Hydroxyphosphonate peptidomimetics as inhibitors of aspartyl proteases

Compounds of Formula I are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathepsin D. The compounds are therefore useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is an dialkoxyphosphonate,...

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Bibliographische Detailangaben
Hauptverfasser:	DOLLE, III, ROLAND ELLWOOD, SHIMSHOCK, YVONNE CLASS, HERPIN, TIMOTHEE FELIX, CARROLL, CAROLYN DIIANNI
Format:	Patent
Sprache:	eng
Schlagworte:	ACYCLIC OR CARBOCYCLIC COMPOUNDS ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM CHEMISTRY COMPOSITIONS BASED THEREON HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVINGCARBON-TO-CARBON UNSATURATED BONDS MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY ORGANIC MACROMOLECULAR COMPOUNDS PEPTIDES PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES THEIR PREPARATION OR CHEMICAL WORKING-UP
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Beschreibung
Zusammenfassung:	Compounds of Formula I are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathepsin D. The compounds are therefore useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is an dialkoxyphosphonate, or alpha -hydroxyamide group and Z is an acyl or alpha -ketocarbamate functionality. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid support, are also disclosed.