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


Posted by kinasepro on October 12, 2006

Hello Kirin Brewing Company,

**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 putting the Tarceva/Iressa-like quinazoline core onto kinase active lipophillic groups. But what made Kinasepro’s left eyebrow raise noticeably was when he came upone a Kirin patent application exemplifying the first use of a kinase active acyl urea.  High Five Man! Diaryl-ureas put the ‘ol KP to sleep you know, 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 was quick to pick 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 to find c-Met activity with some pyridine compounds that too remind one of Nexavar (US2005245530). As per an earlier post, it appears that BMS has found some creative isosteres, namely that 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.

Basically what Kinasepro sees here is Kirin stealing back what BMS stole first. Hey man, fair is fair..

Domo Arigato

3 Responses to “WO2006104161”

  1. JC said

    LOVE your new site. I’m a kinase med chem jockey by trade (for 6 yrs now and counting! we’ll see into the future who knows)

    I’m big into SYK & JAK.

    Good luck with your site; so far so good!

  2. Kinasepro said

    Indeed, indeed, so far so good.

    As may be apparent. Kinasepro is having trouble with Chemdraw. At work he has chemdraw 10 which makes nice, uniform, pretty pictures with excellent font sizes and nice looking bonds.

    When the KinasePro don’s his cape, boots, and mask however there is only chemdraw 6 to be found, from which the images leave something to be desired.

    Thanks for sticking it out as works towards ironing out some of the details.

  3. RK said

    KS, I have a solution for you if you like. Email me at “azulene at gmail dot com”

    Awsome site by the way. It nice to have someone covering all this kinase madness.

Leave a Reply

Fill in your details below or click an icon to log in: Logo

You are commenting using your account. Log Out / Change )

Twitter picture

You are commenting using your Twitter account. Log Out / Change )

Facebook photo

You are commenting using your Facebook account. Log Out / Change )

Google+ photo

You are commenting using your Google+ account. Log Out / Change )

Connecting to %s

%d bloggers like this: