KinasePro

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

Archive for the ‘Astra’ Category

AZ’s got PI3K

Posted by kinasepro on July 30, 2009

O=C(O)C1=CC=CC=C1N[C@@H](C2=CC(C)=CN(C2=NC(N3CCOCC3)=C4)C4=O)Caz-pi3k-table

WO/2009/093972 reminds you of…

Advertisements

Posted in Astra, pi3k | 3 Comments »

MK n AZ

Posted by kinasepro on June 2, 2009

Two allosteric inhibitors are better then one!

AZD-6244 is Array’s MEK inhibitor [ARRY-886] which failed a solo ph2 endpoint not too long ago.

MK-2206 is Merck’s ph1 AKT inhibitor

Posted in Array, Astra, Merck & Co. | Leave a Comment »

ARRY-704 ?

Posted by kinasepro on October 23, 2008

aka ARRY-424704 / AZD-8330 is the Array / Astra Mek Ph1 backup to ARRY-886 / AZD-6244 which was put in a holding pattern when it didn’t meet a ph2 endpoint. The pictured strucuture is ‘Mek Inhibitor II’ in the combination app WO/2008/125820:O=C(C(C=C1C)=C(NC2=CC=C(I)C=C2F)N(C)C1=O)NOCCO

Posted in Array, Astra, MEK | 2 Comments »

AZ: More GSK3

Posted by kinasepro on October 11, 2008

Likely backup series.  Pictured: WO/2008/121064, and similar WO/2008/121063

O=C(C1=CC=C(C2=NC3=C(C4=CC=C(OC)C=C4)C(F)=CN=C3N2)C=C1)N5CCN(C)CC5

Previously…

Posted in Astra, GSK3 | Leave a Comment »

Astra’s got IGF1R

Posted by kinasepro on October 2, 2008

Its not in the pipeline, but it is a candidate. WO/2008/117051 has xrpd, and lots of data.

CC1=CC(NC2=NC(N3CCC[C@H]3C4=NOC(C5=NC=CC=N5)=C4)=NC(OC)=C2)=NN1

10x enough?

‘o’; mode

Posted in Astra, IGF | 1 Comment »

AZD-7762

Posted by kinasepro on September 25, 2008

It’s going ph1, it’s from WO/2005/066163, and it’s been described.

O=C(C1=C(NC(N)=O)C=C(C2=CC=CC(F)=C2)S1)N[C@H]3CNCCC3

Somebody send it to AmbitXL-844PF-477736, IC-83 are the known competition.

Posted in Astra, Chk1 | Leave a Comment »

AZ’s Bis-Morpholine

Posted by kinasepro on September 4, 2008

+ XRPD on multiple salt forms of this EphB4 inhibitor:

OCC1=CC=C(C)C(N(C2=NC(NC3=CC(N4CCOCC4)=CC(N5CCOCC5)=C3)=NC=C2)C)=C1

WO/2008/104754

Posted in Astra, EphB4 | Leave a Comment »

AZ’s GSK3 Indolinone

Posted by kinasepro on August 10, 2007

WO/2007/089192 is a use app, and WO/2007/089191 is salt forms application of the pictured GSK3 inhibitor originally from WO/2003/08285.  The YM-231146 / YM-359445 series bears similarity, albeit for Vegf.

N#CC1=CC2=C(NC(/C2=C3C=CC(CN4CCOCC4)=CN\3)=O)C=C1

The PDB used for alignment is 1UV5, and you can also check out AZ’s publicized interest in selective GSK3 inhibition in an ’03 JBC and 1q5k.

Posted in Astra, biotech, GSK3 | 2 Comments »

WO/2007/071955

Posted by kinasepro on July 2, 2007

Title’d app is from AstraZeneca and has ’bout 82 thiazoles said to hit c-Fms.

O=C(NC1=CN=C(C)S1)C2=CC(NC(C3=CC=CC(C(F)(F)F)=C3)=O)=CC=C2Cl

click for the guess Read the rest of this entry »

Posted in Astra, c-fms | 2 Comments »

Zactima

Posted by kinasepro on June 19, 2007

aka vandetanib, ZD-6474 is Astra’s Vegf / EGF doublet inhbitor.

CN1CCC(CC1)COC2=CC3=NC=NC(NC4=CC=C(C=C4F)Br)=C3C=C2OC

wiki, clinic, WO/2001/032651

Posted in Astra, EGF, Phase III, VEGF | 1 Comment »