MLN-518

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

AC-220

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

polymorph app: WO/2009/038757

TG-101348

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:

News of the day

• Ambit grabs 50M in a Series D. Their Lead is AC-220 a ph1 selective Flt3 compound.  In WO/2007/109120?

 

aetiology and limited data in: WO/2005/048953

• Rigel tacks on 3M for the Japanese rights to R-763.

R-788 (Fostamatinib disodium)

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.

ABT-869

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

ENMD-981693

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.

Lestaurtinib

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

US20070004763

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

US20060281764

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

US20060281768

 

Hmm… is LG293 TRKb?