Taisho Pharmaceutical Co., Ltd.

Other

Toyama Chemical Co., Ltd.

Naoya Ono

Fumie Sato

Tohru Tanami

Kazuya Kameo

Makoto Yagi

Jun Goto

Takehiro Amano

Masaru Mutoh

Hideo Tanaka

Tetsuya Yabuuchi

Tetsuo Takayama

Fumiyasu Shiozawa

Hironori Katakai

Hitomi Hirano

Kenji Yamada

Masakazu Sato

Yoshinori Sekiguchi

Tomomi Ota

Fumihito Ushiyama

Yusuke Oka

Shoichi Kuroda

Shigeru Okuyama

Takeshi Koami

Rie Nishikawa

Toru Yamaguchi

Hajime Asanuma

Takahiro Oi

Tetsuya Tanikawa

Madoka Kawamura

Yasuhiro Tsutsui

Yasunobu Ushiki

Fumito Uneuchi

Daisuke Wakasugi

Yoshihisa Shirasaki

Risa Tsuruta

Noritomo Fujino

Keiko Yamamoto

Ayumu Mori

Provided are novel compounds that bind to FKBP12 or pharmaceutically acceptable salts thereof, as well as new therapeutics useful in the prevention or treatment of alopecia which comprise those compounds or pharmaceutically acceptable salts thereof. Specifically, compounds represented by formula (1) [where Rrepresents either the following formula (2) or (3)] or pharmaceutically acceptable salts thereof are provided.

Azole derivative

An amidine compound represented by formula (I) (wherein Arepresents a nitrogen atom or a group represented by formula CR; Aand Aare the same as or different from each other and independently represent a nitrogen atom or a group represented by formula CH; Rrepresents an aryl group which may be substituted by 1 to 5 substituents independently selected from a substituent group (2) or the like; Rand Rare the same as or different from each other and independently represent a hydrogen atom, a halogen atom, a Calkyl group, a Chaloalkyl group or a Calkoxy group; and Rand Rare the same as or different from each other and independently represent a hydrogen atom, a Chaloalkyl group, a Calkyl group or the like) or a salt thereof. The compound is useful as an anti-fungal agent.

Amidine compound or salt thereof

A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a preventive or a remedy for allergic diseases such as asthma, atopic dermatitis and allergic rhinitis.

Isoquinoline derivative

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 prostaglandin derivative represented by Formula (I): wherein X is a halogen atom in the &#x3b1;- or &#x3b2;-substitution, Y is an ethylene group, a vinylene group or an ethynylene group, Ris a Ccycloalkyl group, a Ccycloalkyl group substituted with a Cstraight or branched chain alkyl group or a Ccycloalkylalkyl group, Ris a hydrogen atom or a CORgroup (Ris a hydrogen atom, a Cstraight or branched chain alkyl group or a Cstraight or branched chain alkenyl group), n is an integer of 1 to 4 and p is 0, 1 or 2,a pharmaceutically acceptable salt thereof or a hydrate thereof.

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Toshima-ku, Japan

Naoya Ono