Gamma secretase inhibitors

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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Details

C546S018000, C546S148000, C546S186000, C546S339000, C546S001000, C546S236000, C548S542000, C548S952000, C548S950000, C540S604000, C514S210010, C514S418000, C514S345000, C514S212010

Reexamination Certificate

active

10358898

ABSTRACT:
This invention discloses novel gamma secretase inhibitors of the formula:wherein:R1is a substituted aryl or substituted heteroaryl group;R2is an R1group, alkyl, —X(CO)Y, or alkylene-X(CO)Y wherein X and Y are as defined herein;each R3and each R3Aare independently H, or alkyl;R11is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.

REFERENCES:
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patent: 6166037 (2000-12-01), Budhu et al.
patent: WO 99/45006 (1999-09-01), None
patent: WO 00/58285 (2000-10-01), None
patent: WO 02/02554 (2002-01-01), None
Ohno et al., “2-Ethynylaziridines as Chiral Carbon Nucleophiles . . . ”, Journal of Organic Chemistry (2001), 66(5), 1867-1875.
International Search Report; International Application No. PCT/US 03/03471; filing date Feb. 5, 2003; Priority Date Feb. 6, 2002.
S. Chackalamannil et al., “Total Synthesis of (+)-Himbacine and (+)-Himbeline,”J. Org. Chem.64: 1932-1940 (1999).
Zhang et al., “Biochemical Characterization of the γ-Secretase Activity That Produces β-Amyloid Peptides,”Biochemistry40(16): 5049-5055 (2001).
Zhang et al., “Calpain Ihhibitor I Increases β-Amyloid Peptide Production by Inhibiting the Degradation of the Substrate of γ-Secretase,”J. Biol. Chem.274(13): 8966-8972 (1999).

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