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

Archive for the ‘Flt3’ Category


Posted by kinasepro on April 1, 2009

aka Tandutinib is Takeda’s Ph2 FLT3, cKIT, PDGFR inhibitor Blood.


Posted in Flt3, PDGFR, Takeda | Leave a Comment »


Posted by kinasepro on March 26, 2009

Is the screening company’s Ph1 FLT-3 compound:


polymorph app: WO/2009/038757

Posted in Ambit, Flt3 | Leave a Comment »


Posted by kinasepro on December 7, 2007

Targegen’s got a press release:

Plans to initiate a multi-center clinical trial of TG101348, an internally discovered, oral, potent, and highly selective JAK2 inhibitor in January, 2008

A poster at ASH:

…Dual-Acting JAK2/FLT3 Small Molecule Kinase Inhibitor for the Treatment of AML

and some pyrimidines in WO/2007/053452:


Posted in biotech, clinical, Flt3, JAK | Leave a Comment »

News of the day

Posted by kinasepro on November 14, 2007


aetiology and limited data in: WO/2005/048953

Posted in Ambit, Aurora, Deals, Flt3, Rigel | 16 Comments »

R-788 (Fostamatinib disodium)

Posted by kinasepro on November 9, 2007

R-788 is Rigel’s SYK / Flt3 inhibiting prodrug of R-406, and despite a positive sounding press release on their Ph2 ITP study, the market is reacting negatively so far by knocking 20% off of the stock price.

the name suggests disodium.

Posted in Flt3, Rigel, SYK | 15 Comments »


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…


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 »


Posted by kinasepro on June 1, 2007

So Entremed is over in Boston stumping for their Aurora inhibitor and they happened to drop the MW and cLogP:


Only two compounds from WO/2007/041358 fit that bill. That one, and the Z isomer.

Posted in Aurora, biotech, Flt3, multi-target | 4 Comments »


Posted by kinasepro on May 28, 2007


Lestaurtinib / CEP-701 is currently in trials for a handful of indications and first appeared in WO/1988/07045 (US,4,923,986) via Kyowa Hakko Kogyo. The series was first described as a group of PKC inhibitors, but later came this ’98 press release: (emphasis mine)

CEP-701 is one of a series of specific receptor trk kinase inhibitor derived from the indolocarbazole K252a, which was originally synthesized by Kyowa Hakko Kogyo Co., Ltd., Tokyo, Japan

Read the rest of this entry »

Posted in c-Met, Cephalon, Flt3, JAK, Trk, VEGF | 3 Comments »


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.


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


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.


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



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




Hmm… is LG293 TRKb?


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