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

Archive for the ‘Janssen’ Category


Posted by kinasepro on July 7, 2007

A reader comment got me to take a closer look at the titled JnJ application.¬† I don’t see it making their blog, but given its similarity to a recent a Vertex application of course it’s going to make this one.


1 nM autophos

 regression @ 25 mg / kg ?  Them some lucky mice.

clogp= 1.28 MW=377

Yah, I’d say your compounds are getting jealous right about now.

Posted in c-Met, J&J, Janssen | 16 Comments »


Posted by kinasepro on November 5, 2006

Hey there Jannsen, I see you and Schering AG have been hitting the Macrocyclic button for kinase inhitors for a little while now. Schering on pyrimidines for Tie2 (EP1674470 / WO2006108695) and you guys on the quinazolines for EGF. They’re a little kookie, but hey I like it. Got to be an entropy thing, eh?

This application looks at a handful of linkers, as you may expect, made via amid coupling, olefin metathesis, and even reductive amination.

Tot ziens

Posted in EGF, Janssen | Leave a Comment »


Posted by kinasepro on October 5, 2006

Hi Janssen Pharmaceutica,

Nice c-Met application. This is one of those ‘hey didn’t Sugen already do this stuff?’ oxindole patents (Sugen: WO2005005378). The Sugen application focuses on the different regioisomer though. They also fairly conservatively claimed the H2 aryl’s. Anyways, the
hydrazones certainly do have both style and grace but the Jannsen application leaves Kinasepro wanting more. Kudo’s for working so close to Sugen’s matter, otherwise no soup for you.

Here’s a gratuitous hydrazone bound to CDK: 1KE6 (The carbon analog 1ke5 binds identically)

And here’s a gratuitous review on the c-Met as a target

c-Met pdb’s:


Posted in c-Met, Janssen | 4 Comments »