Joseph T Monahan

US Patent:

54648432, Nov 7, 1995

Filed:

Oct 8, 1993

Appl. No.:

8/133496

Inventors:

Donald W. Hansen - Skokie IL
Karen B. Peterson - Vernon Hills IL
Joseph B. Monahan - Black Jack MO

Assignee:

G.D. Searle & Co. - Chicago IL

International Classification:

C07D47104
A61K 3144

US Classification:

514300

Abstract:

A class of imidazo[1,2-a]pyridinyldiacid compounds is described for cognitive enhancement and for treatment of cognitive disorders and which have activity as a cognitive enhancer. Such compounds are also useful to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective as an agonist or partial agonist to modulate, or 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 each R. sup. 20 is independently selected from hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl; wherein each of Y. sub. m and Y. sub. n is a spacer group selected from methylene and ethylene radicals; wherein m is an integer of one or two; wherein n is an integer of from zero to two; wherein X is one or more groups independently selected from hydrogen, alkyl, cycloalkyl, halo, haloalkyl, hydroxy, hydroxyalkyl, alkoxy, alkoxyalkyl and alkanoyl; or a pharmaceutically-acceptable salt thereof.

US Patent:

57212236, Feb 24, 1998

Filed:

Oct 3, 1995

Appl. No.:

8/538525

Inventors:

Donald W. Hansen - Skokie IL
Karen B. Peterson - Vernon Hills IL
Joseph B. Monahan - Black Jack MO

International Classification:

C07D47104
C07F 958
A61K 3144

US Classification:

514 89

Abstract:

A class of imidazo�1,2-a!pyridinyldiacid compounds is described for cognitive enhancement and for treatment of cognitive disorders and which have activity as a cognitive enhancer. Such compounds are also useful to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective as an agonist or partial agonist to modulate, or 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 each R. sup. 20 is independently selected from hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl; wherein each of Y. sub. m and Y. sub. n is a spacer group selected from methylene and ethylene radicals; wherein m is an integer of one or two; wherein n is an integer of from zero to two; wherein X is one or more groups independently selected from hydrogen, alkyl, cycloalkyl, halo, haloalkyl, hydroxy, hydroxyalkyl, alkoxy, alkoxyalkyl and alkanoyl; or a pharmaceutically-acceptable salt thereof.