Opiate receptor ligands

US5536868A · kind A · utility

Assignee

• Chiron Corporation · US

Inventors

• Simon Ng · Walnut Creek, US
• Robert L. Warne · San Francisco, US
• Ronald N. Zuckermann · Corona, US
• Eric Martin · Corona, US
• Reyna J. Simon · Felton, US

Key dates

• Filing date: Feb 21, 1995
• Grant date: Jul 16, 1996
• Expiry date: Feb 21, 2015

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2602/42
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Compounds of Formula 1 bind to the opioid receptors: ##STR1## wherein R.sub.1 is a group of the formula ##STR2## where W is --(CH.sub.2).sub.a -- (where a is 0, 1, or 2), --O--, --NH--, --S--, --SO--, or --SO.sub.2 --, and Ar is phenyl, phenyl-alkyl, phenyl substituted with 1-3 halo, nitro, lower alkyl, hydroxy, amino, alkylamino, dialkylamino, and/or hydroxy-lower alkyl groups, and n is 0, 1, 2, 3, or 4; PA0 R.sub.2 and R.sub.3 are each independently H, lower alkyl, or ##STR3## where X is H, OH, lower alkyl, or lower alkoxy, and p is 0, 1, 2, or 3; R.sub.4 is ##STR4## where m is 0, 1, 2, or 3, and R is 1-3 halo, nitro, lower alkyl, hydroxy, amino, alkylamino, dialkylamino, and/or hydroxy-lower alkyl groups; PA0 R.sub.5 is cycloalkyl, bicycloalkyl, or tricycloalkyl; and PA0 R.sub.6, R.sub.7, R.sub.8, and R.sub.9 are each independently H or lower alkyl.