kinasepro thinks this application has a bit in common with another recent offering. This one has one of the more characteristic 6-5 heterocycles we’ve come to know and love from your labs only with a few twists.

There’s a fair amount of diversity to be respected in this patent, and Kinasepro won’t do it justice with just a 30Kb jpeg, but I see three things of note which I’ll post here as representative examples. Looking over their examples it appears they look at most are the various permutations of A, B, and C.

Compounds like A are Kinasepro’s favorite. I can’t seem to find any relevant PDBs to compare with, but BMS has described the binding mode of these 5-6s in the past to be quite similar to the Tarceva/Iressa style 6-6 quinazolines.


2 Responses to “US20060211695”

  1. […] So what came upon the Kinasepro to rouse him from his slumber was a J. Med. Chem. like a cup-a-joe in the morning.  A french roast as it were ~ You see , I’ve inadvertantly attributed the novelty of accessing the ribose binding region off of the quinazoline 5 position to BMS (here and here).  For Shame! AstraZeneca in France has quite clearly been at this for a while, and in ASAP today they’ve reported a fair amount about their SRC / ABL candidate: AZD0530. […]

  2. […] **Hmm… Maybe brand-name is all part of the business model… Kinasepro’s Japanese is worse then his German, but your name popping onto his radar obviated a little digging. So it seems that for a while Kirin has been trying to put the Tarceva/Iressa-like quinazoline core onto kinase active lipophillic groups. In fact Kinasepro’s left eyebrow raise noticeably as he came upone a Kirin patent of what appears to show the first application exemplifying a kinase active acyl urea. High Five Man! Diaryl-ureas put the ‘ol KP to sleep, but show me something new like an acyl urea, and woohoo! The kinasepro is walking on air. (EGF; WO2003000660) Esai took the idea and ran with some Nexavar-Like followons (VEGF: WO2005082854 [a 600 pager]), and BMS picked up the structural fragment first in a series of PP1 analogs (US2005239820), and to their credit then applied the modification in a similar fasion to Esai and found c-Met activity with some pyridine compounds that too remind one of Nexavar (US2005245530). As per my earlier post, it appears that BMS has found some creative isosteres, namely that a pyridones fit (US20060211695) , and they’ve even patented a process route to get to the amides (US20050288289) suggesting a developement candidate can’t be far behind. So basically what Kinasepro sees here is Kirin stealing back what BMS stole first. Fair is fair after all. […]

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