KinasePro

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Archive for April, 2007

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.

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Posted in CK2, Exelixis | Leave a Comment »

ARQ-197

Posted by kinasepro on April 27, 2007

Hard to spit in the sink at ‘30 million for the Asian rights‘ to a ph1 compound…

O=C(NC1=O)[C@](C2=CNC3=C2C=CC=C3)([H])[C@@]1([H])C4=CN5C6=C4C=CC=C6CCC5

WO/2006/086484

Posted in c-Met, Deals | Leave a Comment »

The Thursday List

Posted by kinasepro on April 27, 2007

US20070093537 p38 BMS
US20070093532 Raf Merck DE
US20070093516 Lyn
US20070093513 Rho Senju
US20070093512 egf GSK
US20070093506 Novartis
US20070093491 ?
US20070093446
US20070093480 IGF1R+ Sanofi Aventis
US20070093488 Aurora/CDK Sanofi Aventis
US20070093490 PCK / Alk
WO/2007/046426 ATR NIIGATA
WO/2007/047646 Aurora Janssen
WO/2007/048064 CK2 Exelixis
WO/2007/048065 CK2 Exelixis
WO/2007/048066 CK2 Exelixis
WO/2007/048070 Amgen
WO/2007/048088 Flt3 Janssen

Posted in Application List | 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 »

PDB Update

Posted by kinasepro on April 24, 2007

>> Update >> Biochemistry article on the Plk1 structure.

Woohoo! First published kinase domain Plk1 structures from Pfizer:

2OWB Plk1 w/ pyrrolopyrazole inhibitor
2OU7 Plk1 w/ ANP

and a Chk1 structure from Merck: 2HOG; BMCL

Posted in Chk1, PDB, Plk1 | 4 Comments »

Takeda w/ more-a Aurora

Posted by kinasepro on April 23, 2007

Takeda has been looking at compounds similar to vx-680 for a while now, and the same group now has WO/2007/044779. The pretty colors give an idea whats going on, but frankly we all suck at drawing squishy things… for now your stuck with pymol!

CC1=CC2=C(NC3=C2C(C4=CC=CC(S(=O)(CC)=O)=C4)=CC(C(NCCN5CCCC5)=O)=C3C)N=C1

2BFY shows a sulfonamide down thereabout in Aurora-B.

Posted in Aurora, Takeda | Leave a Comment »

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 »

The Thursday List

Posted by kinasepro on April 19, 2007

This here’s gonna make for a busy weekend.

US20070087393 ZAP-70 Assay…
US20070088019 Gsk3 &/or PKC J&J
US20070088031 Gsk3 GSK
US20070088033 p38 Pharmacia
US20070088037 TGFb Pfizer
US20070088041 Gsk3 Sanofi-aventis
US20070088044 EGFR AstraZeneca
US20070088051 Boehringer Ingelheim
US20070088080 Gsk3 Neuropharma

WO/2007/042298 Syk GSK
WO/2007/042299 Syk GSK
WO/2007/042321 AGC Devgen
WO/2007/042784 Cyclacel
WO/2007/042786 Cyclacel
WO/2007/042806 LIFCR +
WO/2007/042810 Astellas +
WO/2007/044050 IKK BMS
WO/2007/044084 Mek Array
WO/2007/044401 CDK Schering
WO/2007/044407 Schering
WO/2007/044410 Schering
WO/2007/044420 CDK Schering
WO/2007/044426 Schering
WO/2007/044441 Schering
WO/2007/044449 Schering
WO/2007/044515 Mek Exelixis
WO/2007/044698 PI3Kα Exelixis
WO/2007/044724 Pim1 Exelixis
WO/2007/044729 PI3K Exelixis
WO/2007/044779 Takeda
WO/2007/044813 PI3Kα Exelixis
WO/2007/044932 Methods… ActiveSite

Posted in Application List | Leave a Comment »

Kinase PDBs

Posted by kinasepro on April 19, 2007

Here’s an interestingly derived big list of kinase structures in the PDB. I guess the answer is 112.

Posted in PDB | 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 »