.omega.-[2-(phosphonoalkyl)phenyl]-2-aminoalkanoic acids as antagonists of excitatory amino acid receptors

US5395827A · kind A · utility

Assignee

• Guilford Pharmaceuticals, Inc. · US

Inventors

• Waclaw J. Rzeszotarski · Millersville, US
• Suzanne R. Ellenberger · Reisterstown, US
• Maria E. Guzewska · Pasadena, US
• John W. Ferkany · Baltimore, US
• Gregory S. Hamilton · Catonsville, US
• Raymond J. Patch · Yardley, US
• Edward W. Karbon, Jr · Ellicott City, US

Key dates

• Filing date: Dec 22, 1993
• Grant date: Mar 7, 1995
• Expiry date: Dec 22, 2013

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07F9/3834
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention pertains to antagonists of excitatory amino acid neurotransmitter receptor antagonists, their method of preparation as well as compositions containing them which have the general formula: ##STR1## wherein n and m independently are 0, 1, 2, or 3; R.sub.1 is selected from the group consisting of hydrogen and R.sub.2 ; R.sub.2 is selected from the group consisting of hydrogen, halogen, halomethyl, nitro, amino, alkoxy, hydroxyl, hydroxymethyl, C.sub.1 to C.sub.6 lower alkyl, C.sub.7 to C.sub.12 higher alkyl, aryl and aralkyl, wherein if R.sub.2 is hydrogen, R.sub.1 is not hydrogen; R.sub.3 is selected from the group consisting of hydrogen and C.sub.1 to C.sub.6 lower alkyl; the stereoisomers thereof in their resolved or racemic form, and pharmaceutically acceptable salts thereof.