HETEROAROMATIC COMPOUNDS AND THEIR USE AS DOPAMINE D1 LIGANDS

The present invention provides D1 agonists with reduced D1R desensitization, D1 agonists with a reduced ²-arrestin recruitment activity relative to Dopamine, D1 agonists interacting significantly with the Ser188 but not significantly with the Ser202 of a D1R when binding to the D1R, D1 agonists inte...

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Main Authors DOUNAY, Amy, Beth, HARRIS, Anthony, Richard, SUBRAMANYAM, Chakrapani, COE, Jotham, Wadsworth, GUILMETTE, Edward, Raymond, HELAL, Christopher, John, EFREMOV, Ivan, Viktorovich, GRAY, David, Lawrence, Firman, ALLEN, John, Arthur, NASON, Deane, Milford, II, O'NEIL, Steven, Victor, MENTE, Scot, Richard, DAVOREN, Jennifer, Elizabeth, HENDERSON, Jaclyn, Louise, XU, Wenjian
Format Patent
LanguageEnglish
French
German
Published 27.09.2017
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:The present invention provides D1 agonists with reduced D1R desensitization, D1 agonists with a reduced ²-arrestin recruitment activity relative to Dopamine, D1 agonists interacting significantly with the Ser188 but not significantly with the Ser202 of a D1R when binding to the D1R, D1 agonists interacting less strongly with the Asp103 and interacting less strongly with the Ser198 of a D1R when binding to the D1R, and their uses.
Bibliography:Application Number: EP20130820922