Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Reexamination Certificate
2008-05-20
2008-05-20
O'Sullivan, Peter (Department: 1621)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
C564S099000
Reexamination Certificate
active
07375136
ABSTRACT:
NMDA receptor blockers, including pH-sensitive NMDA receptor blockers, are provided as neuroprotective drugs that are useful in stroke, traumatic brain injury, epilepsy, and other neurologic events that involve acidification of brain or spinal cord tissue. Compositions and methods of this invention are used for treating neurodegeneration resulting from NMDA receptor activation. The compounds described herein have enhanced activity in brain tissue having lower-than normal pH due to pathological conditions such as hypoxia resulting from stroke, traumatic brain injury, global ischemia that may occur during cardiac surgery, hypoxia that may occur following cessation of breathing, pre-eclampsia, spinal cord trauma, epilepsy, chronic pain, vascular dementia and glioma tumors. Compounds described herein are also useful in preventing neurodegeneration in patients with Parkinson's Alzheimer's, Huntington's chorea, ALS, and other neurodegenerative conditions known to the art to be responsive to treatment using NMDA receptor blockers. Preferably the compounds provided herein are allosteric NMDA inhibitors.
REFERENCES:
patent: 4906779 (1990-03-01), Weber et al.
patent: 4924008 (1990-05-01), Abou-Gharbia et al.
patent: 4957909 (1990-09-01), Abou-Gharbia et al.
patent: 4959366 (1990-09-01), Cross et al.
patent: 4994467 (1991-02-01), Zimmerman
patent: 5013540 (1991-05-01), Redburn
patent: 5034400 (1991-07-01), Olney
patent: 5039528 (1991-08-01), Olney
patent: 5093525 (1992-03-01), Weber
patent: 5095009 (1992-03-01), Whitten
patent: 5106847 (1992-04-01), Salituro
patent: 5118675 (1992-06-01), Jirkovsky
patent: 5124319 (1992-06-01), Baudy
patent: 5132313 (1992-07-01), Kozikowski
patent: 5179085 (1993-01-01), Bigge
patent: 5189054 (1993-02-01), Salituro
patent: 5190976 (1993-03-01), Weber
patent: 5192751 (1993-03-01), Thor
patent: 5194430 (1993-03-01), Whitten
patent: 5262568 (1993-11-01), Weber
patent: 5318985 (1994-06-01), McDonald
patent: 5321012 (1994-06-01), Mayer
patent: 5326756 (1994-07-01), Whitten
patent: 5336689 (1994-08-01), Weber
patent: 5385903 (1995-01-01), Steppuhn
patent: 5385947 (1995-01-01), Godel
patent: 5395822 (1995-03-01), Izumi
patent: 5441963 (1995-08-01), McDonald
patent: 5470844 (1995-11-01), Whitten
patent: 5474990 (1995-12-01), Olney
patent: 5489579 (1996-02-01), McDonald
patent: 5491153 (1996-02-01), Salituro
patent: 5498610 (1996-03-01), Chenard
patent: 5502058 (1996-03-01), Mayer
patent: 5519048 (1996-05-01), Salituro
patent: 5538958 (1996-07-01), Whitten
patent: 5556838 (1996-09-01), Mayer
patent: 5559154 (1996-09-01), Weber
patent: 5563157 (1996-10-01), Harrison
patent: 5587384 (1996-12-01), Zhang
patent: 5594007 (1997-01-01), Chenard
patent: 5605911 (1997-02-01), Olney
patent: 5606063 (1997-02-01), Harrison
patent: 5614509 (1997-03-01), Turski
patent: 5616580 (1997-04-01), Olney
patent: 5629307 (1997-05-01), Olney
patent: 5633379 (1997-05-01), Allgeier
patent: 5637622 (1997-06-01), Weber
patent: 5654281 (1997-08-01), Mayer
patent: 5675018 (1997-10-01), Salituro
patent: 5703107 (1997-12-01), Salituro
patent: 5710139 (1998-01-01), Swahn
patent: 5710168 (1998-01-01), Chenard
patent: 5714500 (1998-02-01), Griffith
patent: 5753657 (1998-05-01), Aloup
patent: 5767130 (1998-06-01), Olney
patent: 5767162 (1998-06-01), Weber
patent: 5777114 (1998-07-01), Aloup
patent: 5783572 (1998-07-01), Mowbray
patent: 5783700 (1998-07-01), Nichols
patent: 5798390 (1998-08-01), Weber
patent: 5834465 (1998-11-01), Olney
patent: 5834479 (1998-11-01), Mayer
patent: 5840731 (1998-11-01), Mayer
patent: 5863922 (1999-01-01), Mayer
patent: 5866585 (1999-02-01), Fogel
patent: 5869498 (1999-02-01), Mayer
patent: 5888996 (1999-03-01), Farb
patent: 5889026 (1999-03-01), Alanine
patent: 5902815 (1999-05-01), Olney
patent: 5919826 (1999-07-01), Caruso
patent: 5922716 (1999-07-01), Aloup
patent: 5925634 (1999-07-01), Olney
patent: 5952344 (1999-09-01), Alanine
patent: 5958919 (1999-09-01), Olney
patent: 5962472 (1999-10-01), Bourson
patent: RE36397 (1999-11-01), Zhang
patent: 5981553 (1999-11-01), Farr
patent: 5990126 (1999-11-01), Park
patent: 6007841 (1999-12-01), Caruso
patent: 6025369 (2000-02-01), Rosenquist
patent: 6034134 (2000-03-01), Gold
patent: 6054451 (2000-04-01), Caruso
patent: 6057358 (2000-05-01), Chung et al.
