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

Archive for the ‘c-fms’ 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

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

PLX-5568

Posted by kinasepro on September 3, 2008

Plexxikon’s Ph1 in healthy volunteers underway with plans for and pain and PKD. They’re not advertising the target, but my guess is c-fms. We’ve been following their earlier cFms / cKkit double-stuff, and its likely they found a group to tune out the Kit, maybe something like: WO/2008/080015

still no partner…

Posted in c-fms, Plexxikon | 2 Comments »

WO/2007/071955

Posted by kinasepro on July 2, 2007

Title’d app is from AstraZeneca and has ’bout 82 thiazoles said to hit c-Fms.

O=C(NC1=CN=C(C)S1)C2=CC(NC(C3=CC=CC(C(F)(F)F)=C3)=O)=CC=C2Cl

click for the guess Read the rest of this entry »

Posted in Astra, c-fms | 2 Comments »

ABT-869

Posted by kinasepro on June 26, 2007

Phase 2 on the doorstep, Genentech and Abbott just announced a collaboration to include development of the compound w/ backups. No terms disclosed…

O=C(NC1=CC=C(C=C1)C2=CC=CC3=C2C(N)=NN3)NC4=CC(C)=CC=C4F

Vegf, Flt3, Tie2, c-FMS, Pdgf, c-kit yadda yadda

j med chem, blood, molec cancer ther., WO/2004/113304

Posted in Abbott, c-fms, Flt3, Genentech, PDGFR, TIE2, VEGF | Leave a Comment »

Axitinib

Posted by kinasepro on June 19, 2007

aka AG-013736 is a Pfizer Vegf / c-FMS compound via Agouron.

O=C(NC)C1=CC=CC=C1SC2=CC3=C(C=C2)C(/C=C/C4=NC=CC=C4)=NN3

Salt: Tosylate?
Clinic Ph iii: Pancreatic Cancer
WO/2001/002369; process app; ‘06 Asco,

Posted in c-fms, Pfizer, Phase III, VEGF | Leave a Comment »

Plexxikon’s cFms/cKit stuff:

Posted by kinasepro on February 10, 2007

Some of Plexxicon’s latest cKit / cFms stuff has published, and surprise-surprise its got their ‘scaffold’. The choice of where to tag on amines suggests the following motif:

ClC1=CC=C(C=C1)CNC2=NC=C(CC3=CNC4=NC=C(OCCN5CCOCC5)C=C43)C=C2

This week: US20070032519
Last week: WO/2007/013896
Last year: WO/2006/009797

Posted in c-fms, c-Kit, Plexxikon | Leave a Comment »

Kinase PDB’s: c-FMS

Posted by kinasepro on November 28, 2006

c-FMS (CSF1R if your from Cytopia.) is on the docket this week: 2IOV, 2IOY, 2I1M These are the first cFMS published methinks?

Well consider this colony stimulated.

Posted in c-fms, PDB | 1 Comment »

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 »

CYT645

Posted by kinasepro on November 19, 2006

Tag Cytopia, I see you nominated a c-fms inhibitor, neet-0, but no patent app published yet? There’s an article in FASEB, but whats say we stick with calling it c-fms, eh? If you want to get creative, lets go with c-FMS, or fms, or maybe even CFMS, but CSF-1R? Aww c’mon, we’ve got enough names to keep up with 😦 How about a little standardization here, people?!

From application WO2004054977 it appears the cross screens for your JAK2/3 programs included c-fms, hck, zap70, fes, and abl. I like it, nice way to determine selectivity profile, and to find the serendipitous hit here and there. Good show, my guess is you found something with a little fms selectivity.

Also, I’m a little behind the times, so a belated congrats on partnering your JAK3 program with Novartis.

Tschüss

Posted in biotech, c-fms | 2 Comments »