Eisai Company, Limited

Eisai R&d Management Co., Ltd.

National Cancer Center

Akihiko Tsuruoka

Keiko Takahashi

Yuji Yamamoto

Junichi Kamata

Kazumasa Nara

Yasuhiro Funahashi

Toru Haneda

Yoshimasa Machida

Shigeto Negi

Norihiro Ueda

Motosuke Yamanaka

Isao Sugiyama

Tomohiro Matsushima

Tadashi Okabe

Kanemasa Katsu

Yuuki Komatu

Takashi Owa

Taro Semba

Shinichi Hamaoka

Toshiaki Wakabayashi

Naoko Hata

Atsushi Kamata

Masayuki Matsukura

Kazuki Miyazaki

Yoshio Fukuda

Yoichi Ozawa

Tatsuo Watanabe

Hiroshi Obaishi

Itaru Tsukada

Toshihiko Naito

Katsura Hata

Noako Tsukahara

Yumiko Kaku

Manabu Yanagisawa

Toshio Toyosawa

Junji Matsui

Atsumi Yamaguchi

Katsuji Nakamura

Fusayo Mimura

Sachi Suzuki

Ken-ichi Nomoto

Yasuyuki Suzuki

Takahisa Sakaguchi

Kenichi Nomoto

Naoko Tsukahara

Takayuki Nakagawa

Itaru Arimoto

Saori Miyano

Takako Yoshiba

Tatsuhiro Shibata

Kenji Matsui

Tomio Nakamura

Yasuhito Arai

Masayuki Okada

Ken-Ichi Nomoto

The present invention provides a therapeutic agent for bile duct cancer comprising 5-((2-(4-(1-(2-hydroxyethyl)piperidin-4-yl)benzamide)pyridin-4-yl)oxy)-6-(2-methoxyethoxy)-N-methyl-1H-indole-1-carboxamide or a pharmacologically acceptable salt thereof.

Therapeutic agent for bile duct cancer

The present invention relates to a therapeutic agent represented by the General formula (I), or a pharmacologically acceptable salt thereof, or a solvate of the compound or the salt thereof:  The therapeutic agent comprises a substance having the activity of inhibiting kinase activity of fibroblast growth factor receptor 2 ('FGFR2'). The therapeutic agent can be used for treating undifferentiated gastric cancer, and can also be used to treat organisms comprising a cell overexpressing FGFR2 or a cell expressing mutant FGFR2, or both. The present invention further relates to a pharmaceutical composition comprising an FGFR2 inhibitory and methods of treatment therewith. The present invention also relates to a method for predicting the effect of an FGFR2 inhibitory substance on a patient.

Antitumor agent for undifferentiated gastric cancer

It was discovered that a compound represented by the general formula (I) shows strong c-Kit kinase inhibitory activity, and it inhibits proliferation of c-Kit kinase activated-cancer cells in vitro and in vivo. A novel anticancer agent showing c-Kit kinase inhibitory activity was discovered. The general formula (I): (wherein Rrepresents methyl etc., Rrepresents cyano etc., Rrepresents hydrogen etc., Rrepresents hydrogen etc.).

c-Kit kinase inhibitor

The present invention provides an integrin expression inhibitor, and an agent for treating arterial sclerosis, psoriasis, cancer, retinal angiogenesis, diabetic retinopathy or inflammatory diseases, an anticoagulant, or a cancer metastasis suppressor on the basis of an integrin inhibitory action. Namely, it provides an integrin expression inhibitor comprising, as an active ingredient, a sulfonamide compound represented by the following formula (I), a pharmacologically acceptable salt thereof or a hydrate of them, wherein in the formula, B means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated; K means a single bond, &#x2014;CH&#x2550;CH&#x2014; or &#x2014;(CRR)&#x2014; (wherein Rand Rare the same as or different from each other and each means hydrogen atom or a C1-C4 alkyl group; and mmeans an integer of 1 or 2); Rmeans hydrogen atom or a C1-C6 alkyl group; Z means a single bond or &#x2014;CO&#x2014;NH&#x2014;; and R means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated, respectively.

