Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-09-03
1998-04-21
Dentz, Bernard
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514411, 514529, 514574, 548429, 549239, 549268, 549299, 549354, 560106, 560127, 562509, 564153, 568326, 568633, A61K 3134, C07D30793
Patent
active
057418144
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP95/00128 filed Feb. 1, 1995.
1. Technical Field
The present invention relates to a novel cyclooctadiene derivative, and to an agrohorticultural (agricultural and horticultural) fungicide, an antimold and an antithrombocytic agent each containing the derivative as the active ingredient.
2. Background Art
Some cyclooctadiene derivatives have been reported in Journal of Polymer Science: Polymer Chemistry Edition, Vol. 13, p. 171 (1975), and Journal of Organic Chemistry, Vol. 42, p. 2601 (1977). However, these are used in the field of electronic materials and as organic synthetic compounds. Nothing is referred to therein about their physiological activities such as fungicidal activity, antimold activity and antithrombocytic activity.
Various antimolds and fungicides have heretofore been developed but are problematic in that their effects are unsatisfactory and that some fungi which are resistant to them have appeared. Therefore, novel antimolds and fungicides are desired.
In addition, since many of the fungicides that have heretofore been developed are artificially-synthesized compounds, their use has become considered problematic in these days in that they have been found to have some negative influences on the environment. For these reasons, an increasing interest is being taken in compounds to be derived from natural substances, which will have few influences on the environment, and the development of fungicides comprising such compounds is therefore desired.
On the other hand, the development of novel antithrombotic agents is also desired for the reasons mentioned below.
It has been clarified that thrombocytoagglutination is one important factor in thrombogenesis in relation to its pathomorphism. Thrombogenesis is known to cause various thrombotic disorders, of which some typical ones include, for example, cerebral thrombosis, pulmonary thrombosis, myocardial infarction, stenocardia and peripheroarterial obstruction. It is desired to develop medicines efficacious against such disorders. As medicines for preventing and curing such thrombotic disorders, antithrombotic agents having an anti-thrombocytoagglutinative activity are specifically noted. The effect of aspirin has heretofore been widely studied, and recently, ticlopidine and cilostazol have been put into clinical demonstrations. At present, however, it is still desired to obtain more efficacious medicines.
Apart from the above-mentioned thrombotic disorders, some other disorders are said to have relation to thrombocytes. Such disorders include, for example, nephritis and metastasis of cancer cells. Recently, a wide variety of studies are being made on the effects of various antithrombotic agents having the ability to retard the functions of thrombocytes, essentially for preventing and curing these disorders (see Journal of Royal College of Physicians, Vol. 7, No. 1, pp. 5-18, 1972; Nippon Rinsyo, Vol. 4, No. 6, pp. 130-136, 1988; Anticancer Research, Vol. 6, pp. 543-548, 1986).
DISCLOSURE OF THE INVENTION
Given the situation, the present inventors have variously studied in order to develop excellent compounds and, as a result, have found that cyclooctadiene derivatives to be obtained through various chemical modifications of Compound A that is produced by microorganisms belonging to the genus Zopfiella and also their analogs as obtained through chemical synthesis have excellent fungicidal activity and antimold activity. On the basis of these findings, the inventors have completed the present invention.
The present inventors also have found that the compounds of the present invention additionally have antithrombocytic activity.
Specifically, the present invention relates to a cyclooctadiene derivative of the following formula (1) and also to an agrohorticultural fungicide, an antimold and an antithrombocytic agent each comprising the derivative as the active ingredient. ##STR3## wherein A.sup.1, A.sup.2, A.sup.3 and A.sup.4 each independently represent COOR.sup.5 (where R.sup.s represents a hydrogen atom, a C.sub.
REFERENCES:
patent: 5346919 (1994-09-01), Watanabe et al.
patent: 5460814 (1995-10-01), Watanabe et al.
Adachi Michiaki
Furusato Takashi
Futagawa Mitsugu
Nakajima Yasuyuki
Nishioka Masanori
Dentz Bernard
Nissan Chemical Industries Ltd.
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