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


Posted by kinasepro on October 16, 2006

Hello Exelixis,

Kinasepro must lament that many of your claimed compounds he’s seen before. They appear in the recent Kirin application which published a mere 7 days before yours. WO2006104161 (published 10/5/06) Ooooh, 7 Days? I haven’t figured out the priority dates but you guys probably need a beer right about now, eh? Hopefully everybody signed their notebooks…

Sure there’s probably enough room room in the c-Met sandbox for both Excelixis and Kirin to play. Both groups appear to have found interesting heterocyclic tail pieces, and the Excelixis application relies less heavily on the acyl-ureas claiming also some things like phenethyl oxalamides, and a noteworthy benzothiazole-amide (scheme on p142-144).

Mostly this is just a continuation of: WO2005030140 where they were looking at the quinazoline analogs. Bit of a snoozer if you ask me, but KP does like some of your mesylate intermediates:

Somebody should write a review on morpholine isosteres.

O=C(C5(CC5)C(NCC4=CC=C(F)C=C4)=O)NC(C=C3)=CC=C3OC2=CC=NC1=CC(OC)=C(OC)C=C12 O=C(C(NCCC5=CC=CC=C5)=O)NC(C=C3F)=CC=C3OC2=CC=NC1=CC(OCCCN4CCOCC4)=C(OC)C=C12 O=C(OC(C)(C)C)N2C[C@]([C@]([H])(C2)CC(C1)OS(=O)(C)=O)1[H] O=C(OC(C)(C)C)N1C2CC(CC1CC2)CCOS(=O)(C)=O

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