KinasePro

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

BI & PLK1

Posted by kinasepro on October 14, 2006

Hi BI, More aminopyrimidines?

More the merrier I say. No sulfur this series, but Kinasepro likes the ground you cover with these applications: EP1598343 (published 11/25/05)

The amine in example one is nice, and thanks for the experimental. (1>reductive amination 2>Pd/C, p54.) It looks as though you like it too, because it and some isosteres are heavily represented in the later generations. EP1630163 (published 3/1/06)

Not the standard solvent exposed yada-yada, though quite a bit different from the Amgen imidazalones. Second and a half generation: WO2006021378 (published 8/19/06) Looks as though you just realized the anilines were active, and rushed to cover them in this app. Hoho, otherwise this is the same as the previous, just reverse the [L]&C=O in the previous Markush.

Third Generation: WO2006021547, and WO2006021548 (Published 3/2/06) Kinasepro’s trick elbow tells him BI is closing in on something though he thinks you should have a talk with the guy who put your patents together. Is the the jumbled up A, R2, and R3 on page 43 enough to invalidate? Neh, but KP hopes your attorney lays off the 3-Heineken lunches. Nice set of amines anyhow. 

Tschüss 
smiles: yah, KP is trying a new thing with smiles.  to see if they’er searchable.
COC1=CC(C(N[C@@H]4CC[C@@H](N5CCOCC5)CC4)=O)=CC=C1NC2=NC(NC3=C(C(N)=O)C(OC)=CC=C3)=C(C(F)(F)F)C=N2
COC1=CC(C(NCCC)=O)=CC=C1NC2=NC(NC3=C(C(N)=O)C(OCC[C@@H](CC(C)C)N)=CC=C3)=C(C(F)(F)F)C=N2
CC(C)N([C@H](C)C(N6C)=O)C1=C6C=NC(NC2=CC=C(C(N[C@@H]3CC[C@@H](N4CCN(CC5CC5)CC4)CC3)=O)C=C2OC)=N1
CN(C1=C(N(C(C)C)[C@@H]4CC)N=C(NC2=CC=C(N3CCC(N5CCC5)CC3)C=C2OC)N=C1)C4=O
O=C(NC3CCN(C)CC3)C(C=C2)=CC=C2NC1=NC(N(C5CCCC5)C(C=C4C)=O)=C4C=N1

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