Heteroaromatic compounds and their use as dopamine D1 ligands

US9617275B2 · kind B2 · utility

Assignee

• PFIZER INC. · US

Inventors

• Jotham Wadsworth Coe · Niantic, US
• John Arthur Allen · Galveston, US
• Jennifer Elizabeth Davoren · Cambridge, US
• Amy Beth Dounay · Colorado Springs, US
• Ivan Viktorovich Efremov · Sharon, US
• David Lawrence Firman Gray · Groton, US
• EDWARD RAYMOND GUILMETTE · Franklin, US
• ANTHONY RICHARD HARRIS · Narragansett, US
• Chris Helal · Mystic, US
• Jaclyn Louise Henderson · Cambridge, US
• Scot Richard Mente · Arlington, US
• DEANE MILFORD NASON · Norwich, US
• Steven Victor O'Neil · East Lyme, US
• Chakrapani Subramanyam · South Glastonbury, US
• WENJIAN XU · Waterford, US

Key dates

• Filing date: Aug 7, 2015
• Grant date: Apr 11, 2017
• Expiry date: Aug 7, 2035

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D519/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

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 β-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.