Abstract: Provided are M1 muscarinic acetylcholine receptor (mAChR) agonists, for use in the treatment of a neurological or neurodegenerative disease by promoting microglia and/or macrophage viability and/or activation. Microglia and macrophage survival and activation are thereby achieved by increasing levels of sTREM2 released by microglia cells. In addition, pharmaceutical compositions and methods of preparing the same are described, which are suitable for the treatment or prevention of conditions or diseases that require microglia and/or macrophage modulation, as well as methods for monitoring treatments and enhancing microglia and/or macrophage survival and/or activation.
Type:
Grant
Filed:
March 22, 2019
Date of Patent:
January 21, 2025
Assignee:
NSC Therapeutics GmbH
Inventors:
Abraham Fisher, Stefan Grathwohl, Roger Nitsch
Abstract: Provided are novel crystalline forms of a spiro-compound which acts as a muscarinic acetylcholine receptor agonist. In particular, isolated crystalline polymorphs of (S)-2-ethyl-8-methyl-1-thia-4,8-diazaspiro[4.5]decane-3-one are described which have favorable properties in pharmaceutical manufacture. Also provided are methods to prepare said crystalline polymorphs, and to convert them into each other as well as methods for preparing medicaments containing the same which are suitable for use in the treatment of diseases and disorders that respond to modulation of the muscarinic acetylcholine receptor.
Type:
Grant
Filed:
December 22, 2020
Date of Patent:
January 9, 2024
Assignee:
NSC Therapeutics GmbH
Inventors:
Abraham Fisher, Nira Bar-Ner, Manfred Windisch
Abstract: Provided are novel crystalline forms of a spiro-compound which acts as a muscarinic acetylcholine receptor agonist. In particular, isolated crystalline polymorphs of (S)-2-ethyl-8-methyl-1-thia-4,8-diazaspiro[4.5]decane-3-one are described which have favorable properties in pharmaceutical manufacture. Also provided are methods to prepare said crystalline polymorphs, and to convert them into each other as well as methods for preparing medicaments containing the same which are suitable for use in the treatment of diseases and disorders that respond to modulation of the muscarinic acetylcholine receptor.
Type:
Grant
Filed:
October 5, 2017
Date of Patent:
May 18, 2021
Assignee:
NSC Therapeutics GmbH
Inventors:
Abraham Fisher, Nira Bar-Ner, Manfred Windisch