The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Feb. 18, 2020

Filed:

Jun. 23, 2017
Applicants:

Neurolixis, Labruguiere, FR;

Universite Jagellone, Cracow, PL;

Inventors:

Joanna Sniecikowska, Wieliczka, PL;

Adam Bucki, Wieliczka, PL;

Adrian Newman-Tancredi, Castres, FR;

Mark Andrew Varney, Dana Point, CA (US);

Assignees:

NEUROLIXIS, Labruguiere, FR;

UNIVERSITE JAGELLONE, Cracow, PL;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 211/38 (2006.01); C07D 401/12 (2006.01); C07D 405/12 (2006.01); A61P 25/14 (2006.01); A61P 25/22 (2006.01); A61P 25/24 (2006.01); C07D 401/14 (2006.01);
U.S. Cl.
CPC ...
C07D 211/38 (2013.01); A61P 25/14 (2018.01); A61P 25/22 (2018.01); A61P 25/24 (2018.01); C07D 401/12 (2013.01); C07D 401/14 (2013.01); C07D 405/12 (2013.01);
Abstract

The invention concerns compounds that possess a high affinity at 5-HTreceptors 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.


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