KinasePro

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

Archive for March, 2007

The Thursday List

Posted by kinasepro on March 29, 2007

US20070072934 Vegf Scripps
US20070072932 Novartis (diabetes / use)
US20070072901 alk5 GSK
US20070072898 MAPKAP-K2 Teijin Pharma
US20070072896 c-Jun Esai
US20070072885 EGFR Pfizer
US20070072882 Cdk Schering-Plough
US20070072881 Cdk Schering-Plough
US20070072880 Cdk Schering-Plough
US20070072874 c-Met Sugen
US20070072866 Gsk-3 Sanofi-Aventis
US20070072862 Lck / c-Kit Amgen
US20070072851 Lck / Ack-1 Amgen

WO/2007/035428 c-Met BMS
WO/2007/035309 c-Met Merck
WO/2007/034143 EGFR Astra-Zeneca
WO/2007/034144 EGFR Astra-Zeneca

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Posted in Application List | Leave a Comment »

PDB Update

Posted by kinasepro on March 27, 2007

2GHG Abbott – Chk1 with A431994 (Akt inhibitor) BMCL ’06, 3424

O=C1NC2=C(C=C(C3=CC(OC[C@@H](N)CC4=CNC5=C4C=CC=C5)=CN=C3)C=C2)/C1=C/C6=CC=CN6

I haven’t read the article yet, but to my eye the PDB suggests a ligand conformation responsible for some off target activity. Abbott’s indole-aminoethoxides in last weeks update (2OH0, 2OJF) seem to be the more typical (potent?) conformation.

Posted in Abbott, PDB | 2 Comments »

Schering’s latest CDK stuff

Posted by kinasepro on March 27, 2007

Schering-Plough has a series of CDK inhibitors of which the latest installment is: US20070066621. Earlier app’s in this series appear as a combined effort via SP and PCOP, and Pharmacopeia has a press release suggesting that the collaboration has an oncology candidate in Ph1. Hrmph, No ph1 oncology trials via ScheringP in the US and the press on this stuff is a little thin.

NCC1=C(C2=CC=CC=C2Cl)C(C#N)=C(NCC3=CN=CC=C3)C4=NNC(Br)=C14

Vernalis described related series’ in Bioorg Med Chem Lett ’05, 863; 1Y8Y 1Y91 and Bioorg Med Chem Lett ’06, 1353; 2C68, 2C69, 2C6T, 2C6O, 2C6M, 2C6L, 2C6K, 2C6I

Posted in CDK2, Pharmacopeia, Schering-Plough | Leave a Comment »

The Thursday List

Posted by kinasepro on March 22, 2007

US20070066666 Plk GSK
US20070066660 Raf Merck DE
US20070066641 Ret and/or FGFR Plexxikon
US20070066633 Vegf AstraZeneca
US20070066632 Tgf-b Scios
US20070066621 CDK Schering-Plough
US20070066610 c-Met JnJ
US20070066606 Vegf+ Merck DE
US20070066660 Vegf+ Merck DE

WO/2007/033232 c-Fms JnJ
WO/2007/033196 c-Met BMS
WO/2007/033137 c-Fms JnJ
WO/2007/032936 CDK Schering Plough
WO/2007/032445 Kyowa Hakko Kogyo
WO/2007/031745 IGF-IR AstraZeneca
WO/2007/031739 Glukokinase AstraZeneca
WO/2007/031428 Raf Roche

Posted in Application List | 3 Comments »

PDB Update

Posted by kinasepro on March 20, 2007

Lots ‘o’ structures released this week.

2P2H Vegfr2 Amgen (J Med Chem)
2P2I Vegfr2

2OSC Tie2
2OO8 Tie2
2P4I Tie2

2GDO Chk1

2JBO MK2
2JBP MK2

2OIB IRAK4 Roche (J. Immunology)
2OIC IRAK4 Roche
2OID IRAK4 Roche

2OIQ SRC w/ Gleevec

2OH0 PKA Abbott (BMC)
2OJF PKA Abbott (related)

and 2UV2 is an update to 2JAO where I guess they forgot an atom in the ligand (benzonitrile 2JAO vs. benzylnitrile 2UV2)

Posted in biotech | 2 Comments »

Roche ‘n Raf

Posted by kinasepro on March 19, 2007

US20070060607 is ‘nother thienopyridine application from Roche. The listed in vitro assay uses c-Raf, but selectivity isn’t described.

O=C(C1=CN=C(N)C2=C1SC=C2COC3=C(C)C=CC(NC(C4=CC=C(Cl)C=C4)=O)=C3)NCCO

Posted in RAF, Roche | Leave a Comment »

The Thursday List

Posted by kinasepro on March 19, 2007

WO/2007/030680 Axl Rigel
WO/2007/030377 Novartis
WO/2007/030361 GSK
WO/2007/030359 PLK GSK
WO/2007/029107 IGF1R Analytecon
WO/2007/029106 IGF1R Analytecon
WO/2007/028445 Syk GSK

US20070060551 QLT
US20070060570 Takeda
US20070060572 p38 Vertex
US20070060577 cfms JnJ
US20070060578 cfms JnJ
US20070060582 raf Novartis
US20070060594 JNK or Gsk3 Applied Research Systems
US20070060616 JNK
US20070060607 Raf Roche
US20070060598 JNK
US20070060595 c-Jun

Posted in Application List | 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 »

SGC at it again

Posted by kinasepro on March 14, 2007

The remarkably prolific group at the SGC has released the coordinates of yet another kinase crystal structure: CAMK1: 2JAM

Posted in PDB | Leave a Comment »

Abbott: not done with P38 either

Posted by kinasepro on March 14, 2007

WO/2007/028051 is another p38 application suggesting that Abbott isn’t throwing in the towel just yet

CC(C)OC1=NC=CN2C1=NC(C3=CC=C(F)C=C3)=C2C4=CC=NC(NCC(C)(C)CO)=N4

Posted in Abbott, p38 | 3 Comments »