Roger C Whiting

US Patent:

52527360, Oct 12, 1993

Filed:

Nov 7, 1991

Appl. No.:

7/789230

Inventors:

Jean C. Pascal - Cachan, FR
Chi-Ho Lee - Palo Alto CA
Brian J. Alps - Linlithgow, GB6
Henri Pinhas - Paris, FR
Roger L. Whiting - Los Altos CA

Assignee:

Syntex Pharmaceuticals, Ltd. - Maidenhead

International Classification:

A61K 31495
C07D40302

US Classification:

544370

Abstract:

Substituted imidazolyl-alkyl-piperazine and diazepine derivatives of Formula A: ##STR1## wherein: R. sup. 1 is aryl, lower alkyl, cycloalkyl or hydrogen; R. sup. 2 is aryl, lower alkyl or hydrogen; R. sup. 3 is lower alkyl, hydroxy, or hydrogen; R. sup. 4 is aryl or hydrogen; R. sup. 5 is aryl or hydrogen; m is two or three; n is zero, one or two, provided that when R. sup. 3 is hydroxy, n is one or two; and q is zero, one, two, or three; and the pharmaceutically acceptable salts thereof, are calcium channel antagonists useful for treating mammals having a variety of disease states, such as stroke, epilepsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism and also for treatment of spinal injuries.

US Patent:

49354175, Jun 19, 1990

Filed:

Feb 21, 1989

Appl. No.:

7/313656

Inventors:

Jean C. Pascal - Cachan, FR
Chi-Ho Lee - Palo Alto CA
Brian J. Alps - Linlithgow, GB6
Henri Pinhas - Paris, FR
Roger L. Whiting - Los Altos CA

Assignee:

Syntex Pharmaceuticals Ltd. - Hamilton

International Classification:

A61K 3155

US Classification:

514218

Abstract:

Substituted imidazolyl-alkyl-piperazine and diazepine derivatives of Formula A: ##STR1## wherein: R. sup. 1 is aryl, lower alkyl, cycloalkyl or hydrogen; R. sup. 2 is aryl, lower alkyl or hydrogen; R. sup. 3 lower alkyl, hydroxy, or hydrogen; R. sup. 4 aryl or hydrogen; R. sup. 5 aryl or hydrogen; m is two or three; n is zero, one or two, provided that when R. sup. 3 hydroxy, n is one or two; and q is zero, one, two, or three; and the pharmaceutically acceptable salts thereof, are calcium channel antagonists useful for treating mammals having a variety of disease states, such as stroke, epilipsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism and also for treatment of spinal injuries.

US Patent:

50434470, Aug 27, 1991

Filed:

Oct 21, 1988

Appl. No.:

7/260969

Inventors:

Jean C. Pascal - Cachan, FR
Chi-Ho Lee - Palo Alto CA
Brian J. Alps - Linlithgow, GB6
Henri Pinhas - Paris, FR
Roger L. Whiting - Los Altos CA
Calum B. Macfarlane - Linlithgow, GB6
Serge Beranger - Bretigny-Sur-Cedres, FR
Robert J. Dow - Edinburgh, GB6

Assignee:

Syntex Pharmaceuticals, Ltd. - Berkshire

International Classification:

C07D 4006

US Classification:

544370

Abstract:

Substituted imidazolyl-alkyl-piperazine and diazepine derivatives of Formula A: ##STR1## wherein: R. sup. 1 is aryl, lower alkyl, cycloalkyl or hydrogen; R. sup. 2 is aryl, lower alkyl or hydrogen; R. sup. 3 is lower alkyl, hydroxy, or hydrogen; R. sup. 4 is aryl or hydrogen; R. sup. 5 is aryl or hydrogen; m is two or three; n is zero, one or two, provided that when R. sup. 3 is hydroxy, n is one or two; and q is zero, one, two, or three; and the pharmaceutically acceptable salts thereof, are useful for treating mammals having any of a variety of disease states including: diseases treated by direct neuronal protection, such as ischemia including focal and global ischemia, spinal injuries, head trauma, and neurological diseases such as Alzheimer's and Huntington's chorea; diseases treated by inhibition of sodium ion, such as uremic and hyponatremic encephalopathy; and diseases treated with calcium channel antagonists, including: diseases treated by inhibiting cerebrovascular vasospasm and by cerebrovascular vasodilation, such as migraine, stroke, vasospasm due to subarachnoid hemorrhage, epilepsy or epileptic psychotic symptoms, and cerebrovascular ischemia induced by cocaine abuse; and cardiovascular diseases, such as hypertension, angina, stable and unstable angina, Prinzmetal angina, arrhythmia, thrombosis, embolism, and congestive heart failure such as chronic or acute cardiac failure; and ischemia of lower legs due to peripheral vascular disease, e. g. , intermittent claudication; spasms of smooth muscle: such as the ureter, the bladder, uterine cramps, diuresis, and irritable bowel syndrome; and uses during surgery: such as bypass grafts, angiography, angioplasty, organ preservation during transplant, hypertensive crisis, or post operative hypertension.

