International Celery Development Alliance Pty. Ltd.

The University of Queensland

Alchemia Pty Ltd

Ross Peter McGeary

Desley Ethel Butters

Michael Wellesley Whitehouse

Craig Kendall Charles Davis

Kim Drummond Rainsford

Michael Christopher Powanda

Gregory Thomas Bourne

David P Fairlie

Mark Leslie Smythe

Robert C Reid

Karl Schafer

Istvan Toth

Karl Hansford

Wim Denis Frans Meutermans

Robert Falconer

Shaun Emmanuel De Cruz

Benjamin Paul Ross

Christopher I Clark

Martin J Stoermer

This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programs. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganising peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.

Synthesis of cyclic peptides

The invention relates to compounds which are useful in the delivery of a wide variety of therapeutically useful molecules. In particular, the invention relates to compounds which are able to act as carriers for therapeutically useful molecules, and to pharmaceutical agents comprising these carriers. The compounds of the invention comprise a mono- or oligosaccharide, a lipidic moiety, and optionally a linker and/or a spacer. The pharmaceutical agents of the invention are particularly useful for oral administration.

Delivery systems

The present invention relates generally to amino acid derivatives and to methods of making the same. In particular, the invention relates to compounds bearing a stereochemical identity, that is, the same stereochemistry, with the chiral &#x3b1;-carbon of D-&#x3b1;-amino acids and their use in methods of therapy, including the treatment of inflammatory diseases, and to compositions and enantiomeric mixtures containing them.

Compounds and inhibitors of phospholipases

Biologically active extracts of celery seed are produced by controlled ethanolic extraction, distillation and drying, and further processing by supercritical fluid extractions (SFE), and may be further fractionated by column fractionation, distillation, LiAlH reduction and the like. These extracts possess activity for the treatment and prevention of acute and chronic pain, inflammation and gastrointestinal irritation.

Extracts of celery seed for the prevention and treatment of pain, inflammation and gastrointestinal irritation

Biologically active extracts of celery seed are produced by controlled ethanolic extraction, distillation and drying, and further processing by supercritical fluid extractions (SFE), and may be further fractionated by column fractionation, distillation, LiAIH reduction and the like. These extracts possess activity for the treatment and prevention of acute and chronic pain, inflammation and gastrointestinal irritation.

Growing community of inventors

St. Lucia, Australia

Ross Peter McGeary