KinasePro

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Archive for April, 2009

RDEA-119

Posted by kinasepro on April 29, 2009

Its Ardeas’s $35 million non-hydroxamate MEK inhibitor in Ph1.  The pictured structure is one of three claimed in the ‘combination w/ Nexavar’ app: WO/2009/018238.

rdeaArdea will grant Bayer a worldwide, exclusive license to develop and commercialize Ardea’s MEK inhibitors for all indications”

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Posted in Bayer, MEK | 1 Comment »

PF-3758309

Posted by kinasepro on April 26, 2009

Described as a Pfizer PAK4 candidate of indeterminate status.

CC1(C)N(C(N[C@H](CN(C)C)C2=CC=CC=C2)=O)CC3=C1NN=C3NC4=C(SC=C5)C5=NC(C)=N4

Read the rest of this entry »

Posted in biotech | 3 Comments »

AS-703026

Posted by kinasepro on April 24, 2009

>> Update – this structure has been revised from the butyl amide – This is (i believe) the correct structure >>

EMD-Serono’s got ‘a ph1 non-hydroxamate ‘ATP Collaborative’ Mek inhibitor.

O=C(C1=C(C=NC=C1)NC2=CC=C(C=C2F)I)NC[C@H](O)CO

via Ghost, & WO/2006/045514

Posted in MEK, Merck DE | 5 Comments »

CH-4987655

Posted by kinasepro on April 23, 2009

Some have walked a country mile to get away from the hydroxamate, others think nothing of tacking ‘nother one on:  Its Chugai’s ‘ATP-Collaborative’  Ph1 MEK inhibitor: Ro-4987655 / CH-4987655.  More potent, stable, and soluble…

O=C(NOCCO)C1=C(NC2=CC=C(I)C=C2F)C(F)=C(F)C(CN3OCCCC3=O)=C1

Reduced signs of hydrolysis to the inactive acid and no BBB penetration.(preclinically)

Posted in biotech, MEK, Roche | Leave a Comment »

MK-2206

Posted by kinasepro on April 23, 2009

Merck‘s Ph1 allosteric AKT inhibitor:

NC1(CCC1)C(C=C2)=CC=C2C3=NC4=C(C=C3C5=CC=CC=C5)C(N6C=C4)=NNC6=OBinds to the Pleckstrin homology domain
@
Akt1 8 nM
Akt2 12 nM
Akt3 65 nM

thanks Ghost and Redferret for the structure

Posted in AKT, Merck | 6 Comments »

WO/2009/047163

Posted by kinasepro on April 22, 2009

WO/2009/047163 show’s a series of minimalist designed CK1 inhibitors:

O=C(N)C1=CC(C2=CC=NC=C2)=CN1

Compound A

roche-data

Posted in CK1, Roche | 2 Comments »

@ AACR?

Posted by kinasepro on April 19, 2009

Send Structures / Will Post!

Email me smiles/inchi/chemdraw/iupac – whatever.  Structure and a corporate number is good enough, but any other info – feel free. (please include whether you want to be anon)

Posted in General Interest | Leave a Comment »

CX-4945

Posted by kinasepro on April 19, 2009

Cylene’s CK2-α selective inhibitor currently in Ph1:

OC(C1=CC2=C(C3=CN=CC=C3C(NC4=CC=CC(Cl)=C4)=N2)C=C1)=O

Ki 0.38 nM

Posted in CK2 | 9 Comments »

WO/2009/035159

Posted by kinasepro on April 13, 2009

Possibly SAR-502250 its a Mitsubishi / Sanofi TPK1/GSK3 inhibitor:

CC1=NOC(C(C=C2)=CC=C2[C@H](OCC3)CN3C(N4C)=NC(C5=NC=NC=C5)=CC4=O)=N1

for Alzheimer’s & Diabetes

Posted in GSK3, Sanofi-Aventis | 2 Comments »

AV-412

Posted by kinasepro on April 13, 2009

Aveo’s Ph1 irreversible  Erbb inhibitor:

C=CC(NC1=CC2=C(N=CN=C2C=C1C#CC(C)(C)N3CCN(CC3)C)NC4=CC=C(C(Cl)=C4)F)=O

via Mitsubishi

Posted in EGF | 2 Comments »