Wista Laboratories Ltd.

Steven John Kemp

John Mervyn David Storey

Colin Marshall

Scott Clunas

Christopher Paul Larch

John Mervyn Storey

Claude Michel Wischik

James Peter Sinclair

Charles Robert Harrington

Janet Elizabeth Rickard

Tobias Heinrich

Craig Williamson

Michael Simpson

Sarah Louise Nicoll

Helen Sarah Gibbard

Lynda Jane Storey

Tobias Kerst Heinrich

The present invention pertains generally to the field of chemical synthesis, and more particularly to methods of chemical synthesis which include the step of preparing a substituted 10H-phenothiazine-3,7-diamine compound of Formula (1) by a step of selective alkylation by reductive amination, in which the corresponding unsubstituted diamine of Formula (4) is reacted with aldehyde/ketone, under reductive amination conditions. The present invention also relates to such methods which incorporate additional subsequent and/or preceding steps, for example, to prepare compounds of Formulae (2) and (3) from compounds of Formula (1), and to prepare compounds of Formula (4) from, for example, compounds of Formulae (5), (6), (7), (8), and (9). Compounds of Formula (1), Formula (2), and Formula (3) are useful, for example, in the treatment of diseases of protein aggregation, such as Alzheimer's disease.

Methods of chemical synthesis of substituted 10H-phenothiazine-3,7-diamine compounds

Provided are certain benzothiazole, imidazothiazole, imidazopyrimidine and imidazopyridine compounds, including, for example: formula (I) and pharmaceutically and physiologically acceptable salts, hydrates, and solvates thereof. Such compounds can be used as diagnostic ligands or labels of tau protein and PHF. 

Ligands for aggregated tau molecules

Described are methods of synthesizing and purifying certain 3,7-diamino-phenothiazin-5-ium compounds (referred to herein as 'diaminophenothiazinium compounds') including Methylhioninium Chloride (MTC) (also known as Methylene Blue). In one embodiment, the method comprises the steps of, in order: a thiosulfonic acid formation (TSAF); an oxidative coupling (OC); and a ring closure (RC). Also described are resulting compounds and compositions comprising them (e.g., tablets, capsules) for use in methods of medical treatment and diagnosis, etc., for example, for tauopathies, or Alzheimer's disease (AD). 

Methods of chemical synthesis of diaminophenothiazinium compounds involving the use of persulfate oxidants

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Old Aberdeen, United Kingdom

Steven John Kemp