Integrin expression inhibitor

Compounds represented by the following general formula: [wherein Ais an optionally substituted 5- to 14-membered heterocyclic group, etc.; Xis &#x2014;O&#x2014;, &#x2014;S&#x2014;, etc.; Yis an optionally substituted Caryl group, an optionally substituted 5- to 14-membered heterocyclic group, etc.; and Tis a group represented by the following general formula: (wherein Eis a single bond or &#x2014;N(R)&#x2014;, Rand Reach independently represent a hydrogen atom, an optionally substituted Calkyl group, etc. and Zrepresents a Calkyl group, a Calicyclic hydrocarbon group, a Caryl group, etc.)], salts thereof or hydrates of the foregoing.

Nitrogen-containing aromatic derivatives

An amorphous form of a salt of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide.

Amorphous salt of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide and process for preparing the same

A compound represented by the general formula: wherein Xrepresents a nitrogen atom or a group represented by the formula &#x2014;CR&#x2550;; Xrepresents a nitrogen atom or a group represented by the formula &#x2014;CR&#x2550;; Y represents an oxygen atom or the like; Rrepresents a Calkoxy group, an optionally substituted Caryloxy group, a group represented by the formula &#x2014;NRRor the like; Rrepresents a hydrogen atom, an optionally substituted Calkyl group, or the like; R, R, R, R, R, R, Rand Reach independently represent a hydrogen atom, a halogen atom, an optionally substituted Calkyl group, or the like; Rrepresents a group represented by the formula &#x2014;NRRor the like; and R, R, Rand Reach independently represent a hydrogen atom, an optionally substituted Calkyl group, or the like,a salt thereof, or a hydrate of the foregoing.

Compounds represented by the following general formula: [wherein Ais an optionally substituted 5- to 14-membered heterocyclic group, etc.; Xis &#x2014;O&#x2014;, &#x2014;S&#x2014;, etc.; Yis an optionally substituted Caryl group, an optionally substituted 5- to 14-membered heterocyclic group, etc.; and Tis a group represented by the following general formula: (wherein Eis a single bond or &#x2014;N(R)&#x2014;, Rand Reach independently represent a hydrogen atom, an optionally substituted Calkyl group, etc. and Zrepresents a Calkyl group, a Calicyclic hydrocarbon group, a Caryl group, etc.)],

A compound represented by the general formula: wherein Xrepresents a nitrogen atom or a group represented by the formula &#x2014;CR&#x2550;; Xrepresents a nitrogen atom or a group represented by the formula &#x2014;CR&#x2550;; Y represents an oxygen atom or the like; Rrepresents a Calkoxy group, an optionally substituted Caryloxy group, a group represented by the formula &#x2014;NRRor the like; Rrepresents a hydrogen atom, an optionally substituted Calkyl group, or the like; R, R, R, R, R, R, Rand Reach independently represent a hydrogen atom, a halogen atom, an optionally substituted Calkyl group, or the like; Rrepresents a group represented by the formula &#x2014;NRRor the like; and Rand Reach independently represent a hydrogen atom, an optionally substituted Calkyl group, or the like, a salt thereof, or a hydrate of the foregoing.

Sulfonamide-containing heterocyclic compounds

Sulfonamide-containing indole compounds

A compound represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 denote a halogen atom or hydrogen atom; R.sup.3 means a hydrogen atom or lower alkyl group; l, r and m stand for 0 or 1; A is N or CH; W denotes an aromatic ring or a condensed ring thereof; X means another aromatic ring, an alkanediyl group, an alkenediyl group, or an alkynediyl group; Y stand for --S--, etc.; Z denotes a hydrogen atom, etc., or a salt thereof, and intermediates thereof or a salt thereof as well as processes for the preparation thereof, and pharmaceutical composition suitable for use as an antifungal agent.

Antifungal agents, processes for the preparation thereof, and

A compound represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 denote a halogen atom or hydrogen atom; R.sup.3 means a hydrogen atom or lower alkyl group; l, r and m stand for 0 or 1; A is N or CH; W denotes an aromatic ring or a condensed ring thereof; X means another aromatic ring, an alkanediyl group, an alkenediyl group, or an alkynediyl group; Y stand for --S--, etc.; Z denotes a hydrogen atom, etc., or a salt thereof, and intermediates thereof or a salt thereof as well as processes for the preparation thereof, and pharmacetical composition suitable for use as an antifungal agent.

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Tsukuba, Japan

Akihiko Tsuruoka