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

Archive for the ‘MEK’ Category

RDEA-119

Posted by kinasepro on September 1, 2009

This PDB entry confirms the structure.

RDEA-119

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

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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.

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 »

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.

O=C(C1=C(C=NC=C1)NC2=CC=C(C=C2F)I)NC[C@H](O)CO

via Ghost, & WO/2006/045514

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…

O=C(NOCCO)C1=C(NC2=CC=C(I)C=C2F)C(F)=C(F)C(CN3OCCCC3=O)=C1

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 »

WO/2007/96259

Posted by kinasepro on September 5, 2007

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

IC1=CC=C(NC([C@H](C(C)C)N2C([C@@H]([C@@]3=CC=C(OCC(N4CCCC4)=O)C=C3)NC2=O)=O)=O)C(Cl)=C1

 > hydroxamates?

Posted in MEK, Roche | Leave a Comment »

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

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.

Read the rest of this entry »

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

XL518

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 »