NMDA-blocking pharmaceutical compositions

US5284867A · kind A · utility

Assignees

• YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD. · IL
• Ramot University Authority for Applied Research and Industrial Development, Ltd. · IL

Inventors

• Yoel Kloog · Herzliya, IL
• Jeffrey J. Feigenbaum · Chicago, US
• Raphael Mechoulam · Jerusalem, IL
• Mordechai Sokolovsky · Nes Ziona, IL
• Simon Benita · Jerusalem, IL

Key dates

• Filing date: Apr 8, 1992
• Grant date: Feb 8, 1994
• Expiry date: Apr 8, 2012

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D405/06
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The use of a compound of the formula: ##STR1## having the (3S,4S) configuration, and which is essentially free of the (3R,4R) enantiomer, wherein A--B designates a 1(2) or a 6(1) double bond, R designates --CH.sub.3 or --CH.sub.2 OH, R.sup.1 designates a hydrogen atom or a lower acyl group, and R.sup.2 designates (A) a straight-chained or branched C.sub.6-12 alkyl radical; or (B) a group --O--R.sup.3, in which R.sup.3 is a straight-chained or branched C.sub.5-9 alkyl radical or a straight-chained or branched alkyl radical substituted at the terminal carbon atom by a phenyl group in the manufacture of a medicament for reducing or preventing glutamate neurotoxicity. Some of the above compounds are novel, and their preparation is described. Also described is a method of treating acute injuries to the central nervous system associated with excitatory amino acid neurotoxicity, a method of treating chronic degenerative disease associated with gradual selective neuronal loss and a method of treating poisonings affecting the central nervous system by administering a pharmaceutical composition containing the above compound.