Heteroaromatic compounds and their use as dopamine D1 ligands
The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides thereof; processes and intermediates for preparation of; and compositions and uses thereof. The present invention further provides D1 agonists with reduced D1R desensitization,...
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Format | Patent |
Language | English |
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23.04.2015
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Abstract | The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides thereof; processes and intermediates for preparation of; and compositions and uses thereof. The present invention further provides D1 agonists with reduced D1R desensitization, D1 agonists with a reduced - 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. |
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AbstractList | The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides thereof; processes and intermediates for preparation of; and compositions and uses thereof. The present invention further provides D1 agonists with reduced D1R desensitization, D1 agonists with a reduced - 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. |
Author | DOUNAY, AMY BETH HARRIS, ANTHONY RICHARD XU, WENJIAN COE, JOTHAM WADSWORTH GUILMETTE, EDWARD RAYMOND MENTE, SCOT RICHARD ALLEN, JOHN ARTHUR SUBRAMANYAM, CHAKRAPANI DAVOREN, JENNIFER ELIZABETH HELAL, CHRISTOPHER JOHN O'NEIL, STEVEN VICTOR HENDERSON, JACLYN LOUISE GRAY, DAVID LAWRENCE FIRMAN EFREMOV, IVAN VIKTOROVICH NASON II, DEANE MILFORD |
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Snippet | The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides thereof; processes and... |
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SubjectTerms | 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 |
Title | Heteroaromatic compounds and their use as dopamine D1 ligands |
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