AV-412

Aveo’s Ph1 irreversible  Erbb inhibitor:

via Mitsubishi

AEE-788

aka: NVP-AEE788 is Novartis’ VEGF / EGF ‘Nib (&src, &flt, etc.) in Ph1 for the last 6 years… and unceremoniously off the pipeline.

Cancer Res

WO/2008/124161

Exel’s got Pi3K-a in combination: Reminds one of the XL-147 combo study.

So thats XL-647 ?  I hadn’t heard.

PDB Update

Berkeley’s got a Nature 2007, 450, 741 on a peptide that inhibits EGF 

and the PDB’s released yesterday: 2RFD 3.6 Å, 2RF9 3.5 Å, 2RFE 2.9 Å

To understand what they’re talking about I had to read the earlier piece in Cell.   You could probably just skip it because the Monkey Wrench breaks it down for you.

Bayer ‘n Egf

Set of covalent ErbB inhibitors from Bayer:

WO/2007/109279

BIBW-2992

BI’s irreversible ErbB inhibitor to join the Ph3 club.

>> update they’ve named it Tovok

More Her

‘nother ErbB 1,2,4 crystal forms app from BMS in US20070191375:

…

ARRY-380: an Array ErbB2 IND

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.

Oximes from J&J

So J&J has a BMCL describing the amino-pyrimidine-oxime moiety as quinazoline isostere, and a there’s a handful of other applications describing the motif.   Here’s a Lapatinib-esque example where they describe the EGF activity: WO/2007/081630

< 2g/d plz

Zactima

aka vandetanib, ZD-6474 is Astra’s Vegf / EGF doublet inhbitor.

wiki, clinic, WO/2001/032651