Schering’s Macrocycles

Aurora Eh? What can I say, I like’m: WO/2007/079982

Related series, complete w/ a Chem Med Chem.

US20060252782

Hi Schering AG, err Bayer, err, whoever you are these days, TIE2 / VEGF Sulfoximine macrocycles I see. Those 5% cyclizations are going to need a little work… But what I really want to see is you guys resolve the enantiomers!

DE102005020104

and DE102005020105. Guten Tag Schering AG,

Further along the road with the thiazolidinones, eh?  I like the title: New thiazolidinone without basic nitrogen, their production and use as drugs

Kinasepro is always happy to see more Plk1 inhibitors, but hey I’ll admit that I haven’t a clue whats going on with these – and now consider an earlier post on your analogous series, ummm, wrong. The only PDBs that give KP a hint as to what could be going on here are from some compounds bound to PI3K: 2A4Z, and 2A5U. O=C(N(CC)/C(S2)=C(C(NCC(F)(F)F)=O)\C#N)/C2=C/C1=C(C)N=CN1 O=C(N(CC)/C(S2)=C(C(NCC#C)=O)\C#N)/C2=C/C1=CC=C(N3CCCC3)C=C1

WO2006063806

Guten Tag Schering AG,

Nice antibacterial you’ve got there posing as a kinase inhibitor. It seems like there’s a handful of these thiazolidinone PLK1 patent applications floating around. This offering from Schering isn’t their first of the series (WO2003093249, WO2005042505, WO2006082107) but it will be the first to get Kinasepro’s meat cleaver approach to figuring out how it’s binding. All Schering’s applications embody matter around the thiazolidinone core, with some subtle some not-so-subtle changes to the pendant functional groups.

To the best of KP’s knowledge there are no published Xrays of the kinase domain. It was looking like MIT had a patented one until you read the fine print and find its only another of the ‘polo-box-domain’ Pshaw Acadamics. Schering has a patent application on using a homology model for making these suckers, so don’t you even think about using this at home kids.

So what I’m getting at is that this is really just a guess, if there’s something public that your aware of that could help my understanding please feel free to chime in.