Wista Laboratories Ltd.

The University Court of the University of Aberdeen

Charles Robert Harrington

Janet Elizabeth Rickard

David Horsley

Claude Michel Wischik

John Mervyn David Storey

James Peter Sinclair

Colin Marshall

Thomas Craven Baddeley

Scott Clunas

John Mervyn Storey

Karrar Ahmad Khan

Craig Williamson

Michael Simpson

Ahtsham Ishaq

Barry Alan Wood

Yin Sze Loh

Christopher Paul Larch

Patricia Carol Edwards

Martin Roth

Aaron Klug

Damon Jude Wischik

Tobias Heinrich

Han Wan Tan

Steven John Kemp

Lynda Jane Storey

Franz Theuring

Karsten Stamer

Claudia Zabke

John M D Storey

Aaron King

Michel Wischik Claude

Tobias Kerst Heinrich

Described are methods of preparing reduced 3,7-diamino-10H-phenothiazine (DAPTZ) compounds of formula: wherein: Rand Rare independently selected from: —H; Calkyl; Calkenyl; and halogenated Calkyl; each of Rand Ris independently selected from: —H; Calkyl; Calkenyl; and halogenated Calkyl; each of Rand Ris independently selected from: —H; Calkyl; Calkenyl; and halogenated Calkyl; each of HXand HXis independently a protic acid; and pharmaceutically acceptable salts, solvates, and hydrates thereof. These methods are particularly useful for producing stable reduced forms, and with high purity. The stability and purity are especially relevant for pharmaceutical compositions for the treatment of disease. The compounds are useful for treatment of e.g. tauopathies, such as Alzheimer's disease, and also as prodrugs for the corresponding oxidized thioninium drugs.

3, 7-diamino-10H-phenothiazine salts and their use

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

Described are methods of preparing reduced 3,7-diamino-10H-phenothiazine (DAPTZ) compounds of formula: wherein: Rand Rare 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 Rand Ris independently selected from: &#x2014;H; Calkyl; Calkenyl; and halogenated Calkyl; each of HXand HXis independently a protic acid; and pharmaceutically acceptable salts, solvates, and hydrates thereof. These methods are particularly useful for producing stable reduced forms, and with high purity. The stability and purity are especially relevant for pharmaceutical compositions for the treatment of disease. The compounds are useful for treatment of e.g. tauopathies, such as Alzheimer's disease, and also as prodrugs for the corresponding oxidized thioninium drugs.

Described are a compound of formula (II) or (III):  The compounds are effective in the treatment of disease, including a tauopathy condition or a disease of tau protein aggregation.

3,6-disubstituted xanthylium salts

Described are methods and materials for use in the treatment or prophylaxis of diseases, for example cognitive disorders, using diaminophenothiazines. In particular it relates to treatments having optimized pharmacokinetic properties, and dosage forms are intended to improve the relative cognitive or CNS benefits of the diaminophenothiazines, for instance compared to haematological effects.

Therapeutic use of diaminophenothiazines

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. 

3,7-diamino-10H-phenothiazine salts and their use

The present invention relates generally to methods and materials for use in the treatment or prophylaxis of diseases, for example cognitive disorders, using diaminophenothiazines. In particular it relates to treatments having optimised pharmacokinetic properties, and dosage forms are intended to improve the relative cognitive or CNS benefits of the diaminophenothiazines, for instance compared to haematological effects.

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

This invention pertains generally to the field of phenothiazine compounds, and more particularly to certain stably reduced phenothiazine compounds, specifically, certain 3,7-diamino-10H-phenothiazine (DAPTZ) compounds of the following formula: 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 Rand Ris independently selected from: &#x2014;H; Calkyl; Calkenyl; and halogenated Calkyl; each of HXand HXis independently a protic acid; and pharmaceutically acceptable salts, solvates, and hydrates thereof. These compounds are useful as drugs, for example, in the treatment of tauopathies, such as Alzheimer's disease, and also as prodrugs for the corresponding oxidized thioninium drugs (for example, methylthioninium chloride, MTC).

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Aberdeen, United Kingdom

Charles Robert Harrington