Selective neurokinin antagonists

US6436928B1 · kind B1 · utility

Assignee

• SCHERING CORPORATION · US

Inventors

• Neng-Yang Shih · Lexington, US
• Ho-Jane Shue · Pine Brook, US
• Gregory A. Reichard · Lovettsville, US
• Sunil Paliwal · Manalapan, US
• David J. Blythin · North Caldwell, US
• John J. Piwinski · Lebanon, US
• Dong Xiao · Hackettstown, US
• Xiao-Tao Chen · New York, US

Key dates

• Filing date: Dec 14, 2000
• Grant date: Aug 20, 2002
• Expiry date: Dec 14, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07F9/6506
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

A compound represented by the structural formula or a pharmaceutically acceptable salt thereof, whereinAr1 and Ar2 are optionally substituted heteroaryl or optionally substituted phenyl;X1 is —O—, —SO0-2—, —NR12—, —NCOR12— or —NR12SO2R15;  is X2 is —O—, —S— or optionally substituted nitrogen;Y is ═O, ═S or ═NR11;Y1 is H, alkyl, —NR17R13, —SCH3, R19-aryl(CH2)n6—, R19-heteroaryl-(CH2)n6—, —(CH2)n6-heterocycloalkyl, -alkyl-NH—C(O)O-alkyl or —NHC(O)R15;R1, R2, R3 and R7 are H, alkyl, OH-alkyl, cycloalkyl, —CHF2, —CH2F or —CF3; or R1 and R2 form an alkylene ring; or R1 and R2 together are ═O;R6 is H, alkyl, —OR13 or —SR12;and the remaining variables are as defined in the specification, is disclosed, as well as a pharmaceutical compositions comprising said compound, methods of using said compound as a neurokinin antagonist, and the combination of said compounds with a selective serotonin reuptake inhibitor.