US Patent:

55148000, May 7, 1996

Filed:

Sep 20, 1993

Appl. No.:

8/124518

Inventors:

Jean C. Pascal - Cachan, FR
Chi-Ho Lee - Palo Alto CA
Brian J. Alps - Linlithgow, GB6
Henri Pinhas - Paris, FR
Roger L. Whiting - Los Altos CA
Calum B. MacFarlane - Linlithgow, GB6
Serge Beranger - Bretigny-Sur-Cedres, FR

Assignee:

Syntex Pharmaceuticals, Ltd. - Maidenhead

International Classification:

C07D40306
C07D24308

US Classification:

544370

Abstract:

Substituted imidazolyl-alkyl-piperazine and diazepine derivatives of Formula A: ##STR1## wherein R. sup. 1, R. sup. 2, R. sup. 3, R. sup. 4, R. sup. 5, m, n and q are defined as in the specification, and the pharmaceutically acceptable salts thereof. The compounds have calcium entry blocking activity with selectivity for cerebral blood vessels, and have protective activity against some of the deleterious effects resultant upon cerebral ischemia.

US Patent:

50914286, Feb 25, 1992

Filed:

Feb 7, 1991

Appl. No.:

7/652141

Inventors:

Jean C. Pascal - Cachan, FR
Chi-Ho Lee - Palo Alto CA
Brian J. Alps - Linlithgow, GB6
Henri Pinhas - Paris, FR
Roger L. Whiting - Los Altos CA

Assignee:

Syntex Pharmaceuticals, Ltd. - Hamilton

International Classification:

A61K 31495
A61K 3155
C07D24308
C07D40306

US Classification:

514252

Abstract:

Substituted imidazolyl-alkyl-piperazine and diazepine derivatives of Formula A: ##STR1## wherein: R. sup. 1 is aryl, lower alkyl, cycloalkyl or hydrogen; R. sup. 2 is aryl, lower alkyl or hydrogen; R. sup. 3 is lower alkyl, hydroxy, or hydrogen; R. sup. 4 is aryl or hydrogen; R. sup. 5 is aryl or hydrogen; m is two or three; n is zero, one or two, provided that when R. sup. 3 is hydroxy, n is one or two; and q is zero, one, two, or three; and the pharmaceutically acceptable salts thereof, are calcium channel antagonists useful for treating mammals having a variety of disease states, such as stroke, epilepsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism and also for treatment of spinal injuries.

US Patent:

50100750, Apr 23, 1991

Filed:

Apr 6, 1990

Appl. No.:

7/505379

Inventors:

Jean C. Pascal - Cachan, FR
Chi-Ho Lee - Palo Alto CA
Brian J. Alps - Linlithgow, GB6
Henri Pinhas - Paris, FR
Roger L. Whiting - Los Altos CA

Assignee:

Syntex Pharmaceuticals Ltd. - Berkshire

International Classification:

C07D24308
C07D40306
A61K 3155

US Classification:

514218

Abstract:

Substituted imidazolyl-alkyl-piperazine and diazepine derivatives of Formula A: ##STR1## wherein: R. sup. 1 is aryl, lower alkyl, cycloalkyl or hydrogen; R. sup. 2 is aryl, lower alkyl or hydrogen; R. sup. 3 is lower alkyl, hydroxy, or hydrogen; R. sup. 4 is aryl or hydrogen; R. sup. 5 is aryl or hydrogen; m is two or three; n is zero, one or two, provided that when R. sup. 3 is hydroxy, n is one or two; and q is zero, one, two, or three; and the pharmaceutically acceptable salts thereof, are calcium channel antagonists useful for treating mammals having a variety of disease states, such as stroke, epilepsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism and also for treatment of spinal injuries.

US Patent:

48290653, May 9, 1989

Filed:

Apr 24, 1987

Appl. No.:

7/042181

Inventors:

Jean C. Pascal - Cachan, FR
Chi-Ho Lee - Palo Alto CA
Brian J. Alps - Linlithgow, GB6
Henri Pinhas - Paris, FR
Roger L. Whiting - Los Altos CA

Assignee:

Syntex Pharmaceuticals, Ltd. - Maidenhead

International Classification:

A61K 31495

US Classification:

514255

Abstract:

Substituted imidazolyl-alkyl-piperazine and diazepine derivatives of Formula A: ##STR1## wherein: R. sup. 1 is aryl, lower alkyl, cycloalkyl or hydrogen; R. sup. 2 is aryl, lower alkyl or hydrogen; R. sup. 3 is lower alkyl, hydroxy, or hydrogen; R. sup. 4 is aryl or hydrogen; R. sup. 5 is aryl or hydrogen; m is two or three; n is zero, one or two, provided that when R. sup. 3 is hydroxy, n is one or two; and q is zero, one, two, or three; and the pharmaceutically acceptable salts thereof, are calcium channel antagonists useful for treating mammals having a variety of disease states, such as stroke, epilepsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism and also for treatment of spinal injuries.

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.