Small molecule inhibitors of rotamase enzyme activity

本发明涉及具有FKBP型亲免蛋白亲合性的神经营养性N-乙醛酰基脯氨酰基酯化合物,其制备方法和作为与亲免蛋白有关的酶活性抑制剂,特别是肽基-脯氨酰基异构酶或旋转异构酶活性抑制剂的应用。 This application relates to 3-phenyl-1-prbpyl(2S)-1-(3,3-dimethyl-1,2-dioxopentyl)-2-pyrrolidinecarboxylate. It further relates to a method of preparing such a compound comprising the step of reacting (2S)-1-...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: G.S. HAMILTON, J.P. STEINER
Format: Patent
Sprache:chi ; eng
Schlagworte:
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:本发明涉及具有FKBP型亲免蛋白亲合性的神经营养性N-乙醛酰基脯氨酰基酯化合物,其制备方法和作为与亲免蛋白有关的酶活性抑制剂,特别是肽基-脯氨酰基异构酶或旋转异构酶活性抑制剂的应用。 This application relates to 3-phenyl-1-prbpyl(2S)-1-(3,3-dimethyl-1,2-dioxopentyl)-2-pyrrolidinecarboxylate. It further relates to a method of preparing such a compound comprising the step of reacting (2S)-1-(1,2-dioxo-3,3-dimethylpentyl)-2-pyrrolidinecarboxylic acid with 3-phenyl-1-propanol and dicyclohexylcarbodiimide. Finally, the application relates to the intermediate compound (2S)-1-(1,2-dioxo-3,3-dimethylpentyl)-2-pyrrolidinecarboxylic acid which may be used to produce 3-phenyl-1-propyl(2S)-1-(3,3-dimethyl-1,2-dioxopentyl)-2-pyrrolidinecarboxylate. 3-phenyl-1-propyl (2S)-1-(3,3-dimethyl-1,2-dioxopentyl)-2-pyrrolidinecarboxylate functions as a rotamase enzyme inhibitor and is therefore useful as a component in pharmaceutical compositions, in particular for promoting neuronal growth and regeneration and for treating neurological disorders.