Chugai Seiyaku Kabushiki Kaisha

Ryoichi Saitoh

Tatsuhiko Kodama

Takao Hamakubo

Masayuki Tsuchiya

Nobuo Shimma

Susumu Komiyama

Toshihiko Ohtomo

Kiyoshi Hasegawa

Takuo Tsukuda

Yoshiki Yamada

Tadakatsu Hayase

Kihito Hada

Masami Kohchi

Iwao Ohizumi

Hiroshi Koyano

Toshikazu Yamazaki

Atsushi Suda

Ken-Ichi Kawasaki

Naomi Ono

The present invention provides a novel class of compounds that have the activity of inhibiting HSP90 enzyme and are useful as anti-cancer agents or such, and compounds that are useful as synthetic intermediates thereof. Specifically, the present invention provides compounds represented by the following formula (1), and pharmaceutically acceptable salts thereof: wherein X, R, R, R, R, R, R, R, L, L, and Lare as defined in the specification.

Macrocyclic compound

The present inventors discovered that the PepT-binding antibodies have the ability to inhibit the transport activity of peptide transporters, as a result of dedicated research. These antibodies may be utilized as cell growth inhibitors, for example, for treating and preventing cancer.

Antibodies that inhibit transport activity of peptide transporters

The present inventors extensively studied and found that an antibody binding to PepT has cytotoxic activity and inhibits cell growth. These results suggest that an antibody binding to PepT, particularly an antibody having a cytotoxic activity, can be used as a cell growth inhibitor, for example, in treating and preventing cancer.

Cell growth inhibitor containing anti-PepT antibody

Methods for measuring transporter activity using budding baculoviruses that do not express endogenous transporters on their envelope have a low background level and can measure the target activity with a high sensitivity. Such methods can be used to measure functional changes due to transporter SNPs over a more extensive range of substrates, and can be applied to tailor-made therapies.

Expressing transporters on viral envelopes

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Shizuoka, Japan

Ryoichi Saitoh