The Thursday List

US20070149594 Raf Merck DE
US20070149572 FLT3 JnJ
US20070149561 Aurora GSK
US20070149560 Chk1 AstraZeneca
US20070149558 “Cytoprotection activity against…LY-294002” Takeda
US20070149548 Rho Alcon
US20070149546 erbB2 AstraZeneca
US20070149538 c-Kit Novartis
US20070149536 Akt Merck
US20070149535 EphB4 Oncalis
US20070149534 Trk BMS
US20070149533 Raf Millennium
US20070149523 Aurora + 4SC
US20070149521 IGF-1R + Osi
US20070149519 Ikk-e GSK
US20070149508 Abl (T315I) Targegen
US20070149506 Jak BMS
US20070149484 Zentaris
US20070149481 NAD AG

WO/2007/073117
WO/2007/072158 Fak Pfizer
WO/2007/072153 PAK4 Pfizer
WO/2007/072017 Chroma Therapeutics
WO/2007/071963 AstraZeneca
WO/2007/071955 c-Fms AstraZeneca

PDB Update

2UZB CDK2 w/ Thiazolidinones Vernalis
2UZD
2UZE
2UZL
2UZN
2UZO
2V0D; Some other thiazolidinones… even more

2J0J FAK Harvard, Cell, 129, 1177
2J0L

2PVR CK2 J.Mol.Biol.

2Q0N Pak4 [SGC]

KP Tech

RSS.  Quit clicking your bookmarks and go get an RSS aggregator.  Don’t ask me how or why you just go figure it out. If C-Lo can check 600 blogs every damn day (thanks for the j/k tip), you could easily hit 50 journals.  No I’m not kidding, if your relying on lifting stacks of paper bound by glue for inspiration then your only using 10% of your brain!  Oh and Elsevier subscription only RSS sux.  Plz fix ktx.

The journals I pretend to read are sindicated in the sidebar,  here, and of course there’s a feed .

Smiles. Today smiles are here to copy and paste structures from the web, period. So Sorry.  If your not using firefox, umm start using firefox.  Yes even at work – there’s a portable app.  If you’re already on FF then you can right click an image -> click properties -> alt text: copy the smiles and paste into chemdraw, isis, etc.

Searching. I search the USPTO here (leave off the US in the number its updated ~6am est Thursday), and the WIPO here (updated thursdays when they get around to it), the PDB here (updated Tuesday, usually around 4pm est [advanced search->Ligand->smiles 4tw]) the US clinic here, and EU clinic here.

ABT-869

Phase 2 on the doorstep, Genentech and Abbott just announced a collaboration to include development of the compound w/ backups. No terms disclosed…

Vegf, Flt3, Tie2, c-FMS, Pdgf, c-kit yadda yadda

j med chem, blood, molec cancer ther., WO/2004/113304

Novartis ‘n’ PKC

PKC412 (Midostaurin)?

So staurosporine analogs are old news? Novartis has a 1 compound PKC application.

US20070142401 / WO/2005/039549

A-[CEP-701]

So, what’s Abbott doing making solid forms of Lestaurtinib?

WO/2007/070444, US20070135628, US20070135401

Oh, and CC pointed out that CEP-701 / lestaurtinib is claimed to be in Ph3 trials for AML, so add that one to the list, I guess. I can’t find the trial in the US or EU databases, so may be in Asia?

The Thursday List

US20070142412 p38 pfizer
US20070142413 Trk AZ
US20070142414 Cdk Pharmacia Italia
US20070142415 Cdk Pharmacia Italia
US20070142417 IKK-b Aventis
US20070142429 Gprk Aerie
US20070142437 Vegf CDK2 CDK4 GSK
US20070142440 Vegf Tie2 Raf Merck DE
US20070142454 CK1-e Sanofi-Aventis
US20070142476 P38 GSK
US20070142409 Tau Mitsubishi
US20070142408 alk-5 Millenium
US20070142405 p38 Novartis
US20070142402 Jak/Axl/Syk Rigel
US20070142401 PKC etc Novartis
US20070142390 c-kit, bcr-abl, FGFR3 and/or Flt-3 AB Science
US20070142388 AKT Merck
US20070142372 p38 GSK
US20070142371 p38 Bhoeringer
US20070142368 Aurora Enmd
US20070142366 Jnk Eisai
US20070142334 ZAP70 or P38 ? Vertex
US20070142305 Pdgfr-b JnJ

WO/2007/070872 Rigel
WO/2007/070514 JAK Incyte
WO/2007/070444 Lestaurtinib Abbott
WO/2007/068473 Pi3k Novartis
WO/2007/068619 Nerviano
WO/2007/068637 Nerviano
WO/2007/068728 Pfizer IT
WO/2007/070398 Erk Schering
WO/2007/070319 Wyeth
WO/2007/068894 Astra
WO/2007/068465 Roche

KX2-391

Kinex filed an IND today for this ‘ere compound:

KX-01, KX2-391, ALB-30350, wait, ALB-30350? yah…

from WO/2006/071960:

Note that KX2-391 has weak activity against isolated kinases because the peptide binding site is not well formed outside of cells (a close analog, KX2-394 is a little more potent against isolated Src [KP note: 394 is the piperazine]), but have very potent activity inside whole cells. Without wishing to be bound by theory, it is thought that the difference in activity is attributed to the fact that the peptide binding site is now fully formed in cells due to the allosteric effects of the binding protein partners in the multi-protein signaling complexes, relative to isolated kinase assays.

PDB Update

2DS1: CDK2 + macrocycle: BMCL
2HXL: Chk1 + indole-indazole
2HXQ: Chk1 + indole-quinolone
2HY0: Chk1 + indole-quinolone
2P33: Jnk + novel aminopyrimidine
2PE2: PDK1 + indolinone

I don’t know’s on third

Because? oh he’s centerfield…

So TM asked for it, and while most of these are scatterred about the site… It’s not such a bad idea to have all the not-yet-approved kinase inhibitors currently active in US phase three clinical trials here in one place:

In a maybe-not-so-chronoligical order: Arxxant, Enzastaurin, Recentin, Zactima, Axitinib, Motesanib, CP-690,550, Pazopanib, and Tasigna.

Missing any?