Tetraoxaspriro anti-malarials

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

C549S336000, C549S333000

Reexamination Certificate

active

07407984

ABSTRACT:
The present invention is to provide an antimalarial agent having excellent antimalarial activity with little side effects, in particular, having remarkable antimalarial activity against drug-resistant malaria parasites, and being capable of increasing solubility not only to organic solvent including olive oil, but also to water, and therefore, being usable not only as oral drugs but also as injectable solutions. The antimalarial agent of the present invention contains a compound represented by the following general formula (I) [wherein Z represents an unsubstituted or optionally substituted alicyclic hydrocarbon group, R0represents a water-soluble functional group, m represents any one of integers of from 0 to 6, n represents any one of integers of from 0 to 10.].

REFERENCES:
patent: 2000-229965 (2000-08-01), None
patent: WO 93/07119 (1993-04-01), None
Yuji Nonami, Takahiro Tokuyasu, Araki Masuyama, Masatomo Nojima, Kevin J. McCullough, Hye-Sook Kim and Yusuke Wataya “Synthesis, crystal structure and anti-malarial activity of functionalized spiro-1,2,4,5-tetraoxacycloalkanes from unsaturated hydroperoxy peracetals” Tetrahedron Letters 2000, 41, 4681-4684.
Kim et. al. “Synthesis and Antimalarial Activity of Novel Medium-Sized 1,2,4,5-Tetraoxacycloalkanes” Journal of Medicinal Chemistry 2001, 44, 2357-2361.
Yuji Nonami et al., “Synthesis, Crystal Structure and Antimalarial Activity of Functionalized Spiro-1,2,4,5-Tetraoxacycloalkanes From Unsaturated Hydroperoxy Peracetals”, Tetrahedron Letters, (2000), vol. 41, No. 23, pp. 4681-4684.
Translated under the supervision of Hiroshi Nagase, “Saishin Soyaku Kagaku”, last volume, Technomics, Inc., 1993, pp. 368-372.
Kaoru Tsuchiya et al., “Synthesis, Crystal Structure and Anti-Malarial Activity of Novel Spiro-1,2,4,5-Tetraoxacycloalkanes”, Tetrahedron Letters, (1999), vol. 40, No. 21, pp. 4077-4080.
Hye-Sook Kim et al., “Synthesis and Antimalarial Activity of Novel Medium-Sized 1,2,4,5-Tetraoxacycloalkanes”, J. Med. Chem., 2001, vol. 44, No. 14, pp. 2357-2361.
Yuji Nonami et al., “Synthesis of Novel Hydroperoxy-Substituted 1,2,4,5-Tetroxepanes and 1,2,4,5-Tetroxocanes”, 1998, vol. 39, No. 36, pp. 6597-6600.

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