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

Archive for December, 2006

Wyeth gets Jak’d up!

Posted by kinasepro on December 30, 2006

via Jak3 but of course – in an underanounced deal with Pharmacopeia:

…Wyeth will pay Pharmacopeia $5 million initially, as much as $9 million of research funding over the next three years, and as much as $175 million for reaching certain goals with the JAK3 kinase inhibitor drug.

While it’s likely they have a few which haven’t published yet, WO/2006/108103 is the most recent PCOP Jak3 application.

O=C1NC2=C(N=C(N3C4=CC(F)=CC=C4N=C3)N=C2)N1[C@H]5CCC(C6=C5C=CC=C6)=O

They’ve been at this stuff for a while – I reckon since WO/2001/047921 and have a recent Tet Lett on a related series. Check 2HK5 for a clue on how they bind.

>> update 1/25/07 >> US20070021443 Jak3 Pharmacopeia patent application

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Posted in Deals, JAK, Pharmacopeia, Wyeth | 3 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 »

US20060293358

Posted by kinasepro on December 28, 2006

Merck MA‘s got Met

O=C1C2=CC(NC(C)C)=CC=C2C=CC3=NC=C(C4=CN(C)N=C4)C=C31

Posted in c-Met, Merck & Co. | Leave a Comment »

The Thursday List

Posted by kinasepro on December 28, 2006

US20060293358 Met Merck
US20060293348 p38 GSK
US20060293340 Raf Novartis
US20060293342 Tie2 EXEL
US20060293311 Jak3 Rigel
US20060292681 Interdomain kinase inhibitors
WO/2006/137598 c-Jun Sumitomo
WO/2006/136837 AKT Astex
WO/2006/136402 Mnk Develogen

Posted in Application List | Leave a Comment »

Tykerb + Xeloda 4TW

Posted by kinasepro on December 27, 2006

Good news for Tykerb and GSK.

Xeloda + Avastin ph ii was reported earlier this month.

Posted in EGF, GSK | Leave a Comment »

PDB Update

Posted by kinasepro on December 26, 2006

2NP8: Aurora Kinase. Novartis has a series of these kinds of compounds described in: JACS ’06 – 2182, but its looking like this came out of Takeda, and the companion article to this xray is in the ‘to be published’ category. Only other Aurora relevant Xray is a mutant: 2C6E, and of course the Abl mutant with VX680: 2F4J.

O=C(C1CC1)NC2=CC(NC3=NC(NC4=CC=CC(C(F)(F)F)=C4)=CC=N3)=CC=C2

Interesting, looks that there’s a lysine residue on the glycine rich loop which is fairly specific to Aurora and appears to hydrogen bond the trifluromethyl group. Else these look to be in a similar conformation to the Rigel pyrimidines.

Also new today: 2FGA; Chk1 Apo: Bioorg Med Chem Lett ’06 – 2293 Peculiar, this is a low resolution apo with identity to the much earlier high resolution Chk1 apo: 1IA8.

Posted in Aurora, Chk1, PDB | Leave a Comment »

WO2006135604

Posted by kinasepro on December 26, 2006

WO2006135604 is a recent Chk1 offering via Merck.

O=C(NCC(F)(F)F)C1=CN=CC(C2=CN=C(NC3=NC=NC(N4CCC(F)(F)CC4)=C3C)S2)=C1

Posted in Chk1, Merck & Co. | Leave a Comment »

ENMD-981693

Posted by kinasepro on December 26, 2006

Entremed has an ‘Aurora A selective’ preclinical candidate ENMD-981693, which is likely MKC-1693 or closely related. Here’s a poster given earlier this month. The structure has not been divulged, but the compound most likely came from the purchase of Miikana’s IP. There’s only one Miikana publication on Aurora and its the patent application: WO2006055831 which comprise a series of amides (and esters):

NC1=C(C(NCCN(C)C)=O)N=C(SC2=CC=C(NC(C3CC3)=O)C=C2)N=C1NC4=NNC(C)=C4
look familar?

So lets review:

  VX680 (nM) ENMD-981693 (nM)
Aurora A 0.6 15
Aurora B 18 290
Aurora C 4

Read the rest of this entry »

Posted in Aurora | 3 Comments »

New Greene

Posted by kinasepro on December 24, 2006

1082 pages? Drats, didn’t make my Christmas list: 4th Edition. Don’t forget the 25% off for authors.

Posted in General Interest | Leave a Comment »

Just in time for Christmas

Posted by kinasepro on December 23, 2006

It usually takes KP a year and a half to find information because that’s when the applications publish… In this case the only excuse is that he’s a little slow. I’m talking about the BindingDB and it appears to be a (smiles substructure searchable) resource with a ton of potential that’s been around since 5/05 but didn’t find the other end of my mouse button till today.

Also Current Opinion in Structural Biology has stuffed our stocking a little early with a thematic issue on you guessed it: kinases. Ok so is not all kinases, but 5 reviews aint bad.

Posted in General Interest | Leave a Comment »