KinasePro

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

Archive for the ‘EGF’ Category

AV-412

Posted by kinasepro on April 13, 2009

Aveo’s Ph1 irreversible  Erbb inhibitor:

C=CC(NC1=CC2=C(N=CN=C2C=C1C#CC(C)(C)N3CCN(CC3)C)NC4=CC=C(C(Cl)=C4)F)=O

via Mitsubishi

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Posted in EGF | 2 Comments »

AEE-788

Posted by kinasepro on March 16, 2009

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

C[C@H](C1=CC=CC=C1)NC2=C3C(NC(C4=CC=C(C=C4)CN5CCN(CC5)CC)=C3)=NC=N2

Cancer Res

Posted in EGF, Novartis, VEGF | Leave a Comment »

WO/2008/124161

Posted by kinasepro on October 22, 2008

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

COC1=CC2=C(NC3=CC=C(Cl)C(Cl)=C3F)N=CN=C2C=C1OCC(C4)C[C@]5([H])[C@@]4([H])CN(C)C5

So thats XL-647 ?  I hadn’t heard.

Posted in EGF, Exelixis, pi3k | Leave a Comment »

PDB Update

Posted by kinasepro on December 5, 2007

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.

Posted in EGF | 1 Comment »

Bayer ‘n Egf

Posted by kinasepro on October 2, 2007

Set of covalent ErbB inhibitors from Bayer:

O=C(/C=C/CN(CC)C)N(CC3)CC2=C3C1=C(NC4=CC(C=CN5CC6=NC=CC=C6)=C5C=C4)N=CN=C1S2

WO/2007/109279

Posted in Bayer, EGF | 3 Comments »

BIBW-2992

Posted by kinasepro on September 7, 2007

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

O=C(/C=C/CN(C)C)NC3=CC2=C(N=CN=C2C=C3O[C@H]4COCC4)NC1=CC=C(C(Cl)=C1)F

>> update they’ve named it Tovok

Posted in BI, EGF, Phase III | 4 Comments »

More Her

Posted by kinasepro on August 21, 2007

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

COC1=CC=CC(NC2=NC=NN3C2=C(CN4C[C@@H](O)[C@H](N)CC4)C=C3)=C1

Posted in BMS, EGF | 2 Comments »

ARRY-380: an Array ErbB2 IND

Posted by kinasepro on August 4, 2007

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

 

CC1=CC(NC2=NC=NC3=CC=C(C4=CC=C(CNCCS(=O)(C)=O)O4)C=C32)=CC=C1OC5=CC6=NC=NN6C=C5

ARRY-380, a selective, orally-active ErbB-2 inhibitor, has shown efficacy and is well-tolerated in preclinical models of human cancer.

Posted in Array, EGF | 1 Comment »

Oximes from J&J

Posted by kinasepro on July 22, 2007

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

NC1=C(/C=N/OCCN2CCOCC2)C(NC3=CC(Cl)=C(OCC4=CC=CC=C4)C=C3)=NC=N1

< 2g/d plz

Posted in EGF, J&J | 6 Comments »

Zactima

Posted by kinasepro on June 19, 2007

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

CN1CCC(CC1)COC2=CC3=NC=NC(NC4=CC=C(C=C4F)Br)=C3C=C2OC

wiki, clinic, WO/2001/032651

Posted in Astra, EGF, Phase III, VEGF | 1 Comment »