KinasePro

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

Archive for the ‘Flt3’ Category

MLN-518

Posted by kinasepro on April 1, 2009

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

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

AC-220

Posted by kinasepro on March 26, 2009

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

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polymorph app: WO/2009/038757

Posted in Ambit, Flt3 | Leave a Comment »

TG-101348

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:

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

News of the day

Posted by kinasepro on November 14, 2007

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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.

r-788
the name suggests disodium.

Posted in Flt3, Rigel, SYK | 15 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…

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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 »

ENMD-981693

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:

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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 »

Lestaurtinib

Posted by kinasepro on May 28, 2007

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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 »

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.

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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.

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

 

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

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US20060281768

 

Hmm… is LG293 TRKb?

 

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