Chugai Seiyaku Kabushiki Kaisha

Kihito Hada

Takeshi Murata

Satoshi Niizuma

Hatsuo Kawada

Hiroshi Koyano

Hideaki Shimada

Atsushi Suda

Sousuke Hara

Hiroshi Tanaka

Yoshito Nakanishi

Masami Hasegawa

Kousuke Aso

Miyuki Asai

Yasuko Sato

Kenichi Kawasaki

Nobuo Shimma

Susumu Komiyama

Kiyoshi Hasegawa

Takuo Tsukuda

Masahiro Sakaitani

Kazuo Hattori

Yoshiaki Isshiki

Tadakatsu Hayase

Fumio Watanabe

Masami Kohchi

Toshihiro Aoki

Ryoichi Saitoh

Toshikazu Yamazaki

Ikumi Hyodo

Toshiyuki Mio

Ken-Ichi Kawasaki

Naomi Ono

Masaki Tomizawa

The present disclosure provides, for example, a compound represented by the general formula below or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of the compound or salt: wherein X, X, Xand Xare each independently —CR═ or N═, Ris, for example, a halogen atom, Ris, for example, —S(═O)—NH—R, Ris, for example, a Calkyl group, Ris, for example, a hydrogen atom, Ris, for example, a halogen atom, Ris, for example, a hydrogen atom, and Ris, for example, a cyclopropyl group. The compounds, salts or solvates provided by the present disclosure exhibit high RAF/MEK complex-stabilizing activity and can be used for the treatment or prevention of cell proliferative disorders, particularly cancers.

Arylamide derivative having antitumor activity

The present invention relates to quinazolinone and isoquinolinone derivatives represented by formula (I) or pharmaceutically acceptable salts thereof. 

Quinazolinone and isoquinolinone derivative

The present invention relates to benzamide derivatives represented by formula (I) or pharmaceutically acceptable salts thereof. 

Benzamide derivative

The present invention relates to quinazolinedione derivatives represented by formula (I) or pharmaceutically acceptable salts thereof. 

Quinazolinedione derivative

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

Compounds having high angiogenesis inhibiting activity useful as agents for effective treatment and prevention of diseases involving pathologic angiogenesis, e.g. cancer and cancer metastasis, are of formula (II), where Ais C&#x2014;Xor N; Qis -A=A-, or a heteroatom selected from &#x2014;O&#x2014;, &#x2014;S&#x2014;, and &#x2014;N(R)&#x2014;; Qis -A=A-, or a heteroatom selected from &#x2014;O&#x2014;, &#x2014;S&#x2014;, and &#x2014;N(R)&#x2014;; provided that Qand Qare not heteroatoms at the same time; Ais C&#x2014;Xor N, Ais C&#x2014;Xor N, Ais C&#x2014;Xor N, and Ais C&#x2014;Xor N; Y is Calkyl, Ccycloalkyl, Calkenyl, Calkynyl, Calkoxy, Calkenyloxy, Calkynyloxy, or Calkylthio; Z is a hydrogen atom, hydroxy, Calkyl, Ccycloalkyl, or &#x2014;NRR; and L is selected from the formula: 

To provide compounds which have high angiogenesis inhibiting activity, and are useful as agents for effective treatment and prevention of diseases involving pathologic angiogenesis, for example, cancer and cancer metastasis, methods for producing the compounds, intermediate compounds useful for their production, and pharmaceutical compositions containing these compounds. The present invention provides compounds of formula (II), or prodrugs thereof, or pharmaceutically acceptable salts of the compounds or the prodrugs, and pharmaceuticals, and pharmaceutical compositions containing these compounds: where Ais C&#x2014;Xor N; Qis &#x2014;A&#x2550;A&#x2014;, or a heteroatom selected from &#x2014;O&#x2014;, &#x2014;S&#x2014;, and &#x2014;N(R)&#x2014;; Qis &#x2014;A&#x2550;A&#x2014;, or a heteroatom selected from &#x2014;O&#x2014;, &#x2014;S&#x2014;, and &#x2014;N(R)&#x2014;; provided that Qand Qare not heteroatoms at the same time; Ais C&#x2014;Xor N, Ais C&#x2014;Xor N, Ais C&#x2014;Xor N, and Ais C&#x2014;Xor N; Y is Calkyl, Ccycloalkyl, Calkenyl, Calkynyl, Calkoxy, Calkenyloxy, Calkynyloxy, or Calkylthio; Z is a hydrogen atom, hydroxy, Calkyl, Ccycloalkyl, or &#x2014;NRR; and L is selected from the formula: 

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Kanagawa, Japan

Kihito Hada