β secretase inhibitor

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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Details

C514S383000, C514S392000, C548S262600, C548S300100, C548S251000

Reexamination Certificate

active

07816387

ABSTRACT:
The present invention relates to a compound of the formula (1):wherein R1is group of the formula (2):(wherein X is nitrogen atom or C(R5), Y is nitrogen atom or C(R6), R5and R6are each independently hydrogen atom, etc.) etc., m is 1 to 6, L1is single bond, etc., R2is hydrogen atom, substituted or unsubstituted alkyl group, etc., R3is hydrogen atom, etc., L2is single bond, etc., R4is hydrogen atom, substituted or unsubstituted aryl group, etc., or pharmaceutically acceptable salt thereof, being useful for preventing or treating Alzheimer's disease.

REFERENCES:
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patent: 2005/0075327 (2005-04-01), Flohr et al.
patent: 2007/0004637 (2007-01-01), Kiso
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patent: WO-2004/050609 (2004-06-01), None
patent: WO-2004/076478 (2004-09-01), None
patent: WO-2004/080376 (2004-09-01), None
patent: WO-2005/040126 (2005-05-01), None
patent: WO-2006/036664 (2006-04-01), None
Neurotherapeutics, 5(3), pp. 399-408 (2008).
Sinha, Sukanto et al., “Purification and cloning of amyloid precursor protein β-secretase from human brain”,Nature, Dec. 2, 1999, vol. 402, pp. 537-540.
Ghosh, Arun K. et al., “Design of potent inhibitors for human brain memapsin 2 (β- secretase)”,J. Am. Chem. Soc., 2000, vol. 122, pp. 3522-3523.
Kimura, Tooru et al., “KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine”,Bioorganic&Medicinal Chemistry Letters, 2004, vol. 14, pp. 1527-1531.
Kimura, Tooru et al., “Design and synthesis of highly active Alzheimer's β-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability”,Bioorganic&Medical Chemistry Letters, 2005, vol. 15, pp. 211-215.

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