KinasePro

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

WO/2007/103308

Posted by kinasepro on September 19, 2007

It’s an Array / Genentech c-Met app:

CCN(CC3)C[C@H](F)[C@H]3NC1=NNC2=C1C(OC4=CC=C(N([H])C(C5=CC=NN(C6=CC=C(F)C=C6)C5=O)=O)C=C4F)=CC=N2

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8 Responses to “WO/2007/103308”

  1. David said

    Hi, Pro,
    I like your patent publication list published on every Thursday. Any reason you discontinue the list?

  2. Derek Lowe said

    Boy, is that a heavy beast.

  3. That’s un ugly brute of a molecule! Fluorine on piperidine is unusual and will lower pKa. Not sure how stable it wil be with respect with respect to elimination of HF but should make for interesting NMR. Kill off the ionization too much and you’ll be left with solubilising group that doesn’t. And that beast is going to need all the help it can get.

  4. kinasepro said

    In and out web-traffic put publishing the Thursday List into the ‘more trouble then its worth’ column. I’m still keeping a list, and I might share it in another form, for now I’m not.

    The compounds of this application are really no bigger then XL-880, which I’d imagine must have fine PK, or it wouldn’t have advanced to Ph2? It holds particular interest for putting together a handful of interesting features, likely borrowing inspiration from prior Methylgene, and BMS applications, and indeed a handful of compounds look at the Merck piperidines

  5. For what it’s worth —I miss the Thursday list too (alot)

  6. chalker said

    I thought the list may have gone the way of Tenderbutton.

  7. milkshake said

    I wonder if there is any way of you starting the subscription – it could be a nominal fee, like $1 per week – but it would keep the automated page grabs that probably generate lots of traffics away.

  8. GMC: It’s interesting that you raise that point about F. Interesting because the F is axial, not equatorial, and because of this axial fluorine, the pKa is raised slightly over what we would assume.

    http://ashutoshchemist.blogspot.com/2007/06/pretty-basic-stuff.html

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