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.
Type:
Grant
Filed:
December 8, 1997
Date of Patent:
April 6, 1999
Assignee:
Pharmacopeia, Inc.
Inventors:
Roland Ellwood Dolle, III, Hitesh K. Patel
Abstract: A method and apparatus is provided for the generation and representation of chemical libraries. More particularly, a computer-implemented method and apparatus is provided for the generation and representation of combinatorial chemistry libraries.
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.
Type:
Grant
Filed:
December 8, 1997
Date of Patent:
February 16, 1999
Assignee:
Pharmacopeia, Inc.
Inventors:
Roland Ellwood Dolle, III, Hitesh K. Patel, Theodore O. Johnson, Jr., Carolyn DiIanni Carroll, Shiwei Tao