Tetrahydroquinoline derivatives as EAA antagonists

US6479488B1 · kind B1 · utility

Assignee

• Glaxo Wellcome S.A. · ES

Inventors

• Romano Di-Fabio · Verona, IT
• Alessandra Pasquarello · Verona, IT
• Fabio Maria Sabbatini · Siena, IT

Key dates

• Filing date: Oct 30, 2000
• Grant date: Nov 12, 2002
• Expiry date: May 1, 2021

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Compounds of formula (I) or salt, or metabolically labile ester thereof wherein R represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy, trifluoromethoxy, nitro, cyano, SO2R2 or COR2 wherein R2 represents hydroxy, methoxy, amino, alkylamino or dialkylamino; m is zero or an integer 1 or 2; R1 represents cyano or the group (CH2)nCN, —CH═CHR3, CH2)nNHCOCH2R4 or O(CH2)pNR5R6; R3 represents cyano or the group COR7; R4 represents alkoxy or a group NHCOR8; R5 and R6 each represent independently hydrogen or alkyl, or R5 and R6 together with the nitrogen atom to which they are attached represent a heterocyclic group, or R5 is hydrogen and R6 is the group COR9; R7 represents an alkoxy, amino or hydroxyl group; R8 represents a hydrogen atom or optionally substituted alkyl, alkoxy, aryl, or heterocyclic group; R9 is the group R8 or the group NR10R11 wherein R10 represents hydrogen or alkyl group; R11 represents optionally substituted alkyl, aryl, heterocyclic or cycloalkyl group; n is zero or an integer from 1 to 4, p is an integer from 2 to 4, processes for their preparation and to their use in medicine.