Cocaine receptor binding ligands

US5380848A · kind A · utility

Assignees

• Research Triangle Institute · US
• The United States of America, as represented by the Department of Health and Human Services · US

Inventors

• Michael J. Kuhar · Baltimore, US
• John W. Boja · Baltimore, US
• Frank Ivy Carroll · Durham, US
• Anita H. Lewin · Chapel Hill, US
• Philip Abraham · Cary, US

Key dates

• Filing date: Apr 26, 1994
• Grant date: Jan 10, 1995
• Expiry date: Apr 26, 2014

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K2123/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Novel compounds show high affinity for specific cocaine receptors in the brain, particularly dopamine transporter sites, and have the formula ##STR1## Wherein Y=CH.sub.2 R.sub.3, CO.sub.2 R.sub.2 or ##STR2## R.sub.1 =hydrogen, C.sub.1-5 alkyl, R.sub.2 =hydrogen, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.1-4 alkoxy, C.sub.1-6 alkynyl, halogen or amine, PA1 R.sub.3 =OH, hydrogen, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.1-4 alkoxy, Cl Br, I, CN, NH.sub.2, NHC.sub.1-6 alkyl, NC.sub.1-6 alkyl, OCOC.sub.1-6 alkyl, OCOC.sub.1-3 alkylaryl, PA1 A=S, 0 or NH PA1 X=H, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.1-4 alkoxy, C.sub.1-6 alkynyl, halogen, amino, acylamido, and PA1 Z=H, I, Br, Cl, F, CN, CF.sub.3 NO.sub.2, N.sub.3, OR.sub.1, CO.sub.2 NH.sub.2, CO.sub.2 R.sub.1, C.sub.1-6 alkyl , NR.sub.4 R.sub.5, NHCOR.sub.5, NHCO.sub.2 R.sub.6, wherein R.sub.4 -R.sub.6 are each C.sub.1-6 alkyl.