KinasePro

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Archive for the ‘BI’ Category

BI-6727

Posted by kinasepro on May 12, 2009

BI’s PhII follow on to BI-2536

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=C5N(C)C6=O)C(OC)=C4

PDB: 3FC2; Clin Can Res

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BI-2536

Posted by kinasepro on April 2, 2009

BI’s Ph2 PLK1 inhibitor

O=C(C1=CC=C(C(OC)=C1)NC2=NC=C(N(C3=O)C)C(N([C@@H]3CC)C4CCCC4)=N2)NC5CCN(CC5)C

IV / 0.8 nM

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R & D @ B I

Posted by kinasepro on September 13, 2008

With BIRB-796 a distant memory, BIBW-2992 in ph3 and given the new name Tovok, BIBF-1120 headed into ph3 and given the name Vargatef,  BI-2536 in multiple Ph2s, a new Ph1 Aurora inhibitor, and another backup PLK1 inhibitor undisclosed, but likely in-clinic or clinic-bound – what could possibly be next?

I can haz pyrimidines

PDK mod prolly from Berlex

Posted in BI, PDK1, PKC, Plk1 | 2 Comments »

BIBW-2992

Posted by kinasepro on September 7, 2007

BI’s irreversible ErbB inhibitor to join the Ph3 club.

O=C(/C=C/CN(C)C)NC3=CC2=C(N=CN=C2C=C3O[C@H]4COCC4)NC1=CC=C(C(Cl)=C1)F

>> update they’ve named it Tovok

Posted in BI, EGF, Phase III | 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

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BI ‘n’ Aurora B

Posted by kinasepro on February 12, 2007

Boehringer-Ingelheim’s got a series of 5-lipophile-substituted-pyrimidines claimed as ‘Aurora B’ inhibitors.

O=C(NC1CCN(C)CC1)C2=CC=C(NC3=NC=C(C(F)(F)F)C(N[C@@H]4[C@H]([C@](NC(C)C)=O)CCC4)=N3)C=C2

15 inventors / 148 examples / no data

US20070032514
WO/2007/003596

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US20060270671

Posted by kinasepro on December 4, 2006

Hi BI, nice IKK inhibitors. These seem to hav evolved from alcohol hits first published in that ’03 application, which led to these aminoalcohols (WO2005056562).

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US20060270672

Posted by kinasepro on December 1, 2006

Hi Boehringer Ingelhiem, KP likes the BI piperidines/ pyran / cyclohexyl wrinkle on the quinazoline EGF compound series. More derivatives in this continuation, otherwise nothing much to see here.

Move along.

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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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