Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Reexamination Certificate
2001-08-22
2004-08-03
Wilson, James O. (Department: 1623)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
C536S004100, C536S055000, C536S118000, C435S184000
Reexamination Certificate
active
06770629
ABSTRACT:
This application is based upon and claims the benefit of priority from the prior Japanese Patent Application No. 11-051397, filed Feb. 26, 1999, the entire contents of which are incorporated herein by reference.
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to a medicament containing at least one compound selected from the group consisting of sulfopyranosylacylglycerol derivatives and pharmaceutically acceptable salts thereof, as an active ingredient.
2. Description of the Related Art
Sulfur-containing glycolipids contained in natural products derived from, e.g., algae and higher plants are known to have physiological activities.
For example, in a document of Ohta et al. (Chemical & Pharmaceutical Bulletin, 46(4), (1998)), it is described that a specific sulfoquinovosyldiacylglycerol derivative derived from red algae,
Gigartina tenella,
exhibits not only inhibitory activities against DNA polymerases &agr; and &bgr; of higher organisms but also an HIV-derived reverse-transcriptase inhibitory activity. The sulfoquinovosyldiacylglycerol derivative disclosed in the Ohta document is the one whose fatty acid that bonded, through ester-bond, at the C1 carbon atom of the glycerol is an unsaturated fatty acid having carbon atoms with 5 double bonds, and whose another fatty acid that bonded at the C2 carbon atom of the glycerol is a saturated fatty acid having 16 carbon atoms.
Furthermore, in a document of Mizushina et al. (Biochemical Pharmacology 55, 537-541 (1998)), it is described that a mixture of specific sulfoquinovosyldiacylglycerol derivatives derived from a pteridophyte exhibits inhibitory activities against a calf DNA polymerase &agr; and a rat DNA polymerase &bgr;, however, the mixture has no effect upon an HIV-derived reverse-transcriptase activity.
On the other hand, in a document of Sahara et al. (British Journal of Cancer, 75(3), 324-332 (1997)), it is described that a fraction of sulfoquinovosylmonoacylglycerols contained in an acetone extract from a sea urchin intestine exhibits anticancer activities in-vivo and in-vitro. However, the sulfoquinovosylmonoacylglycerol fraction for which Sahara found the anticancer activities principally contains sulfoquinovosylmonoacylglycerol having, bonded thereto through an ester-bond, a saturated fatty acid with 16 carbon atoms. In the sulfoquinovosylmonoacylglycerol fraction, sulfoquinovosylmonoacylglycerols whose acyl moiety is that of an unsaturated fatty acid, are contained only in an extremely small amount. In addition, Sahara et al. have not yet investigated on anticancer activities with respect to individual components contained in the sulfoquinovosylmonoacylglycerol mixture.
Furthermore, National Patent Publication No. 5-501105 describes that a sulfoquinovosyldiacylglycerol derivative has an anti-virus activity. More specifically, it discloses that the derivative has an anti-HIV (human immunodeficiency virus) activity, however it does not disclose that the derivative has DNA polymerase inhibitory activities and anticancer activities.
BRIEF SUMMARY OF THE INVENTION
An object of the present invention is to provide a medicament containing a sulfopyranosylacylglycerol derivative as an active ingredient.
The present inventors found that specific sulfopyranosylacylglycerol derivatives have medicinal activities and achieved the present invention. The present invention provides a medicament containing, as an active ingredient, at least one compound selected from the group consisting of:
compounds represented by the following General Formula (1):
wherein R
101
represents an acyl residue of an unsaturated higher fatty acid, and R
102
represents a hydrogen atom or an acyl residue of an unsaturated higher fatty acid; and
pharmaceutically acceptable salts thereof.
Additional objects and advantages of the invention will be set forth in the description which follows, and in part will be obvious from the description, or may be learned by practice of the invention. The objects and advantages of the invention may be realized and obtained by means of the instrumentalities and combinations particularly pointed out hereinafter.
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Fujita Tatsuya
Masaki Kazuyoshi
Nakayama Kotaro
Ohta Keisuke
Sahara Hiroeki
Crane Lawrence E
Frishauf Holtz Goodman & Chick P.C.
Toyo Suisan Kaisha Ltd.
Wilson James O.
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