patent: 6057373 (2000-05-01), Fogel
patent: 6071929 (2000-06-01), Alanine
patent: 6071966 (2000-06-01), Gold
patent: 6080743 (2000-06-01), Acklin
patent: 6083941 (2000-07-01), Farb
patent: 6096743 (2000-08-01), Shishikura
patent: 6177434 (2001-01-01), Kopke
patent: 6180786 (2001-01-01), Metz, Jr.
patent: 6184236 (2001-02-01), Alanine et al.
patent: 6187338 (2001-02-01), Caruso
patent: 6194000 (2001-02-01), Smith
patent: 6197820 (2001-03-01), Sontheimer
patent: 6200990 (2001-03-01), Namil
patent: 6242456 (2001-06-01), Shuster
patent: 6251948 (2001-06-01), Weber
patent: 6258827 (2001-07-01), Chenard
patent: 6265426 (2001-07-01), Alanine
patent: 6274633 (2001-08-01), Franks
patent: 6284774 (2001-09-01), Wright
patent: 6284776 (2001-09-01), Meltzer
patent: 6294583 (2001-09-01), Fogel
patent: 6339093 (2002-01-01), Alanine
patent: 91/13865 (1991-09-01), None
patent: WO 91/13865 (1991-09-01), None
patent: WO 01/02406 (2001-01-01), None
Connors et al., Chem. Abst. 114:228481.
Alanine, A. et al., “1-benzyloxy-4,5-dihydro-1H-imidzzol-2-yl-amines, a novel class of NR1/2B subtype selective NMDA receptor antagonists,” Bioorganic & Medicinal Chemistry Letters 13:3155-3159, 2003.
Bradford, H. R., “Glutamate, GABA, and epilepsy,” Progress in Neurobiology 47:477-511, 1995.
Choi, D., “Antagonizing excitotoxicity: A therapeutic strategy for stroke?” Mount Sinai J. Med. 65(2):133-138, 1998.
Claiborne, C. F. et al., “Orally efficacious NR2B-selective NMDA receptor antagonists,” Bioorganic & Medicinal Chemistry Letters 13:697-700, 2003.
Curtis, N. R., “Novel N1-(benzyl)dinnamamidine derived NR2B subtype-selective NMDA receptor antagonists,” Bioorganic & Medicinal Chemistry Letters 13:693-696, 2003.
Dingledine, R. et al., “The glutamate receptor ion channels,” Pharmacological Reviews 51(1):7-61, 1999.
Dirnagl, U. et al., “Pathobiology of ischaemic stroke: An integrated view,” TINS 22(9):391-397, 1999.
McNamara, J. O., “Drugs effective in the therapy of the epilepsies,” Chapter 21 In Goodman & Gliman's:The Pharmacological Basis of Therapeutics, J. G. Hardman and L. E. Limbird (eds.), McGraw Hill, New York, pp. 521-547, 2001.
Mott, D. D. et al., “Phenylethanolamines inhibit NMDA receptors by enhancing proton inhibition,” Nature Neuroscience 1(8):659-667, 1998.
Muir, K. W. et al., “Clinical experience with excitatory amino acid antagonist drugs,” Stroke 26:503-513, 1995.
Obrenovitch, T. P. et al., “Is high extracellular glutamate the key to excitotoxicity in traumatic brain injury?” J. Neurotrauma 14(10):677-698, 1997.
Rothstein, J. D. et al., “Excitotoxic destruction facilitates brain tumor growth,” Nature Medicine 7(9):994-995, 2001.
Rzeski, W. et al., “Glutamate antagonists limit tumor growth,” Proc. Natl. Acad. Sci. 98(11):6372-6377, 2001.
Takano, T. et al., “Glutamate release promotes growth of malignant gliomas,” Nature Medicine 7(9):1010-1015, 2001.
Traynelis, S. F. et al., “Proton inhibition of N-methyl-D-aspartate receptors in cerebellar neurons,” Nature 345:347-350, 1990.
Traynelis, S. F. et al., “Control of proton sensitivity of the NMDA receptor by RNA splicing and polyamines,” Science 268:873-876-1995.
International Search Report of International Application No. PCT/US02/07053, date of mailing Sep. 11, 2002, 2 pages.
Altas Yesim
Dingledine Raymond J.
Doherty, Jr. James J.
Liotta Dennis C.
Mott David D.
Emory University
King & Spalding
O'Sullivan Peter
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