Nancy A Gray

US Patent:

51379104, Aug 11, 1992

Filed:

Mar 1, 1990

Appl. No.:

7/484530

Inventors:

Nancy M. Gray - Ellisville MO
Brian K. Cheng - St. Charles MO
William F. Hood - St. Louis MO
Michael S. Dappen - Chesterfield MO
Alex A. Cordi - St. Louis MO

Assignee:

C.D. Searle & Co. - Chicago IL

International Classification:

A01N 4338
A61K 3140
A61K 31405

US Classification:

514419

Abstract:

Compositions containing certain indole-2-carboxylate compounds and derivatives are described as being therapeutically effective in treatment of CNS disorders resulting from neurotoxic damage or neurodegenerative diseases, particularly those CNS disorders resulting from ischemic events. Preferred compounds are of the formula ##STR1## wherein each of R. sup. 5 and R. sup. 6 is independently selected from hydrido, bromo, chloro and fluoro, and wherein each of R. sup. 10 and R. sup. 12 is independently selected from hydrido and lower alkyl, and pharmaceutically-acceptable salts thereof.

US Patent:

50989162, Mar 24, 1992

Filed:

Mar 29, 1990

Appl. No.:

7/501216

Inventors:

Nancy M. Gray - Ellisville MO
Brian K. Cheng - St. Charles MO

Assignee:

G. D. Searle & Co. - Chicago IL

International Classification:

A61H 31445
C07D21114

US Classification:

514325

Abstract:

Certain propanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each R. sup. 1, R. sup. 2, R. sup. 3, R. sup. 4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R. sup. 3 and R. sup. 4 may be taken together to form oxo; wherein each of R. sup. 9, R. sup. 10, R. sup. 11, R. sup. 12, R. sup. 13 and R. sup. 14 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, henalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R. sup. 15 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl; wherein each of R. sup. 16 and R. sup. 17 is independently selected from hydrido, hydroxy, alkyl, phenalkyl, phenyl, alkoxy, fluoroalkyl and fluoro; wherein m is one or two; wherein p is a number selected from zero through four, inclusive; wherein each of q and r is a number independently selected from one through three, inclusive, with the proviso that sum of q and r is a number from three through six, inclusive; with the further proviso that the nitrogen-containing cyclohetero moiety must be attached at one position selected from R. sup. 3, R. sup.

US Patent:

52159922, Jun 1, 1993

Filed:

Dec 2, 1991

Appl. No.:

7/801148

Inventors:

Nancy M. Gray - Ellisville MO
Brian K. Cheng - St. Charles MO

Assignee:

G. D. Searle & Co. - Chicago IL

International Classification:

A61K 31495
C07D29500

US Classification:

514255

Abstract:

Certain ethanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each of R. sup. 1, R. sup. 2, R. sup. 3, R. sup. 4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R. sup. 3 and R. sup. 4 may be taken together to form oxo; wherein each of R. sup. 5, R. sup. 6, R. sup. 7, R. sup. 8, R. sup. 9 and R. sup. 10 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, phenalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R. sup. 11 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl; wherein each of R. sup. 12 and R. sup. 13 is independently selected from hydrido, hydroxy, alkyl phenalkyl, phenyl, alkoxy, fluoroalkyl and fluoro; wherein m is one or two; wherein p is a number selected from zero through four, inclusive; wherein each of q and r is a number independently selected from one through three, inclusive with the proviso that sum of q and r is a number from three through six, inclusive; with the further proviso that the nitrogen-containing cyclohetero moiety must be attached at one position selected from R. sup. 3, R. sup.

US Patent:

50895060, Feb 18, 1992

Filed:

Apr 30, 1990

Appl. No.:

7/516364

Inventors:

Nancy M. Gray - Ellisville MO
Brian K. Cheng - St. Charles MO

Assignee:

G. D. Searle & Co. - Chicago IL

International Classification:

A61K 31445
A61K 31495
C07D21106
C07D29500

US Classification:

514325

Abstract:

Certain ethanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each of R. sup. 1, R. sup. 2, R. sup. 3, R. sup. 4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R. sup. 3 and R. sup. 4 may be taken together to form oxo; wherein each of R. sup. 5, R. sup. 6, R. sup. 7, R. sup. 8, R. sup. 9 and R. sup. 10 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, phenalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R. sup. 11 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl wherein each of R. sup. 12 and R. sup. 13 is independently selected from hydrido, hydroxy, alkyl, phenalkyl, phenyl, alkoxy, fluoroalkyl and fluoro; wherein m is one or two; wherein p is a number selected from zero through four, inclusive; wherein each of q and r is a number independently selected from one through three, inclusive, with the proviso that sum of q and r is a number from three through six, inclusive; with the further proviso that the nitrogen-containing cyclohetero moiety must be attached at one position selected from R. sup. 3, R. sup.

US Patent:

52294137, Jul 20, 1993

Filed:

Feb 3, 1992

Appl. No.:

7/830108

Inventors:

Nancy M. Gray - Ellisville MO
Brian K. Cheng - St. Charles MO
William F. Hood - St. Louis MO
Michael S. Dappen - Chesterfield MO
Alex A. Cordi - St. Louis MO

Assignee:

G. D. Searle & Co. - Chicago IL

International Classification:

A61K 3140
A61K 31405
C07D20918
C07D20942

US Classification:

514415

Abstract:

Compositions containing certain indole-2-carboxylate compounds and derivatives are described as being therapeutically effective in treatment of CNS disorders resulting from neurotoxic damage or neurodegenerative diseases, particularly those CNS disorders resulting from ischemic events. Preferred compounds are of the formula ##STR1## wherein each of R. sup. 5 and R. sup. 6 is independently selected from hydrido, bromo, chloro and fluoro, and wherein each of R. sup. 10 and R. sup. 12 is independently selected from hydrido and lower alkyl, and pharmaceutically-acceptable salts thereof.