Janet A Julien

US Patent:

52624269, Nov 16, 1993

Filed:

Jan 22, 1993

Appl. No.:

8/007461

Inventors:

Richard M. Weier - Lake Bluff IL
Ish K. Khanna - Vernon Hills IL
Michael A. Stealey - Libertyville IL
Janet A. Julien - Glenview IL

Assignee:

G. D. Searle & Co. - Chicago IL

International Classification:

A61K 31435
C07D47104

US Classification:

514303

Abstract:

A class of N,N'-cycloalkyl/alkyl benzamides of certain 4H-imidazo[4,5-b]pyridine compounds is described for treating cardiovascular and immuno-inflammatory related disorders mediated by platelet activating factor (PAF). Compounds of particular interest are those of the formula: ##STR1## wherein R. sup. 1 is selected from hydrido, alkyl, hydroxyalkyl, alkoxyalkyl, phenyl, halophenyl, pyridinyl, alkylsilyloxyalkyl, amino, monoalkylamino, dialkylamino, aminoalkyl, monoalkylaminoalkyl and dialkylaminoalkyl; wherein each of R. sup. 5, R. sup. 6, R. sup. 7 and R. sup. 8 is independently selected from hydrido, hydroxy, alkyl, alkoxy, fluoro, chloro, bromo, haloalkyl, alkylthio, alkoxyalkyl, hydroxyalkyl, alkylthioalkyl, cyano, amino, monoalkylamino and dialkylamino; wherein each of R. sup. 9 and R. sup. 10 is independently selected from hydrido, alkyl, cycloalkyl, bicycloalkyl, heterocyclic, heterocyclicalkyl, aryl, alkenyl and cycloalkenyl, and wherein any of said R. sup. 9 and R. sup. 10 substituents may be further substituted with one or more groups selected from linear or branched lower alkyl, lower alkoxy, fluoro, chloro and bromo; or a pharmaceutically-acceptable salt thereof.

US Patent:

53590732, Oct 25, 1994

Filed:

Nov 24, 1992

Appl. No.:

7/981957

Inventors:

Richard M. Weier - Lake Bluff IL
Ish K. Khanna - Vernon Hills IL
Michael A. Stealey - Libertyville IL
Janet A. Julien - Glenview IL
Kirk T. Lentz - Niles IL

Assignee:

G. D. Searle & Co. - Chicago IL

International Classification:

C07D47104
C07D47106

US Classification:

546118

Abstract:

A class of N,N'-cycloalkyl/alkyl benzamides of certain 1H-imidazo[4,5-b]pyridine and 3H-imidazo[4,5-b]pyridine compounds is described for treating cardiovascular and immuno-inflammatory related disorders mediated by platelet activating factor (PAF). Compounds of particular interest are those of the formula: ##STR1## wherein each of X. sup. a and X. sup. b is independently selected from nitrogen atom and --CH--, with the proviso that when one of X. sup. a and X. sup. b is selected as nitrogen atom, then the other of X. sup. a and X. sup. b must be --CH--; wherein R. sup. 1 is selected from hydrido, alkyl, hydroxyalkyl, alkoxyalkyl, phenyl, halophenyl, alkylsilyloxyalkyl, amino, monoalkylamino, dialkylamino, aminoalkyl, monoalkylaminoalkyl and dialkylaminoalkyl; wherein each of R. sup. 5, R. sup. 6, R. sup. 7 and R. sup. 8 is independently selected from hydrido, hydroxy, alkyl, alkoxy, fluoro, chloro, bromo, haloalkyl, alkylthio, alkoxyalkyl, hydroxyalkyl, alkylthioalkyl, cyano, amino, monoalkylamino and dialkylamino; wherein each of R. sup. 9 and R. sup. 10 is independently selected from hydrido, alkyl, cycloalkyl, bicycloalkyl, heteroaryl, aryl, alkenyl and cycloalkenyl, and wherein any of said R. sup. 9 and R. sup.