Kyowa Hakko Kogyo Co., Ltd.

Kazuhito Akasaka

Yutaka Saitoh

Hirofumi Nakano

Tamio Mizukami

Yutaka Kanda

Shiro Akinaga

Yoshinori Yamashita

Katsushige Gomi

Masami Okabe

Isami Takahashi

Tsutomu Agatsuma

Masami Kaneko

The present invention relates to radicicol derivatives represented by the following formula (I) or pharmacologically acceptable salts thereof: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each represents hydrogen, alkanoyl, alkenoyl or tert-butyldimethylsilyl; (1) when X represents halogen, Y represents an oxygen atom or R.sup.4 --O--N (wherein R.sup.4 represents hydrogen or substituted or unsubstituted lower alkyl); and R.sup.3 represents hydrogen, alkanoyl, alkenoyl or the like; and (2) when X and R.sup.3 are combined with each other to represent a single bond; Y represents R.sup.4B --O--N (wherein R.sup.4B has the same meaning as R.sup.4). The radicicol derivatives of the present invention demonstrate tyrosine kinase inhibition activity and pharmacological activities such as antitumor, antimicrobial or immunosuppression effects.

Radicicol derivatives

The present invention relates to a farnesyltransferase inhibitor and an antitumor agent comprising, as an active ingredient, a piperazinedione derivative represented by formula (I): ##STR1## wherein R.sup.1 and R.sup.2 independently represent lower alkyl, lower alkoxyalkyl, substituted or unsubstituted aryl, or aralkyl; R.sup.3 and R.sup.4 independently represent mercapto, lower alkanoylthio, aroylthio, lower alkoxycarbonylthio, or aryloxycarbonylthio, or alternatively R.sup.3 and R.sup.4 are combined together to form disulfide; and R.sup.5 and R.sup.6 independently represent hydrogen, lower alkyl, lower alkoxyalkyl, hydroxyalkyl, lower alkanoyloxyalkyl, aroyloxyalkyl, aralkyloxyalkyl, or aralkyl.

Farnesyltransferase inhibitor

Epoxycyclohexenedione derivatives

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Shizuoka, Japan

Kazuhito Akasaka