Ono Pharmaceutical Co., Ltd.

Takaki Komiya

Kensuke Kusumi

Hiromu Habashita

Shinji Nakade

Haruto Kurata

Hiroshi Hagiya

Toshihide Watanabe

Takeji Ono

Masashi Minami

Hirotaka Mizuno

Kazuhiro Ohtsuki

Hiroshi Saga

Naomi Tsuburaya

Toshimitsu Endo

Satomi Imaide

Shiro Shibayama

Hiroshi Ochiai

Kazuhiko Takeda

Natsuko Tokuda

Noriki Watanabe

A compound represented by the general formula (V) wherein all the symbols are as defined in the specification, has an improved balance of the agonist activity against the S1Preceptor relative to the S1Preceptor, and can thus serve as a therapeutic agent for S1P-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases.

Compounds having S1P5 receptor agonistic activity

A compound having an ability to bind to an SIP receptor and represented by formula (I), a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention and/or treatment of rejection of transplantation, graft-versus-host disease, autoimmune disease, allergic disease and the like: 

Compound capable of binding S1P receptor and pharmaceutical use thereof

A compound having an ability to bind to an S1P receptor (particularly EDG-6, preferably EDG-1 and EDG-6), for example, the compound represented by formula (I) of the present invention, a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention and/or treatment of rejection of transplantation, graft-versus-host disease, autoimmune disease, allergic disease and the like. wherein ring A is a cyclic group; ring B is a cyclic group which may have substituent(s); X is a spacer having 1 to 8 atoms in its main chain, etc.; Y is a spacer having 1 to 10 atoms in its main chain, etc.; n is 0 or 1, wherein when n is 0, m is 1 and Ris a hydrogen atom or a substituent, and wherein when n is 1, m is 0 or an integer of 1 to 7 and Ris a substituent, and wherein m is 2 or more, Rs are the same or different.

The present invention relates to a compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof, and medical use thereof (the symbols in the formula are as described in the specification). The compound represented by formula (I) has chemokine receptor (especially in CCR4 and/or CCR5) antagonistic activity. Therefore it is useful for prevention and/or treatment of a chemokine receptor-mediated disease such as inflammatory and/or allergic diseases [systemic inflammatory response syndrome (SIRS), anaphylaxis, anaphylactoid reaction, allergic angiitis, transplant rejection reaction, hepatitis, nephritis, nephropathy, pancreatitis, rhinitis, arthritis, inflammatory ocular disease, inflammatory bowel disease, disease in cerebro and/or circulatory system, respiratory disease, dermatosis, autoimmune disease, and the like], infection [viral disease (human immunodeficiency virus infection, acquired immunodeficiency syndrome, SARS, etc.), and the like], and the like.

Chemokine receptor antagonist and medical use thereof

Growing community of inventors

Tsukuba, Japan

Takaki Komiya