4-phenylpiperazine derivatives with functionalized linkers as dopamine D3 receptor selective ligands and methods of use

US8748608B2 · kind B2 · utility

Assignees

• The United States of America as Represented by the Secretary of the Department of Health and Human Services · US
• University of North Texas Health Science Center at Fort Worth · US

Inventors

• Amy Hauck Newman · Phoenix, US
• Peter Grundt · Baltimore, US
• George C. Cyriac · Severna Park, US
• Robert Luedtke · Fort Worth, US
• Jianjing Cao · Ellicott City, US

Key dates

• Filing date: Jun 15, 2007
• Grant date: Jun 10, 2014
• Expiry date: Feb 12, 2029

Classification

• Technology area (CPC G): Physics
• CPC primary: G01N33/566
• WIPO field: Measurement
• WIPO sector: Instruments

Abstract

Dopamine D3 receptor antagonists and partial agonists are known to modulate the reinforcing and drug-seeking effects induced by cocaine and other abused substances. By introducing functionality into the butylamide linking chain of the 4-phenylpiperazine class of ligands, improved D3 receptor affinity and selectivity, as well as water solubility, is achieved. A series of linking-chain derivatives are disclosed wherein functionality such as OH or OAc groups have been introduced into the linking chain. In general, these modifications are well tolerated at D3 receptors and achieve high selectivity over D2 and D4 receptors.