Compounds for treating disorders sensitive to serotoninergic regulation controlled by the 5-HT1A receptors
US10562853B2 · kind B2 · utility
Assignees
Inventors
Key dates
| Filing date | Jun 23, 2017 |
| Grant date | Feb 18, 2020 |
| Priority date | — |
| Expiry date | Jun 23, 2037 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D405/12
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.