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Archive for the ‘pi3k’ Category

AZ’s got PI3K

Posted by kinasepro on July 30, 2009

O=C(O)C1=CC=CC=C1N[C@@H](C2=CC(C)=CN(C2=NC(N3CCOCC3)=C4)C4=O)Caz-pi3k-table

WO/2009/093972 reminds you of…

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Posted in Astra, pi3k | 3 Comments »

Pi3k @ Bayer

Posted by kinasepro on July 25, 2009

This one hones in on the sulphonamides: (from the former site in CT)O=C(C1=CC=CN=C1)NC2=NC3=C(OC)C(OCCOCCNS(C)(=O)=O)=CC=C3C4=NCCN24

WO/2009/091550; They stuck morpholines out there previously: WO/2008/070150

Posted in Bayer, pi3k | 1 Comment »

Best place to hide a PI3K review?

Posted by kinasepro on January 7, 2009

Somewhere like Biochimica et Biophysica Acta sure would do the trick.

You could also try and bury one somewhere over here or there too…

The BPA one’s good!  Go check it out, thanks VC for the tip.

>> And another one >>  Mol Cancer Ther now in on the act.

Posted in pi3k | 1 Comment »

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 »

US20080255162

Posted by kinasepro on October 22, 2008

Pfizer’s got PI3K:

O=C(C1=CC(NC2=NC(C)=C(C=CC(N3C4CCCCC4)=O)C3=N2)=CN1C)O

previously:

Posted in Pfizer, pi3k | Leave a Comment »

Plethora ‘o’ PDB’s

Posted by kinasepro on October 14, 2008

GSK’s AKT stuff: 3d0e, 3E8D, 3E87, 3E88; J Med Chem, KP

SGX: Jak2 3E64, 3E63, 3E62, BMCL

Shokat: SRC, SRC, SRC, SRC, PI3K-Gamma, PI3K-Gamma

reminds me of OSI-906 or vice versa

Astrazeneca: CDK2 BMCL: 2W05

Amgen: P38 J Med Chem; 3DT1

LCK: 2ZM4, 2ZM1

Posted in AKT, CDK2, JAK, Lck, p38, PDB, pi3k | Leave a Comment »

A new PI3K PDB

Posted by kinasepro on September 2, 2008

UCB published they’re spin on LY-294002: 3DPD: BMCL

see also: 1E7V

Posted in biotech, PDB, pi3k | 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 »

PX-866

Posted by kinasepro on April 17, 2007

PX-866 is a Wortmannin analog that came to Biomira as part of the Prolx deal.

O=C1/C(C([C@]2(C)[C@@H](COC)O1)=C(O)C(C3=C2[C@H](OC(C)=O)C[C@@]4(C)[C@@]3([H])CCC4=O)=O)=C/N(CC=C)CC=C

You synthetic junkies should recognize at least one of the names on the patent app. Appears to be a simple improvement to the michael acceptor.

1E7U shows the natural product covalently bound to Pi3k

O=C1C2=COC3=C2[C@](C([C@H](OC(C)=O)C[C@]45C)=C([C@@]5([H])CCC4=O)C3=O)(C)[C@@H](COC)O1

Posted in biotech, pi3k | Leave a Comment »

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 »