Taisho Pharmaceutical Co., Ltd.

Yohei Kobashi

Hiroyuki Kakinuma

Takahiro Oi

Yuki Iwata

Hitomi Takahashi

Fumiyasu Shiozawa

Tomomichi Chonan

Yuko Hashimoto

Kenichi Kawabe

Yuji Ito

Hiroaki Tanaka

Kazuaki Suzuki

Makoto Hamada

Hideaki Amada

Yohei Matsuda

Norikazu Otake

Madoka Kawamura

Daisuke Matsuda

Hideaki Tabuse

Minoru Moriya

Ayako Bohno

Rie Shimono

Kosuke Funayama

Tomokazu Tamaoki

The present invention provides a compound represented by formula [I] shown below or a pharmaceutically acceptable salt thereof that has an inhibitory effect on 20-HETE producing enzyme. (in formula [I] above, the structure represented by formula [II] below: represents any of the structures represented by formula group [III] below: R, R, R, and Rindependently represent a hydrogen atom, a fluorine atom, methyl, or the like, Rrepresents any of the structures represented by formula group [IV]: 

Pyridine compound substituted with azole

A novel process for producing optically active 2-(2-fluorobiphenyl-4-yl)propanoic acid is disclosed. This production process is characterized in that a compound of formula [1] is reacted with magnesium and so forth to prepare an organometallic reagent, which is reacted with a compound of formula [2] in the presence of a catalytic amount of a nickel compound and a catalytic amount of an optically active compound of formula [3] to obtain a compound represented by formula [4] which is subsequently converted to a compound represented by formula [5] or a pharmaceutically acceptable salt thereof. 

Method for producing optically active 2-(2-fluorobiphenyl-4-yl) propanoic acid

A compound, which inhibits SGLT1 (sodium-dependent glucose transporter 1) activity to suppress absorption of glucose or the like, thereby suppressing abnormal glucose tolerance or postprandial hyperglycemia in diabetes, is provided. Specifically, a 4-isopropyl-6-methoxyphenyl glucitol compound represented by the following formula (I), or a pharmaceutically acceptable salt thereof, is provided: 

4-isopropyl-6-methoxyphenyl glucitol compound

The present invention provides 4-isopropylphenyl glucitol compounds which have no tendency to accumulate in the body and which inhibit SGLT1 activity to suppress postprandial hyperglycemia (or impaired glucose tolerance) through suppression of glucose absorption in the small intestine, whereby the compounds, for example, can suppress the onset of diabetes and metabolic syndrome or can treat these diseases. A 4-isopropylphenyl glucitol compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein Rrepresents a hydrogen atom, etc., Rrepresents a methyl group, etc., Rrepresents a Calkyl group substituted with an amino group(s), etc., and Rrepresents a hydrogen atom, etc.

4-isopropylphenyl glucitol compounds as SGLT1 inhibitors

C-phenyl 1-thioglucitol compounds of the following formula (I) or pharmaceutically acceptable salts thereof or hydrates thereof: [wherein

C-phenyl 1-thioglucitol compound

Provided is a novel C-phenyl glycitol compound that may serve as a prophylactic or therapeutic agent for diabetes by inhibiting both SGLT1 activity and SGLT2 activity, thereby exhibiting a glucose absorption suppression action and a urine glucose excretion action. A C-phenyl glycitol compound represented by Formula (I) below or a pharmaceutically acceptable salt thereof or a hydrate thereof  

C-phenyl glycitol compound

Growing community of inventors

Tokyo, Japan

Yohei Kobashi