Wista Laboratories Ltd.

Janet Elizabeth Rickard

Claude Michel Wischik

Charles Robert Harrington

David Horsley

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

Tobias Heinrich

Han Wan Tan

Steven John Kemp

Lynda Jane Storey

Franz Theuring

Karsten Stamer

Claudia Zabke

John M D Storey

Tobias Kerst Heinrich

Michel Wischik Claude

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

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

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).

This invention pertains generally to processes, uses, methods and materials utilizing particular xanthylium compounds, including compounds of formula (I) and (II), as further defined herein. These compounds are useful as drugs, for example, in the treatment of tauopathies, such as Alzheimer's disease. 

3,6-disubstituted xanthylium salts and use thereof in treatment of tauopathies

The invention relates generally to the use of diaminophenothiazine compounds to inhibit or reverse the aggregation of synuclein, and for their use in the manufacture of medicaments for this purpose (e.g. for the treatment of Parkinson's Disease). Also provided are related methods of detecting or labelling of aggregated synuclein.

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Aberdeen, United Kingdom

Janet Elizabeth Rickard