High affinity ligands for nociceptin receptor ORL-1

US6455527B2 · kind B2 · 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: Jan 25, 2001
• Grant date: Sep 24, 2002
• Expiry date: Jan 25, 2021

Classification

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

Abstract

Novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein:the dotted line represents an optional double bond;X1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl;X2 is —CHO, —CN, optionally substituted amino, alkyl, or aryl;or X1 is optionally substituted benzofused heterocyclyl and X2 is hydrogen;or X1 and X2 together form an optionally benzofused spiro heterocyclyl groupR1, R2, R3 and R4 are independently H and alkyl, or (R1 and R4) or (R2 and R3) or (R1 and R3) or (R2 and R4) together can form an alkylene bridge of 1 to 3 carbon atoms;Z1 is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or —CO2(alkyl or substituted amino) or CN ; Z2 is H or Z1; Z3 is H oralkyl; or Z1, Z2 and Z3, 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 of pain, anxiety, cough, asthma, depression and alcohol abuse are disclosed.