Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Patent
1997-03-04
1998-03-31
Owens, Amelia Averill
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
549 12, C07D31314
Patent
active
057340676
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP95/01975 filed Sep. 28, 1995.
TECHNICAL FIELD OF THE INVENTION
The present invention relates to a novel tricyclic, condensed heterocyclic compound. The novel tricyclic, condensed heterocyclic compound in accordance with the present invention is a useful substance with an anti-oxidant action.
BACKGROUND ART
The relation between phenomena such as cancer, arteriosclerosis and aging and biological oxidative reaction has been remarked in recent years, and therefore, attention has been drawn increasingly toward anti-oxidative agents as substances capable of controlling the biological oxidizing mechanism.
The present inventors have extracted dibenzoxepin derivatives from bakery's yeast and have then found that the derivatives belong to a group of substances with an anti-oxidant action. The applicant has already filed the application thereof (Japanese Unexamined Patent Publication No. Hei 5-153990 (1993)). The application describes clearly that the dibenzoxepin derivatives represented by the following formula (1): ##STR2## (wherein R.sub.1 represents hydrogen atom or an acyl group; and R.sub.2 represents an alkyl group) has an anti-oxidant action.
DISCLOSURE OF THE INVENTION
Focusing attention to the finding that the dibenzoxepin derivatives described in the Unexamined Patent Publication No. Hei 5-153990 have an anti-oxidant action, the present inventors have synthesized the intermediates and derivatives thereof by organic synthesis, to investigate the properties of the resulting compounds. Then, the inventors have found the following new anti-oxidative compounds.
The present invention is to provide a novel anti-oxidative, tricyclic, condensed heterocyclic compound represented by the following formula (2): ##STR3## (wherein X--Y represents CH.sub.2 --C.dbd.O(provided that X is CH.sub.2 and Y is C.dbd.O), CH.sub.2 --CH.sub.2 or CH.dbd.CH; Z represents O, S, or S.dbd.O; R.sub.1 to R.sub.8 represent independently those selected from the group consisting of hydrogen atom, a hydroxyl group, a halogen group, a lower alkyl group, a lower alkoxyl group, a lower alkyl ketone group and CF.sub.3 ; and at least two of R.sub.1 to R.sub.4 are hydroxyl groups) and the salts thereof.
In accordance with the present invention, the term "lower alkyl group" means a linear or branched group with one up to 8 carbon atoms. In accordance with the present invention, the term "lower alkoxyl group" means --O-- lower alkyl. In accordance with the present invention, the term "lower alkyl ketone group" means --(C.dbd.O)-- lower alkyl. The salts of the inventive compound mean the pharmaceutically acceptable salts thereof, including for example the sodium salt, potassium salt, calcium salt, ammonium salt and aluminium salt thereof.
The novel tricyclic, condensed heterocyclic compound represented by the formula (2) in accordance with the present invention is a novel compound produced by chemical synthesis, having an anti-oxidizing activity and useful as a chemical substance for use in pharmaceutical agents, cosmetics, chemical products and the like.
It has been confirmed that the novel tricyclic, condensed heterocyclic compound of the present invention has an outstanding action of inhibiting lipid peroxides with low toxicity. Thus, the novel tricyclic, condensed heterocyclic compound of the present invention is useful as a therapeutic agent for a variety of diseases for which it is believed that lipid peroxides in organisms may be responsible, for example, cancer, arteriosclerotic disorders and liver disorders. For this purpose, the compound of the present invention may be formulated into a variety of formulations produced by the conventional pharmaceutical techniques, such as oral agents including powders, granules, tablets, sugar-coated agents, ampoules, and capsules; subcutaneous agents; intramuscular agents; intravenous agents; or suppositories. For such formulations, routine additives such as fillers, binders, disintegrators, pH adjusting agents and dissolving agents may be used.
The dose of the no
Jinno Shuji
Kogure Yasuyo
Okita Taka-aki
Onuki Hiroyuki
Nippon Suisan Kaisha Ltd.
Owens Amelia Averill
LandOfFree
Anti-oxidative tricyclic, condensed heterocyclic compound does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Anti-oxidative tricyclic, condensed heterocyclic compound, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Anti-oxidative tricyclic, condensed heterocyclic compound will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-53541