KinasePro

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

Archive for the ‘PKC’ Category

R & D @ B I

Posted by kinasepro on September 13, 2008

With BIRB-796 a distant memory, BIBW-2992 in ph3 and given the new name Tovok, BIBF-1120 headed into ph3 and given the name Vargatef,  BI-2536 in multiple Ph2s, a new Ph1 Aurora inhibitor, and another backup PLK1 inhibitor undisclosed, but likely in-clinic or clinic-bound – what could possibly be next?

I can haz pyrimidines

PDK mod prolly from Berlex

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Posted in BI, PDK1, PKC, Plk1 | 2 Comments »

Novartis ‘n’ PKC

Posted by kinasepro on June 25, 2007

PKC412 (Midostaurin)?

So staurosporine analogs are old news? Novartis has a 1 compound PKC application.

O=C(C(C1=CC(N2CCN(C)CC2)=CC(C(F)(F)F)=C1Cl)=C3C4=CNC5=C4C=CC=C5)NC3=O

US20070142401 / WO/2005/039549

Posted in Novartis, PKC | Leave a Comment »

Enzastaurin

Posted by kinasepro on June 19, 2007

aka LY-317615 is a Lilly ‘PKC’ inhibitor

O=C(C(C1=CN(C)C2=C1C=CC=C2)=C3C4=CN(C5CCN(CC6=NC=CC=C6)CC5)C7=C4C=CC=C7)NC3=O

WO/1995/17182
BMCL ’03; Cancer Res. ’05; Clinic

Posted in Lilly, Phase III, PKC | Leave a Comment »

Arxxant

Posted by kinasepro on June 19, 2007

aka Ruboxistaurin / LY333531 is a Lilly PKC-b inhibitor

O=C(N1)C(C2=CN(CCO[C@]([H])(CN(C)C)CC3)C4=CC=CC=C42)=C(C5=CN3C6=C5C=CC=C6)C1=O

J Med Chem ’96; Org Lett ’01; Science ’96; clinic

Posted in Lilly, Phase III, PKC | Leave a Comment »