Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2010-03-15
2011-10-25
Saeed, Kamal (Department: 1626)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C548S131000
Reexamination Certificate
active
08044077
ABSTRACT:
The present disclosure provides novel deuterated alpha-(N-sulfonamido)acetamide compounds, their pharmaceutical composition, processes thereof and a method for the treatment of Alzheimer's disease, head trauma, traumatic brain injury, and/or dementia pugilistica and/or other conditions associated with β-amyloid peptide.
REFERENCES:
patent: 5274094 (1993-12-01), Whittaker et al.
patent: 5516783 (1996-05-01), Whittaker et al.
patent: 6153612 (2000-11-01), Ortwine et al.
patent: 6221335 (2001-04-01), Foster
patent: 6313123 (2001-11-01), Levin et al.
patent: 6603008 (2003-08-01), Ando et al.
patent: 7300951 (2007-11-01), Kreft et al.
patent: 7517990 (2009-04-01), Ito et al.
patent: 7687666 (2010-03-01), Chan et al.
patent: 7786122 (2010-08-01), Parker et al.
patent: 7838550 (2010-11-01), Chan et al.
patent: 2007/0197695 (2007-08-01), Potyen et al.
patent: 11-343279 (1999-12-01), None
patent: WO 98/03166 (1998-01-01), None
patent: WO 00/44716 (2000-08-01), None
patent: WO 00/50391 (2000-08-01), None
patent: WO 03/053912 (2003-07-01), None
patent: WO 2005/042489 (2005-05-01), None
patent: WO 2005/095334 (2005-10-01), None
patent: WO 2006/005486 (2006-01-01), None
patent: WO 2006/034480 (2006-03-01), None
patent: WO 2007/098030 (2007-08-01), None
patent: WO 2008/112249 (2008-09-01), None
patent: WO 2009/005688 (2009-01-01), None
patent: WO 2009/058552 (2009-05-01), None
patent: WO 2009/137657 (2009-11-01), None
patent: WO 2010/107435 (2010-09-01), None
patent: WO 2010/107997 (2010-09-01), None
patent: WO 2010/108067 (2010-09-01), None
patent: WO 2010/120662 (2010-10-01), None
patent: WO 2010/120755 (2010-10-01), None
Dyck et al. Journal of Neurochemistry, 46(2) (1986) 399-404 ( Abstract Only).
U.S. Appl. No. 12/840,612, filed Jul. 21, 2010, Parker et al.
Chapman, P.F. et al., “Impaired synaptic plasticity and learning in aged amyloid precursor protein transgenic mice”, Nature Neuroscience, vol. 2, No. 3, pp. 271-276 (1999).
Clarke, W.J. et al., “Gender Differences in Oral Drug Exposure in the Rat with the Gamma-Secretase Inhibitor BMS-708163”, Drug Metab. Rev., Abstract No. 126, vol. 41, pp. 58-59 (2009).
Dahlgren, K.N. et al., “Oligomeric and Fibrillar Species of Amyloid-β Peptides Differentially Affect Neuronal Viability”, The Journal of Biological Chemistry, vol. 277, No. 35, pp. 32046-32053 (2002).
Freebern, W.J. et al., “From Phenotyping to Host Resistance Models: A Comprehensive Immunotoxicologic Investigation of a Gamma Secretase Inhibitor in Rats”, International Journal of Toxicology, Abstract No. P12, vol. 29, No. 1, pp. 91-92 (2010).
Gillman, K.W. et al., “Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor”, ACS Medicinal Chemistry Letters, vol. 1, pp. 120-124 (2010).
Golde, T.E., “Alzheimer's disease therapy: Can the amyloid cascade be halted?”, The Journal of Clinical Investigation, vol. 111, No. 1, pp. 11-18 (2003).
Götz, J. et al., “Formation of Neurofibrillary Tangles in P301L Tau Transgenic Mice Induced by Aβ 42 Fibrils”, Science, vol. 293, pp. 1491-1495 (2001).
Leil, T.A. et al. “Model-Based Trial Simulation for Optimal Collection of CSF Aβ Samples in Clinical Studies: Application for BMS-708163”, Clin. Pharmacol. Ther., Abstract No. OII-B-2, vol. 87, Suppl. 1, p. S38 (2010).
Lewis, J. et al., “Enhanced Neurofibrillary Degeneration in Transgenic Mice Expressing Mutant Tau and APP”, Science, vol. 293, pp. 1487-1491 (2001).
Loane, D.J. et al., “Amyloid precursor protein secretases as therapeutic targets for traumatic brain injury”, Nature Medicine, Advance Online Publication, pp. 1-3 (Mar. 15, 2009).
Maharvi, G.M. et al., “A synthesis of the γ-secretase inhibitor BMS-708163”, Tetrahedron Letters, online Oct. 14, 2010.
Mayer, S.C. et al., Discovery of Begacestat, a Notch-1-Sparing γ-Secretase Inhibitor for the Treatment of Alzheimer's Disease, Journal of Medicinal Chemistry, vol. 51, No. 23, pp. 7348-7351 (2008).
