KinasePro

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

Archive for April, 2007

PDB Update

Posted by kinasepro on April 17, 2007

Abbott’s got an anilinopyrimidine bound to Jnk1 with 2No3; BMCL. Their other JNK1 structure is 2g01

Posted in Abbott, Jnk, PDB | Leave a Comment »

AACR

Posted by kinasepro on April 15, 2007

Don’t be jealous just because your not here. AACR ’07 has some webcasts too.

AMG-273 MultiKinase Amgen
AMG-706 Vegf Amgen
AMN-107 Abl Novartis
ARQ-197 selective c-Met Arqule
AS-703569 Aurora A Merck Serono
AT-7519 CDK Astex
AT-9283 Aurora A B / JAK2/Abl Astex
AV-412 EGFR Aveo
AZD-0530 src/abl AstraZeneca
AZD-1152 Aurora B AstraZeneca
AZD-2171 pan-VEGF AstraZeneca
AZD-6244 Mek1/2 Array / AZ
BMS-536924 IGF-IR BMS
BMS-582664 VEGF and FGF BMS
CE-245,677 Tie2 Pfizer
CGP-76030 Src Pfizer
CYC-202 CDK2,7,9 Cyclacel
GFB-204 Vegf Pdgf Tigris Pharma
GSK-461364 plk1 GSK
INNO-406 abl/lyn Innovive
Ki-23057 FGF Kirin
KX-O1 Src Kinex
LY-2401401   Lilly
LY-317615 PKC Lilly
MP-529 Aurora A Supergen
NVP-AEW541 IGF-IR Novartis
PD-0325901 Mek Pfizer
PF-2362376 c-Met Pfizer
PF-371,989 Tie2 Pfizer
PF-562,271 Fak Pfizer
PHA-739358 Aurora Nerviano
PHA-665752 c-Met Nerviano
PKC-412 PKC Novartis
PX-866 pi3k Biomira
SF-1126 pi3k Semafore
SGX-523 c-Met SGX pharma
SKI-606 Src/Abl Wyeth
SNS-314 Aurora A B Sunesis
TKI-258 multi-target’ Novartis
VX-680 Aurora Vertex / Merck
WP-1066 JAK2 Callisto
ZD-6474 Vegf/EGF AstraZeneca
ZK-261991 Vegf  
ZM-447439 Aurora AstraZeneca

Read the rest of this entry »

Posted in meetings | 2 Comments »

The Thursday List

Posted by kinasepro on April 12, 2007

US20070083044 CDK Chk Schering-Plough
US20070082906 Akt Merck
US20070082902 CDK Chk Schering-Plough
US20070082901 CDK Chk Schering-Plough
US20070082900 CDK Chk Schering-Plough
US20070082898 p38 Astex
US20070082884 Rsk (Covalent) UCSF
US20070082880 PKC theta Wyeth

WO/2007/041712 CDK Chk Schering-Plough
WO/2007/041379 Met BMS
WO/2007/041365 glucokinase Novartis
WO/2007/041358 Aurora Miikana
WO/2007/041195 AKT GSK3 Janssen
WO/2007/041130 Jak Vertex
WO/2007/040440 GSK3β AZ
WO/2007/040439 AZ
WO/2007/040438 AZ
WO/2007/040436 AZ
WO/2007/040208 p38 Ono
WO/2007/039285 Mk2 Novartis
WO/2007/039216 Novartis

Posted in Application List | 2 Comments »

PDB Update

Posted by kinasepro on April 11, 2007

>>  update: Amanda‘s already on the scene… and fascinated.

2OI4’s ‘nother one of them CP-Ruthenium/Stuarosporine things bound to PIM1

related: 2BZH, 2BZI, 2BZJ

Posted in PDB, pim1 | Leave a Comment »

‘Nother “Novel” VEGF candidate

Posted by kinasepro on April 10, 2007

BMS-582664 / Brivanib alaninate

WO/2007/038648 is a development ‘crystalline forms’ application from BMS.

CC(C(OC[C@@H](C)OC([C@@H](C)N)=O)=C1)=C2N1N=CN=C2OC3=C(F)C(C=C(C)N4)=C4C=C3

Discovery: WO/2004/009784. Process: WO/2006/130657. It’s a prodrug / isostere rip on AZD-2171 / Cediranib / Recentin; WO/2000/047212

Posted in BMS, VEGF | Leave a Comment »

Kinase Inhibitors: On the market

Posted by kinasepro on April 8, 2007

Nothing new to see here, but its about time I got around to it. Here are the currently approved small molecule kinase inhibitors, with a few quick facts and links for each. Xcovery’s got what they’re worth.
Tykerb® , Sprycel®, Sutent®, Nexavar®, Tarceva®, Iressa®, and of course Gleevec®.

Posted in Approved | 2 Comments »

Tykerb ®

Posted by kinasepro on April 8, 2007

Tykerb ®, lapatinib, GW-572016

ClC1=CC(NC2=NC=NC3=CC=C(C4=CC=C(CNCCS(=O)(C)=O)O4)C=C32)=CC=C1OCC5=CC(F)=CC=C5

Discovery: Glaxo UK: WO/1999/35146
US Approval: March 2007

wiki; fda; PDB: 1XKK; Nature Reviews Drug Discovery

Posted in Approved, GSK | Leave a Comment »

Sprycel ®

Posted by kinasepro on April 8, 2007

Sprycel ®, dasatinib, BMS-354825

CC1=NC(NC2=NC=C(C(NC3=C(Cl)C=CC=C3C)=O)S2)=CC(N4CCN(CCO)CC4)=N1

Discovery: Bristol-Myers Squibb WO/2000/062778
US Approval: June 2006

wiki; PDB: 2GQG; FDA; J Med Chem ’06 6819;

Named after its inventor?

Posted in Approved, BMS | Leave a Comment »

Sutent ®

Posted by kinasepro on April 8, 2007

Sutent ®, sunititnib malate, SU11248

O=C(C1=C(C)NC(/C=C2C(NC3=C/2C=C(F)C=C3)=O)=C1C)NCCN(CC)CC

Discovery: Sugen: Provisional filed February 15, 2000 WO/2001/060814. Sugen was bought by Pharmacia-Upjohn which in turn merged with Pfizer.
US Approval: January 2006

wiki; 557795-19-4

Posted in Approved, Pfizer | Leave a Comment »

Nexavar ®

Posted by kinasepro on April 8, 2007

Nexavar ®, sorafenib tosylate, BAY-439006

O=C(C1=NC=CC(OC2=CC=C(NC(NC3=CC=C(Cl)C(C(F)(F)F)=C3)=O)C=C2)=C1)NC

Discovery: Bayer WO/2000/042012
US Approval: December 2005

wiki; Org.Proc.Res.Dev. ’02, 777

PDB: 1UWH; 1UWJ; 2HZN

Posted in Approved, Bayer | Leave a Comment »