Takeda Pharmaceutical Company Limited

Fujisawa Pharmaceutical Company, Ltd.

Dot Therapeutics-1, Inc.

Day One Biopharmaceuticals, Inc.

Masato Kitayama

Yoshiyuki Takeda

Masatoshi Yamada

Sayuri Hirano

Jun-ichi Kawakami

Motoki Ikeuchi

Koji Nakamoto

Mitsuo Yamamoto

Hiroki Ono

Yasuhiro Sawai

Kentaro Iwata

Jun-Ichi Kawakami

Miyuki Hohokabe

Koya Kimoto

Kazuo Ohkawa

Masaru Hayashi

Masaru Ohnishi

The aim of the present invention is to provide a method capable of producing an optically active pyrimidinamide derivative on an industrial scale. Compound (I) or a salt thereof is subjected to an asymmetric reduction reaction, the obtained compound (II) or a salt thereof is subjected to a deprotection reaction, and the obtained compound (III) or a salt thereof is reacted with compound (VI) or a salt thereof to obtain compound (V) or a salt thereof.

Method for producing optically active compound

The aim of the present invention is to provide a method capable of producing an optically active pyrimidinamide derivative on an industrial scale. Compound (I) or a salt thereof is subjected to an asymmetric reduction reaction, the obtained compound (II) or a salt thereof is subjected to a deprotection reaction, and the obtained compound (III) or a salt thereof is reacted with compound (VI) or a salt thereof to obtain compound (V) or a salt thereof. wherein each symbol is as defined in the specification.

The present invention provides a cocrystal of (S)-3-(1-((1-acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-1H-1,2,4-triazol-5(4H)-one and an organic acid capable of forming a cocrystal with the compound.

Cocrystal, production method thereof, and medicament containing cocrystal

Provision of crystal of 1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]-1H-benzimidazole-2-carboxamide hydrochloride which has a superior rennin inhibitory activity and is useful as a prophylactic or therapeutic agent for hypertension and various organ disorders caused by hypertension, and the like. Crystal of 1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]-1H-benzimidazole-2-carboxamide hydrochloride having an X-ray powder diffraction pattern showing characteristic peaks at interplanar spacings (d) of around 26.43&#xb1;0.2, 7.62&#xb1;0.2 and 4.32&#xb1;0.2 angstroms.

Crystal of amide compound

This invention provides a novel industrial process for preparation of an anhydride of 2-(2-aminothiazole-4-yl)-2-hydroxy compound.

Process for producing anhydride of aminothiazole derivative

Growing community of inventors

Osaka, Japan

Masato Kitayama