KinasePro

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

Archive for the ‘PDGFR’ Category

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…

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

Masitinib

Posted by kinasepro on April 3, 2009

aka: Masivet, Kinavet & AB-1010 quietly joined the Phase iii club when it went Ph3 back in December.

O=C(NC1=CC=C(C)C(NC2=NC(C3=CC=CN=C3)=CS2)=C1)C4=CC=C(CN5CCN(C)CC5)C=C4

WO/2008/98949

Posted in c-Kit, gleevec, PDGFR, Phase III | 3 Comments »

MLN-518

Posted by kinasepro on April 1, 2009

aka Tandutinib is Takeda’s Ph2 FLT3, cKIT, PDGFR inhibitor Blood.

O=C(NC1=CC=C(C=C1)OC(C)C)N2CCN(CC2)C3=C4C=C(C(OCCCN5CCCCC5)=CC4=NC=N3)OC

Posted in Flt3, PDGFR, Takeda | Leave a Comment »

ABT-869

Posted by kinasepro on June 26, 2007

Phase 2 on the doorstep, Genentech and Abbott just announced a collaboration to include development of the compound w/ backups. No terms disclosed…

O=C(NC1=CC=C(C=C1)C2=CC=CC3=C2C(N)=NN3)NC4=CC(C)=CC=C4F

Vegf, Flt3, Tie2, c-FMS, Pdgf, c-kit yadda yadda

j med chem, blood, molec cancer ther., WO/2004/113304

Posted in Abbott, c-fms, Flt3, Genentech, PDGFR, TIE2, VEGF | Leave a Comment »

Motesanib

Posted by kinasepro on June 19, 2007

Motesanib diphosphate, AMG-706 hits: Vegfr1,2,3, c-kit, Pdgfr-b, and Ret

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

Salt: bisphosphonate
Clinic Ph iii: NSCLC
Cancer Res.; WO/2002/066470

Posted in Amgen, c-Kit, PDGFR, Phase III, VEGF | Leave a Comment »

E7080

Posted by kinasepro on May 29, 2007

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

US20070117842 is a polymorph application, and there’s been a fair amount of IP activity around the compound. Indications are its E7080: an oral PhI Vegf, FGF, Pdgf, C-Kit, etc compound which first touched down in WO/2004/080462.

Posted in c-Kit, Eisai, Fgf, PDGFR, VEGF | 2 Comments »

Axitinib

Posted by kinasepro on May 13, 2007

aka AG-013736 is Pfizer’s Vegf / PDGF / cKit inhibitor.

O=C(C1=CC=CC=C1SC2=CC3=C(C(/C=C/C4=NC=CC=C4)=NN3)C=C2)NC

’06 Asco, clinic: ph 2; process app; pct

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

DE102005015253

Posted by kinasepro on October 10, 2006

Hi Merck KgAa,

Yours is another one of those patent applications that has Kinaspro thinking “this has got to be covered somewhere, by someone”

So did Bayer/Onyx not exemplify the N-Me Carboxamide in their earlier work?

HoHoHo-
Derek Lowe-
Wont’ ya Go-

and… umm… well… Maybe you could just walk down the hall and poke someone in the eye for me?

No, I guess there’s no need for that, they did indeed claim a handful of disubstituted pryazoles. (RAF: WO199932106, WO199932110, WO199932111, and TrkA WO2005110994), Seems to Kinasepro that these partygoers are a few years late particularly when Merck is doing what Bayer did back in 1999, and BI did first with BIRB796 and then also later with (US6492529), hell even Kirin Beer has one of these: (WO2002088110)

Wait did someone say Kirin Beer?

So Merck think’s they’ve found a way around the Bayer patent estate, and must have some kind of PK / CYP / Drug-like-property / selectivity bump that’s not obvious. They’ve got something similar going on in: WO2006040056 where they are clearly looking at one-offs of Nexavar. You have to remember these are those Crazy-evil-genius-brilliant-German Merck types…

Hmmm, so what’s new in these patents? Well, one of the claims is on TIE2, and you can tell by the Markush they are only attempting to make very narrow claims around the two Pyrazole substituents. I didn’t translate all the structure names, but it appears there are a number of furans exemplified with a handful of other R group modifications. The one example they draw a structure for:

Of note Deciphera has 2 similar applications which published in July. WO2006071940, and WO2006081034 they are labelled VEGF/PDGF/Bcr-Abl applications


And the companies with advanced Angiogenesis programs that any potential candidate has to beat:

Bayer……… Check (http://www.nexavar.com)
Pfizer…….. Check (http://www.sutent.com/)
Astra-Zeneca.. Check (http://www.zactima.net/)
Genentech….. Check (http://www.avastin.com)
Bristol-Myers Squibb, Novartis, Glaxo, Roche, Amgen, Kirin Brewing Company, check, check, checkitty, check, check, check – yah, he did say Kirin Beer.

Posted in Merck DE, PDGFR, TIE2, VEGF | 3 Comments »

WO2006094600

Posted by kinasepro on October 4, 2006

Hello Crazy Germans, errr I mean Hi Merck KGaA.

While everyone else is making pyrimidines, quinazolines, and assorted one or two-offs here comes Merck with umm this:?

I guess they look a little like the CDK compounds from J. Med. Chem. 2006, 44, 4628, but not really.

Kinaspro’s German isn’t all that good, but it looks as though they too speak Kinese:

Posted in Merck DE, PDGFR, TIE2, VEGF | Leave a Comment »