Gamma-secretase inhibitors

Details Gamma-secretase inhibitors Gamma-secretase inhibitors

2006-12-14

2008-10-14

Habte, Kahsay T (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C514S363000, C514S364000, C514S365000, C514S372000

Reexamination Certificate

active

07435748

ABSTRACT:
Compounds of formula I:inhibit gamma-secretase and hence find use in treatment of Alzheimer's disease.

REFERENCES:
patent: WO 01/70677 (2001-09-01), None
patent: WO 02/36555 (2002-05-01), None
M. N. Pangalos et al., “Disease modifying strategies for the treatment of Alzheimer's disease targeted at modulating levels of the beta-amyloid peptide”, Biochemical Society Transactions, vol. 33, Part 4, pp. 553-558 (2005).
I. Churcher et al., “Gamma-Secretase as a Therapeutic Target for the Treatment of Alzheimer's Disease”, Current Pharmaceutical Design, vol. 11, pp. 3363-3382 (2005).
D. M. Barton et al., “Dynamics of Beta-Amyloid Reductions in Brain, Cerebrospinal Fluid and Plasma of Beta-Amyloid Precursor Protein Transgenic Mice Treated with a gamma-secretase Inhibitor”, JPET, vol. 312, No. 2, pp. 635-643 (2005).
E. R. Siemers et al., “Effects of a gamma-secretase inhibitor in a randomized study of patients with Alzheimer disease”, Neurology, vol. 66, pp. 602-604 (2006).
G. Evin et al., “Inhibition of gamma-secretase as a Therapeutic Intervention for Alzheimer's Disease”, CNS Drugs, vol. 20, No. 5, pp. 351-372 (2006).
M. S. Shearman et al., “L-685,458, and Aspartyl Protease Transition State Mimic, Is A Potent Inhibitor of Amyloid Beta-Secretase Precursor gamma-secretase Activity”, Biochemistry, vol. 39, pp. 8698-8704 (2000).
H. Josien, “Recent advances in the development of gamma-secretase inhibitors”, Current Opinion in Drug Discovery & Development, vol. 5, No. 4, pp. 513-525 (2002).
M. S. Wolfe, “Secretase Targets for Alzheimer's Disease: Identification and Therapeutic Potential”, J. Med. Chem., vol. 44, No. 13, pp. 2039-2060 (2001).
E. E. Clarke et al., “Quantitation of amyloid-beta peptides in biological milieu using a novel homogeneous time-resolved fluorescence (HTRF) assay”, J. of Neuroscience Methods, vol. 102, pp. 61-68 (2000).

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