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Archive for the ‘Exelixis’ Category

WO/2008/124161

Posted by kinasepro on October 22, 2008

Exel’s got Pi3K-a in combination: Reminds one of the XL-147 combo study.

COC1=CC2=C(NC3=CC=C(Cl)C(Cl)=C3F)N=CN=C2C=C1OCC(C4)C[C@]5([H])[C@@]4([H])CN(C)C5

So thats XL-647 ?  I hadn’t heard.

Posted in EGF, Exelixis, pi3k | Leave a Comment »

Piper Jaffray

Posted by kinasepro on December 3, 2007

…It’s an investor dog and pony show, and it was last week. Who was there?

Exelixis: George Scangos had this to say on Kinase selectivity:

We get a lot of questions about whether we think that less specific multi-targeted kinase inhibitors are better then more specific kinase inhibitors. I think there is no general answer to that question. Personal view is when your working on the outside of the cell inhibiting a single molecule leads to efficacy, but the efficacy is limited and you can greatly increase the potency by hitting multiple targets at the same time without increasing the toxicity significantly, and I think there is plenty of clinical data now to show that that’s true.

On the other hand when your working downstream inside the cell in the biochemical pathway I think its important to be very specific and so we have a number of other compounds that work downstream within those pathways that are very specific so we tailor the compounds to what we think will optimize balance between efficacy and safety. We have some multi-targeted inhibitors we have some highly selective inhibitors, and we have some that hit a couple of targets.

They keep taunting us with bubble images of XL-880 and XL-184, So here have a guess:

FC1=CC=C(NC(C2(C(NC3=CC=C(OC4=C5C(NC=C5)=NC=N4)C(F)=C3)=O)CC2)=O)C=C1

There was also a bit on you should buy XL-647: its ‘More potent’, ‘More safe’ & ‘hits the T790M mutation’

Incyte: /Flexed on the impressive JAK inhibitor results they expect to tell you all about at ASH and beyond.

OSI: Now profitable with Tarceva, whose main competition interestingly enough is Alimta. It sounds like they are keeping OSI-906 for now, but OSI-930 and OSI-632 seem to be for sale.

Infinity: was there dropping some knowledge on the chaperoneness of HSP90 as it relates to kinase inhibitors and resistance.

Posted in biotech, Exelixis, OSI | 2 Comments »

WO/2007/089768

Posted by kinasepro on August 14, 2007

27 Authors, 586 pages, a whole bunch of examples, and 20 MB of Jak-2 goodness.

O=C(C)NC(C=C1)=CC=C1C2=NC(NC3=CC=C(N4CCOCC4)C=C3)=NC=C2

Seems likely that XL-019 came out of this series.

Posted in Exelixis, JAK | 1 Comment »

XL-019 = #14

Posted by kinasepro on May 24, 2007

IND application in the books.

First JAK2 inhibitor in development?

Posted in Exelixis, IND, JAK | 8 Comments »

EXEL & CK2

Posted by kinasepro on April 30, 2007

And then theres those 3 applications on CK2 from Exelixis WO/2007/048064, WO/2007/048065, & WO/2007/048066… The latter two with and / or Pim1 & 2 inhibition.

O=C1C=C(C2=CC(C)=C(O)C=C2)C=C(C3=CC=C(C(NCCN(CC)CC)=O)C=C3)N1

Seems plausible that CK2 could be one of the ‘undisclosed’ targets of the BMS collaboration.

Posted in CK2, Exelixis | Leave a Comment »

XL-765

Posted by kinasepro on April 25, 2007

mTOR / Pi3k inhibitor IND application reported today. XL-147 is their other one, and three pi3k applications published last Thursday. WO/2007/044698, WO/2007/044729, WO/2007/044813

Till Nature disables hotlinking: here’s who’s got what from here.

Posted in Exelixis, pi3k | 2 Comments »

XL-518

Posted by kinasepro on April 19, 2007

My guess is XL-518 is in WO/2007/044515.

O=C(C1=CC=C(C(F)=C1NC2=CC=C(C=C2F)I)F)N3CC(O)([C@H]4NCCCC4)C3

362 examples, 15 inventors.

IND beating first app is unusual. kudos.
Read the rest of this entry »

Posted in Exelixis, Genentech, MEK | 4 Comments »

XL147

Posted by kinasepro on March 18, 2007

>> 3 Exelixis Pi3K applications published 4/19/07

Exelixis filed an IND application for XL147, a PI3k inhibitor, the other day. Here’s another one where its not obvious which series its likely from.

Posted in Exelixis, pi3k | 3 Comments »

XL418

Posted by kinasepro on January 31, 2007

IND in the books.

Looking something like: WO/2005/117909 WO/2006/071819

CC1=C(CCCN2CCCC2)C=C(Cl)C=C1N3CCN(C4=C5C(NN=C5Br)=NC=N4)CC3

Posted in AKT, Exelixis | 4 Comments »

XL518

Posted by kinasepro on January 4, 2007

>> update >>   An Exelixis Mek application WO/2007/044515 published 4/19/07

So did the IND and deal actually beat the patent application? Either that or I’m missing something, because I can’t find it.

“XL518 is the second Exelixis compound designed to inhibit the RAS/RAF/MEK/ERK pathway with high potency and specificity, and the first to specifically target MEK,”

They’ve got an interesting RAF application in the stable, but I was under the impression that was the one to house the XL281 series.

hat tip: Xcovery, but of course.

Posted in Deals, Exelixis, Genentech, MEK | 2 Comments »