KinasePro

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

Archive for January, 2007

XL418

Posted by kinasepro on January 31, 2007

IND in the books.

Looking something like: WO/2005/117909 WO/2006/071819

CC1=C(CCCN2CCCC2)C=C(Cl)C=C1N3CCN(C4=C5C(NN=C5Br)=NC=N4)CC3

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Posted in AKT, Exelixis | 4 Comments »

WO/2007/009898 (Nerviano)

Posted by kinasepro on January 31, 2007

Nerviano’s been looking at the thienopyrroles since the Pharmacia IT days, but the priority date on this one is 7/05… So whats new I ask? Well, appears they found some ortho substituents that work.

O=C(C(S1)=CC2=C1NN=C2NC(C3=CC=CC=C3N([H])C(C)=O)=O)NC(C4=CC=CC=C4)(C)C

Most notably amides and benzamides
Hmm… See a little quinazoline isostere in these?

Posted in Aurora, Nerviano | Leave a Comment »

WO2007011065

Posted by kinasepro on January 28, 2007

Mitsubishi has an app covering the intermediates for their GSK3 Sanofi-Aventis stuff. I still think the spiro compounds are sexier, but the morpholines are further explored so here we have a pretty solid looking asymmetric method to make 2-aryl morpholines via CBS reduction:

FC1=CC=C(C(CCl)=O)C=C1 FC1=CC=C([C@H](O)CCl)C=C1
FC1=CC=C([C@H](O)CNCC2=CC=CC=C2)C=C1 FC1=CC=C([C@H](OC2)CN(CC3=CC=CC=C3)C2=O)C=C1
FC1=CC=C([C@H]2CN(CC3=CC=CC=C3)CCO2)C=C1 FC1=CC=C([C@H]2CNCCO2)C=C1
Route starts on page 79 example 1, 2 & 5 shown here.

Array might have something to say with how novel the approach is, y’know given how they sell the (rac) stuff?

Posted in GSK3, Mitsubishi, Sanofi-Aventis | 2 Comments »

The Thursday List

Posted by kinasepro on January 25, 2007

US20070021456 Vegf Merck DE
US20070021452 Aurora Cyclacel
US20070021447 Pi3k Applied Research Systems
US20070021446 Aurora+ 4SC AG
US20070021443 Jak3 Pharmacopeia
US20070021436 flt3/c-kit/TrkB J&J
US20070021435 flt3/c-kit/TrkB J&J
US20070021427 IKK? Chemtech Research Inc.
US20070021419 Cyclacel
US20070021407 AstraZeneca

WO/2007/012042 Millenium (MLN518)
WO/2007/011065 GSK3 Mitsubishi-Sanofi (process/intermediates)
WO/2007/010013 flt3 NOVARTIS
WO/2007/009898 NERVIANO

Posted in Application List | Leave a Comment »

WO2007006926

Posted by kinasepro on January 25, 2007

Just another pyrimidine series? Maybe, but Sanofi-Aventis has a bunch of these sulfonamides in WO/2007/006926. They’ve got an IKK collaboration Millenium with “MLN0415 a phase one inhaled IKK-beta inhibitor taking the lead, but this aint that.

O=S(C1=CC=C(NC2=NC=CC(NC3=CC=C(F)C=C3)=N2)C=C1)(N(C4CCN(CCP(OCC)(OCC)=O)CC4)C[C@H]5CCCN5)=O

They’re not all phosphonates, but this subseries has me crooking an eyebrow. Perhaps this is the AVE8680 Sanofi series, but I’d expect this app to have Sxx# given that its a French application… eh… Beats me.

Posted in IKK, Sanofi-Aventis | Leave a Comment »

Speed has some wisdom for you.

Posted by kinasepro on January 23, 2007

With the many layoffs over the last months, and damnit even years, I’m sure many are wondering: Is science still a viable profession?

Here’s what C. S. “Speed” Marvel has to say on the issue.

…the business cycle slumped. Companies made less profits. Research began to be curtailed and abandoned by some of the major chemical companies…

Read the rest of this entry »

Posted in Monday Night Off Topic | 7 Comments »

Aurora dev compounds

Posted by kinasepro on January 22, 2007

Crimson Canary has a Rockin spreadsheet on Aurora inhibitors in development.

Read the rest of this entry »

Posted in Aurora, Nerviano | 3 Comments »

US20070015207

Posted by kinasepro on January 22, 2007

The triazolopyrimidine series hit the street with WO2005012304 where the chemistry was from Belgium, and Jannsen was calling them GSK3 inhibitors. Ahh, ’twas a simpler time… Then in WO/2006076442 they started claiming similar compounds: ‘produce a Fak/Cak enzyme inhibitory effect.’ So a) The series aint none too selective, b) there’s some subtle change that I’m not seeing where they can turn the activity around, c) GSK3 inhibitors ‘produce a fak/cak enzyme inhibitory effect,’ or of course d) I’m way over-thinking this. (yah, there is an indan in the earlier stuff too.)

O=C(NCCN(CC)CC)C1=CC=C(NC2=NC=C(N=NN3C4=CC5=C(CCC5)C=C4)C3=N2)C=C1 N#CCC1=CC(N2N=NC3=CN=C(NC4=CC=C(CN5CCN(C)CC5)C=C4)N=C32)=CC=C1

ClickClick – Beats me…

… but Kemia’s got some (gsk3 inhibitors with the core) in WO2006091737 Read the rest of this entry »

Posted in biotech, GSK3, J&J | Leave a Comment »

Pfizer

Posted by kinasepro on January 20, 2007

mmmm Gossip… Monday ~1PM eastern: tune in, turn on, and drop out – for the Pfizer Webcast. Since Peter Brandt (senior vp of Pfizer Global) and Kathy Donovan (vp of Human Resources) are not inventors of kinase inhibitors we likely hopefully won’t spend much time on this event here at KP.

For a more reasoned analysis, check Pipeline.

>> update. Dang worse then I thought… 10,000 gone and Upjohn up in smoke. :[ WTG PFE :[

Posted in General Interest, Pfizer | 1 Comment »

WO/2007/007919

Posted by kinasepro on January 19, 2007

Astellas’ Jak3 application has an interesting twist on the azaindole core.

O=C(N1CC2=CC(Cl)=CC3=C2OCOC3)N([C@H]4CCCC[C@H]4C)C5=C1C=NC6=C5C=CN6 O=C(N1)N([C@H]2CCCN(C(C3(CC3)C4=CC=C(Cl)C=C4)=O)C2)C5=C1C=NC6=C5C=CN6

14 inventors 666 examples

Posted in biotech, JAK | 1 Comment »