Eisai R&d Management Co., Ltd.

Eisai Company, Limited

Tomohiro Matsushima

Keiko Takahashi

Yoshio Fukuda

Akihiko Tsuruoka

Naoki Yoneda

Hiroshi Obaishi

Makoto Kotake

Masayuki Matsukura

Kazuki Miyazaki

Junichi Kamata

Shuji Shirotori

Jean-Christophe P Harmange

Mark Spyvee

Kenzo Muramoto

Yasuhiro Funahashi

Satoshi Yamamoto

Yuji Yamamoto

Atsushi Kamada

Atsushi Inoue

Hong Du

Fabian Gusovsky

Yoshiharu Mizui

Isao Tanaka

Masaki Goto

John (Yuan) Wang

Tatsuo Watanabe

Makoto Okita

Shinya Abe

Yasuyuki Suzuki

Seiichi Kobayashi

Yoshiyuki Kawakami

Kenichi Chiba

Hiroshi Shirota

Yoshikazu Kuboi

Yoshihito Eguchi

Takahisa Sakaguchi

Hideki Sakurai

Masanori Fujita

Akifumi Kimura

Takatoshi Kawai

Setsuo Funasaka

Megumi Kawada

Yong-Chun Shen

Kazutoshi Miyake

Hitoshi Oinuma

Hideyuki Adachi

Roch Boivin

Toru Haneda

Junji Matsui

Yimin Jiang

Masanori Mizuno

Mamoru Saito

Toshiyuki Matsuoka

Xiang-Yi Li

Shinji Suda

Jesse Chow

Charles-André Lemelin

Atsumi Yamaguchi

Itaru Arimoto

Takayuki Nakagawa

Masayuki Namiki

Takeshi Sudo

Katsuji Nakamura

Kazunori Wakasugi

Ken-ichi Nomoto

Sachi Suzuki

Fusayo Mimura

Mitsuo Nagai

Kazumasa Nara

Kazuhiro Yoshizawa

Taiju Nakamura

Yusuke Ayata

Masaharu Gotoda

Takako Yoshiba

Ray Wood

Kenji Matsui

Naoko Suzuki

John (yuan) Wang

Ken-Ichi Nomoto

John Wang

An antitumor agent for combined use of a compound or pharmaceutically acceptable salt thereof represented by Formula (I) and a compound or pharmaceutically acceptable salt thereof represented by Formula (II) exhibits an excellent antitumor effect compared to cases where these are individually used, and exhibits antitumor effects against various cancer types: wherein Ris azetidinyl and the like, Rto Ris a hydrogen atom or a halogen atom, Ris Ccycloalkyl and the like, Ris a hydrogen atom and the like, and Ris a halogen atom and the like.

Antitumor agent using compounds having kinase inhibitory effect in combination

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

The invention provides acid addition salts of the compounds represented by formula (1) or (2), or crystals thereof, and processes for preparing the same. The salts or crystals have HGFR inhibitory activity and excellent physical properties (solubility, safety, etc.) and are therefore useful as anti-tumor agents, angiogenesis inhibitors and inhibitors for metastasis for a various types of tumor. 

Phenoxypyridine derivative salts and crystals thereof, and process for preparing the same

The present invention provides methods for the use of compounds having formula (I) in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis, wherein R-R, t, X, Y, Z, and n are as defined herein.

Macrocyclic compounds useful as pharmaceuticals

A compound represented by the following formula, or a salt thereof or a hydrate of the foregoing, has excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity, and cancer metastasis inhibitory activity. Rrepresents a 3- to 10-membered non-aromatic heterocyclic group or the like; Rand Rrepresent hydrogen; R, R, R, and Rmay be the same or different and each represents hydrogen, halogen, Calkyl or the like; Rrepresents hydrogen or the like; Rrepresents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents &#x2014;CH&#x2550;, nitrogen or the like.

Pyridine derivatives and pyrimidine derivatives (3)

The present invention provides compositions comprising compounds having formula (I): 

A compound represented by the following formula, a salt thereof or a hydrate of the foregoing has an excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity and cancer metastasis inhibitory activity. [Rrepresents a 3- to 10-membered non-aromatic heterocyclic group or the like; Rand Rrepresent hydrogen; R, R, R, and Rmay be the same or different and each represents hydrogen, halogen, Calkyl or the like; Rrepresents hydrogen or the like; Rrepresents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents &#x2014;CH&#x2550;, nitrogen or the like.]

The present invention provides compounds having formula (I): 

A process for preparing a compound represented by the formula (I): comprising reacting a compound represented by the formula (II) or salt thereof: with a compound represented by the formula (III): in the presence of a condensation reagent,wherein Rrepresents 1) optionally substituted azetidin-1-yl, 2) optionally substituted pyrrolidin-1-yl, 3) optionally substituted piperidin-1-yl, etc.; R, R, Rand Rmay be the same or different and each represents hydrogen or fluorine; and Rrepresents hydrogen or fluorine.

Process for preparing phenoxypyridine derivatives

A crystal of a 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide hydrochloride, hydrobromide, p-toluenesulfonate, sulfate, methanesulfonate or ethanesulfonate, or a solvate thereof.

Crystalline form of the salt of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide or the solvate of the salt and a process for preparing the same

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

A compound represented by the following formula, a salt thereof or a hydrate of the foregoing has an excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity and cancer metastasis inhibitory activity. [Rrepresents Calkyl or the like; Rand Rrepresent hydrogen; R, R, R, and Rmay be the same or different and each represents hydrogen, halogen, Calkyl or the like; Rrepresents hydrogen or the like; Rrepresents Calkyl or the like; Vrepresents oxygen or the like; Vrepresents oxygen or sulfur; W represents &#x2014;NH&#x2014; or the like; X represents &#x2014;CH&#x2550;, nitrogen or the like; and Y represents oxygen or the like.]

Pyridine derivative and pyrimidine derivative

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.

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Tsukuba, Japan

Tomohiro Matsushima