Wista Laboratories Ltd.

Michael Simpson

John Mervyn David Storey

James Peter Sinclair

Colin Marshall

Scott Clunas

Claude Michel Wischik

Charles Robert Harrington

Janet Elizabeth Rickard

David Horsley

Thomas Craven Baddeley

Karrar Ahmad Khan

Craig Williamson

Christopher Paul Larch

Ahtsham Ishaq

Barry Alan Wood

Yin Sze Loh

Sarah Louise Nicoll

Steven John Kemp

Helen Sarah Gibbard

John Mervyn Storey

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 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

The invention relates to compounds of general formula (I): wherein: each of Rand Ris independently selected from: &#x2014;H, Calkyl, Calkenyl, and halogenated Calkyl; each of Rand Ris independently selected from: &#x2014;H, Calkyl, Calkenyl, and halogenated Calkyl; each of R7NA and R7NB is independently selected from: &#x2014;H, Calkyl, Calkenyl, and halogenated Calkyl; and wherein: each of Rand Ris independently selected from: Calkyl, halogenated Calkyl, and Caryl; or Rand Rare linked to form a group selected from: Calkylene and Carylene; and pharmaceutically acceptable salts thereof, which are useful in the treatment of, for example, Alzheimer's disease. In other aspects the invention also relates to novel formulations of 3,7-diamino-10H-phenothiazinium salts. 

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Old Aberdeen, United Kingdom

Michael Simpson