Abstract: The invention concerns compounds that possess a high affinity at 5-HT1A receptors and an agonist efficacy, as measured by Emax values from a cellular activation assay, that is higher than that of the compounds described in prior art. The capacity of the compounds of the invention to activate an effector protein complex is higher than that the most efficacious agonist described in prior art. Compounds of the invention also exhibit an exceptionally high selectivity (Ki ratio greater than 1000-fold) with respect, in particular, to dopamine D2 receptors and adrenergic receptors of the alpha1 subtype. This selectivity which constitutes a great advantage since it means that the compounds will avoid inducing (central and peripheral) effects associated with activating or inhibiting such receptors.
Type:
Grant
Filed:
June 23, 2017
Date of Patent:
February 18, 2020
Assignees:
NEUROLIXIS, UNIVERSITE JAGELLONE
Inventors:
Joanna Sniecikowska, Adam Bucki, Adrian Newman-Tancredi, Mark Andrew Varney
Abstract: The invention concerns compounds that possess a high affinity at 5-HT1A receptors and an agonist efficacy, as measured by Emax values from a cellular activation assay, that is higher than that of the compounds described in prior art. The capacity of the compounds of the invention to activate an effector protein complex is higher than that the most efficacious agonist described in prior art. Compounds of the invention also exhibit an exceptionally high selectivity (Ki ratio greater than 1000-fold) with respect, in particular, to dopamine D2 receptors and adrenergic receptors of the alpha1 subtype. This selectivity which constitutes a great advantage since it means that the compounds will avoid inducing (central and peripheral) effects associated with activating or inhibiting such receptors.
Type:
Application
Filed:
June 23, 2017
Publication date:
June 27, 2019
Applicants:
NEUROLIXIS, UNIVERSITE JAGELLONE
Inventors:
Joanna SNIECIKOWSKA, Adam BUCKI, Adrian NEWMAN-TANCREDI, Mark Andrew VARNEY
Abstract: The present invention relates to a pipecolic linker and its use as a solid-phase linker in organic synthesis. Said pipecolic solid-phase linker may be used for coupling functional groups chosen between primary amines, secondary amines, aromatic amines, alcohols, phenols and thiols. In particular, said pipecolic solid-phase linker may be used for peptide or pseudopeptide synthesis, such as the reverse N to C peptide synthesis or the retro-inverso peptide synthesis, or for the synthesis of small organic molecules.
Type:
Grant
Filed:
August 28, 2009
Date of Patent:
October 1, 2013
Assignees:
Centre National de la Recherche Scientifique (CNRS), Universite de Montpellier 1, Universite Jagellone, Universite Montpellier 2—Sciences et Techniques
Inventors:
Jean Martinez, Pawel Zajdel, Maciej Pawlowski, Gilles Subra