University of London

Queen Mary & Westfield College

Lesley Robson

Alice Caroline Sullivan

John Robert Howe Wilson

Siud Pui Man

Adina Michael-Titus

The invention relates to novel and known substituted phosphonates for use in ameliorating amyloid aggregates, particularly for use in the treatment of Alzheimer's disease. 

Substituted phosphonates and their use in decreasing amyloid aggregates

The invention relates to new compounds of formula (1) wherein R is hydrogen or a linear or branched Calkyl; where X is O, S, or NRwhere Ris a hydrogen, a linear or branched Calkyl, Calkenyl or Calkynyl group, an aryl, a heteroaryl or Calkylaryl or alkylheteroaryl group and where one or both of C and D is OR, SR, NRRwhere R, Rand Rare each independently hydrogen, a linear or branched Calkyl, Calkenyl or Calkynyl group, an aryl or Calkylaryl group or a linear or branched Calkyl NRRchain where Rand Rare each independently hydrogen, a linear or branched Calkyl; or an optionally complex metal ion M/n wherein n is an integer from 1 to 8; or where one or both of C and D are amino acids or nucleic acids attached via either N, O or S; and wherein m is an integer from 1 to 8; and wherein either: I) A is a known aryl or heteroaryl fluorescent group and B is hydrogen, a linear or branched Calkyl, Calkenyl or Calkynyl group, an aryl, a heteroaryl or Calkylaryl or alkylheteroaryl group or phosphonate P(O)(OR); II) B is a known aryl or heteroaryl fluorescent group and A is hydrogen, a linear or branched Calkyl, Calkenyl or Calkynyl group, an aryl, a heteroaryl or Calkylaryl or alkylheteroaryl group or a linear or branched Calkyl NRRchain, or a linear or branched Cmono or di ester Calkylphosphonate or a linear or branched Calkylphosphonic acid; III) Both A and B are known aryl or heteroaryl fluorescent groups. The compounds are useful as fluorescent sensors for metal cations and have the advantages of excellent water solubility, selectivity and sensitivity to a variety of metal cations even in the presence of high concentrations of CaNaand K, good cell permeability, flexible and simple syntheses, ease of attachment to polymers and bio-polymers to aid the identification of both chemical and biological processes as well as for assaying physiological samples and for the attachment to surfaces such as glasses, ceramics and apatites. 

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London, United Kingdom

Lesley Robson