Patents by Inventor Brian R. de Costa
Brian R. de Costa 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: 6656930Abstract: Certain aralkyl diazabicycloalkyl compounds are disclosed for treatment of CNS disorders, such as cerebral ischemia, psychosis, and convulsions.Type: GrantFiled: September 4, 2001Date of Patent: December 2, 2003Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Wayne D Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
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Publication number: 20020045624Abstract: Certain aralkl diazabicycloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions.Type: ApplicationFiled: September 4, 2001Publication date: April 18, 2002Inventors: Wayne D. Bowen, Brian R. De Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
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Patent number: 6310064Abstract: Certain aralkyl diazabicycloalkyl compounds are disclosed for treatment of CNS disorders, such as cerebral ischemia, psychosis, and convulsions.Type: GrantFiled: July 6, 1999Date of Patent: October 30, 2001Assignee: The United States of America as represented by the of Department of Health and Human ServicesInventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
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Patent number: 5958920Abstract: Certain aralkyl diazabicycloalkyl compounds are disclosed for treatment of CNS disorders, such as cerebral ischemia, psychosis and convulsions.Type: GrantFiled: October 20, 1997Date of Patent: September 28, 1999Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
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Patent number: 5856318Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower alkyl, benzyl, and haloloweralkyl;wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 11, 1997Date of Patent: January 5, 1999Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
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Patent number: 5739158Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychotic disorders, convulsions and parkinsonism. Compounds of particular interest are of the formula ##STR1## wherein R.sup.1 is selected from hydrido, loweralkyl, cycloalkylalkyl of four to six carbon atoms and loweralkenylloweralkyl; wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and loweralkyl; wherein each of R.sup.4 through R.sup.7, R.sup.10 and R.sup.Type: GrantFiled: July 1, 1992Date of Patent: April 14, 1998Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Brian R. de Costa, Kenner C. Rice, Nancy M. Gray, Patricia C. Contreras, Arthur E. Jacobson, Andrew Thurkauf, Lilian A. Radesca, Wayne D. Bowen, J. Michael Walker
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Patent number: 5679679Abstract: Certain aralkyl diazabicyloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein: each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from the group consisting of hydrido, loweralkyl, benzyl and haloloweralkyl;each of R.sup.2, R.sup.3, and R.sup.8 through R.sup.Type: GrantFiled: December 2, 1994Date of Patent: October 21, 1997Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
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Patent number: 5679673Abstract: Certain aralkyl diazabicycloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R, R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower-alkyl, benzyl, and haloloweralkyl; wherein each of R.sup.2, R.sup.3 and R.sup.10 through R.sup.13 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein each of R.sup.8 and R.sup.Type: GrantFiled: November 21, 1994Date of Patent: October 21, 1997Assignee: The United States of America, represented by the Department of Health and Human ServicesInventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
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Patent number: 5656625Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower alkyl, benzyl, and haloloweralkyl;wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 17, 1995Date of Patent: August 12, 1997Assignees: The United States of America as represented by the Department of Health and Human Services, Brown University Research FoundationInventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
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Patent number: 5571832Abstract: Compounds comprising a pyrrolidinyl ring are disclosed for use in the treatment of cerebral ischemia.Type: GrantFiled: June 20, 1994Date of Patent: November 5, 1996Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Brian R. de Costa, Wayne D. Bowen, Xiao-Shu He, Lilian Radesca, Kenner C. Rice
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Patent number: 5468854Abstract: Conjugates of fluorescent labels with specific, selective, and high affinity ligands for receptors have been synthesized and used to directly measure binding to receptors. In the examples, fluorescein conjugates of the high-affinity benzodiazepine receptor ligands Ro 15-1788 and Ro 7-1986 were synthesized. The binding of these fluorescent ligands (BD 621, BD 623 and BD 607) to benzodiazepine receptors was characterized by direct fluorescence measurement. Both the equilibrium dissociation constants (K.sub.D) of BD 621 and BD 607 and the maximum number of binding sites (B.sub.max) estimated by fluorescence monitoring were consistent with values obtained by using radioligand binding techniques. The binding of BD 621 and BD 607 assessed by fluorescence measurement was reversible, abolished by photoaffinity labeling with Ro 15-4513, and unaffected by a variety of substances that do not bind to benzodiazepine receptors.Type: GrantFiled: July 22, 1993Date of Patent: November 21, 1995Assignee: Pharmaceutical Discovery CorporationInventors: R. Tyler McCabe, Brian R. de Costa
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Patent number: 5346908Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower alkyl, benzyl, and haloloweralkyl; wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 25, 1992Date of Patent: September 13, 1994Assignees: National Institutes of Health, Brown UniversityInventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
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Patent number: 5336483Abstract: The present invention is directed to radiolabeled N-substituted-6-iodo-3,14-dihydroxy-4,5.alpha.-epoxymorphinans, intermediates for producing the same, and a process for the preparation and methods of detecting opioid receptors. The radioimaging agent of the present invention has the following formula: ##STR1## wherein I is selected from the group consisting of .sup.123 L and .sup.125 ; and where R is alkyl, cycloalkylloweralkyl or allyl.Type: GrantFiled: January 13, 1993Date of Patent: August 9, 1994Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Brian R. de Costa, Michael J. Iadarola, Kenner C. Rice, Richard B. Rothman, Karen F. Berman
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Patent number: 5208338Abstract: The present invention is directed to radiolabeled N-substituted-6-iodo-3,14-dihydroxy-4,5.alpha.-epoxymorphinans, intermediates for producing the same, and a process for the preparation and methods of detecting opioid receptors.The radioimaging agent of the present invention has the following formula: ##STR1## wherein I is selected from the group consisting of .sup.123 I and .sup.125 I; and where R is alkyl, cycloalkylloweralkyl or allyl.Type: GrantFiled: June 14, 1991Date of Patent: May 4, 1993Assignee: The United States of America as represented by the Department of Health & Human Services.Inventors: Brian R. de Costa, Michael J. Iadarola, Kenner C. Rice, Richard B. Rothman, Karen F. Berman
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Patent number: 5130330Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychotic disorders and convulsions. Compounds of particular interest are of the formula ##STR1## wherein R.sup.1 is selected from hydrido, loweralkyl, cycloalkylalkyl of four to six carbon atoms, and loweralkenylloweralkyl; wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and loweralkyl; wherein each of R.sup.4 through R.sup.7, R.sup.10 and R.sup.Type: GrantFiled: January 31, 1990Date of Patent: July 14, 1992Assignee: G. D. Searle & Co.Inventors: Brian R. de Costa, Kenner C. Rice, Nancy M. Gray, Patricia C. Contreras, Arthur E. Jacobson, Andrew Thurkauf, Lilian A. Radesca, Wayne D. Bowen