Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Reexamination Certificate
2007-12-25
2007-12-25
Gupta, Anish (Department: 1654)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
C424S185100, C424S193100, C530S300000
Reexamination Certificate
active
10546914
ABSTRACT:
Provided are excellent β-secretase inhibitors, that is, compounds represented by the general formula (1) or prodrugs thereof:wherein A is amino or protected amino; B1and B2are each a single bond, alkylene of 1 to 3 carbon atoms, or the like; D is a single bond, —NHCO, or the like; E is —COOH, tetrazole ring, or the like; n is an integer of 1 to 3; m is an integer of 1 to 3; G is hydroxyl, a group represented by the general formula (2), or the like:in which Z is —NH, -Asp-Ala-NH—, -Asp-Ala-, -Asp-NH—, or the like; L is a 5-to 10-membered ring optionally containing a heteroatom and/or unsaturated bond; X is —COOH, tetrazole ring, or the like; Y is hydrogen, —COOH, or the like; and k is an integer of 1 to 4; and R1, R2, and R3are each alkyl of 1 to 6 carbon atoms, or the like.
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J. Marcinkeviciene et al., “Mechanism of Inhibition of β-Site Amiloid Precursor Protein-Cleaving Enzyme (BACE), by a Statine-Based Peptide”, J. Biol. Chem., vol. 276, No. 26, pp. 23790-23794, 2001.
Y. Hayashi et al., “An Approach for Peptidic Aspartic Protease Inhibitors using Ala-containing Oligopeptides Independent of the Substrate Sequence”, Peptide Science, No. 39, pp. 295-296, Mar. 2003.
D. Shuto et al., “KMI-008, A Novel β-Secretase Inhibitor Containing a Hydroxymethyl Carbonyl Isostere as a Transition-State Mimic: Design and Synthesis of Substrate-Based Octapeptides”, Bioorganic & Medical Chemistry Letters, vol. 13, pp. 4273-4276, 2003.
J. Marcinkeviciene et al., “Mechanism of Inhibition of β-Site Amiloid Precursor Protein-Cleaving Enzyme (BACE), by a Statine-Based Peptide”, J. Biol. Chem., vol. 276, No. 26, pp. 23790-23794, 2001.
Y. Hayashi et al., “An Approach for Peptidic Aspartic Protease Inhibitors using Ala-containing Oligopeptides Independent of the Substrate Sequence”, Peptide Science, No. 39, pp. 295-296, Mar. 2003.
D. Shuto et al., “KMI-008, A Novel β-Secretase Inhibitor Containing a Hydroxymethyl Carbonyl Isostere as a Transition-State Mimic: Design and Synthesis of Substrate-Based Octapeptides”, Bioorganic & Medical Chemistry Letters, pp. 4273-4276, Dec. 13, 2003.
Gupta Anish
Ha Julie
Wenderoth , Lind & Ponack, L.L.P.
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