Taisho Pharmaceutical Co., Ltd.

Fumiyasu Shiozawa

Tetsuya Yabuuchi

Tetsuo Takayama

Hironori Katakai

Naoya Ono

Masakazu Sato

Takahiro Oi

Kenichi Kawabe

Tomomi Ota

Hiroyuki Kakinuma

Makoto Yagi

Yohei Kobashi

Takeshi Koami

Tomomichi Chonan

Yuki Iwata

Masato Takahashi

Tsuyoshi Shibata

Hajime Asanuma

Yuki Shimizu

Makoto Hamada

Fumihito Ushiyama

Hideaki Amada

Yoshihisa Shirasaki

Daisuke Matsuda

Akira Hiratate

Yuko Matsunaga

Rie Nishikawa

Sota Kato

Chie Koizumi

Hiroki Umemiya

Akiko Ikeda

There are provided compounds having a superior PHD2 inhibitory effect that are represented by general formula (I'): (in the above-mentioned general formula (I&#x2032;),W, Y, R, R, R, and Yare as described hereinabove), or pharmaceutically acceptable salts thereof.

Partially saturated nitrogen-containing heterocyclic compound

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

A compound represented by formula (I) or a pharmaceutically acceptable salt thereof: (wherein Yrepresents a nitrogen atom or a group represented by CR, Yrepresents a nitrogen atom or a group represented by CR, Yrepresents a nitrogen atom or a group represented by CR, R, Rand R, which may be the same or different, each represent a hydrogen atom, etc. (excluding the case where Yis CR, Yis CRand Yis CR), X represents an oxygen atom, etc., Rrepresents a C-Calkyl group, etc., Rrepresents a C-Calkyl group, etc., Rrepresents an optionally substituted phenyl group, etc., Rrepresents a hydrogen atom, etc., and Rrepresents an optionally substituted phenyl group, etc.) has an inhibitory effect on the binding between S1P and its receptor Edg-1(S1P), and is useful as a therapeutic agent for autoimmune diseases, rheumatoid arthritis, asthma, atopic dermatitis, rejection after organ transplantation, cancer, retinopathy, psoriasis, osteoarthritis, or age-related macular degeneration, etc.

[object Object]

An object of the present invention is to provide a compound having an action of inhibiting binding between S1P and its receptor, Edg-1 (S1P), and is useful as a pharmaceutical compound. A compound or a pharmaceutically acceptable salt thereof, which compound is represented by the formula below (where A represents an oxygen atom, a sulfur atom, a group represented by Formula &#x2014;SO&#x2014;, a group represented by Formula &#x2014;SO&#x2014;, or the like, Rrepresents a hydrogen atom, an alkyl group having 1-6 carbon atoms, or the like, Rrepresents a hydrogen atom or the like, Rrepresents an alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-6 carbon atoms, or the like, Rrepresents an aryl group, Rrepresents a hydrogen atom or an alkyl group having 1-6 carbon atoms and optionally substituted with a carboxyl group, and Rrepresents an alkyl group having 1-10 carbon atoms, a cycloalkyl group having 3-8 carbon atoms, an aryl group which is optionally substituted, or the like).

Triazole derivative

A compound represented by the formula (I) below or a pharmaceutically acceptable salt thereof has an effect of inhibiting binding between S1P and its receptor Edg-1(S1P), and is useful as a pharmaceutical product. 

The present invention aims to provide compounds which have an inhibitory effect on the binding between S1P and its receptor Edg-1(S1P) and which are useful for pharmaceutical purposes. A compound represented by formula (I) or a pharmaceutically acceptable salt thereof: [wherein Ar represents a monocyclic heterocyclic ring containing one or two nitrogen atoms, A represents an oxygen atom or the like, Y, Yand Yeach represent a carbon atom or a nitrogen atom, Rrepresents a hydrogen atom, a C-Calkyl group or the like, Rrepresents a C-Calkyl group, a C-Ccycloalkyl group or the like, Rrepresents a C-Calkyl group or the like, Rrepresents a hydrogen atom or a C-Calkyl group, and Rrepresents a C-Calkyl group or the like].

Binding inhibitor of sphingosine-1-phosphate

A thiazolylimidazole derivative represented by the formula or a pharmaceutically acceptable salt thereof, and an ALK5 inhibitor, an therapeutic agent for alopecia or a hair growth agent having the above as an active ingredient,wherein:  The present invention provides an inhibitory substance against ALK5 which is a TGF-&#x3b2; type I receptor and provides a hair growth stimulant or a hair growth agent based on its novel activities.

Thiazole derivative

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Toshima-ku, Japan

Fumiyasu Shiozawa