Eisai R&d Management Co., Ltd.

Masaharu Gotoda

Shigeto Negi

Keisuke Matsuyama

Kenji Hayashi

Masanobu Shinoda

Tomohiro Matsushima

Fumiyoshi Matsuura

Atsushi Kamada

Manabu Sasho

Kazuhiro Yoshizawa

Taiju Nakamura

Yusuke Ayata

Takahisa Sakaguchi

Kenshi Yoshida

Kaoru Murata

Mamoru Miyazawa

Susumu Inoue

Naoki Ozeki

Katsutoshi Nishiura

Itaru Arimoto

Teiji Takigawa

Yoshihiko Hisatake

Naoko Suzuki

Nao Shibuguchi

Kazuhiro c/o Eisai Co Ltd Yoshizawa

Itaru c/o Eisai Co Ltd Arimoto

Yusuke c/o Eisai Co Ltd Ayata

The invention provides an amorphous form of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide.

Amorphous form of quinoline derivative, and method for producing same

The present invention relates to calcium bis[(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy) -2-fluoropropoxy]phenyl]-2-isopropoxypropionate] represented by formula (I), a hydrate thereof, a crystal of the compound of formula (I), and a crystal of the hydrate of the compound of formula (I) which are useful as pharmaceuticals, and to processes for producing the same, and intermediates therefore, and processes for production thereof. There is need for (2S)-3-[3-[(2S)-3-(4 -chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, in the form of a drug substance, purified so as to minimize a residual solvent content and having a uniformized specification and a highly favorable workability, and a process for producing the same. Crystalline calcium bis[(2S)-3-[3-[(2S)-3-(4 -chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionate], a calcium salt of (2S) -3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, solves the above problem.

Calcium bis [(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl ]-2-isopropoxypropionate] and intermediate thereof

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

Growing community of inventors

Tsukuba, Japan

Masaharu Gotoda