McLean, C.A. et al., “Soluble Pool of Aβ Amyloid as a Determinant of Severity of Neurodegeneration in Alzheimer's Disease”, Annals of Neurology, vol. 46, No. 6, pp. 860-866 (1999).
Seiffert, D. et al., “Presenilin-1 and -2 are Molecular Targets for γ-Secretase Inhibitors”, The Journal of Biological Chemistry, vol. 275, No. 44, pp. 34086-34091 (2000).
Selkoe, D.J., “Alzheimer's Disease: Genes, Proteins, and Therapy”, Physiological Reviews, vol. 81, No. 2, pp. 741-766 (2001).
Selkoe, D.J., “Cell Biology of the Amyloid β-Protein Precursor and the Mechanism of Alzheimer's Disease”, Annu. Rev. Cell Biol., vol. 10, pp. 373-403 (1994).
Siemers, E.R. et al., “Effects of a γ-secretase inhibitor in a randomized study of patients with Alzheimer disease”, Neurology, vol. 66, pp. 602-604 (2006).
Thal, D.R. et al., “Two Types of Sporadic Cerebral Amyloid Angiopathy”, Journal of Neuropathology and Experimental Neurology, vol. 61, No. 3, pp. 282-293 (2002).
Walsh, D.M. et al., “Naturally secreted oligomers of amyloid β protein potently inhibit hippocampal long-term potentiation in vivo”, Nature, vol. 416, pp. 535-539 (2002).
Watkins, T.A. et al., “Distinct Stages of Myelination Regulated by γ-Secretase and Astrocytes in a Rapidly Myelinating CNS Coculture System”, Neuron, vol. 60, pp. 555-569 (2008).
Wolfe, M.S., “Secretase Targets for Alzheimer's Disease: Identification and Therapeutic Potential”, Journal of Medicinal Chemistry, vol. 44, No. 13, pp. 2039-2060 (2001).
Zhang D. et al., “Disposition of a Gamma-Secretase Inhibitor 14C-Labeled BMS-708163 in Mice, Rats, Rabbits, Dogs, and Humans. Applications of Bile Collection in Differentiating Oxidative Versus Reductive Metabolic Pathways”, Drug Metab. Rev., Abstract No. 127, vol. 41, pp. 59-60 (2009).
2008 CSHL Meeting on Neurodegenerative Diseases, Oral Presentation: “BMS-708163, A Potent and Selective Gamma-Secretase Inhibitor, Decreases CSF A-Beta at Safe and Tolerable Doses in Animals and Humans”, Dec. 5, 2008.
2009 BMS URG Symposium, Oral Presentation: “The Discovery of BMS-708163: A Potent and Selective Gamma-Secretase Inhibitor for the Treatment of Alzheimer's Disease”, May 1, 2009.
237th National American Chemical Society Meeting, Salt Lake City, UT, Oral Presentation: “The Discovery of BMS-708163: A Potent and Selective Gamma-Secretase Inhibitor Which Lowers CSF Beta-Amyloid in Humans”, Mar. 22, 2009.
Alzheimer's Association International Conference on Alzheimer's Disease, Chicago, IL, Abstract, Jul. 26, 2008.
Alzheimer's Association International Conference on Alzheimer's Disease, Chicago, IL, Oral Presentation: “BMS-708163, A Potent and Selective Gamma-Secretase Inhibitor, Decreases CSF A-Beta at Safe and Tolerable Doses in Animals and Humans”, Jul. 30, 2008.
Alzheimer's Association International Conference on Alzheimer's Disease, Honolulu, HI, Poster: “A Comprehensive Immunotoxicologic Investigation of a Gamma Secretase Inhibitor in Rats”, Jul. 10-15, 2010.
Alzheimer's Association International Conference on Alzheimer's Disease, Honolulu, HI, Poster: “A Placebo-Controlled Ascending Multiple-Dose Study to Evaluate the Safety, Pharmacokinetics, and Pharmacodynamics of BMS-708163 in Healthy Young and Elderly Subjects”, Jul. 10-15, 2010.
Alzheimer's Association International Conference on Alzheimer's Disease, Honolulu, HI, Poster: “A Study to Evaluate the Effects of Single Oral Doses of BMS-708163 on the Cerebrospinal Fluid A-Beta Level in Healthy Young Men”, Jul. 10-15, 2010.
Alzheimer's Association International Conference on Alzheimer's Disease, Honolulu, HI, Poster: “Effect of Concomitant Administration of Multiple Doses of BMS-708163 on Safety and Tolerability and the Pharmacokinetics of
Gillman Kevin W.
Olson Richard E.
Starrett, Jr. John E.
Bristol--Myers Squibb Company
Mingo Pamela A.
Saeed Kamal
LandOfFree
Alpha-(N-sulfonamido)acetamide compounds incorporating... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Alpha-(N-sulfonamido)acetamide compounds incorporating..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Alpha-(N-sulfonamido)acetamide compounds incorporating... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-4275254