KinasePro

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

Archive for the ‘JAK’ Category

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Merck’s got Azaindoles

Posted by kinasepro on May 4, 2009

pan-Jak:

CCN(N=C1)C=C1C2=CN=C3C(C(C4=NC(OC5CCNCC5)=CN=C4)=CN3)=C2WO/2009/054941

Posted in JAK, Merck & Co., PDK1 | Leave a Comment »

INCB018424

Posted by kinasepro on March 28, 2009

Incyte’s Ph2 Jak 1, 2 inhibitor: Org Lett; see also: WO/2008/157208

N#CC[C@H](C1CCCC1)N2N=CC(C3=NC=NC4=C3C=CN4)=C2

Keeping pace with CP-690550

Posted in JAK | 9 Comments »

AT-9283

Posted by kinasepro on March 18, 2009

Astex’s unpartnered JAK/Aur/Abl Ph1b nibO=C(NC1=CNN=C1C2=NC3=C(N2)C=CC(CN4CCOCC4)=C3)NC5CC5

poster; clinic; PDB: 2W1G & 2W1I

Posted in Astex, Aurora, JAK, bcr abl | Leave a Comment »

CP-690,550

Posted by kinasepro on February 10, 2009

CP-690,550 is Pfizer’s Ph3 Jak inhibitor. J Mol Biol. JAK2: 3FUP & JAK1?: 3EYG

N#CCC(N1C[C@H](N(C)C2=C3C(NC=C3)=NC=N2)[C@H](C)CC1)=O

Thanks Cytopia & no I didn’t forget 3EYH

Posted in JAK, PDB | 3 Comments »

Plethora ‘o’ PDB’s

Posted by kinasepro on October 14, 2008

GSK’s AKT stuff: 3d0e, 3E8D, 3E87, 3E88; J Med Chem, KP

SGX: Jak2 3E64, 3E63, 3E62, BMCL

Shokat: SRC, SRC, SRC, SRC, PI3K-Gamma, PI3K-Gamma

reminds me of OSI-906 or vice versa

Astrazeneca: CDK2 BMCL: 2W05

Amgen: P38 J Med Chem; 3DT1

LCK: 2ZM4, 2ZM1

Posted in AKT, CDK2, JAK, Lck, PDB, p38, pi3k | Leave a Comment »

Palau ‘n’ Jak3

Posted by kinasepro on October 11, 2008

Palau’s got Jak3: WO/2008/119792, purines for Jak3: WO/2008/090181 too.  From the sound of their pipeline DP1’s in there somewhere.

OCC1CCN(C2=C3C(NC=C3)=NC(NC4=CC=C(N5CCS(CC5)(=O)=O)C=C4)=N2)CC1

Posted in JAK, biotech | 1 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:

CC1=CN=C(NC3=CC=C(OCCN4CCCC4)C=C3)N=C1NC2=CC=C(Cl)C(OC)=C2

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

WO/2007/089768

Posted by kinasepro on August 14, 2007

27 Authors, 586 pages, a whole bunch of examples, and 20 MB of Jak-2 goodness.

O=C(C)NC(C=C1)=CC=C1C2=NC(NC3=CC=C(N4CCOCC4)C=C3)=NC=C2

Seems likely that XL-019 came out of this series.

Posted in Exelixis, JAK | 1 Comment »

LS-104

Posted by kinasepro on August 9, 2007

The news today is that LS-104 is in Ph1 and now owned by Aegera from Lymphosign who in turn licsensed it from HSC. Their portfolio of patent applications suggests the compound is likely a tyrphostin derivative.

LS104 is a novel small molecule tyrosine kinase inhibitor of therapeutically significant kinases including Jak2 and Bcr-Abl…In contrast to marketed kinase inhibitor drugs, LS104 inhibits its targets in a non-ATP-competitive manner

N#C/C(C(NCC1=CC=C(O)C(O)=C1)=O)=C\C=C\C2=CC(OC)=C(O)C(OC)=C2

WO/2005/092904

I don’ t know about you but I needed a history lesson to get a handle on these…

Posted in JAK, bcr abl, biotech | 2 Comments »

Correction

Posted by kinasepro on July 18, 2007

Pfizer’s Jak3 inhibitor CP-690,550 was described earlier listed as Ph ii-iii. For some reason that was changed, and all of its furthest advanced trials are Phase 2.

Posted in JAK, Phase III | 1 Comment »

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