Pharmacopeia Inc.

Cullen Lee Cavallaro

Roland Ellwood Dolle

Timothee Felix Herpin

Yvonne Class Shimshock

Combinatorial chemical libraries of the Formula &lsqb;S&rsqb;&mdash;C(O)&mdash;L&prime;&mdash;Z containing dihyroxy amides and hydroxyphosphonate amides are disclosed, in which &lsqb;S&rsqb; represents a solid support and &mdash;L&prime;&mdash;Z is a linker/ligand residue. In these libraries, Z is

Process for preparing combinatorial amide alcohol libraries

A combinatorial chemical library comprising a plurality of members of the Formula &lsqb;S&rsqb;&mdash;C(O)&mdash;L&prime;-Z containing hydroxyamides is disclosed, in which &lsqb;S&rsqb; represents a solid support and L&prime;-Z is a linker/compound residue. In this library, Z is

Combinatorial library of substituted statine esters and amides via a novel acid-catalyzed rearrangement

Hydroxypropylamide peptidomimetics as inhibitors of aspartyl proteases

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.

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.

Growing community of inventors

Hightstown, NJ, United States of America

Cullen Lee Cavallaro