Kyowa Hakko Kogyo Co., Ltd.

Kyowa Hakko Kirin Co., Limited

Takayuki Nakashima

Yutaka Kanda

Yukimasa Shiotsu

Shinji Nara

Shiro Soga

Jiro Kajita

Hiroshi Nakagawa

Shiro Akinaga

Yushi Kitamura

Jun-ichi Saito

Mitsunobu Hara

Shun-ichi Ikeda

Rieko Nakatsu

Junji Kanazawa

Yuko Uosaki

Shinpei Yamaguchi

Yoko Takata

Masami Hamano

The present invention provides Hsp90 family protein inhibitors comprising, as an active ingredient, a benzoic acid derivative represented by General Formula (I): [wherein n represents an integer of 0 to 10; Rrepresents substituted or unsubstituted lower alkoxycarbonyl, substituted or unsubstituted aroyl, or the like; Rrepresents &#x2014;NRR(wherein Rand Rmay be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl or the like); Rand Rmay be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl or the like; and Rand Rmay be the same or different and each represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl or the like] or a prodrug thereof, or a pharmaceutically acceptable salt of said benzoic acid derivative or said prodrug.

Hsp90 family protein inhibitors

The present invention provides a benzenoid ansamycin derivative represented by Formula (I) (wherein Rand Reach represent a hydrogen atom or are combined together to form a bond,

Benzenoid ansamycin derivative

The present invention provides Hsp90 family protein inhibitors comprising, as an active ingredient, a benzoyl compound represented by general formula (I): (wherein n represents an integer of 0 to 10; Rrepresents substituted or unsubstituted lower alkoxy, substituted or unsubstituted lower alkoxycarbonyl, CONRRor the like; Rrepresents substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic group or the like; Rand R, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl or the like; and Rand R, which may be the same or different, each represent a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl or the like) or a prodrug thereof, or a pharmaceutically acceptable salt of said benzoyl compound or said prodrug.

(wherein n is an integer of 0 to 10; Rrepresents substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, substituted or unsubstituted cycloalkyl, substituted or unsubstituted lower alkoxycarbonyl, substituted or unsubstituted heterocyclic-alkyl, substituted or unsubstituted aryl, &#x2014;CONRR, &#x2014;NRR, etc.; Rrepresents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, etc.; Rand Rmay be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, etc.; Rand Rmay be the same or different, each represent a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, etc.) Provided are an Hsp90 family protein inhibitor comprising, as an active ingredient, a benzene derivative of formula (I) or a prodrug thereof or a pharmaceutically-acceptable salt thereof, etc.

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

Growing community of inventors

Sunto-gun, Japan

Takayuki Nakashima