This PDB entry confirms the structure.
as always, being 18 months behind the times put you 6 months ahead of the curve.
Archive for the ‘MEK’ Category
RDEA-119
Posted by kinasepro on September 1, 2009
Posted in MEK | 3 Comments »
RDEA-119
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.
“Ardea will grant Bayer a worldwide, exclusive license to develop and commercialize Ardea’s MEK inhibitors for all indications”
Posted in Bayer, MEK | 1 Comment »
AS-703026
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.
CO](http://kinasepro.files.wordpress.com/2009/04/as-703026r.jpg "as-703026r")
Posted in MEK, Merck DE | 5 Comments »
CH-4987655
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:
Posted in Array, Astra, MEK | 2 Comments »
C)N2C([C@@H]([C@@]3=CC=C(OCC(N4CCCC4)=O)C=C3)NC2=O)=O)=O)C(Cl)=C1](http://img530.imageshack.us/img530/2332/rmekaa4.jpg)
XL-518
Posted by kinasepro on April 19, 2007
My guess is XL-518 is in WO/2007/044515.
![O=C(C1=CC=C(C(F)=C1NC2=CC=C(C=C2F)I)F)N3CC(O)([C@H]4NCCCC4)C3](http://img80.imageshack.us/img80/9206/xl518dw9.jpg)
362 examples, 15 inventors.
IND beating first app is unusual. kudos.
Read the rest of this entry »
Posted in Exelixis, Genentech, MEK | 4 Comments »
XL518
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.
Posted in Array, biotech, Lexicon, MEK | 5 Comments »
