Chugai Seiyaku Kabushiki Kaisha

The University of Tokyo

Kenji Morikami

Nobuya Ishii

Nobuhiro Oikawa

Nobuo Shimma

Hiroshi Sakamoto

Takashi Emura

Yoshiyuki Ono

Hidenori Takahashi

Hatsuo Kawada

Eisaku Mizuguchi

Toshiyuki Tsukaguchi

Sawako Ozawa

Toshiya Ito

Noriyuki Furuichi

Hirosato Ebiike

Kazutomo Kinoshita

Yasuharu Kato

MinJeong Park

WooSang Hong

Kohsuke Asoh

Jun Ohwada

Fumio Watanabe

Yoshito Nakanishi

Mitsuaki Nakamura

Masami Hasegawa

Miyuki Yoshida

Kohei Koyama

Nukinori Akiyama

Shun Yamamoto

Yasuhiro Tamaki

The present inventors successfully identified novel gatekeeper mutations for FGFR. Further, they discovered that mutant FGFR having the mutations demonstrate resistance to known FGFR inhibitors such as AZD4547, and at the same time demonstrate sensitivity to specific compounds. Mutant polypeptides having the mutations may be used as biomarkers in cancer treatment by FGFR inhibitors to prevent the development of side effects in therapy by conventional FGFR inhibitors, and to control the therapeutic mode for receiving the best therapeutic effect, thus making individualized treatment possible.

FGFR gatekeeper mutant gene and drug targeting same

A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: 

Tetracyclic compound

The present invention provides a compound represented by the formula (1):  

Heteroarylphenylurea derivative

It is intended to provide a compound represented by the formula (1): [wherein Ar is an arylene group to be attached selected from the following formula (2): (wherein * represents a binding site to a nitrogen atom and ** represents a binding site to T); T represents &#x2014;(O)&#x2014;R; R represents a C-Calkyl group or the like; n represents 0 or 1; X represents O or the like; R, Rand Rare independently selected from a hydrogen atom or C-Calkyl; or Rand Rmay join together with an urea structure containing the nitrogen atoms to which they bind to form a 5- or 6-membered heterocycle; Y represents CH or N], or a pharmaceutically acceptable salt thereof or a prodrug thereof and a pharmaceutical composition containing the same.

Pyrazolopyridine and pyrrolopyridine multikinase inhibitors

A drug is provided that is useful as a preventive or therapeutic for cancer as a result of having superior PI3K inhibitory effects as well as superior stability in the body and water-solubility. A compound, or pharmaceutically acceptable salt thereof, represented by formula (I): [wherein, X represents a single bond, etc.; Y represents a single bond, etc. (provided that X and Y are not simultaneously single bonds); Z represents a hydrogen atom, etc.; m represents an integer of 1 or 2; and Rrepresents a cyclic substituent].

Pyrimidine derivatives as PI3K inhibitor and use thereof

Growing community of inventors

Kamakura, Japan

Kenji Morikami