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Archive for the ‘J&J’ Category

JNJ-

Posted by kinasepro on May 8, 2009

WO/2009/058801 is a use application for the pictured c-FMS inhibitor.

O=C(CN(C)C)N(CC1)CCC1C2=CC=C(NC(C3=NC(C#N)=CN3)=O)C(C4=CCCCC4)=C2

it’s JnJ-141 in the application, but does it have a dev #?

2I1M suggests a binding mode:

jnj-art-1

Posted in c-fms, J&J | Leave a Comment »

JNJ-38877605

Posted by kinasepro on May 8, 2009

Still in the clinic:  It’s JnJ’s ph1 c-Met inhibitor.

FC(C1=NN=C2N1N=C(C3=CN(C)N=C3)C=C2)(C4=CC5=C(N=CC=C5)C=C4)F

Posted in c-Met, J&J | 16 Comments »

Janssen’s got PLK4

Posted by kinasepro on February 9, 2009

COC(C=C(NC1=NC=NC2=C1C(C3)=CN2)C=C4OCC(N(C)CCCN3C)=O)=C4OCCCN5CCOCC5

WO/2009/016132

Posted in J&J | Tagged: | Leave a Comment »

Oximes from J&J

Posted by kinasepro on July 22, 2007

So J&J has a BMCL describing the amino-pyrimidine-oxime moiety as quinazoline isostere, and a there’s a handful of other applications describing the motif.   Here’s a Lapatinib-esque example where they describe the EGF activity: WO/2007/081630

NC1=C(/C=N/OCCN2CCOCC2)C(NC3=CC(Cl)=C(OCC4=CC=CC=C4)C=C3)=NC=N1

< 2g/d plz

Posted in EGF, J&J | 6 Comments »

WO/2007/075567

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.

FC(C1=CC(C=CC=N2)=C2C=C1)(F)C3=NN=C4N3N=C(C5=CN(C)N=C5)C=C4

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 »

JnJ’s got Aurora-A

Posted by kinasepro on May 1, 2007

Neet ideas in wo/2007/047646… I don’t understand the Kyowa Hakko / Janssen / JnJ triangle, but I hope there’s a deal under here somewhere. Else wo/2006/112479 is going to make for some fancy lawyering if you guys are going to keep these…

O=C1C(C(C2=CC(C=C(OCCN3CCN(CC)CC3)C=C4)=C4N2)=CC=C5)=C5CN1

>> here, have a model based on the Aurora-b PDB 2BFY: >>

Read the rest of this entry »

Posted in J&J | 4 Comments »

US20070015207

Posted by kinasepro on January 22, 2007

The triazolopyrimidine series hit the street with WO2005012304 where the chemistry was from Belgium, and Jannsen was calling them GSK3 inhibitors. Ahh, ’twas a simpler time… Then in WO/2006076442 they started claiming similar compounds: ‘produce a Fak/Cak enzyme inhibitory effect.’ So a) The series aint none too selective, b) there’s some subtle change that I’m not seeing where they can turn the activity around, c) GSK3 inhibitors ‘produce a fak/cak enzyme inhibitory effect,’ or of course d) I’m way over-thinking this. (yah, there is an indan in the earlier stuff too.)

O=C(NCCN(CC)CC)C1=CC=C(NC2=NC=C(N=NN3C4=CC5=C(CCC5)C=C4)C3=N2)C=C1 N#CCC1=CC(N2N=NC3=CN=C(NC4=CC=C(CN5CCN(C)CC5)C=C4)N=C32)=CC=C1

ClickClick – Beats me…

… but Kemia’s got some (gsk3 inhibitors with the core) in WO2006091737 Read the rest of this entry »

Posted in biotech, GSK3, J&J | Leave a Comment »

US20070004763

Posted by kinasepro on January 5, 2007

These are part of a Flt3 and/or TrkB series which JnJ has been putting a beat down on lately.

O=C(NC1CCN(C2=C3C=CC(OCCCN4CCN(C)CC4)=CC3=NC=N2)CC1)NC5=CC=C(C(C)C)C=C5

Posted in Flt3, J&J, Trk | Leave a Comment »

US20060281764

Posted by kinasepro on December 16, 2006

WTF J&J, Oxime-aldehydes? FLT3, TRKb, cKit inhibitors… Shinogi has some related EGF compounds: WO2006106721, and there’s a Biorg Med Chem Lett with the motif in CDK so its not unheard of. Quinazoline isosteres… Cool.

O=C(NC1=CC=C(C(C)C)C=C1)CC2CN(C3=NC=NC(N([H])[H])=C3/C=N/OC)CC2

Update >> There’s a couple other relatives that make this a family of applications which all published last Thursday:

 

O=C(N(CC1)CCC1C2=C(C=CC(N(C)C)=C3)C3=NC=N2)NC4=CC=C(OC(C)C)C=C4

This looks like the primary series, and the aniline appears to dial in TRKB – albeit not all that dramatically: US20060281772

O=C(OC1CN(C2=C3C(C=CS3)=NC=N2)CC1)NC4=CC=C(N5CCCC5)N=C4

US20060281768

 

Hmm… is LG293 TRKb?

 

Posted in c-Kit, Flt3, J&J | 2 Comments »

US20060258666

Posted by kinasepro on November 20, 2006

Hey Hey J & J,  Nice c-FMS inhibitors.  As kinase inhibitors go these are new to me, but I see you’ve been banging away at these for a few years so there’s got to be a candidate in there somewhere, eh?

Posted in c-fms, J&J | Leave a Comment »