KinasePro

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

Archive for August, 2007

Chemical descriptors of clinical stage kinase inhibitors

Posted by kinasepro on August 25, 2007

– pretty pictures – no data –

Read the rest of this entry »

Posted in Drug Like Properties, General Interest | 2 Comments »

Rule of 5

Posted by kinasepro on August 24, 2007

>> Update: Here.
rule of 5 v 1.0
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Posted in Drug Like Properties, General Interest | 13 Comments »

Obligatory Scivee Post

Posted by kinasepro on August 21, 2007

looks neet-o

Posted in General Interest | 1 Comment »

More Her

Posted by kinasepro on August 21, 2007

‘nother ErbB 1,2,4 crystal forms app from BMS in US20070191375:

COC1=CC=CC(NC2=NC=NN3C2=C(CN4C[C@@H](O)[C@H](N)CC4)C=C3)=C1

Posted in BMS, EGF | 2 Comments »

PDB Update

Posted by kinasepro on August 21, 2007

BMS has a p38 BMCL with a PDB publishing today as well: 2QD9

O=C(N1C[C@@H](O)CC1)C(C2=CNC3=C2C=C(C(N4CC5=CN=C(C6=CC=C(F)C=C6F)N5CC4)=O)C(OC)=N3)=O

This one gives a little pespective to SCIO-469 and the related Scripps stuff: WO/2007/082079,

Posted in p38, PDB | Leave a Comment »

Hey C&EN

Posted by kinasepro on August 20, 2007

Nice cover story on c-Met and thanks for link. Have a look around and don’t miss the perennial favorites:

The KinaverseKinase drugs & the Phase III compounds

Posted in c-Met | 6 Comments »

Nerviano ‘n CDK

Posted by kinasepro on August 19, 2007

>> Update >> its really PHA-848125

WO/2007/90794 is a CDK inhibitor in combination with yada yada… from Nerviano.  The single compound claimed is pictured and potentially the phase one compound: PHA-793887.

O=C(C1=NN(C)C2=C1C(C)(C)CC3=CN=C(NC4=CC=C(N5CCN(C)CC5)C=C4)N=C23)NC

Discovery: Pharmacia IT WO/2004/104007

Posted in CDK, Nerviano | 4 Comments »

BI’s PLK1 compound

Posted by kinasepro on August 19, 2007

WO/2007/90844 is a salt form application of a compound that we’ve seen before ’round here.

O=C(N[C@@H]1CC[C@@H](N2CCN(CC3CC3)CC2)CC1)C4=CC=C(NC(N=C5N(C(C)C)[C@@H]6CC)=NC=C5[N](C)(C)C6=O)C(OC)=C4

discovery: WO/2003/020722, WO/2004/076454

Posted in BI, Plk1 | Leave a Comment »

Don’t abuse inventorship: Scientist

Posted by kinasepro on August 16, 2007

So a guy named Brian Druker wrote this piece on how Gleevec is overpriced, eh? Who is he? Well he appears to have written his own byline in case you hadn’t heard:

THE?

A quick googlification suggests he has plenty of nice things to say about Brian Druker and his role in Gleevec’s discovery… To his credit he does list Jürg Zimmermann (the named inventor on a series of patents starting with EP564409) as one of the ‘unsung heroes‘ in a history of Gleevec essay.

According to Zimmermann the discovery went something like this:

etc.

ht: spicy ip, via pharmalot

Posted in General Interest, gleevec, Novartis | 13 Comments »

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 »