KinasePro

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

Archive for the ‘Phase III’ Category

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 »

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 »

Correction

Posted by kinasepro on July 18, 2007

Pfizer’s Jak3 inhibitor CP-690,550 was described earlier listed as Ph ii-iii. For some reason that was changed, and all of its furthest advanced trials are Phase 2.

Posted in JAK, Phase III | 1 Comment »

I don’t know’s on third

Posted by kinasepro on June 19, 2007

Because? oh he’s centerfield…

So TM asked for it, and while most of these are scatterred about the site… It’s not such a bad idea to have all the not-yet-approved kinase inhibitors currently active in US phase three clinical trials here in one place:

In a maybe-not-so-chronoligical order: Arxxant, Enzastaurin, Recentin, Zactima, Axitinib, Motesanib, CP-690,550, Pazopanib, and Tasigna.

Missing any?

Posted in Phase III | 7 Comments »

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 »

Pazopanib

Posted by kinasepro on June 19, 2007

aka GW-786034 is GSK’s ‘pan Vegfr’ inhibitor:

O=S(C1=CC(NC2=NC=CC(N(C)C3=CC4=NN(C(C)=C4C=C3)C)=N2)=CC=C1C)(N)=O

salt: hydrochloride
some chemistry here.
clinic: ph iii: RCC, WO/2002/05911

Posted in GSK, Phase III, 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 »

Axitinib

Posted by kinasepro on June 19, 2007

aka AG-013736 is a Pfizer Vegf / c-FMS compound via Agouron.

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

Salt: Tosylate?
Clinic Ph iii: Pancreatic Cancer
WO/2001/002369; process app; ‘06 Asco,

Posted in c-fms, Pfizer, Phase III, VEGF | Leave a Comment »

Zactima

Posted by kinasepro on June 19, 2007

aka vandetanib, ZD-6474 is Astra’s Vegf / EGF doublet inhbitor.

CN1CCC(CC1)COC2=CC3=NC=NC(NC4=CC=C(C=C4F)Br)=C3C=C2OC

wiki, clinic, WO/2001/032651

Posted in Astra, EGF, Phase III, VEGF | 1 Comment »

Recentin

Posted by kinasepro on June 19, 2007

aka cediranib, AZD-2171 is Astra’s Vegfr-1 & 2 inihbitor.

COC1=CC2=C(OC3=C(F)C4=C(NC(C)=C4)C=C3)N=CN=C2C=C1OCCCN5CCCC5

wiki; Clinic: a, b, c
WO/2000/047212

Posted in Astra, Phase III, VEGF | Leave a Comment »