IP Library Granted Patent US 10,772,884
Granted Patent B2
US 10,772,884 · App. 16/552,436 · Granted Sep 15, 2020

Sulphate salts of N-(3-(4-(3-(diisobutylamino)propyl)piperazin-1-yl)propyl)-1H-benzo[d]imidazol-2-amine, preparation thereof and use of the same

Inventors: Stéphane Burlet (Crox, FR); Cécilia Estrella (Lomme, FR); Mathieu Barrier (Wavrin, FR); Patricia Melnyk (Annoeullin, FR); Nicolas Sergeant (Ronchin, FR); Luc Buee (Templemars, FR); Philippe Verwaerde (Santes, FR)
Assignees: Alzprotect; Universite De Lille 2 Droit Et Sante; INSERM (Institut National De La Sante Et De La Recherche)
A61K31/496A61K9/0053A61P25/28C07D235/30
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Quick Facts
Patent No.
US 10,772,884
App. No.
16/552,436
Granted
Sep 15, 2020
Kind
B2
Abstract

The present invention relates to sulphate salts of N-(3-(4-(3-(diisobutylamino)propyl)piperazin-1-yl)propyl)-1H-benzo[d]imidazol-2-amine and pharmaceutically acceptable solvates thereof, preparation thereof, pharmaceutical compositions containing them and use of the same in the treatment and/or prevention of neurodegenerative diseases.

Claims (11)

1. A method for treating a disease selected from tauopathies comprising administering to a patient in need thereof a pharmaceutically effective amount of a sulphate salt of N-(3-(4-(3-(diisobutylamino)propyl)piperazin-1-yl)propyl)-1H-benzo[d]imidazol-2-amine or a pharmaceutically acceptable solvate thereof.

2. The method according to claim 1 , wherein the disease is selected from amyotrophic lateral sclerosis (ALS) with frontotemporal dementia, inclusion body myopathy with Paget's disease of bone and/or frontotemporal dementia (IBMPFD), frontotemporal lobar degeneration, and frontotemporal dementia with Parkinsonism linked to chromosome 17.

3. A method for delaying in a patient the onset of a disease selected from tauopathies comprising administering to the patient in need thereof a pharmaceutically effective amount of a sulphate salt of N-(3-(4-(3-(diisobutylamino)propyl)piperazin-1-yl)propyl)-1H-benzo[d]imidazol-2-amine or a pharmaceutically acceptable solvate thereof.

4. The method according to claim 3 , wherein the disease is selected from amyotrophic lateral sclerosis (ALS) with frontotemporal dementia, inclusion body myopathy with Paget's disease of bone and/or frontotemporal dementia (IBMPFD), frontotemporal lobar degeneration, and frontotemporal dementia with Parkinsonism linked to chromosome 17.

5. A method for inhibiting pathological Tau protein phosphorylation while alleviating oxidative stress processes in a human patient in need of treatment for tauopathies, which comprises administering to said human patient an effective amount of a sulphate salt of N-(3-(4-(3-(diisobutylamino)propyl)piperazin-1-yl)propyl)-1H-benzo[d]imidazol-2-amine or a pharmaceutically acceptable solvate thereof.

6. The method according to claim 1 wherein the sulphate salt has Formula II

wherein x designates the number of equivalents of sulphuric acid and x is 0.5 to 4, or a pharmaceutically acceptable solvate thereof.

7. The method according to claim 3 wherein the sulphate salt has Formula II

wherein x designates the number of equivalents of sulphuric acid and x is 0.5 to 4, or a pharmaceutically acceptable solvate thereof.

8. The method according to claim 5 wherein the sulphate salt has Formula II

wherein x designates the number of equivalents of sulphuric acid and x is 0.5 to 4, or a pharmaceutically acceptable solvate thereof.

Assignments (2)
MERGER Recorded Dec 8, 2020
From: UNIVERSITÉ DE LILLE 2 DROIT ET SANTÉ
To: UNIVERSITÉ DE LILLE
Reel/Frame 054582/0120 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 5, 2020
From: BURLET, STÉPHANE; ESTRELLA, CÉCILIA; BARRIER, MATHIEU; MELNYK, PATRICIA; SERGEANT, NICOLAS; BUEE, LUC; VERWAERDE, PHILIPPE
To: ALZPROTECT; UNIVERSITE DE LILLE 2 DROIT ET SANTE; INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE)
Reel/Frame 051730/0629 →
Priority Claims (1)
EP 12306690 · Dec 27, 2012 · regional
Continuity (3)
Continuation 15388349 · Dec 22, 2016
Division 14655642
Related Publication 20190381036A1 · Dec 19, 2019