KinasePro

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

Archive for July, 2007

A Gleevec Cartoon?

Posted by kinasepro on July 13, 2007

Bangup Job

Posted in gleevec | 2 Comments »

TargaGen closes…

Posted by kinasepro on July 13, 2007

Closes a 40M series D that is. Kudos Pros. Some of the more recent thiazole apps like US20070161645 appear to my eye to be the Src/Abl backup brigade.

CC1=NC(NC2=NC=C(/C=C/C3=CC(O)=CC=C3)S2)=CC(N4CCNCC4)=N1

wt Abl 1.5 nM
T315I 18 nM

So you like pictures?

Read the rest of this entry »

Posted in bcr abl, biotech, SRC | 2 Comments »

The Thursday List

Posted by kinasepro on July 12, 2007

WO/2007/079445 Aurora (constructs) Sunesis
WO/2007/079164 Vegf+ Abbott
WO/2007/078113 SK Corp
WO/2007/078034 c-Kit Amorepacific
WO/2007/077949 Jak3 Astellas
WO/2007/077574 p38 Cadila Healthcare
WO/2007/077435 multi Astex

US20070161704 Abl [IN]
US20070161684 p38 GSK
US20070161680 Raf Novartis (Chiron)
US20070161677 Raf Merck De
US20070161673 p38 GSK
US20070161666 Jak Pfizer
US20070161662 Bayer
US20070161651 Tie2 Exelixis
US20070161649 p38
US20070161648 Aurora JnJ
US20070161645 Abl TargeGen
US20070161635
US20070161632 Egf Novartis
US20070161615 CDK2 AstraZeneca

Posted in Application List | Leave a Comment »

K-252a

Posted by kinasepro on July 11, 2007

This week’s pdb update was a little light on inhibitors so here’s a shot of K-252a bound to c-Met: 1R0P: PNAS

Other c-met structures: 2G15, 1R1W.

Posted in c-Met | Leave a Comment »

PDB Update

Posted by kinasepro on July 10, 2007

2JII VRK3 – Apo SGC

Posted in PDB | Leave a Comment »

WO/2007/075567

Posted by kinasepro on July 7, 2007

A reader comment got me to take a closer look at the titled JnJ application.¬† I don’t see it making their blog, but given its similarity to a recent a Vertex application of course it’s going to make this one.

FC(C1=CC(C=CC=N2)=C2C=C1)(F)C3=NN=C4N3N=C(C5=CN(C)N=C5)C=C4

1 nM autophos

 regression @ 25 mg / kg ?  Them some lucky mice.

clogp= 1.28 MW=377

Yah, I’d say your compounds are getting jealous right about now.

Posted in c-Met, J&J, Janssen | 16 Comments »

More kinase-blogging…

Posted by kinasepro on July 6, 2007

…over at Het.Chem. Check 2uv2 for the binding mode. WO/2007/071348

CC1=CC(NC2=NC(SC3=CC=CC=C3F)=C4C=CC(OC)=CC4=C2)=NN1

(Rumors of my imperfection are greatly exaggerated.)

Posted in Aurora, Roche | Leave a Comment »

The Thursday List

Posted by kinasepro on July 5, 2007

WO/2007/075896 p38 Kemia

WO/2007/076474 Raf Kalypsys
WO/2007/076473 Raf Kalypsys
WO/2007/076460 Raf Kalypsys
WO/2007/076360 Rho Alcon
WO/2007/076348 Aurora GSK
WO/2007/076286 IKK GSK
WO/2007/076247 PKC BI
WO/2007/076245 AZ/Array
WO/2007/076127 TGF Biogen
WO/2007/076086 TGF Biogen
WO/2007/076092 Raf Amgen
WO/2007/076087 Prolexys
WO/2007/076085 Prolexys
WO/2007/076228 ITK BI
WO/2007/076320 PKB GSK
WO/2007/076423 AKT GSK
WO/2007/075896 Kemia
WO/2007/075869 Vegf+ Ariad
WO/2007/075650 Bayer
WO/2007/075567 c-Met Jannsen
WO/2007/075783 Wyeth
WO/2007/075847 Glukokinase Takeda
WO/2007/075307 Lestaurtinib Abbott

US20070155817 PKC Novartis
US20070155816 CDK (KR)
US20070155807 [U]
US20070155794 Tec Vertex
US20070155735 Sanofi-Aventis
US20070155746 Raf Kalypsys
US20070155751 CDK S-P
US20070155764 Raf Kalypsys
US20070155776 Abbott
US20070155777 IRAK / IKK Amgen
US20070154576 ‘hops and Acacia’ Metagenics
US20070154428 alk5 Taisho Pharm

Posted in Application List | 2 Comments »

RAF a la MLNM

Posted by kinasepro on July 4, 2007

US20070149533 is a Raf app from Millennium. I see it as a napthalene – amide cousin to the Birb and Nexavar style ureas. Amgen’s been in the area but not right on top.

O=C(CCN1CCN(C)CC1)NC2=NC=CC(OC3=CC(C=CC(C(NC4=CC(C(C)(C)C)=CC=C4)=O)=C5)=C5C=C3)=C2

Good thing too, b/c you know, I was’t really feeling the whole ‘hydrocinnamides’ thing in US20060160803

Posted in Millenium, RAF | Leave a Comment »

Happy Independance Day

Posted by kinasepro on July 4, 2007

Posted in General Interest | Leave a Comment »

 
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