Patents by Inventor Roger L. Whiting
Roger L. Whiting has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 5538988Abstract: 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.Type: GrantFiled: March 17, 1995Date of Patent: July 23, 1996Inventors: Gregory R. Martinez, Owen W. Gooding, David B. Repke, Philip J. Teitelbaum, Keith A. M. Walker, Roger L. Whiting
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Patent number: 5514800Abstract: 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.Type: GrantFiled: September 20, 1993Date of Patent: May 7, 1996Assignee: Syntex Pharmaceuticals, Ltd.Inventors: Jean C. Pascal, Chi-Ho Lee, Brian J. Alps, Henri Pinhas, Roger L. Whiting, Calum B. MacFarlane, Serge Beranger
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Patent number: 5276034Abstract: Substituted imidazolyl-alkyl-piperazine and diazepine derivatives and the pharmaceutically acceptable salts thereof are useful for treating mammals having any of a variety of disease states. These disease states include: 1) diseases treated by direct neuronal protection, including focal and global ischemia, spinal injuries, and head trauma, and neurological diseases including Alzheimer's and Huntington's chorea; 2) uraemic and hyponatraemic encephalopathy; 3) diseases treated by diuresis; 4) diseases treated by calcium channel antagonism, including cardiovascular diseases (i.e. hypertension, angina, stable and unstable angina, Prinzmetal angina, arrhythmia, thrombosis, embolism, and congestive heart failure including chronic or acute cardiac failure), diseases characterized by ischemia of lower legs due to peripheral vascular disease (e.g., intermittent claudication), diseases characterized by spasms of smooth muscle (i.e.Type: GrantFiled: April 19, 1991Date of Patent: January 4, 1994Assignee: Syntex Pharmaceutical Ltd.Inventors: Jean C. Pascal, Chi-Ho Lee, Brian J. Alps, Henri Pinhas, Roger L. Whiting, Calum B. MacFarlane, Serge Beranger, Robert J. Dow
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Patent number: 5252736Abstract: 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 oneor two; andq 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.Type: GrantFiled: November 7, 1991Date of Patent: October 12, 1993Assignee: Syntex Pharmaceuticals, Ltd.Inventors: Jean C. Pascal, Chi-Ho Lee, Brian J. Alps, Henri Pinhas, Roger L. Whiting
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Patent number: 5091428Abstract: 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; andq 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.Type: GrantFiled: February 7, 1991Date of Patent: February 25, 1992Assignee: Syntex Pharmaceuticals, Ltd.Inventors: Jean C. Pascal, Chi-Ho Lee, Brian J. Alps, Henri Pinhas, Roger L. Whiting
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Patent number: 5043447Abstract: 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.Type: GrantFiled: October 21, 1988Date of Patent: August 27, 1991Assignee: Syntex Pharmaceuticals, Ltd.Inventors: Jean C. Pascal, Chi-Ho Lee, Brian J. Alps, Henri Pinhas, Roger L. Whiting, Calum B. Macfarlane, Serge Beranger, Robert J. Dow
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Patent number: 5010075Abstract: 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; andq 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.Type: GrantFiled: April 6, 1990Date of Patent: April 23, 1991Assignee: Syntex Pharmaceuticals Ltd.Inventors: Jean C. Pascal, Chi-Ho Lee, Brian J. Alps, Henri Pinhas, Roger L. Whiting
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Patent number: 4935417Abstract: 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; andq 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.Type: GrantFiled: February 21, 1989Date of Patent: June 19, 1990Assignee: Syntex Pharmaceuticals Ltd.Inventors: Jean C. Pascal, Chi-Ho Lee, Brian J. Alps, Henri Pinhas, Roger L. Whiting
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Patent number: 4829065Abstract: 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; andq 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.Type: GrantFiled: April 24, 1987Date of Patent: May 9, 1989Assignee: Syntex Pharmaceuticals, Ltd.Inventors: Jean C. Pascal, Chi-Ho Lee, Brian J. Alps, Henri Pinhas, Roger L. Whiting
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Patent number: 4497818Abstract: 2-(1,4-Benzodioxan-2-ylalkyl)imidazoles having the general formula: ##STR1## wherein R.sup.1, and R.sup.2 and R.sup.3 are independently selected from the group consisting of hydrogen, and alkyl (1-6C), and wherein n is an integer equal to 0, 1 or 2, and the pharmaceutically acceptable acid addition salts thereof, are .alpha..sub.2 blockers and thus are useful as affectors of the CNS, specifically as platelet aggregation inhibitors and as antihypertensives.Type: GrantFiled: August 5, 1981Date of Patent: February 5, 1985Assignee: Syntex (U.S.A.) Inc.Inventors: Arthur F. Kluge, Arthur M. Strosberg, Roger L. Whiting, George A. Christie
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Patent number: 4436914Abstract: Compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein:n is an integer equal to 0, 1, 2 or 3;R.sup.1 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenyl lower alkyl;each R is independently hydrogen, lower alkyl, optionally substituted phenyl, or optionally substituted phenyl lower alkyl;are .alpha..sub.2 blockers, and, therefore, are useful in treating essential hypertension and depression, and in inhibiting platelet aggregation.Type: GrantFiled: August 3, 1981Date of Patent: March 13, 1984Inventors: Arthur F. Kluge, Arthur M. Strosberg, Roger L. Whiting, George A. Christie