Inventors:
Kenner C. Rice - Rockville MD
Arthur E. Jacobson - Potomac MD
Andrew Thurkauf - Laurel MD
Mariena V. Mattson - Rockville MD
Thomas L. O'Donohue - Chesterfield MO
Patricia C. Contreras - Ballwin MO
Nancy M. Gray - Ellisville MO
Assignee:
The United States of America as represented by the Department of Health
and Human Services - Washington DC
G. D. Searle & Co. - Skokie IL
International Classification:
C07D40904
A61K 3140
Abstract:
Compounds, compositions and methods of treatment are described to control brain damage associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of an N-(1-thienylcycloalkyl)alkenylamine compound as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula ##STR1## wherein R. sup. 1 is one or more groups selected from hydrido, alkyl of one to about five carbon atoms, cycloalkyl of three to about five carbon atoms, alkenyl of two to about five carbon atoms, hydroxyl and alkoxy; wherein each of R. sup. 2 is one or more groups selected from hydrido, alkyl of one to about five carbon atoms, cycloalkyl of three to about five carbon atoms, alkenyl of two to about five carbon atoms, hydroxyl, oxo and alkoxy; wherein R. sup. 5 is one or more groups selected from hydrido, alkyl of one to about five carbon atoms, cycloalkyl of three to about five carbon atoms, alkenyl of two to about five carbon atoms, hydroxyl and alkoxy; and wherein the broken line within the N-containing ring represents a double bond between any two adjacent carbon atoms.