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Archive for the ‘Novartis’ Category

AEW-541

Posted by kinasepro on March 16, 2009

aka: NVP-AEW541 is Novartis’ IGF1R ‘Nib been ’round a while, but its off the pipeline?

NC1=C2C(N([C@H]3C[C@H](CN4CCC4)C3)C=C2C5=CC=C(OCC6=CC=CC=C6)C=C5)=NC=N1

Org Proc Res Dev; ASCO, Nature, Gist, Cancer Cell

Posted in IGF, Novartis | 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 »

Chiron’s got Pim

Posted by kinasepro on September 4, 2008

WO/2008/106692 is Novartis’ Emeryville’s Pim1,2,3 < 1uM offering:

O=C(C1=C(N)C=CC(C2=CC(C(N(C)C)=O)=CC=C2F)=N1)NC3=C(N4C[C@@H](N)CCC4)C=CN=C3

Posted in Novartis, pim1 | 2 Comments »

Tasigna Approved

Posted by kinasepro on October 30, 2007

aka nilotinib, AMN-107 is a Novartis‘ follow-on to Gleevec now approved for CML.

O=C(C1=CC=C(C(NC2=NC=CC(C3=CC=CN=C3)=N2)=C1)C)NC4=CC(C(F)(F)F)=CC(N5C=C(N=C5)C)=C4

wiki; clinic; WO/2002/022597

Posted in Approved, bcr abl, gleevec, Novartis | 4 Comments »

Don’t abuse inventorship: Scientist

Posted by kinasepro on August 16, 2007

So a guy named Brian Druker wrote this piece on how Gleevec is overpriced, eh? Who is he? Well he appears to have written his own byline in case you hadn’t heard:

THE?

A quick googlification suggests he has plenty of nice things to say about Brian Druker and his role in Gleevec’s discovery… To his credit he does list Jürg Zimmermann (the named inventor on a series of patents starting with EP564409) as one of the ‘unsung heroes‘ in a history of Gleevec essay.

According to Zimmermann the discovery went something like this:

etc.

ht: spicy ip, via pharmalot

Posted in General Interest, gleevec, Novartis | 13 Comments »

Novartis ‘n’ PKC

Posted by kinasepro on June 25, 2007

PKC412 (Midostaurin)?

So staurosporine analogs are old news? Novartis has a 1 compound PKC application.

O=C(C(C1=CC(N2CCN(C)CC2)=CC(C(F)(F)F)=C1Cl)=C3C4=CNC5=C4C=CC=C5)NC3=O

US20070142401 / WO/2005/039549

Posted in Novartis, PKC | Leave a Comment »

Tasigna

Posted by kinasepro on June 19, 2007

aka nilotinib, AMN-107 is a Novartis’ follow-on to Gleevec.

O=C(NC1=CC(C(F)(F)F)=CC(N2C=C(C)N=C2)=C1)C3=CC=C(C)C(NC4=NC=CC(C5=CC=CN=C5)=N4)=C3

wiki; clinic; WO/2002/022597

Posted in c-Kit, gleevec, Novartis, Phase III | Leave a Comment »

Subtle… Interesting… and thoroughly Swiss

Posted by kinasepro on June 13, 2007

WO/2007/062805 is a ‘multi-target’ application from Novartis that tags the earlier WO/2006/050946 with the Gleevec H1.

O=C(NC1=CC=C(C)C(NC2=C3C(N(C4=CC=C(N5CCOCC5)C=C4)N=C3)=NC=N2)=C1)C6=CC=CC(C(F)(F)F)=C6

Claim 11 suggests a few targets on their minds in addition to the titled Vegf / Ephb4:

11. The use according to claim 10, where the protein kinase modulation responsive disease is one or more diseases selected from the group consisting of diseases, that respond to the inhibition of one or more protein tyrosine kinases selected from abl kinase, especially v-abl or c-abl kinase, kinases from the family of the src kinases, especially c-src kinase, b-raf (V599E) and/or especially RET-receptor kinase or Ephrin receptor kinases, or mutated forms thereof.

Posted in multi-target, Novartis, VEGF | 1 Comment »

Gleevec ®

Posted by kinasepro on April 8, 2007

Novartis mispells it ‘Glivec’ outside the US, but you can call it imatinib mesylate, STI-571, or even CGP-57148 if you like.

O=C(NC1=CC=C(C)C(NC2=NC=CC(C3=CC=CN=C3)=N2)=C1)C4=CC=C(CN5CCN(C)CC5)C=C4

Discovery: 1992, CIBA-Geigy, Crystallography played no role in the discovery.
US Approval: May 2001

wiki; FDA; PDB: Abl 1IEP; Abl 1OPJ; cKit 1T46; Syk 1XBB; Abl 2HYY; Src 2OIQ

Also inhibits: c-Kit, Pdgfr-a,  LCK

Posted in Approved, Novartis | Leave a Comment »

US20070049622

Posted by kinasepro on March 6, 2007

Novartis has a RAF entry in US20070049622 which looks to combine a few twists to with a familiar theme:

CN1C2=CC=C(OC3=CC(C4=NC=C(C(F)(F)F)N4)=NC=C3)C=C2N=C1NC5=CC=C(Cl)C(C(F)(F)F)=C5

Read the rest of this entry »

Posted in Novartis, RAF | 3 Comments »