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

Archive for August, 2007

AZ’s GSK3 Indolinone

Posted by kinasepro on August 10, 2007

WO/2007/089192 is a use app, and WO/2007/089191 is salt forms application of the pictured GSK3 inhibitor originally from WO/2003/08285.  The YM-231146 / YM-359445 series bears similarity, albeit for Vegf.


The PDB used for alignment is 1UV5, and you can also check out AZ’s publicized interest in selective GSK3 inhibition in an ’03 JBC and 1q5k.

Posted in Astra, biotech, GSK3 | 2 Comments »

The Thursday List

Posted by kinasepro on August 9, 2007

WO/2007/90141 Raf GSK
WO/2007/89768 Jak2 Exelixis
WO/2007/88014 p38 Roche
WO/2007/89646 p38 Array
WO/2007/89192 Gsk3 AstraZeneca
WO/2007/89191 Gsk3 AstraZeneca

US20070185152 AKT GSK
US20070185140 Cdk Sanofi-Aventis
US20070185139 Egf J&J
US20070185133 plk1 Amgen
US20070185125 Tec Vertex
US20070185013 Chk1 ICOS
US20070185081 Egf BI
US20070185091 Egf BI
US20070185098 Flt3, KDR, Tie2, and p38 Locus
US20070185104 GSK3 ARS
US20070185111 Aurora Amgen
US20070185112 p38 Scios
US20070185123 HSC
US20070185134 cdk cyclacel
US20070185143 Aurora Nerviano
US20070185175 p38 BMS
US20070185171 vegf Amgen

Posted in Application List | 1 Comment »


Posted by kinasepro on August 9, 2007

The news today is that LS-104 is in Ph1 and now owned by Aegera from Lymphosign who in turn licsensed it from HSC. Their portfolio of patent applications suggests the compound is likely a tyrphostin derivative.

LS104 is a novel small molecule tyrosine kinase inhibitor of therapeutically significant kinases including Jak2 and Bcr-Abl…In contrast to marketed kinase inhibitor drugs, LS104 inhibits its targets in a non-ATP-competitive manner



I don’ t know about you but I needed a history lesson to get a handle on these

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

Pfizer updates pipeline…

Posted by kinasepro on August 7, 2007

…KP seen jotting notes…

What’s new:

PF-562,271 Fak Ph1
PF-3,814,735 Aur-2 Ph1
PF-477,736 Chk1 Ph1

hat tip: pharmalot.

Posted in Pfizer | Leave a Comment »

ARRY-380: an Array ErbB2 IND

Posted by kinasepro on August 4, 2007

IND: in the books, Market: not impressed. If you’ve been paying attention you already noticed Array’s got ‘n’ ErbB series published 5/24: WO/2007/059257



ARRY-380, a selective, orally-active ErbB-2 inhibitor, has shown efficacy and is well-tolerated in preclinical models of human cancer.

Posted in Array, EGF | 1 Comment »

Amgen ‘n Aurora

Posted by kinasepro on August 2, 2007

WO/2007/087276? How ’bout that.


Posted in Amgen, Aurora | 4 Comments »

The Thursday List

Posted by kinasepro on August 2, 2007

WO/2007/85188 Vegf+ Shanghai Hengrui
WO/2007/85205 Vegf+ Shanghai Hengrui
WO/2007/85540 Syk GSK
WO/2007/85833 EphB4 AstraZeneca
WO/2007/85873 MARK Merck
WO/2007/86943 PI3K Beth Isreal
WO/2007/87026 AMG-706 Amgen
WO/2007/87068 Btk/Lck Pharmacyclics
WO/2007/87245 VX-680 / Ret  Merck / Vertex (43 nM)
WO/2007/87246 VX-680 /Jak2 Merck / Vertex
WO/2007/87276 Aurora Amgen
WO/2007/87283 Plk1 Vertex
WO/2007/87419 Allergan

US20070178573 Tak1 xray Vertex
US20070179118 cdk4 Pfizer (WL)
US20070179125 Aurora Vertex
US20070179127 Rho Asahi Kasei
US20070179130 c-Met, KDR, and flt-3
US20070179130 c-Met Exelixis
US20070179133 Aurora Vertex
US20070179140 Aurora Rigel
US20070179144 hYAK3 GSK
US20070179151 Aurora Roche
US20070179156 Tec Vertex
US20070179161 CDK2 + Vernalis
US20070179177 PLK1 Vertex

Posted in Application List | Leave a Comment »