Patents Assigned to State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University and University of Oregon
  • Patent number: 6251948
    Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: June 26, 2001
    Assignee: State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University and the University of Oregon
    Inventors: Eckard Weber, John F. W. Keana
  • Patent number: 6251903
    Abstract: Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia, and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, and inducing anesthesia are disclosed by administering to an animal in need of such treatment an alkyl or azido-substituted 1,4-dihydroquinoxaline-2,3-dione or pharmaceutically acceptable salts thereof, which have high binding to the glycine receptor.
    Type: Grant
    Filed: September 13, 2000
    Date of Patent: June 26, 2001
    Assignees: Cocensys, Inc., State of Oregon, Acting by and through the Oregon State Board of Higher Education, Acting for and on behalf of the Oregon Health Sciences University and the University of Oregon, The Regents of the University of California
    Inventors: Sui Xiong Cai, Eckard Weber, John F. W. Keana, Sunil Kher
  • Patent number: 6147075
    Abstract: Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia, and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, and inducing anesthesia are disclosed by administering to an animal in need of such treatment an alkyl or azido-substituted 1,4-dihydroquinoxaline-2,3-dione or pharmaceutically acceptable salts thereof, which have high binding to the glycine receptor.
    Type: Grant
    Filed: August 18, 1999
    Date of Patent: November 14, 2000
    Assignees: CoCensys, Inc., State of Oregon, Acting by and Through the Oregon State Board of Higher Education, Acting for and on Behalf of the Oregon Health Sciences University and the University of Oregon, Eugene Oregon, The Regents of the University of California
    Inventors: Sui Xiong Cai, Eckard Weber, John F. W. Keana, Sunil Kher
  • Patent number: 6017910
    Abstract: The invention relates to 5-(iminomethano)-10,11-dihydro-5H-dibenzo[a,d]cycloheptene and derivatives thereof. The invention also relates to the use of such compounds for the treatment or prevention of neuronal loss in ischemia, hypoxia, brain or spinal chord trauma, as well as for the treatment of Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: January 25, 2000
    Assignee: State of Oregon, acting by and through the Oregon State Board of Higher Education acting for and on behalf of the Oregon Health Sciences University and the University of Oregon
    Inventors: Eckard Weber, John F. W. Keana, Peter Barmettler
  • Patent number: 5977107
    Abstract: Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia, and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, and inducing anesthesia are disclosed by administering to an animal in need of such treatment an alkyl or azido-substituted 1,4-dihydroquinoxaline-2,3-dione or pharmaceutically acceptable salts thereof, which have high binding to the glycine receptor.
    Type: Grant
    Filed: January 31, 1997
    Date of Patent: November 2, 1999
    Assignees: Cocensys, Inc., State of Oregon, Acting by and Through the Oregon State Board of Higher Education, acting for and on Behalf of the Oregon Health Sciences University and the University of Oregon, Eugene Oregon, The Regents of the University of California
    Inventors: Sui Xiong Cai, Eckard Weber, John F. W. Keana, Sunil Kher
  • Patent number: 5863916
    Abstract: Disclosed are compounds of the formula: ##STR1## or pharmaceutically acceptable salts thereof; wherein n is zero or 1; R.sup.4, R.sup.5, R.sup.6 are independently hydrogen, nitro, amino, halo, haloalkyl, cyano, alkyl, cycloalkyl, alkenyl, alkynyl, azido, acylamino, alkylsulfonyl, aryl, substituted aryl, heteroaryl, alkoxy, trialkylsilyl-substituted alkoxy, aryloxy, substituted aryloxy, heteroaryloxy, a heterocyclic group, a heterocyclicoxy group, aralkoxy, or haloalkoxy; and R.sup.c and R.sup.d are defined in the specification. These compounds have high binding to the glycine site of the NMDA receptor. Also disclosed are methods of treating pathophysiologic conditions associated with neuronal degeneration, convulsions, anxiety, chronic pain, pyschosis, opiate tolerance, and inducing anesthesia.
    Type: Grant
    Filed: February 4, 1997
    Date of Patent: January 26, 1999
    Assignees: State of Oregon, Acting by and Through the Oregon State Board of Higher-Education, Acting for and on Behalf of the Oregon Health Sciences University and The University of Oregon, The Regents of the University of California, Cocensys, Inc.
