Selective neurokinin antagonists

US6635630B2 · kind B2 · 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: Jun 6, 2002
• Grant date: Oct 21, 2003
• Expiry date: Jun 6, 2022

Classification

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

Abstract

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—, —S—, —SO—, —SO2—, —NR12—, —NCOR12— or —NR12SO2R15;  is selected from the group consisting of X2 is —O—, —S— or —NR5—;Y is ═O, ═S or ═NR11;Y1 is H, C1-C6 alkyl, —NR17R13, —SCH3, R19-aryl(CH2)n6—, R19-heteroaryl-(CH2)n6—, —(CH2)n6—heterocycloalkyl, —(C1-C3)alkyl-NH—C(O)O(C1-C6)alkyl or —NHC(O)R15;R5 is H or —(CH2)n1—G, wherein n1 is 0-5, G is H, —CF3, —CHF2, —CH2F, —OH, —O—(C1-C6 alkyl), —SO2R13, —O—(C3-C8 cycloalkyl), —NR13R14, —SO2NR13R14, —NR13SO2R15, —NR13COR12, —NR12(CONR13R14), —CONR13R14, —COOR12, C3-C8 cycloalkyl, R19-aryl, R19-heteroaryl, and provided when n1=0, G is not H;R1, R2, R3 and R7 are H, alkyl, cycloalkyl, —CHF2, —CH2F or —CF3; or R1 and R2, together with the carbo…