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

Archive for the ‘VEGF’ Category


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…


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 »


Posted by kinasepro on June 19, 2007

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


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

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


Posted by kinasepro on June 19, 2007

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


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

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


Posted by kinasepro on June 19, 2007

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


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 »


Posted by kinasepro on June 19, 2007

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


wiki, clinic, WO/2001/032651

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


Posted by kinasepro on June 19, 2007

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


wiki; Clinic: a, b, c

Posted in Astra, Phase III, VEGF | 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.


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 »


Posted by kinasepro on May 29, 2007


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 »


Posted by kinasepro on May 28, 2007


Lestaurtinib / CEP-701 is currently in trials for a handful of indications and first appeared in WO/1988/07045 (US,4,923,986) via Kyowa Hakko Kogyo. The series was first described as a group of PKC inhibitors, but later came this ’98 press release: (emphasis mine)

CEP-701 is one of a series of specific receptor trk kinase inhibitor derived from the indolocarbazole K252a, which was originally synthesized by Kyowa Hakko Kogyo Co., Ltd., Tokyo, Japan

Read the rest of this entry »

Posted in c-Met, Cephalon, Flt3, JAK, Trk, VEGF | 3 Comments »


Posted by kinasepro on May 13, 2007

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


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

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