University of Pittsburgh

Beijing University of Technology

The University of Melbourne

Maree Patricia Collis

Alan Duncan Robertson

Dennis Patrick Curran

William Roy Jackson

Hui C Liu

Bevyn Jarrott

Alastair George Stewart

Philip Mark Beart

Vijaya Bhaskar Kenche

Phillip Mark Beart

David James McAllister

Alexandra Papanikos

A conjugated prodrug of an estradiol compound conjugated to a biological activity modifying agent.

Estradiol conjugates and uses thereof

This invention relates to compounds to formula (1) wherein B is optionally substituted aryl; Rand Rare the same or different and are independently selected from hydrogen or Calkyl; n is 1 or 2, preferably n is 1; m is 0 or 1; Ris hydrogen or acyl, Rand Rare the same or different and are independently selected from amino, alkylamino, dialkylamino, arylamino and C-Ccycloalkylamino; X and Y are independently selected from C, H or N provided at least one of X and Y is N; and salts thereof, solvates thereof, pharmaceutically acceptable derivatives thereof, prodrugs thereof, tautomers thereof and/or isomers thereof, and processes for their reparation and methods of treatment, pharmaceutical formulations and uses involving them.

Pharmaceutical agents

Arylalkylpiperazine compounds as antioxidants

The present invention provides a short, convergent total synthesis of novel intermediates in the synthesis of (.+-.)-camptothecin and related compounds. The present synthesis scheme includes a novel 4+1 radical annulation followed by another cyclization to simultaneously assemble rings B and C of the camptothecin compound. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.

Intermediates in the synthesis of (.+-.)-camptothecin and related

The present method provides a short, convergent total synthesis of novel intermediates in the synthesis of (.+-.)-camptothecin and related compounds. The synthesis scheme includes a novel 4+1 radical annulation followed by another cyclization to simultaneously assemble rings B and C of the Camptothecin compound. In the synthesis, the following novel precursor is reacted with a phenyl isocyanide: ##STR1## The resulting tetracyclic intermediates comprise a quinoline fused to a pyrrolidine ring, with the pyrrolidine ring being fused to an alpha-pyridone ring. The tetracyclic intermediates thus comprise the A, B, C, and D rings characteristic of camptothecin and camptothecin derivatives, and are easily convertible to camptothecin and camptothecin derivatives via hydroxymethylation and oxidation.

Intermediates in the synthesis of (+) camptothecin and related compounds

Growing community of inventors

Prahran, Australia

Maree Patricia Collis