Cyclic depsipeptides and drugs containing the same as the...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

Reexamination Certificate

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C514S009100, C530S317000, C530S323000

Reexamination Certificate

active

06858585

ABSTRACT:
Cyclic depsipeptides represented by the formulawherein:R is a straight or branched alkyl group of 5-20 carbon atoms or a straight or branched alkoxymethyl group of 5-15-carbon atoms; A, B, D, E and F independently each other are alanine, valine, leucine, isoleucine, phenylalanine, etc.; W and Z independently each other are aspartic acid, asparagine, glutamic acid or glutamine; and m and n independently each other is 0 or 1, or pharmacologically acceptable salts thereof. The present compounds are prepared according to a method conventionally used in peptide synthesis. The present compounds are useful as an agent for promoting the production of apolipoprotein E, a therapeutic agent for neurologic damages, a therapeutic agent for dementia, an agent for inhibiting the production of apolipoprotein B, an agent for promoting the production of apolipoprotein A1 or a therapeutic agent for hyperlipemia.

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Fukuyama et al. ‘Age-dependent decline in the apolipoprotein E level in cerebrospinal fluid from control subjects and its increase in cerebrospinal fluid from patients with Alzheimer's disease’ European Neurology, vol. 43, 3, p. 161-169. Apr. 2000.*
File Medline on STN. An No. 97230053. Urabe et al. ‘Effects of Estrogen Replacement Therapy on Hepatic Triglyceride Lipase, Lipoprotein Lipase and Lipids Including Apolipoprotein e In Climacteric and Elderly Women.’ Endocrinology Journal, vol. 43, No. (V con.t)—6, pp. 737-742. Dec. 1996 Abstract Only.*
File Medline on STN. An No. 2002690364 Auld et al. ‘Alzheimer's Disease and the Basal Forebrain Cholinergic System: Relations to Beta-Amyloid Peptides, Cognition, and Treatment Strategies.’ Progress in Neurobiology, vol. 68, No. 3, p. 209-245.*
Jacqueline, A, et al. Halobacillin: A Cytotoxic Cyclic Acylpeptide of the Iturin Class Produced by a Marine Bacillus. Tetrahedron Letters, 1994, vol. 35, No. 31, (pp. 5571-5574).
Harrigan, G.G. et al., Kailuins A-D, New Cyclic Acyldepsipeptides from Cultures of a Marine-Derived Bacterium. Tetrahedron, Feb. 1997, vol. 53, No. 5 (pp. 1577-1582).
Proc. Natl. Acad. Sci. USA, “Expression of apolipoprotein E during nerve degeneration and regeneration”, Michael J. Ignatius, et al. vol. 83, (pp. 1125-1129).

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