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Archive for the ‘Sanofi-Aventis’ Category

Sanofi’s got’m too…

Posted by kinasepro on May 13, 2009

‘Nother Triazolopyridazine c-Met app:

sanofi-cmetWO/2009/056692

Posted in c-Met, Sanofi-Aventis | Leave a Comment »

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 »

Aventis in the Aurora arena

Posted by kinasepro on February 4, 2007

A combined US/FR effort results in a novel Aurora chemotype in EP1746097:

O=C1CCCC2=C1C(C3=CNN=C3N2)C(O4)=CC=C4SC5=NC6=CC=C(OC(F)F)C=C6N5

This scaffold is not entirely unknown, but it is new for the Auroras afaik. These were likely discovered as hits from an Ambinter or an aptly named Aurora screening library.

Posted in Aurora, Sanofi-Aventis | 7 Comments »

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 »

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 »

Got Spiro?

Posted by kinasepro on January 14, 2007

US20070010539 is a GSK3-beta application. This series goes back to ’01, and the pictured spiro compound hit the streets in ’05. Publications on these? Other then an expert opinion (which my library doesn’t carry) and them naming SAR502250 a preclinical development candidate (also in ‘05), I haven’t seen anything. While I don’t relish posting old news, the novel spiro architecture was enough to make KP lift an eyebrow.

O=C1C=C(C2=CC=NC=C2)N=C3N(C[C@H](O)C4=CC=CC=C4)C5(CCN(C)CC5)CCN31

Only they know if these spiro compounds are the lead structures, but it looks like a well developed chemical series with an interesting story to be told, and since they’re not talking… I will.

Read the rest of this entry »

Posted in GSK3, Mitsubishi, Sanofi-Aventis | Leave a Comment »

WO2007000241

Posted by kinasepro on January 10, 2007

Sanofi-Aventis has a series of BARK1 inhibitors:

NC(C1=NC2=C(C=NN2)C(C3=CN(C)C4=C3C=C(OCCN5CCOCC5)C=C4)=C1)=O

crude apo model; ILE GK, ASP82 looks unique.

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

 
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