    Inventors: Sui Xiong Cai, John F. W. Keana, Eckard Weber
  • Patent number: 5801183
    Abstract: Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, and Down's syndrome, treating or preventing adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, inducing anesthesia, and treating or preventing opiate tolerance are disclosed by administering to an animal in need of such treatment or prevention a substituted or unsubstituted pyridine and pyridine (N-oxide) analogs of 4-hydroxydihydroquinolones, tetrahydroquinoline-trione-oximes and quinoxalones, tautomers and pharmaceutically acceptable salts thereof, which have high binding to the glycine receptor.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 1, 1998
    Assignees: State of Oregon, Acting by and Through the Oregon State Board of Higher Education, Acting for and on Behalf of the Oregon Health Sciences University and the University of Oregon, Cocensys, Inc.
    Inventors: John F. W. Keana, Sui Xiong Cai, Zhang-Lin Zhou, James M. Navratil
  • Patent number: 5798390
    Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: August 25, 1998
    Assignee: State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University and the University of Oregon
    Inventors: Eckard Weber, John F. W. Keana
  • Patent number: 5767162
    Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: June 16, 1998
    Assignee: State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University and the University of Oregon
    Inventors: Eckard Weber, John F. W. Keana
  • Patent number: 5708168
    Abstract: Disclosed are methods of preparing azepines by a multistep synthesis including a Diels-Alder reaction. Also disclosed are methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, inducing anesthesia and treating or preventing opiate tolerance are disclosed by administering to an animal in need of such treatment an azepine which has high binding to the NMDA glycine site.
    Type: Grant
    Filed: October 17, 1995
    Date of Patent: January 13, 1998
    Assignees: State of Oregon, Acting by and through The Oregon State Board of Higher Education, Acting for and on behalf of The Oregon Health Sciences University and The University of Oregon, Eugene Oregon, ACEA Pharmaceuticals, Inc.
    Inventors: John F. W. Keana, Anthony P. Guzikowski, Daniel F. Nogales, Sui Xiong Cai
  • Patent number: 5688789
    Abstract: The invention relates to 5-(iminomethano)-10,11-dihydro-5H-dibenzo?a,d!cycloheptene and derivatives thereof. The invention also relates to the use of such compounds for the treatment or prevention of neuronal loss in ischemia, hypoxia, brain or spinal chord trauma, as well as for the treatment of Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: November 18, 1997
    Assignee: State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University and the University of Oregon
    Inventors: Eckard Weber, John F. W. Keana, Peter Barmettler
  • Patent number: 5637622
    Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: June 10, 1997
    Assignee: State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University and the University of Oregon
    Inventors: Eckard Weber, John F. W. Keana
  • Patent number: 5631373
    Abstract: Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia, and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, and inducing anesthesia are disclosed by administering to an animal in need of such treatment an alkyl or azido-substituted 1,4-dihydroquinoxaline-2,3-dione or pharmaceutically acceptable salts thereof, which have high binding to the glycine receptor.
    Type: Grant
    Filed: August 11, 1994
    Date of Patent: May 20, 1997
    Assignees: State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University and the University of Oregon, Eugene Oregon, Acea Pharmaceuticals, Inc., The Regents of the University of California
    Inventors: Sui X. Cai, Eckard Weber, John F.W. Keana, Sunil Kher
  • Patent number: 5622952
    Abstract: Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, inducing anesthesia and treating psychosis are disclosed by administering to an animal in need of such treatment a compound having high affinity for the glycine binding site, lacking PCP side effects and which crosses the blood brain barrier of the animal.Also disclosed are novel 1,4-dihydroquinoxaline-2,3-diones, and pharmaceutical compositions thereof. Also disclosed are highly soluble ammonium salts of 1,4-dihydroquinoxaline-2,3-diones.
    Type: Grant
    Filed: March 17, 1995
    Date of Patent: April 22, 1997
    Assignees: State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University and the University of Oregon, Eugene Oregon, The Regents of the University of California
    Inventors: Eckard Weber, John F. W. Keana
  • Patent number: 5622965
    Abstract: Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions and inducing anesthesia are disclosed by administering to an animal in need of such treatment a substituted or unsubstituted 4-hydroxy-3-nitro-1,2-dihydroquinolin-2-one or pharmaceutically acceptable salts thereof which have high binding to the glycine receptor.
