Kyowa Hakko Kogyo Co., Ltd.

Junji Kanazawa

Yutaka Kanda

Masaji Kasai

Hiromitsu Saito

Tadashi Ashizawa

Katsushige Gomi

Masami Okabe

Mitsunobu Hara

Shun-ichi Ikeda

Soichiro Sato

Takayuki Nakashima

Uichiro Kimura

Kimihito Sasaki

Yuko Uosaki

Etsuko Nukui

Yoko Takata

Masami Hamano

Shun-Ichi Ikeda

Agents for inducing apoptosis comprising a tetrocarcin derivative represented by the following formula (I) or a salt thereof as an active ingredient ( represents a single bond or a double bond; j and k represent 0 or 1; R to R , R to R and R represent a hydrogen atom, a lower alkyl group and the like; R , R , R , R and R to R represent a hydrogen atom, a hydroxyl group, a lower alkyl group and the like; R and R represents a hydrogen atom, a hydroxyl group, a lower alkyl group, a group represented by the following formula (B) (R represents a formyl group and the like, R to R represent a hydrogen atom, a hydroxyl group, a lower alkyl group and the like); R represents a hydroxyl group, a lower alkoxyl group, a lower alkanoyloxy group and the like). The agents are useful as medicaments for preventive and/or therapeutic treatment of diseases resulting from increased expression of Bcl-2 family proteins, for example, cancers, AIDS and the like.

Agent for inducing apoptosis

The present invention relates to propenone derivatives represented by the following formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, or YR.sup.5 (wherein Y represents S or O; and R.sup.5 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or a substituted or unsubstituted cyclic ether residue); R.sup.2 and R.sup.3 independently represent hydrogen, lower alkyl, or substituted or unsubstituted aralkyl, or alternatively R.sup.2 and R.sup.3 are combined to form substituted or unsubstituted methylene or ethylene; R.sup.4 represents hydrogen, hydroxy, lower alkyl, substituted or unsubstituted aralkyl, lower alkoxy, substituted or unsubstituted aralkyloxy, or halogen; and X represents substituted or unsubstituted indolyl; or pharmaceutically acceptable salts thereof.

Propenone derivatives

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Sizuoka, Japan

Junji Kanazawa