Eisai R&d Management Co., Ltd.

Setsuo Funasaka

Keiko Takahashi

Tomohiro Matsushima

Hiroshi Obaishi

Shuji Shirotori

Keigo Tanaka

Toshimi Okada

Satoshi Nagao

Isao Ohashi

Yoshinobu Yamane

Yusuke Nakatani

Yuki Karoji

The present invention provides a novel compound having FGFR inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same. Specifically, the present invention provides a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein n represents 0 to 2; A represents an arylene group or a heteroarylene group; G represents a single bond, an oxygen atom or &#x2014;CH&#x2014;; E represents a nitrogen-containing non-aromatic heterocycle; Rrepresents an alkoxy group or the like; Rrepresents a hydrogen atom or the like; and Rrepresents a hydrogen atom, an alkyl group, an alkoxy group or the like, with the proviso that when E represents an azetidine ring and Ror Ris present on a nitrogen atom on the azetidine ring, the Ror Rdoes not represent a hydrogen atom.

Monocyclic pyridine derivative

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)

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.]

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

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Tsukuba, Japan

Setsuo Funasaka