    Type: Grant
    Filed: August 2, 1993
    Date of Patent: April 22, 1997
    Assignees: State of Oregon, acting by and through The Oregon State Board of Higher Education, acting for and on behalf of The Oregon Health Sciences University and The University of Oregon, Eugene Oregon, The Regents of the University of California
    Inventors: Sui X. Cai, Eckard Weber, John F. W. Keana
  • Patent number: 5620979
    Abstract: Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, inducing anesthesia and treating psychosis are disclosed by administering to an animal in need of such treatment a compound having high affinity for the glycine binding site, lacking PCP side effects and which crosses the blood brain barrier of the animal.Also disclosed are novel 1,4-dihydroquinoxaline-2,3-diones, and pharmaceutical compositions thereof. Also disclosed are highly soluble ammonium salts of 1,4-dihydroquinoxaline-2,3-diones.
    Type: Grant
    Filed: March 17, 1995
    Date of Patent: April 15, 1997
    Assignees: State of Oregon, Acting By and Through The Oregon State Board of Higher Education, Acting For and On Behalf of The Oregon Health Sciences University and The University of Oregon, Eugene Oregon, The Regents of The University of California
    Inventors: Eckard Weber, John F. W. Keana
  • Patent number: 5620978
    Abstract: Disclosed is a method of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma or hypoglycemia. The method comprises administering to an animal a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof; wherein n is zero or 1; R.sup.4, R.sup.5, R.sup.6 are independently hydrogen, nitro, amino, halo, haloalkyl, cyano, alkyl, cycloalkyl, alkenyl, alkynyl, azido, acylamino, alkylsulfonyl, aryl, substituted aryl, heteroaryl, alkoxy, trialkylsilyl-substituted alkoxy, aryloxy, substituted aryloxy, heteroaryloxy, a heterocyclic group, a heterocyclicoxy group, aralkoxy, or haloalkoxy; and R.sup.c and R.sup.d are defined in the specification. These compounds have high binding to the glycine site of the NMDA receptor.
    Type: Grant
    Filed: January 3, 1995
    Date of Patent: April 15, 1997
    Assignees: State of Oregon, acting by and through The Oregon State Board of Higher Education, acting for and on behalf of The Oregon Health Sciences University and The University of Oregon, Eugene Oregon, The Regents of the University of California, ACEA Pharmaceuticals, Inc.
    Inventors: Sui X. Cai, John F. W. Keana, Eckard Weber
  • Patent number: 5597922
    Abstract: Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions and inducing anesthesia are disclosed by administering to an animal in need of such treatment a compound which has high binding to the glycine receptor.
    Type: Grant
    Filed: July 29, 1994
    Date of Patent: January 28, 1997
    Assignees: State of Oregon, Acting by and through the Oregon State Board of Higher Education, Acting for and on Behalf of the Oregon Health Sciences University and the University of Oregon, Acea Pharmaceuticals, Inc., The Regents of the University of California
    Inventors: Sui X. Cai, John F. W. Keana, Eckard Weber
  • Patent number: 5502255
    Abstract: N,N-disubstituted-guanidines, e.g., of the formula ##STR1## wherein R and R' are substituted or unsubstituted hydrocarbon groups. Methods are provided for the treatment of psychosis and hypertension by administering an effective amount of an N,N'-disubstituted guanidine which, preferably, has a high affinity for the sigma receptor.
    Type: Grant
    Filed: February 23, 1993
    Date of Patent: March 26, 1996
    Assignee: State of Oregon acting by and through the Oregon State Board of Higher Education, acting for and on behalf of The Oregon Health Sciences University and The University of Oregon
    Inventors: John Keana, Eckard Weber
  • Patent number: 5476933
    Abstract: Disclosed are methods of preparing azepines by a multistep synthesis including a Diels-Alder reaction. Also disclosed are methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, inducing anesthesia and treating or preventing opiate tolerance are disclosed by administering to an animal in need of such treatment an azepine which has high binding to the NMDA glycine site.
    Type: Grant
    Filed: November 16, 1994
    Date of Patent: December 19, 1995
    Assignees: State of Oregon, acting by and through The Oregon State Board of Higher Education, acting for and on behalf of The Oregon health Sciences University and The University of Oregon, Acea Pharmaceuticals, Inc.
    Inventors: John F. W. Keana, Anthony P. Guzikowski, Daniel F. Nogales, Sui X. Cai