Synonym:ENMD2076;ENMD2076;ENMD-2076.

IUPAC/ChemicalName:(E)-N-(5-methyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-2-styrylpyrimidin-4-amine.

InChiKey:BLQYVHBZHAISJM-CMDGGOBGSA-N

InChiCode:InChI=1S/C21H25N7/c1-16-14-20(26-25-16)23-19-15-21(28-12-10-27(2)11-13-28)24-18(22-19)9-8-17-6-4-3-5-7-17/h4-9,14-15H,10-13H2,1-2H3,(H2,22,23,24,25,26)/b9-8+

SMILESCode:CN1CCN(C2=CC(NC3=NNC(C)=C3)=NC(/C=C/C4=CC=CC=C4)=N2)CC1

TechnicalData

AdditionalInformation

ENMD-2076isanovelorally-active,AuroraA/angiogenickinaseinhibitorwithpotentactivityagainstAuroraAandmultipletyrosinekinaseslinkedtocancerandinflammatorydiseases.ENMD-2076isrelativelyselectivefortheAuroraAisoformincomparisontoAuroraB.Aurorakinasesarekeyregulatorsoftheprocessofmitosis,orcelldivision,andareoftenover-expressedinhumancancers.ENMD-2076exertsitseffectsthroughmultiplemechanismsofaction,includingantiproliferativeactivityandtheinhibitionofangiogenesis.ENMD-2076hasdemonstratedsignificant,dose-dependentpreclinicalactivityasasingleagent,includingtumorregression,inmultiplexenograftmodels(e.g.breast,colon,leukemia),aswellasactivitytowardsexvivo-treatedhumanleukemiapatientcells.ENMD-2076hascompletedaPhase1studyinpatientswithsolidtumorsandiscurrentlyinamulti-centerPhase2studyinovariancanceraswellasPhase1studiesinmultiplemyelomaandleukemia.ENMD-2076hasreceivedorphandrugdesignationfromtheUnitedStatesFoodandDrugAdmiNISTration(the“FDA”)forthetreatmentofovariancancer,multiplemyelomaandacutemyeloidleukemia(“AML”).IntheUnitedStates,theOrphanDrugActisintendedtoencouragecompaniestodeveloptherapiesforthetreatmentofdiseasesthataffectfewerthan200,000peopleinthiscountry.OrphandrugdesignationprovidesuswithsevenyearsofmarketexclusivitythatbeginsonceENMD-2076receivesFDAmarketingapproval.ItalsoprovidescertainfinancialincentivesthatcanhelpsupportthedevelopmentofENMD-2076.SeeEntreMed'sweb.
 
  
  

References

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