Wista Laboratories Ltd.

Christopher Paul Larch

John Mervyn David Storey

James Peter Sinclair

Colin Marshall

Scott Clunas

Craig Williamson

Michael Simpson

Claude Michel Wischik

Charles Robert Harrington

Janet Elizabeth Rickard

David Horsley

Thomas Craven Baddeley

Karrar Ahmad Khan

Ahtsham Ishaq

Barry Alan Wood

Yin Sze Loh

Sarah Louise Nicoll

Steven John Kemp

John Mervyn Storey

Helen Sarah Gibbard

Michel Wischik Claude

Disclosed are compounds of general formula (I): and pharmaceutically acceptable salts thereof, formulations, methods and uses in, for example, the treatment of disease.

Phenothiazine diaminium salts and their use

The present invention pertains generally to the field of chemical synthesis, and more particularly to methods for the chemical synthesis of a thiosulfonic acid of Formula (1) by a step of periodate mediated oxidative coupling of a thiosulfonic acid of Formula (2) with an aniline of Formula (3), as described herein. The present invention also relates to such methods which incorporate one or more additional (subsequent and/or preceding) steps, for example, to prepare compounds of Formula (5) from compounds of Formula (1); to prepare compounds of Formula (6) from compounds of Formula (5); and to prepare compounds of Formula (2) from compounds of Formula (4), as described herein. 

Synthesis of a thiosulfonic acid by a step of periodate mediated oxidative coupling of a thiosulfonic acid with an aniline

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

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

Christopher Paul Larch