Astellas Pharma Gmbh

Kotobuki Pharmaceutical Co Ltd

Yamanouchi Pharmaceutical Company Ltd.

Kotobuki Pharmaceuticals Co., Ltd.

Masakazu Imamura

Takeshi Murakami

Ryota Shiraki

Yoshinori Kobayashi

Atsushi Noda

Hiroshi Tomiyama

Kazuhiro Ikegai

Kayoko Kitta

Eiji Kurosaki

Minoru Okada

Takashi Sugane

Isao Kinoyama

Nobuaki Taniguchi

Fumiyoshi Iwasaki

Masahiko Hayakawa

Hiroyuki Kaizawa

Takashi Furutani

Kenichi Kawaguchi

Keita Nakanishi

Takenori Kimura

Masaaki Hirano

Takashi Kamikubo

Hiroyuki Moritomo

Mitsuaki Ohta

Takayuki Suzuki

Kenichi Onda

Eiji Kawaminami

Akira Matsuhisa

Akira Toyoshima

Daisuke Sasuga

Yoji Miyazaki

Makoto Kasai

Kiyohiro Samizu

Eisuke Nozawa

Hiroshi Koutoku

Masamichi Yuda

Atsushi Nakamura

Kousuke Komenoi

Ryota Astellas Pharma Inc Shiraki

The present invention provides a method for producing a C-glycoside derivative, which can produce the C-glycoside derivative at a high yield and at a low cost, which conforms to environmental protection, and which is applicable industrially. The C-glycoside derivative is useful for treating and preventing diabetes such as insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes) and the like and various diabetes-related diseases including insulin-resistant diseases and obesity.

Method for producing C-glycoside derivative and intermediate for synthesis thereof

A cocrystal of (1S)-1,5-anhydro-1-[3-(1-benzothien-2-ylmethyl)-4-fluorophenyl]-D-glucitol and L-proline. It is a cocrystal of known compound A, which has a constant quality, is superior in storage stability, has no moisture absorptivity, and is suitable as a crystal of a drug substance used for preparing pharmaceuticals.

Cocrystal of C-glycoside derivative and L-proline

The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via &#x2014;X&#x2014; and A ring is directly bonded to the glucose residue, and it is usable as a Na-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.

C-glycoside derivatives and salts thereof

The present invention relates to a novel N-phenyl-(2R,5S)dimethylpiperazine derivatives useful as antiandrogenic agent which exhibits a sufficient prostate gland reducing effect as compared with conventional compounds and are excellent in oral activity. The compound of the present application is useful in preventing or treating prostate cancer, benign prostatic hyperplasia, and the like. The present invention also provides a novel intermediate useful in producing the compound of the present invention.

N-phenyl-(2R,5S)dimethylpiperazine derivative

N-phenyl-(2R,5S) dimethylpiperazine derivative

The present invention provides an azulene derivative and a salt thereof, wherein an azulene ring is bonded to a benzene ring directly or via a lower alkylene which may be substituted with a halogen atom and the benzene ring is directly bonded to the glucose residue, and it is usable as a Na-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes-related diseases such as insulin-resistant diseases and obesity.

Azulene derivatives and salts thereof

This application relates to a piperazino-substituted novel cyanophenyl derivative in which a substituted carbamoyl or substituted sulfamoyl group having an aryl, heterocyclic or the like group that may have a substituent group is bonded to one nitrogen atom on the piperazine ring. The compound of this application has an anti-androgen action and is useful in preventing or treating prostatic cancer, benign prostatic hyperplasia and the like diseases.

Cyanophenyl derivative

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Tokyo, Japan

Masakazu Imamura