Anthony P Guzikowski

US Patent:

6534522, Mar 18, 2003

Filed:

Feb 7, 2001

Appl. No.:

09/779024

Inventors:

Christopher F. Bigge - Ann Arbor MI
Gian Luca Araldi - Washington DC
Sui Xiong Cai - Foothill CA
Anthony P. Guzikowski - Eugene OR
Donald Lamunyon - Tualatin OR
Nancy C. Lan - South Pasadena CA
John F. W. Keana - Eugene OR

Assignee:

Warner-Lambert Company - Morris Plains NJ
Cocensys, Incorporated - Irvine CA

International Classification:

C07D40112

US Classification:

514307, 546139, 546148

Abstract:

The invention relates to subtype-selective NMDA receptor ligands and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimers disease, amyotrophic lateral sclerosis, Huntingtons disease and Downs syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, Parkinsons disease, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.

US Patent:

6534525, Mar 18, 2003

Filed:

Jun 21, 2000

Appl. No.:

09/598162

Inventors:

Christopher F. Bigge - Ann Arbor MI
John F. W. Keana - Eugene OR
Sui Xiong Cai - Foothill CA
Eckard Weber - Laguna Beach CA
Richard Woodward - Aliso Viejo CA
Nancy C. Lan - South Pasadena CA
Anthony P. Guzikowski - Eugene OR

Assignee:

Warner-Lambert Company - Morris Plains NJ
Cocensys, Inc. - Irvine CA

International Classification:

A61K 31445

US Classification:

514317, 514331, 546229, 546236

Abstract:

Novel 2-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 2-substituted piperidine analogs as selectively active antagonist of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, anxiety, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headaches, chronics pain, glaucoma, CMV retinitis, psychosis, urinary incontinence, opioid tolerance or withdrawal, or neurodegenerative disorders, such as lathyrism, Alzheimers Disease, Parkinsonism and Huntingtons Disease are described.

US Patent:

20030144319, Jul 31, 2003

Filed:

Nov 14, 2002

Appl. No.:

10/293474

Inventors:

Christopher Bigge - Ann Arbor MI, US
Gian Araldi - Washington DC, US
Sui Cai - Foothill CA, US
Anthony Guzikowski - Eugene OR, US
Donald Lamunyon - Junction City OR, US
Nancy Lan - South Pasadena CA, US
John Keana - Eugene OR, US

International Classification:

A61K031/4709
C 07D 4 1/02

US Classification:

514/307000, 546/148000, 546/150000

Abstract:

The invention relates to subtype-selective NMDA receptor ligands and the use thereof for 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 overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, Parkinson's disease, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.

US Patent:

62184040, Apr 17, 2001

Filed:

Sep 16, 1998

Appl. No.:

9/091592

Inventors:

Christopher F. Bigge - Ann Arbor MI
Gian Luca Araldi - Washington DC
Sui Xiong Cai - Foothill CA
Anthony P. Guzikowski - Eugene OR
Donald Lamunyon - Tualatin OR
Nancy F. Lan - South Pasadena CA
John F. W. Keana - Eugene OR

Assignee:

Warner-Lambert Co. - Morris Plains NJ
Cocensys, Inc. - Irvine CA

International Classification:

C07D21106
A61K 31445

US Classification:

514317

Abstract:

The invention relates to subtype-selective NMDA receptor ligands and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neuro-degenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, Parkinson's disease, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.

US Patent:

54769337, Dec 19, 1995

Filed:

Nov 16, 1994

Appl. No.:

8/341154

Inventors:

John F. W. Keana - Eugene OR
Anthony P. Guzikowski - Eugene OR
Daniel F. Nogales - Nampa ID
Sui X. Cai - Irvine CA

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 - Eugene OR
Acea Pharmaceuticals, Inc. - Menlo Park CA

International Classification:

C07D 1504
A61K 3155

US Classification:

540521

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.

US Patent:

6124323, Sep 26, 2000

Filed:

Sep 16, 1998

Appl. No.:

9/091598

Inventors:

Christopher F. Bigge - Ann Arbor MI
Sui Xiong Cai - Foothill CA
Eckard Weber - Laguna Beach CA
Richard Woodward - Aliso Viejo CA
Nancy C. Lan - South Pasadena CA
John F. W. Keana - Eugene OR
Anthony P. Guzikowski - Eugene OR

Assignee:

Warner-Lambert Company - Morris Plains NJ
Cocensys, Incorporated - Irvine CA

International Classification:

A01N 4340
C07D21126
C07D21160
C07D21118
C07D21120

US Classification:

514327

Abstract:

Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs are selective active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, psychosis, anxiety, migraine headaches, glaucoma, CMV retinitis, aminoglycoside antibiotics-induced hearing loss, convulsions, chronic pain, opioid tolerance or withdrawal, urinary incontinence or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.

US Patent:

61243175, Sep 26, 2000

Filed:

Nov 18, 1998

Appl. No.:

9/091593

Inventors:

Christopher F. Bigge - Ann Arbor MI
John F. W. Keana - Eugene OR
Sui Xiong Cai - Foothill CA
Eckard Weber - Laguna Beach CA
Richard Woodward - Aliso Viejo CA
Nancy C. Lan - South Pasadena CA
Anthony P. Guzikowski - Eugene OR

Assignee:

Warner-Lambert Company - Morris Plains NJ
Cocensys, Inc. - Irvine CA

International Classification:

A01N 4340

US Classification:

514317

Abstract:

Novel 2-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 2-substituted piperidine analogs as selectively active antagonists of N-methyl-D-aspartatc (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, anxiety, convulsions, amioglycoside antibiotics-induced hearing loss, migraine headaches, chronic pain, glaucoma, CMV retinitis, psychosis, urinary incontinence, opioid tolerance or withdrawal, or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.

US Patent:

57081689, Jan 13, 1998

Filed:

Oct 17, 1995

Appl. No.:

8/544107

Inventors:

John F. W. Keana - Eugene OR
Anthony P. Guzikowski - Eugene OR
Daniel F. Nogales - Nampa ID
Sui Xiong Cai - Irvine CA

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, Eugene Oregon - Eugene OR
ACEA Pharmaceuticals, Inc. - Irvine CA

International Classification:

C07D22316
C07D22332
A61K 3155

US Classification:

540520

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.