KinasePro

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Archive for the ‘Amgen’ Category

AMG-900

Posted by kinasepro on June 28, 2009

It’s a Ph1 Aurora A/B/C inhibitor for ‘solid tumors’.  Seems likely to be a member of one of the phthalazine series’ WO/2008/124083, WO/2008/057280, WO/2007/100646, or WO/2007/087276.

COC1=CC2=NC=CC(OC3=CC=C(NC(N=N4)=C5C=CC=CC5=C4C6=CC=CC=C6)C=C3)=C2C=C1OCpreviously…

Posted in Amgen, Aurora | 2 Comments »

Amgen: Us too.

Posted by kinasepro on May 14, 2009

As a comment in another thread notes, they have a handful of these too.  The regioismer is the novelty factor:

WO/2008/008539 / US2009012461 / 3CD8 / J Med Chem

COC1=CC2=NC=CC(OCC3=NN=C4C=CC(C5=CC=CC=C5)=NN43)=C2C=C1

amg-cmet-i

Posted in Amgen, c-Met | Leave a Comment »

AMG-458

Posted by kinasepro on March 18, 2009

Here’s one where they do tell us why its off the pipeline:

COC1=CC2=C(C(OC3=CC=C(N=C3)NC(C4=C(C)N(N(C4=O)C5=CC=CC=C5)CC(O)(C)C)=O)=CC=N2)C=C1

J Med Chem -> Chem Res Tox

Read the rest of this entry »

Posted in Amgen, c-Met | 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 »

Amgen ‘n Aurora

Posted by kinasepro on August 2, 2007

WO/2007/087276? How ’bout that.

CC1=CSC(C2=C3C=CC=CC3=C(N=N2)NC4=CC=C(N=C4)OC5=NC=CC=C5C6=NC(N)=NC=C6)=C1

Posted in Amgen, Aurora | 4 Comments »

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 »

Amgen all TIE2d up?

Posted by kinasepro on March 12, 2007

They describe Tie2 and LCK assays in a number of new apps, but it wouldn’t surprise me to learn a handful of other kinases were running in fear at the site of these things.

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app is US20070054916

They’ve also got a C-Met application this week with US20070054903:

O=C(C1=CC=CS1)NC2=CC=C3C=C(C4=CC=CC5=C(NCCCN(C)C)N=CC=C45)C=CC3=C2

Posted in Amgen, c-Met, Lck, TIE2 | 1 Comment »

Amgen ‘n’ IRAK-4

Posted by kinasepro on February 20, 2007

Irak-4? Yah I never heard of it either, but the IRAKs appear to be immunology targets for which Amgen is way out in front. They’ve got a nice paper in Structure, a Biorg. Med. Chem. Lett., and 2 PDB’s: 2NRU, 2NRY.

At first look I was mesmerized by the tyrosine gatekeeper but a second glance on looking over the recent CIP: US20070037803 shows something interesting.

O=C(C1=CC(C(F)(F)F)=CC=C1)\N=C2N([C@@H]3CC[C@@H](O)CC3)C4=CC=C(OCCN5CCOCC5)C=C4N/2

they suggest as much in the BMCL. Read the rest of this entry »

Posted in Amgen, IRAK | 1 Comment »

PDB Update

Posted by kinasepro on December 12, 2006

The highlight is GSK’s SB-590885 bound to B-Raf: 2FB8 (They describe the oxime as a phenol isostere)

O\N=C1CCC2=C/1C=CC(C(N=C(C3=CC=C(OCCN(C)C)C=C3)N4)=C4C5=CC=NC=C5)=C2

Also, Amgen released the structurally interesting IRAK-4 bound to staurosporine (2NRY), and a benzimidazole inhibitor (2NRU). The Bioorg Med Chem Lett came out in March and the Xray is featured in this Structure paper.

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The tyrosine gatekeeper is certainly different

Looks like there’s an indolinone lodged in today’s update as well. 2JAV replaces 2CL1, dunno why, probably some sort of refinement. NEK2 ne1?

Posted in Amgen, GSK, IRAK, PDB, RAF | Leave a Comment »

AMG706

Posted by kinasepro on November 6, 2006

Update>> They named it: Motesanib diphosphate

Xcovery has the roundup on AMG706. I tend to think it’s a little apples and oranges to try and line it up against Sutent at this point. Heck it’s been nearly a year since release and noones come out and said Sutent is really any better then Nexavar.

The compound is second generation to ptk787; a VEGF inhibitor which failed to meet a Phase III endpoint.

There’s an article on the preclinical stuff: Cancer Research (2006), 66(17), 8715

Frankly KP is shocked that noone has yet published an application claiming the Bayer modification, woops scratch that, looks like Bayer has an application floating around: WO2006002383, but they don’t have the magic indoline.

ClC(C=C1)=CC=C1NC2=NN=C(C3=C2C=CC=C3)CC4=C=NC=C4 O=C(NC1=CC(NCC2(C)C)=C2C=C1)C(C=CC=N3)=C3NCC4=CC=NC=C4 O=C(C1=NC=CC(CNC2=CC=CC=C2C(NC3=CC=C(OC(F)(F)O4)C4=C3)=O)=C1)NC5CC5

Posted in Amgen, clinical, VEGF | 1 Comment »