MK n AZ

Two allosteric inhibitors are better then one!

AZD-6244 is Array’s MEK inhibitor [ARRY-886] which failed a solo ph2 endpoint not too long ago.

MK-2206 is Merck’s ph1 AKT inhibitor

Merck’s got Azaindoles

pan-Jak:

WO/2009/054941

Banyu’s WEE1 candidate

Polymorph app: WO/2008/133866

Discovery app: WO/2006/126128

VX-680, VX-667: Done

VX-680 halted as:

one patient experienced QTc prolongation.

and the follow-on, VX-667:

Failed to meet pharmacokinetic objectives in a Phase 1 trial

PDB Update

Merck (WP) Chk1, 2R0U: BMCL

IKK-b or Jak?

So Merck’s got WO/2007/061764 and the wordplay makes me think the bit about JAK is just a diversion and that the primary target is IKK-b.  You have to squint a little to see the similarity with the Millennium series, but as usual: what do I know.  Interesting series none-the-less.

US20060293358

Merck MA‘s got Met

WO2006135604

WO2006135604 is a recent Chk1 offering via Merck.

VX-680

Oh wait I’m sorry Merck. My bad, I didn’t realize we’re calling it MK-0457 now. heh… Phase 1 update presented yesterday. The compound hits Aurora, JAK2, Abl etc. etc. and the current study is in ph1 for colorectal cancer. Looks good.

We’ve talked about the compound before here.

US20060276514

Ok Merck, so what’s with the aldehyde? Ahhah, I see you already dropped the dime in Biochemistry back in ’05. ‘Reductive amination’ with no reducing agent. Somebody needs to break these kinds of things down for me, since I still don’t get it.