KinasePro

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

Archive for May, 2007

Peer-Review is Over-Rated

Posted by kinasepro on May 31, 2007

Putting a kinase domain on the cover is going to get a little attention, but putting this in the abstract is like sending an invitation to amateur hour:

…The success of recent launches of protein kinase inhibitors (Gleevec, Imatinib, Sutent, Iressa, Nexavar, Sprycel) gave another push to this field…

Gleevec is imatinib, I think they ment Tarceva. They missed Tykerb, and yeh they submitted the manuscript before Tyk’s approval, but this very fact outmodes the entry before its even published 😦 They also mispell sprycell in table 1. I could go on, but I’m sort of on the fence whether I like the paper or not. Read it yourself and you decide.

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Posted in General Interest | Leave a Comment »

Biogen’s new stuff

Posted by kinasepro on May 30, 2007

So what is going on with TGF-β anyhow. GSK WO/2002/062794 , Lilly WO/2002/094833, WO/2004/050659, & WO/2005/092894, Biogen WO/2004/072033, and Pfizer (WL) WO/2004/026306 have all been playing in the pyrazole / TGF sandbox but all I’ve seen is some pretty pictures and a few J. Med Chem.’s

Biogen’s got a new one with WO/2007/059359, but not a single mention in during “R&D day.” 😦 Its either supersekrit, or DOA.

O=C1N(C)N(C)C(C2=CC3=NC=CN=C3C=C2)=C1C4=CC=CC(S(=O)(N)=O)=C4

Posted in Biogen, Tgf-b | Leave a Comment »

SGC in DDT

Posted by kinasepro on May 30, 2007

The PDB is kind of light this week – but if the letters SGC mean anything to you then don’t miss this kinase review in Drug Discovery Today.

Posted in General Interest, SGC | Leave a Comment »

E7080

Posted by kinasepro on May 29, 2007

O=C(C1=CC2=C(OC3=CC=C(NC(NC4CC4)=O)C(Cl)=C3)C=CN=C2C=C1OC)N

US20070117842 is a polymorph application, and there’s been a fair amount of IP activity around the compound. Indications are its E7080: an oral PhI Vegf, FGF, Pdgf, C-Kit, etc compound which first touched down in WO/2004/080462.

Posted in c-Kit, Eisai, Fgf, PDGFR, VEGF | 2 Comments »

Lestaurtinib

Posted by kinasepro on May 28, 2007

O=C1NCC2=C1C3=C4N([C@H]5C[C@](O)([C@](C)(N6C4=C2C7=C6C=CC=C7)O5)CO)C8=C3C=CC=C8

Lestaurtinib / CEP-701 is currently in trials for a handful of indications and first appeared in WO/1988/07045 (US,4,923,986) via Kyowa Hakko Kogyo. The series was first described as a group of PKC inhibitors, but later came this ’98 press release: (emphasis mine)

CEP-701 is one of a series of specific receptor trk kinase inhibitor derived from the indolocarbazole K252a, which was originally synthesized by Kyowa Hakko Kogyo Co., Ltd., Tokyo, Japan

Read the rest of this entry »

Posted in c-Met, Cephalon, Flt3, JAK, Trk, VEGF | 3 Comments »

The Thursday List

Posted by kinasepro on May 24, 2007

US20070117800 SGX
US20070117802 c-Met BMS
US20070117804 Schering Plough
US20070117808 Glucokinase JnJ
US20070117816 Takeda
US20070117817 Rho Bayer
US20070117818 hYAK3 GSK (Ibraki JP)
US20070117821 CDK Roche
US20070117833 mTOR Novartis
US20070117842 Esai
US20070117850 Tgfβ PFIZER
US20070117856 Kyowa Hakko Kogyo

WO/2007/059359 Tgfβ Biogen
WO/2007/059341 SGX
WO/2007/059299 Vertex
WO/2007/059257 Array
WO/2007/059219 VERTEX
WO/2007/059202 Bayer
WO/2007/059157 Genentech / Curis
WO/2007/058942 Schering Plough
WO/2007/058879 AKT GSK
WO/2007/058873 CDK Schering Plough
WO/2007/058852 AKT GSK
WO/2007/058850 AKT GSK
WO/2007/058832 Tec BI
WO/2007/057790 GSK3 Sanofia Aventis / Mitsubishi
WO/2007/057093 c-Met Merck DE
WO/2007/057092 c-Met Merck DE

Posted in Application List | Leave a Comment »

XL-019 = #14

Posted by kinasepro on May 24, 2007

IND application in the books.

First JAK2 inhibitor in development?

Posted in Exelixis, IND, JAK | 8 Comments »

PDB Update

Posted by kinasepro on May 23, 2007

2E2B, Abl + INNO-406 aka NS-187, BMCL, Nippon Shinyaku Co.
2JGZ
, CDK2 + CyclinB
2OZO, Zap 70 + ANP, UC Berkeley

Posted in PDB | Leave a Comment »

4SC: Aurora B

Posted by kinasepro on May 23, 2007

COC1=CC2=C(C=C1OCCCN3CCCC3)N=CN=C2NC4=NC=C(CCC(NC5=CC=C(F)C=C5)=O)S4

WO/2007/054357 is another example showing an isosteric relationship between pyrazoles and thiazoles.

Posted in Aurora, biotech | Leave a Comment »

The Kinaverse

Posted by kinasepro on May 22, 2007

Any idea where this is?

go on, take a guess… Read the rest of this entry »

Posted in General Interest | 10 Comments »