KinasePro

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

Banyu / Aurora

Posted by kinasepro on February 1, 2007

Anybody have access to: Expert Opinion on Therepeutic Patents? Think maybe you could read Nerviano’s Aurora A selective patent review of Banyu’s stuff and tell us what it says ? or email me (kinasepro@gmail.com)

Applications: (WO/2006/129842); (WO/2006/046735); (WO/2006/046734)

O=C(N1CCN(CC2=NC(NC3=NC=CS3)=CC(C(N(C)C)=O)=C2)CC1)C4=CC(F)=C(C=C4)Cl

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3 Responses to “Banyu / Aurora”

  1. weirdo said

    “six variable elements . . . are quite narrowly defined” . . . Only 16 molecules exemplified . . . “no yields reported” . . . sub-nanomolar potency against the enzyme, but no assay data reported “thus preventing a complete assessment of the relevance of this data”. Micromolar in cellular assays, but work in vivo (synergistic with paclitaxel).

    Has a table with four aurora inhibitors in the clinic: MLN-8054, AZD-1152, PHA-739358, MK-0457.

  2. ebola1 said

    Again — cellular data and in vivo data give us the readout on phenotype. Good cellular data will give Aurora B the dominance — and thus a B phenotype. Non-selective inhibitors are B inhibitors. These A vs. B thingies are very different at the cellular and in vivo level — look at the readouts from the cell cycle. One needs to be careful what other cell cycle targets are hit — a change will shut different things down.

    i.e.,
    1.Potency is not a good readout on selectivity
    2. solubility and permeability may prevent good target availability
    3. do you want i.v. or oral activity? Huge difference in this arena
    4. cMax or AUC — some of these compounds are striking bad at both

  3. kinasepro said

    Thanks for the replies. I’ve had a look at the paper myself now, and I think its a remarkably succinct synopsys of both the landscape and the Banyu patentscape.

    The nuts and bolts are that structures like the one drawn above are remarkably potent and Aurora A selective vs. Aurora B.

    Only thing I take issue with is the author’s last bit of analysis – which I think I’ll let be the subject of another post.

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