Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2011-03-08
2011-03-08
Davis, Zinna N (Department: 1625)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S307000, C546S113000, C546S149000
Reexamination Certificate
active
07902218
ABSTRACT:
There is provided a series of tetrahydroisoquinoline diaminopropane compounds of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof,wherein R, R8and R9are as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
REFERENCES:
patent: 2006/0046984 (2006-03-01), Thompson, III et al.
patent: WO 03/072535 (2003-09-01), None
patent: WO 2004/013098 (2004-02-01), None
patent: WO 2005/016876 (2005-02-01), None
Luo, Yi, et al., “Mice deficient in BACE1, the Alzheimer's β-secretase, have normal phenotype and abolished β-amyloid generation”,Nature Neuroscience4 (2001) 231-232.
Roberds, S.L. et al., “BACE knockout mice are healthy despite lacking the primary β-secretase activity in brain: implications for Alzheimer's disease therapeutices”,Human Molecular Genetics10 (2001) 1317-1324.
Seiffert, D.; et al., “Presenilin-1 and -2 are molecular targets for γ-secretase inhibitors”,J. Biol. Chem.275 (2000) 34086-34091.
Selkoe, D. J., “Biochemical Analyses of Alzheimer's Brain Lesions lead to the Identification of αβ and its Precursor”,Ann. Rev. Cell Biol.10 (1994) 373-403.
Selkoe, D. J., “Alzheimer's Disease: Genes, Proteins, and Therapy”,Physiol. Rev.81 (2001) 741-766.
Sinha, S., et al., “Purification and cloning of amyloid precursor protein β-secretase from human brain”, Nature 402 (1999) 537-540.
Thal, D.R., et al., “Two Types of Sporadic Cerebral Amyloid Angiopathy”, J. Neuropath. Exp. Neuro. (2002) 61: 282-293.
Vassar, R., et al., “β-Secretase Cleavage of Alzheimer's Amyloid Precursor Protein by the Transmembrane Aspartic Protease BACE”, Science 286 (1999) 735-741.
Wolfe, M. J., “Secretase Targets for Alzheimer's Disease: Identification and Therapeutic Potential”, J. Med. Chem. 44 (2001) 2039-2060.
Yan, R., et al., “Membrane-anchored aspartyl protease with Alzheimer's disease β-secretase activity”, Nature 402 (1999) 533-537.
Boy Kenneth M.
Good Andrew C.
Macor John E.
Marcin Lawrence R.
Shi Jianliang
Algieri Aldo A.
Bristol--Myers Squibb Company
Davis Zinna N
Levis John F.
LandOfFree
Substituted tetrahydroisoquinolines as β-secretase... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Substituted tetrahydroisoquinolines as β-secretase..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Substituted tetrahydroisoquinolines as β-secretase... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2675122