Phenothiazine diaminium salts and their use

Bibliographic Details
Title: Phenothiazine diaminium salts and their use
Patent Number: 9,283,230
Publication Date: March 15, 2016
Appl. No: 13/984841
Application Filed: August 15, 2011
Abstract: The invention relates to compounds of general formula (I): wherein: each of R1 and R9 is independently selected from: —H, C1-4alkyl, C2-4alkenyl, and halogenated C1-4alkyl; each of R3NA and R3NB is independently selected from: —H, C1-4alkyl, C2-4alkenyl, and halogenated C1-4alkyl; each of R7NA and R7NB is independently selected from: —H, C1-4alkyl, C2-4alkenyl, and halogenated C1-4alkyl; and wherein: each of RA and RB is independently selected from: C1-4alkyl, halogenated C1-4alkyl, and C6-10aryl; or RA and RB are linked to form a group selected from: C1-6 alkylene and C6-10 arylene; 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. [chemical expression included]
Inventors: Clunas, Scott (Old Aberdeen, GB); Storey, John Mervyn David (Old Aberdeen, GB); Sinclair, James Peter (Old Aberdeen, GB); Baddeley, Thomas Craven (Old Aberdeen, GB); Ishaq, Ahtsham (Old Aberdeen, GB); Simpson, Michael (Old Aberdeen, GB); Williamson, Craig (Surrey, GB); Wood, Barry Alan (Old Aberdeen, GB); Wischik, Claude Michel (Old Aberdeen, GB); Harrington, Charles Robert (Old Aberdeen, GB); Rickard, Janet Elizabeth (Old Aberdeen, GB); Horsley, David (Old Aberdeen, GB); Loh, Yin Sze (Singapore, SG); Marshall, Colin (Old Aberdeen, GB); Khan, Karrar Ahmad (Old Aberdeen, GB)
Assignees: WisTa Laboratories Ltd. (Singapore, SG)
Claim: 1. A method of treating a tauopathy comprising administering to a subject in need thereof the compound of the following formula: [chemical expression included] or a pharmaceutically acceptable salt, solvate, or hydrate thereof.
Claim: 2. The method of claim 1 , wherein the tauopathy is Alzheimer's disease (AD), Pick's disease, progressive supranuclear palsy (PSP), frontotemporal dementia (FTD), FTD with parkinsonism linked to chromosome 17 (FTDP 17), frontotemporal lobar degeneration (FTLD) syndromes; disinhibition-dementia-parkinsonism-amyotrophy complex (DDPAC), pallido-ponto-nigral degeneration (PPND), Guam-ALS syndrome, pallido nigro luysian degeneration (PNLD), cortico-basal degeneration (CBD), dementia with argyrophilic grains (AgD), dementia pugilistica (DP) or chronic traumatic encephalopathy (CTE), Down's syndrome (DS), dementia with Lewy bodies (DLB), subacute sclerosing panencephalitis (SSPE), Niemann-Pick disease, type C (NPC), Sanfilippo syndrome type B, mucopolysaccharidosis III B (MPS III B)), or myotonic dystrophies (DM), DM1 or DM2.
Claim: 3. The method of claim 2 , wherein the tauopathy is Alzheimer's disease.
Claim: 4. The method of claim 2 , wherein the tauopathy is PSP.
Claim: 5. The method of claim 2 , wherein the tauopathy is FTD, FTDP-17, or FTLD.
Patent References Cited: WO 2007/110627 October 2007
WO 2008/155533 December 2008
WO 2009/044127 April 2009

Other References: International Search Report and Written Opinion issued in related International Patent Application No. PCT/GB2011/001221, mailed Nov. 3, 2011. cited by applicant
Chemical Abstracts Service, XP002661598, Database Accession No. 1236208-20-0, 1 page (2010). cited by applicant
Assistant Examiner: Frazier, Barbara
Primary Examiner: Barham, Bethany
Attorney, Agent or Firm: Foley & Lardner LLP
Accession Number: edspgr.09283230
Database: USPTO Patent Grants
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Language:English