Inventors:
Neng-Yang Shih - North Caldwell NJ
Gregory A. Reichard - Morris Plains NJ
Sunil Paliwal - Scotch Plains NJ
David J. Blythin - North Caldwell NJ
John J. Piwinski - Clinton Township NJ
Dong Xiao - Scotch Plains NJ
Xiao Chen - Edison NJ
Assignee:
Schering Corporation - Kenilworth NJ
International Classification:
A61K 31330
US Classification:
514183, 514396, 514397, 514398, 514400, 5483235, 5483215, 5483251, 5483255, 5483265, 548134
Abstract:
Compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein Ar and Ar are optionally substituted heteroaryl or optionally substituted phenyl; X is âOâ, âSâ, âSOâ, âSO â, âNR â, âNCOR â or âNR SO R ; âis selected from the group consisting of X is âOâ, âSâ or âNR â; Y is O, S or NR ; Y is H, C -C alkyl, âNR R , âSCH , R -aryl(CH ) â, R -heteroaryl-(CH ) â, â(CH ) âheterocycloalkyl, â(C -C )alkyl-NHâC(O)O(C -C )alkyl or âNHC(O)R ; R is H or â(CH ) âG, wherein n is 0-5, G is H, âCF , âCHF , âCH F, âOH, âOâ(C -C alkyl), âSO R , âOâ(C -C cycloalkyl), âNR R , âSO NR R , âNR SO R , âNR COR , âNR (CONR R ), âCONR R , âCOOR , C -C cycloalkyl, R -aryl, R -heteroaryl, and provided when n =0, G is not H; R , R , R and R are H, alkyl, cycloalkyl, âCHF , âCH F or âCF ; or R and R , together with the carbon to which they are attached, form an alkylene ring; or R and R together are O; R is R or âOH; and the remaining variables are as defined in the specification, methods of treating diseases susceptible to treatment with neurokinin antagonists with said compounds, and pharmaceutical compositions comprising said compounds are disclosed. Also disclosed are pharmaceutical compositions comprising an effective amount of a compound of claim 1, at least one pharmaceutically acceptable carrier, and in combination with an effective amount of a selective serotonin reuptake inhibitor.
