Abstract: Disclosed is a method for treating ear disorders, including the administration of (+)-azasetron, or a pharmaceutically acceptable salt and/or solvate thereof.
Abstract: The therapeutic use of azasetron or an analogue thereof for treating and/or preventing a lesion in the central auditory nervous system (CANS) in an individual. The treatment of lesions in the CANS with azasetron also prevents, inhibits, and/or reduces the loss of the central auditory neuron cells in the brainstem.
Abstract: A process for manufacturing 2-isobutyl-6-(3-(methylamino)azetidin-1-yl)pyrimidin-4-amine of Formula (I): including starting from 6-chloro-2-isobutylpyrimidin-4-amine and tert-butyl azetidin-3-yl(methyl)carbamate, or another N-protected N-methylazetidin-3-amine, and performing the following steps: (a) coupling reaction of both compounds in dimethylsulfoxide in presence of potassium carbonate to afford an intermediate protected compound; and (b) deprotection of the protected compound to afford 2-isobutyl-6-(3-(methylamino)azetidin-1-yl)pyrimidin-4-amine. Also, a process for manufacturing the intermediate protected compound, wherein deprotection step (b) is omitted, and the compounds obtained from the processes.
Type:
Grant
Filed:
October 17, 2018
Date of Patent:
November 23, 2021
Assignee:
SENSORION
Inventors:
Daan Copmans, Amandine Mohr, Maurice Hubert Bonten, Dawn Toronto
Abstract: A process for manufacturing 2-isobutyl-6-(3-(methylamino)azetidin-l-yl)pyrimidin-4-amine of Formula (I): including starting from 6-chloro-2-isobutylpyrimidin-4-amine and tert-butyl azetidin-3-yl(methyl)carbamate, or another N-protected N-methylazetidin-3-amine, and performing the following steps: (a) coupling reaction of both compounds in dimethylsulfoxide in presence of potassium carbonate to afford an intermediate protected compound; and (b) deprotection of the protected compound to afford 2-isobutyl-6-(3-(methylamino)azetidin-1-yl)pyrimidin-4-amine. Also, a process for manufacturing the intermediate protected compound, wherein deprotection step (b) is omitted, and the compounds obtained from the processes.
Type:
Application
Filed:
October 17, 2018
Publication date:
August 27, 2020
Applicant:
SENSORION
Inventors:
Daan COPMANS, Amandine MOHR, Maurice Hubert BONTEN, Dawn TORONTO