Progen Pharmaceuticals, Inc.

The Australian National University

Alchemia Limited

Ligong Liu

Tomislav Karoli

Vito Ferro

Jon Krueger Fairweather

Christopher Richard Parish

Michael Leo West

Wim F Meutermans

Craig Geoffrey Freeman

Tracie E Ramsdale

Martin Gerhardt Banwell

Giovanni Abbenante

Giang Thanh Le

Kenneth David Johnstone

Norbert Wimmer

Edward Timothy Hammond

Peter Andrews

Paul Newton Handley

Chris Clark

Giovani Abbenante

Wim Meutermans

Tracie Elizabeth Ramsdale

The invention relates to novel compounds that have utility as inhibitors of heparan sulfate-binding proteins; compositions comprising the compounds, and use of the compounds and compositions thereof for the antiangiogenic, antimetastatic, anti-inflammatory, antimicrobial, anticoagulant and/or antithrombotic treatment of a mammalian subject.

Sulfated oligosaccharide derivatives

New compounds and methods for the preparation of combinatorial libraries of potentially biologically active compounds are based on monosaccharides of formula I being a derivative of a furanose or pyranose form of a monosaccharide, .

Derivatives of monosaccharides for drug discovery

The invention relates to compounds which are polysulfated oligosaccharide derivatives having activity as inhibitors of heparan sulfate-binding proteins and inhibitors of the enzyme heparanase; methods for the preparation of the compounds; compositions comprising the compounds, and use of the compounds and compositions thereof for the antiangiogenic, antimetastatic, anti-inflammatory, antimicrobial, anticoagulant and/or antithrombotic treatment, lowering of blood triglyceride levels and inhibition of cardiovascular disease of a mammalian subject.

The invention relates to compounds of the following formula (I). In these compounds, R, R, Rand Rare each independently a substituted or unsubstituted cyclitol with a ring comprising six carbon atoms, or hydrogen, substituted or unsubstituted alkyl, cycloalkyl, aryl, acyl, alkyloxycarbonyl, or alkylaminocarbonyl. At least two of R, R, Rand Rcomprise the substituted or unsubstituted cyclitol. The linker can be any one of the following: &#x2014;(CH)&#x2014;, &#x2014;(CH)&#x2014;CH&#x2014;(CH)&#x2014;, &#x2014;(CH)&#x2014;NR&#x2014;(CH)&#x2014;, and &#x2014;(CH)&#x2014;HCR&#x2014;(CH)&#x2014;; wherein: w, x, y and z are independently an integer having a value of 0&#x2013;10; Ris a substituted or unsubstituted cyclitol with a ring comprising six carbon atoms; and, Ris &#x2014;OH, &#x2014;OSONa, &#x2014;OSONa substituted with alkyl, cycloalkyl or aryl, or substituted or unsubstituted alkyl, cycloalkyl or aryl. The compounds can also include substituted or unsubstituted cyclitol carbamides with the linker bond at the carbamide nitrogen. In other embodiments, the invention provides pharmaceutical compositions which include the compounds, and use of the compounds in the prevention or treatment in a mammalian subject of a disorder resulting from angiogenesis, metastasis, inflammation and/or coagulation/thrombosis 

Linked cyclitols and their polysulfated derivatives

Growing community of inventors

Sunnybank, Australia

Ligong Liu