Gregory J Martinez

US Patent:

57192804, Feb 17, 1998

Filed:

Apr 7, 1997

Appl. No.:

8/833560

Inventors:

Gregory Ricardo Martinez - Mountain View CA
Owen Will Gooding - Los Gatos CA
David Bruce Repke - Milpitas CA
Philip Jay Teitelbaum - Boulder Creek CA
Keith Adrian Murray Walker - Los Altos Hills CA
Roger Lewis Whiting - Los Altos CA

Assignee:

Syntex (U.S.A.) Inc. - Palo Alto CA

International Classification:

C07D40304
C07D23360

US Classification:

544132

Abstract:

The present invention relates to novel benzocycloalkylazolethione compounds which are dopamine. beta. -hydroxylase inhibitors in which the benzocycloalkyl portion of the compound is selected from indanyl, 1,2,3,4-tetrahydronaphthalenyl and 6,7,8,9-tetrahydro-5H-benzocycloheptenyl (in which the benzo is optionally substituted with one to three substituents) and the azolethione portion of the compound is selected from 2-thioxo-2,3-dihydro-1H-imidazol-3-yl, 5-thioxo-4,5-dihydro-1H-�1,2,4!triazol-4-yl and 5-thioxo-4,5-dihydro-1H-�1,2,4!triazol-1-yl (each optionally substituted with one to three substituents); and the prodrugs, pharmaceutically acceptable salts, individual isomers and mixtures of isomers and the methods of using and preparing such benzocycloalkylazolethione compounds.

US Patent:

47925612, Dec 20, 1988

Filed:

May 29, 1986

Appl. No.:

6/868845

Inventors:

Keith A. M. Walker - Los Altos Hills CA
John J. Bruno - Redwood City CA
Gregory R. Martinez - Palo Alto CA

Assignee:

Syntex (U.S.A.) Inc. - Palo Alto CA

International Classification:

C07D40106
C07D40110
C07D40112
A61K 3147

US Classification:

514312

Abstract:

The invention concerns a method of inhibiting both thromboxane synthetase and cyclic-AMP phosphodiesterase in a mammal having a disease characterized by elevated thromboxane levels or an imbalance of prostacyclin/thromboxane levels with a compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt or ester thereof, wherein: X is chosen from the group consisting of: ##STR2## and a covalent bond in which R. sup. 1 is H, alkyl having 1-6 carbon atoms, optionally substituted phenyl or optionally substituted phenyl lower alkyl, when R. sup. 2 is H or OH, or R. sup. 1 and R. sup. 2 taken together represent oxo, alkylidene having 1-6 carbon atoms or optionally substituted benzylidene; R. sup. 3 is H or alkyl having 1-6 carbon atoms, R. sup. 4 is H and R. sup. 3 and R. sup.

US Patent:

47661275, Aug 23, 1988

Filed:

Feb 10, 1987

Appl. No.:

7/012979

Inventors:

Gregory R. Martinez - Palo Alto CA
John J. Bruno - Redwood City CA

Assignee:

Syntex (U.S.A.) Inc. - Palo Alto CA

International Classification:

A61K 31435
C07D21306

US Classification:

514277

Abstract:

The invention concerns a method of inhibiting thromboxane synthetase with a compound of the formula: ##STR1## or a pharmaceutically acceptable salt or ester thereof, in a mammal having a disease characterized by elevated thromboxane levels or an imbalance of prostacyclinthromboxane levels.

US Patent:

49218620, May 1, 1990

Filed:

Sep 21, 1988

Appl. No.:

7/247134

Inventors:

Keith A. M. Walker - Los Altos Hills CA
John J. Bruno - Redwood City CA
Gregory R. Martinez - Palo Alto CA

Assignee:

Syntex (U.S.A.) Inc. - Palo Alto CA

International Classification:

A61K 3147
C07D40106
C07D40110
C07D40112

US Classification:

514312

Abstract:

The invention concerns a method of inhibiting both thromboxane synthetase and cyclic-AMP phosphodiesterase in a mammal having a disease characterized by elevated thromboxane levels or an imbalance of prostacyclin/thromboxane levels with a compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt or ester thereof, wherein: X is chosen from the group consisting of: ##STR2## and a covalent bond in which R. sup. 1 is H, alkyl having 1-6 carbon atoms, optionally substituted phenyl or optionally substituted phenyl lower alkyl, when R. sup. 2 is H or OH, or R. sup. 1 and R. sup. 2 taken together represent oxo, alkylidene having 1-6 carbon atoms or optionally substituted benzylidene; R. sup. 3 is H or alkyl having 1-6 carbon atoms, R. sup. 4 is H and R. sup. 3 and R. sup.

US Patent:

55389880, Jul 23, 1996

Filed:

Mar 17, 1995

Appl. No.:

8/403209

Inventors:

Gregory R. Martinez - Palo Alto CA
Owen W. Gooding - Palo Alto CA
David B. Repke - Palo Alto CA
Philip J. Teitelbaum - Palo Alto CA
Keith A. M. Walker - Palo Alto CA
Roger L. Whiting - Palo Alto CA

International Classification:

A61K 3141
A61K 31415
C07D23384
C07D24912

US Classification:

514384

Abstract:

The present invention relates to novel benzocycloalkylazolethione compounds which are dopamine. beta. -hydroxylase inhibitors in which the benzocycloalkyl portion of the compound is selected from indanyl, 1,2,3,4-tetrahydronaphthalenyl and 6,7,8,9-tetrahydro-5H-benzocycloheptenyl (in which the benzo is optionally substituted with one to three substituents) and the azolethione portion of the compound is selected from 2-thioxo-2,3-dihydro-1H-imidazol-3-yl, 5-thioxo-4,5-dihydro-1H-[1,2,4]triazol-4-yl and 5-thioxo-4,5-dihydro-1H-[1,2,4]triazol-1-yl (each optionally substituted with one to three substituents); and the prodrugs, pharmaceutically acceptable salts, individual isomers and mixtures of isomers and the methods of using and preparing such benzocycloalkylazolethione compounds.