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

Archive for the ‘MEK’ Category


Posted by kinasepro on September 1, 2009

This PDB entry confirms the structure.


as always, being 18 months behind the times put you 6 months ahead of the curve.


Posted in MEK | 3 Comments »


Posted by kinasepro on April 29, 2009

Its Ardeas’s $35 million non-hydroxamate MEK inhibitor in Ph1.  The pictured structure is one of three claimed in the ‘combination w/ Nexavar’ app: WO/2009/018238.

rdeaArdea will grant Bayer a worldwide, exclusive license to develop and commercialize Ardea’s MEK inhibitors for all indications”

Posted in Bayer, MEK | 1 Comment »


Posted by kinasepro on April 24, 2009

>> Update – this structure has been revised from the butyl amide – This is (i believe) the correct structure >>

EMD-Serono’s got ‘a ph1 non-hydroxamate ‘ATP Collaborative’ Mek inhibitor.


via Ghost, & WO/2006/045514


Posted in MEK, Merck DE | 5 Comments »


Posted by kinasepro on April 23, 2009

Some have walked a country mile to get away from the hydroxamate, others think nothing of tacking ‘nother one on:  Its Chugai’s ‘ATP-Collaborative’  Ph1 MEK inhibitor: Ro-4987655 / CH-4987655.  More potent, stable, and soluble…


Reduced signs of hydrolysis to the inactive acid and no BBB penetration.(preclinically)


Posted in biotech, MEK, Roche | Leave a Comment »

ARRY-704 ?

Posted by kinasepro on October 23, 2008

aka ARRY-424704 / AZD-8330 is the Array / Astra Mek Ph1 backup to ARRY-886 / AZD-6244 which was put in a holding pattern when it didn’t meet a ph2 endpoint. The pictured strucuture is ‘Mek Inhibitor II’ in the combination app WO/2008/125820:O=C(C(C=C1C)=C(NC2=CC=C(I)C=C2F)N(C)C1=O)NOCCO


Posted in Array, Astra, MEK | 2 Comments »


Posted by kinasepro on September 5, 2007

Roche has a 2nd gen series of hydantoins as MEK inhibitors with WO/2007/96259:


 > hydroxamates?


Posted in MEK, Roche | Leave a Comment »


Posted by kinasepro on April 19, 2007

My guess is XL-518 is in WO/2007/044515.


362 examples, 15 inventors.

IND beating first app is unusual. kudos.
Read the rest of this entry »


Posted in Exelixis, Genentech, MEK | 4 Comments »


Posted by kinasepro on January 4, 2007

>> update >>   An Exelixis Mek application WO/2007/044515 published 4/19/07

So did the IND and deal actually beat the patent application? Either that or I’m missing something, because I can’t find it.

“XL518 is the second Exelixis compound designed to inhibit the RAS/RAF/MEK/ERK pathway with high potency and specificity, and the first to specifically target MEK,”

They’ve got an interesting RAF application in the stable, but I was under the impression that was the one to house the XL281 series.

hat tip: Xcovery, but of course.


Posted in Deals, Exelixis, Genentech, MEK | 2 Comments »

Better Chemistry = Better Drugs

Posted by kinasepro on December 29, 2006

Wull Duh? But in this case it’s a webcast on medchem from some mostly non-chemists: David Snitman, Paul Goddard, Arthur Sands, and Jim Mahoney of Array, ARYx, Lexicon, and Surface Logix respectively.

Read the rest of this entry »


Posted in Array, biotech, Lexicon, MEK | 5 Comments »


Posted by kinasepro on December 20, 2006

Exelixis is on fire these days. 518’s IND is in the books.


Posted in clinical, Exelixis, MEK | Leave a Comment »