Inhibitors of transthyretin amyloid fibril formation

Details Inhibitors of transthyretin amyloid fibril formation Inhibitors of transthyretin amyloid fibril formation

2007-12-25

2007-12-25

Kumar, Shailendra (Department: 1621)

Organic compounds -- part of the class 532-570 series

Organic compounds

Amino nitrogen containing

C564S265000, C562S433000, C562S439000

Reexamination Certificate

active

11350664

ABSTRACT:
Bisaryloxime ethers and bisarylhydroazones are shown to be effective for inhibiting formation of amyloid fibrils of transthyretin.

REFERENCES:
patent: 4270947 (1981-06-01), Gutman
patent: 2004/058747 (2004-07-01), None
Aroskar et al, Journal of the Chemical Society, Sep. 1964, pp. 2975-2981.
Miroy, et al., “Inhibiting transthyretin amyloid fibril formation via protein stabilization”,Proc. Natl. Acad. Sci. USA 93: 15051-15056 (1996).
Peterson, et al., “Inhibiting transthyretin conformational changes that lead to amyloid fibril formation”,Proc. Natl. Acad. Sci. USA 95: 12956-12960 (1998).
Baures, et al., “Discovering Transthyretin Amyloid Fibril Inhibitors by Limited Screening”,Bioorg. Med. Chem. 6: 1389-1401 (1998).
Oza, et al., “Synthesis and Evaluation of Anthranilic Acid-Based Transthyretin Amyloid Fibril Inhibitors”,Bioorg. Med. Chem. Lett. 9: 1-6 (1999).
Baures, et al., “Synthesis and Evaluation of Inhibitors of Transthyretin Amyloid Formation Based on the Non-steroidal Anti-inflammatory Drug, Flufenamic Acid”,Bioorg. Med. Chem. 7: 1339-1347 (1999).
Petrassi, et al., “Structure-Based Design ofN-Phenyl Phenoxazine Transthyretin Amyloid Fibril Inhibitors”,J. Am. Chem. Soc. 122: 2178-2192 (2000).
Klabunde, et al., “Rational design of potent human transthyretin amyloid disease inhibitors”,Nature Struct. Biol. 7: 312-321 (2000).
Liu, et al., “A glimpse of a possible amyloidogenic intermediate of transthyretin”,Nature Struct. Biol. 7: 754-757 (2000).
Petrassi, et al., “The Copper-Mediated Cross-Coupling of Phenylboronic Acids and N-Hydroxyphthalimide at Room Temperature: Synthesis of Aryloxyamines”,Org. Lett. 3: 139-142 (2001).
Purkey, et al., “Evaluating the binding selektivity of transthyretin amyloid fibril inhibitors in blood plasma”,Proc. Natl. Acad. Sci. USA 98: 5566-5571 (2001).
Hammarström, et al., “Trans-Suppression of Misfolding in an Amyloid Disease”,Science 293: 2459-2462 (2001).
White, et al., “Support for the multigenetic hypothesis of amyloidosis: The binding stoichiometry of retinol-binding protein, vitamin A, and thyroid hormone influences transthyretin amyloidogenicity in vitro”,Proc. Natl. Acad. Sci. USA 98: 13019-13024 (2001).
Oza, et al., “Synthesis, Structure, and Activity of Dielofenac Analogues as Transthyretin Amyloid Fibril Formation Inhibitors”,J. Med. Chem. 45: 321-332 (2002).
Sacchettini, et al., “Therapeutic Strategies For human Amyloid Diseases”,Nat. Rev. Drug Dis. 1: 267-275 (2002).
Hammarström, et al., “Sequence-dependent denaturation energetics: A major determinant in amyloid disease diversity”,Proc. Natl. Acad. Sci. USA 99: 16427-16432 (2002).
Hammarström, et al., “Prevention of Transthyretin Amyloid Disease by Changing Protein Misfolding Energetics”,Science 299: 713-716 (2003).
Razavi, et al., “Benzoxazoles as Transthyretin Amyloid Fibril Inhibitors: Synthesis, Evaluation, and Mechanism of Action”,Angew. Chem. Int. Ed. 42: 2758-2761 (2003).
Green, et al., “Synthesis and Characterization of Potent Bivalent Amyloidosis Inhibitors That Bind Prior to Transthyretin Tetramerization”,J. Am. Chem. Soc. 125: 13404-13414 (2003).
Cohen, et al., “Therapeutic approaches to protein-misfolding diseases”,Nature 426: 905-909 (2003).
Adamski-Werner, et al., “Diflunisal Analogues Stabilize the Native State of transthyretin. Potent Inhibition of Amyloidogenesis”,J. Med. Chem. 47: 355-374 (2004).
Miller, et al., “Native state stabilization by NSAIDs inhibits transthyretin amyloidogenesis from the most common familial disease variants”,Lab. Inv. 84: 545-552 (2004).
Purkey, et al., “Hydroxylated Polychlorinated Biphenyls Selectively Bind Transthyretin in Blood and Inhibit Amyloidogenesis: Rationalizing Rodent PCB Toxicity”,Chemistry&Biology 11: 1719-1728 (2004).
Petrassi, et al., “Potent and Selective Structure-Bases Dibenzofuran Inhibitors of Transthyretin Amyloidogenesis: Kinetic Stabilization of the Native State”,J. Am. Chem. Soc. 127: 6662-6671 (2005).

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