KinasePro

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

Archive for the ‘VEGF’ Category

BAY 73-4506

Posted by kinasepro on May 20, 2009

So Bayer is in Ph2 with fluoro-sorafenib aka DAST, BAY-734506… Only this time they’re in without Onyx and I gather Onyx is none too happy about this.

BAY-734506The distinct compound is claimed in WO/2005/009961 and the I believe the original Sorafenib app is: WO/2000/042012.  What strikes the chemist inventor about a structure like this isn’t usually about who owns it, but if it can really be considered a new invention? The claim structure in the 2000 Sorafenib application can be schematized:

sorafenib-claimsSo for the purpose of this discussion the only meaningful definition is the ring designated as “L” and whether or not they claim the fluoride:

L-definedAnyhow while this structure and their priority date may be vulnerable to obviousness, all of these applications are assigned to Bayer, and not Onyx, so that disagreement will more likely be resolved based on the wording of the Onyx / Bayer contract.  The Onyx press release suggests this very structure was discovered during the collaboration…  We’ll see.  Given the timing I bet someone saw the structure here on Kinasepro and told Onyx, heh.

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Posted in Bayer, RAF, VEGF | 5 Comments »

DAST (BAY 73-4506)

Posted by kinasepro on April 7, 2009

It’s Bayer’s Ph2 follow-on to Sorafenib.  VEGF / RAF yadda yadda… Don’t have the structure, but maybe it’s one of these:

O=C(C1=NC=CC(OCC2=C(Cl)C(NC(NC3=CC(C(C)(C)C)=NN3C4=CC=CC(CO)=C4)=O)=CS2)=C1)NC.O=C(C5=NC=CC(OC6=CC=C(NC(NC7=CC=C(Cl)C(C(F)(F)F)=C7)=O)C(F)=C6)=C5)NC

from polymorph apps:

WO/2008/058644 –            WO/2008/079968
WO/2008/043446 –            WO/2008/079972

& yeh, that is Fluoro-Nexavar…

Posted in Bayer, c-Kit, PDGFR, RAF, VEGF | Leave a Comment »

E-7080

Posted by kinasepro on March 24, 2009

Eisai’s Ph1 VEGF inhibitor

O=C(N)C1=CC2=C(C=CN=C2C=C1OC)OC3=CC=C(C(Cl)=C3)NC(NC4CC4)=O

Posted in Eisai, VEGF | Leave a Comment »

AV-951

Posted by kinasepro on March 23, 2009

Aveo’s Vegf inhibitor; currently Ph ii in RCC & NSCLC;

O=C(NC1=CC=C(C=C1Cl)OC2=C3C=C(C(OC)=CC3=NC=C2)OC)NC4=NOC(C)=C4

Formerly KRN-951 & pM against 1, 2, & 3

Posted in VEGF | 5 Comments »

ABT-869

Posted by kinasepro on March 18, 2009

Vegf, Etc – Boring & Healthy…Tons of Ph2s in HCC but is it better then Sorafenib?

O=C(NC1=CC=C(C=C1)C2=CC=CC3=C2C(N)=NN3)NC4=CC(C)=CC=C4Fno news is good news?

previously

Posted in Abbott, Genentech, TIE2, VEGF | Leave a Comment »

AEE-788

Posted by kinasepro on March 16, 2009

aka: NVP-AEE788 is Novartis’ VEGF / EGF ‘Nib (&src, &flt, etc.) in Ph1 for the last 6 years… and unceremoniously off the pipeline.

C[C@H](C1=CC=CC=C1)NC2=C3C(NC(C4=CC=C(C=C4)CN5CCN(CC5)CC)=C3)=NC=N2

Cancer Res

Posted in EGF, Novartis, VEGF | Leave a Comment »

Motesanib: A little too good.

Posted by kinasepro on November 20, 2008

Looks like this one might be coming off the ph3 list

O=C(NC1=CC=C(C(C)(C)CN2)C2=C1)C3=CC=CN=C3N([H])CC4=CC=NC=C4

Motesanib‘s got “higher early mortality rates

Posted in Amgen, VEGF | 15 Comments »

PDB Update

Posted by kinasepro on October 7, 2008

Buncha-new Plk1 PDB’s

Plk1: 3DBF, 3DBE, 3DBD, 3DBC, 3DB8

new c-Met: 3EFK, 3EFJ

new Vegf: 3CJG, 3CJF

Posted in c-Met, PDB, Plk1, VEGF | Leave a Comment »

PDB Update

Posted by kinasepro on September 18, 2007

Big week

2QOH; PPY-A bound to Abl via Ariad; Chem Biol Drug Des
2Z60; PPY-A bound to T315I Abl

O=C(C1=CC(C2=CN=C(NC=C3C4=CC=CC=C4OC)C3=C2)=CN=C1)N(C)C

(compounds from SGX)

2OH4; Benzimidazole bound to VEGF via GSK JP; J Med Chem

2V7A; PHA-739358 bound to T315I mutant of Abl via Nerviano; Cancer Res

2IN6 Wee1
2IO6 Wee1

Posted in bcr abl, PDB, VEGF | 5 Comments »

Schering’s Macrocycles

Posted by kinasepro on July 20, 2007

Aurora Eh? What can I say, I like’m: WO/2007/079982

BrC(C=N1)=C2N=C1NC3=CC=C(S(C)(=O)=NC(NCC)=O)C(NCCCCN2)=C3

Related series, complete w/ a Chem Med Chem.

Posted in Aurora, multi-target, Schering AG, VEGF | 12 Comments »