Nancy Marie Gray

US Patent:

51303302, Jul 14, 1992

Filed:

Jan 31, 1990

Appl. No.:

7/473008

Inventors:

Brian R. de Costa - Gaithersburg MD
Kenner C. Rice - Bethesda MD
Nancy M. Gray - Ellisville MO
Patricia C. Contreras - Ballwin MO
Arthur E. Jacobson - Potomac MD
Andrew Thurkauf - Branford CT
Lilian A. Radesca - Brookeville MD
Wayne D. Bowen - East Providence RI

Assignee:

G. D. Searle & Co. - Chicago IL

International Classification:

A61K 3140
C07D295073

US Classification:

514429

Abstract:

Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychotic disorders and convulsions. Compounds of particular interest are of the formula ##STR1## wherein R. sup. 1 is selected from hydrido, loweralkyl, cycloalkylalkyl of four to six carbon atoms, and loweralkenylloweralkyl; wherein each of R. sup. 2 and R. sup. 3 is independently selected from hydrido and loweralkyl; wherein each of R. sup. 4 through R. sup. 7, R. sup. 10 and R. sup. 11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is a number selected from four through six; wherein p is a number selected from zero through four; wherein q is a number selected from three through five; wherein A is selected from phenyl, naphthyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.

US Patent:

54017556, Mar 28, 1995

Filed:

Oct 8, 1991

Appl. No.:

7/774003

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:

G. D. Searle & Co. - Skokie IL
National Institutes of Health - Rockville MD

International Classification:

C07D40908
A61K 3144

US Classification:

514336

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, R. sup. 2, and R. sup. 5 are defined in specification.

US Patent:

57391580, Apr 14, 1998

Filed:

Jul 1, 1992

Appl. No.:

7/877190

Inventors:

Brian R. de Costa - Gaithersburg MD
Kenner C. Rice - Bethesda MD
Nancy M. Gray - Buffalo Grove IL
Patricia C. Contreras - Evanston IL
Arthur E. Jacobson - Potomac MD
Andrew Thurkauf - Banford CT
Lilian A. Radesca - Brookeville MD
Wayne D. Bowen - East Providence RI
J. Michael Walker - Cranston RI

Assignee:

The United States of America as represented by the Department of Health
and Human Services - Washington DC

International Classification:

A61K 3140
C07D295073
C07D295135

US Classification:

514429

Abstract:

Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychotic disorders, convulsions and parkinsonism. Compounds of particular interest are of the formula ##STR1## wherein R. sup. 1 is selected from hydrido, loweralkyl, cycloalkylalkyl of four to six carbon atoms and loweralkenylloweralkyl; wherein each of R. sup. 2 and R. sup. 3 is independently selected from hydrido and loweralkyl; wherein each of R. sup. 4 through R. sup. 7, R. sup. 10 and R. sup. 11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is a number selected from four through six; wherein p is a number selected from zero through four; wherein q is a number selected from three through five; wherein A is selected from phenyl, naphthyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.

US Patent:

50554689, Oct 8, 1991

Filed:

Oct 30, 1989

Appl. No.:

7/428531

Inventors:

Nancy M. Gray - Buffalo Grove IL
Patricia C. Contreras - Evanston IL

Assignee:

G. D. Searle & Co. - Chicago IL

International Classification:

A61K 31495
A61K 3150
A61K 31135

US Classification:

514249

Abstract:

Certain bridged tricyclic amine compounds are described as being therapeutically effective in treatments of CNS disorders resulting from neurotoxic damage or neurodegenerative diseases, particularly those CNS disorders resulting from ischemic events. Compounds of particular interest for use as neuroprotective agents are those of the formula ##STR1## wherein each of R. sup. 1 and R. sup. 2 is independently selected from hydrido, loweralkyl, benzyl and phenyl; wherein each of R. sup. 1 through R. sup. 7 is independently selected from hydrido, loweralkyl, hydroxy, benzyl, phenyl, loweralkoxy, phenoxy, benzyloxy, halo and haloloweralkyl; wherein R. sup. 18 may be selected from hydrido, loweralkyl, cycloalkyl of five or six carbon atoms, cycloalkylalkyl of six or seven carbon atoms, phenyl, hydroxyloweralkyl, and heteroaryl selected from saturated or fully unsaturated heterocyclic rings containing five to seven ring members of which one or two ring members are nitrogen atom; wherein each X is independently one or more groups selected from hydrido, hydroxy, loweralkyl, benzyl, phenyl, loweralkoxy, phenoxy, haloloweralkyl, halo, and lower-alkanoyl; and wherein each of R. sup. 23 through R. sup. 30 is independently selected from hydrido, lower alkyl, benzyl, phenyl and halo; wherein R. sup.

US Patent:

56042558, Feb 18, 1997

Filed:

Nov 23, 1994

Appl. No.:

8/344433

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

US Classification:

514422

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.