Alpha-aryloxyisobutyramide derivatives and the corresponding arylthio and arylsulphonyl compounds

Novel compounds of formula X-A-C(CH3)2-CONR7R8 where X is aryl which may be substituted by one or more halogen atoms or alkyl, alkoxy, aryl or aralkyl radicals, A is oxygen, sulphur or sulphonyl, R7 is hydrogen or an alkyl radical having 1-6 carbon atoms, and R8 is an alkyl radical having 1-6 carbon...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
1. Verfasser: WARING WILSON SHAW
Format: Patent
Sprache:eng
Schlagworte:
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:Novel compounds of formula X-A-C(CH3)2-CONR7R8 where X is aryl which may be substituted by one or more halogen atoms or alkyl, alkoxy, aryl or aralkyl radicals, A is oxygen, sulphur or sulphonyl, R7 is hydrogen or an alkyl radical having 1-6 carbon atoms, and R8 is an alkyl radical having 1-6 carbon atoms substituted by a carboxy radical, and the esters and salts thereof, are prepared by reacting an acid halide of formula X-A-C(CH3)2-COZ where Z is halogen, with an amine of formula HNR7R8.ALSO:Therapeutic compositions useful for the reduction in concentration of cholesterol and/or esterified fatty acids in the blood serum, and also possessing sedative properties, which may be administered orally, contain as active ingredient at least one compound of formula X-A-CR1R2-CONR3R4 wherein X is an aryl radical which may be substituted by one or more halogen atoms, or alkyl, alkoxy, aryl, or aralkyl radicals, A stands for an oxygen or sulphur atom or the sulphonyl radical, and either R1 stands for hydrogen and R2 stands for hydrogen or for an alkyl radical, or R1 and R2 both represent methyl radicals, R3 is hydrogen or an alkyl radical, and R4 is hydrogen, or an alkyl, hydroxyalkyl or alkenyl radical, or an aryl radical optionally substituted by one or more alkyl or alkoxy radicals, or a carboxyalkyl radical or an ester or salt thereof, provided that, when R1 and R2 both represent hydrogen and A is oxygen, X is not a 2-methoxy-4-alkylphenyl radical, in association with a pharmaceutically acceptable diluent or carrier therefor, but excluding simple solutions or suspensions of the active ingredient in water or in common organic solvents. The compositions may also contain a steroid derivative such as an androstane derivative, e.g. androsterone or its acetate or propionate.