Abstract: Compounds of Formula I are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathsepsin D. The compounds are useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is a heterocycle, amide, sulfonamide or carbamate and Z is an acyl or a functionalized acyl. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid phase support, are also disclosed.

Abstract: Azaspirononanes of formula I and their synthesis are disclosed. The compounds are useful as templates for constructing synthetic receptors and as intermediates in the synthesis of enzyme inhibitors. They are prepared by an intramolecular ylide cycloaddition of a 6-hydrazone of 2,10-undecadienoic acid ester.

Abstract: Compounds of Formula I ##STR1## 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.

Abstract: Compounds of Formula I are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathsepsin D. The compounds are useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is a heterocycle, amide, sulfonamide or carbamate and Z is an acyl or a functionalized acyl. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid phase support, are also disclosed.

Abstract: Combinatorial chemical libraries of the Formula [S]-C(O)-L'-Z containing dihyroxy amides and hydroxyphosphonate amides are disclosed, in which [S] represents a solid support and -L'-Z is a linker/ligand residue. In these libraries, Z is ##STR1## and Y is --P(O)(OR.sup.6)(OR.sup.7), --CH(OH)--COR.sup.8, --CH.sub.2 CH.dbd.CH.sub.2 --CH.sub.2 CH(OH)CH.sub.2 OH, --CH.sub.2 CHO, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 OC(O)NHR.sup.26, --CH.sub.2 CH.sub.2 NR.sup.27 R.sup.28, or ##STR2## The combinatorial libraries are optionally encoded with tags. The use of these libraries in assays to discover biologically active compounds is also disclosed.

Abstract: Combinatorial chemical libraries of Formula I ##STR1## and methods for their preparation are disclosed. The libraries allow one to screen large numbers of compounds for a desired biological activity with relative ease. The libraries may be tagged or untagged. In preferred libraries, Y is the residue of an N-acylated amino acid, a substituted 4-aminoproline or a substituted piperazinealkanoic acid. The use of the libraries to discover biologically active compounds is also disclosed.

Abstract: Compounds of Formula I ##STR1## 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.

Abstract: Combinatorial chemical libraries of the Formula ?S!-C(O)-L'-Z containing biaryl amino acids are disclosed, in which ?S! represents a solid support and -L'-Z is a linker/compound residue. In these libraries, Z is --NR.sup.1 R.sup.2. R.sup.1 is chosen from H, C.sub.1 to C.sub.20 hydrocarbon, heteroaralkyl, heterocycloalkyl, substituted arylalkyl, alkoxyalkyl or alkyl-SO.sub.2 NH-alkyl and R.sup.4 is an acyl or sulfonyl residue. R.sup.2 is chosen from ##STR1## The combinatorial libraries are optionally encoded with tags. The use of these libraries in assays to discover biologically active compounds is also disclosed.

Abstract: Compounds of Formula I ##STR1## are disclosed as inhibitors of plasmepsin and cathepsin D. The compounds are therefore useful to treat diseases such as malaria. In preferred compounds of formula I, Y is the residue of an N-acylated amino acid, a substituted 4-aminoproline or a substituted piperazinealkanoic acid. Intermediates in the solid phase synthesis of compounds of formula I, in which the compounds are attached to a solid support, are also disclosed.

Abstract: Compounds of Formula I ##STR1## are disclosed as inhibitors of plasmepsin and cathepsin D. The compounds are therefore useful to treat diseases such as malaria. In preferred compounds of formula I, Y is the residue of an N-acylated amino acid, a substituted 4-aminoproline or a substituted piperazinealkanoic acid. Intermediates in the solid phase synthesis of compounds of formula I, in which the compounds are attached to a solid support, are also disclosed.

Abstract: Compounds of Formula I ##STR1## are disclosed as inhibitors of plasmepsin and cathepsin D. The compounds are therefore useful to treat diseases such as malaria. In preferred compounds of formula I, Y is the residue of an N-acylated amino acid, a substituted 4-aminoproline or a substituted piperazinealkanoic acid. Intermediates in the solid phase synthesis of compounds of formula I, in which the compounds are attached to a solid support, are also disclosed.