High affinity ligands for nociceptin receptor ORL-1

US6262066A · kind A · utility

Assignee

• SCHERING CORPORATION · US

Inventors

• Deen Tulshian · Lebanon, US
• Ginny D. Ho · New Providence, US
• Lisa S. Silverman · Edison, US
• Julius J. Matasi · Monmouth Junction, US
• Robbie McLeod · Readington, US
• John Hey · Lexington, US
• Richard Chapman · Somerville, US
• Ana Bercovici · West Orange, US
• Francis M. Cuss · Berkeley Heights, US

Key dates

• Filing date: Jul 26, 1999
• Grant date: Jul 17, 2001
• Expiry date: Jul 26, 2019

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Novel compounds of the formula ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: PA1 the dotted line represents an optional double bond; PA1 X.sup.1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl; PA1 X.sup.2 is --CHO, --CN, optionally substituted amino, alkyl, or aryl; PA1 or X.sup.1 is optionally substituted benzofused heterocyclyl and X.sup.2 is hydrogen; PA1 or X.sup.1 and X.sup.2 together form an optionally benzofused Spiro heterocyclyl group PA1 R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently H and alkyl, or (R.sup.1 and R.sup.4) or (R.sup.2 and R.sup.3) or (R.sup.1 and R.sup.3) or (R.sup.2 and R.sup.4) together can form an alkylene bridge of 1 to 3 carbon atoms; PA1 Z.sup.1 is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or --CO.sub.2 (alkyl or substituted amino) or CN; Z.sup.2 is H or Z.sup.1 ; Z.sup.3 is H oralkyl; or Z.sup.1, Z.sup.2 and Z.sup.3, together with the carbon to which they are attached, form bicyclic saturated or unsaturated rings; pharmaceutical compositions therefore, and the use of said compounds as nociceptin receptor inhibitors useful in the treatment o…