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Publication Number
US-11787806-B2
Publication Date
2023-10-17
Expiration Date
Abstract
This invention relates to pharmaceutically acceptable ergoline analogues and salts thereof. In particular, though not exclusively, the invention relates to formulations and uses of the same as a medicament.
Core Innovation
The disclosure provides pharmaceutically acceptable ergoline analogue compounds and salts for use as medicaments. The compounds are defined as Formula (I) ergoline analogue compounds with variable substituents X, Y, and Z, including particular embodiment selections of the substituents.
The patent describes ergoline-analog compounds as candidate medicaments for receptor-associated conditions. The document provides specific ergoline-analog compounds together with computational docking and synthetic accessibility evaluations, and the selected compounds are described as synthetically accessible and able to function as medicaments acting on serotonin receptor-associated targets.
The compounds are computationally evaluated with docking scores and synthetic accessibility scores, along with physiochemical and PK-related in silico properties. The document further includes assessments addressing solubility, Lipinski violations, Pgp substrate, and CYP inhibition flags, and these evaluations are used to support selection of the specific compounds as medicament candidates.
Functional receptor assay results are reported for compounds 018 and 019 across serotonin receptor signaling readouts. The document describes assays including cAMP, IP1, Ca2+, and beta-arrestin assays, and emphasizes that compound 019 shows activity across other receptor assays and some 5-HT2A cAMP stimulation.
Claims Coverage
Two independent claims are identified. The claims cover administration of selected ergoline-analog compounds or pharmaceutically acceptable salts thereof as medicaments for depression, anxiety, and/or pain conditions, and a depression treatment claim using a pharmaceutically effective composition in specified dosage forms.
Treatment method for depression, anxiety, or pain condition
A method of treatment of a subject comprising administering a compound or pharmaceutically acceptable salt thereof to the subject, wherein the subject has depression, anxiety, or a pain condition, and wherein the compound is selected from the specified group.
Depression treatment by a pharmaceutically effective composition in selected dosage forms
A method of treatment of a subject comprising administering to the subject a composition comprising a pharmaceutically effective amount of a compound or pharmaceutically acceptable salt thereof, wherein the subject has depression, wherein the composition is formulated in a dosage form selected from a tablet, a capsule, granules, powder, an aerosol, injectable liquid, or a suppository, and wherein the compound is selected from the specified group.
The inventive coverage is focused on medicament administration of a selected compound or pharmaceutically acceptable salt to subjects having depression, anxiety, or pain, and on depression treatment using a pharmaceutically effective composition formulated in specified dosage forms.
Stated Advantages
Documented Applications
No documented applications found
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