University of Pennsylvania

Paul A Sprengeler

Ralph F Hirschmann

Amos B Smith, Iii

Ellen Leahy

Terence Keenan

Akihisa Yokoyama

Ryan C Holcomb

Mark Guzman

John L Wood

Wenqing Yao

Kyriacos Costa Nicolaou

David R Jones

Paul S Anderson

Barry S Cooperman

Catherine D Strader

Alison L Fisher

Alexander Pasternak

P Grant Spoors

Setsuya Sasho

Paul Laub

Rachel D Van Rijn

Shrikumar Nair

Maria A Cichy-Knight

John Hynes, Jr

T R Reisine

Sherrie Pietranico-Cole

Sherrie Pietranico

Joseph M Salvino

Bari A Barwis

David A Favor

Thomas Nittoli

William C Shakespeare

Andrew B Benowitz

Polypyrrolinone based inhibitors of matrix metalloproteases

Compounds are provided which are crossreactive with peptides such as those which bind G-protein-linked receptors, together with preparative and therapeutic methods therefor. The compounds have the general structure:

Non-peptide peptidomimetics

Synthetic methods for pyrrolinone-based compounds are provided. Such compounds mimic or inhibit the biological and/or chemical activity of peptides.

Oxazolidinones and methods for the synthesis and use of same

The invention relates to compositions which are useful for inhibiting ribonucleotide reductase enzymes, including the mammalian ribonucleotide reductase enzyme. The compositions include, but are not limited to, linear peptides, cyclic peptides, peptide analogs, and peptidomimetics. Methods of using the compositions of the invention to treat cancer and viral and bacterial infections are disclosed.

Peptides peptide analogs peptidomimetics and other small molecules

This invention relates to chemical compounds that contain adjacent carbonyl groups, which effectively inhibit the biological, chemical, and/or physical properties of enzymes and other medicinally-significant proteins. In particular, the invention relates to dicarbonyl compounds that are capable of acting as enzyme inhibitors, including irreversible inhibitors of HIV-1 protease.

Dicarbonyl-containing compounds

Compounds are provided which are crossreactive with peptides such as those bound by G-protein-linked receptors, together with preparative and therapeutic methods therefor. The compounds have the general structure: ##STR1## wherein at least one of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 or R.sub.6 comprises a chemical functional group which causes the compounds to be crossreactive with the peptide of interest.

Alicyclic peptidomimetics

Compounds are provided which are crossreactive with peptides such as those which bind G-protein-linked receptors, together with preparative and therapeutic methods therefor.

Non-peptide peptidomimetics and related cyclic hexapeptides

Novel pyrrolinone-based compounds mimic or inhibit the biological and/or chemical activity of peptides, including peptide .beta.-strand conformations. Certain compounds contain functionalized pyrrolinone units in place of one or more amino acids of a target peptide.

Pyrrolinone-based peptidomimetics

2-Hydroxy-3-aminopropylsulfonamides are provided along with methods for synthesizing and using such compounds, and chemical intermediates employed in the synthetic methods.

2-Hydroxy-3-aminopropylsulfonamides

Compounds are provided which are crossreactive with peptides such as those which bind G-protein-linked receptors, together with preparative and therapeutic methods therefor. The compounds have the general structure: ##STR1## wherein at least one of R.sub.1, R.sub.2, R.sub.3, R.sub.4, or R.sub.5 comprises a functional group which is chemically similar to that found in the peptide of interest.

Non-Peptide peptidomimetics

Methods are provided for using 2-hydroxy-3-aminopropylsulfonamides to mimic peptides and to modulate the chemical and/or biological activity of enzymes, particularly proteolytic enzymes. Also provided are compositions comprising the sulfonamides in admixture with a pharmaceutically acceptable carrier, adjuvant, or vehicle.

Sulfonamide-based compositions and methods

This invention relates to monomeric and polymeric pyrrolinone-based compounds, to the use of pyrrolinone-based compounds in place of amino acids in naturally-occurring or synthetic peptides, and to methods for preparing such compounds.

Pyrrolinone-based compounds

Aromatic peptidomimetics

Growing community of inventors

El Granada, CA, United States of America

Paul A Sprengeler