Ono Pharmaceutical Co., Ltd.

Ono Pharmaceuticals Co., Ltd.

Ono Pharmaceuticalco.,ltd.

Atsushi Naganawa

Kensuke Kusumi

Hiroshi Yamamoto

Tetsuya Sekiguchi

Kazuhiro Otsuki

Koji Shinozaki

Kaoru Kobayashi

Akito Kakuuchi

Shigeyuki Nonaka

Takayuki Maruyama

Tetsuji Saito

Shinsuke Hashimoto

Toshihiko Nagase

Yoshihiko Nakai

Fumio Nambu

Maki Iwahashi

Koji Yano

Seiji Ogawa

Atsushi Shimabukuro

Atsushi Kinoshita

Yutaka Okada

Yoko Kishida

Shouji Kawauchi

Kohki Tsukamoto

Yoko Matsunaga

Masaki Asada

Joseph Raker

Mark Allan Wolf

Haruto Kurata

Satonori Higuchi

Yasuko Yamamoto

Yasuhiro Takeda

Yuichi Inagaki

Keisuke Hanada

Yasuyo Kodera

Hiroya Takizawa

Tetsuji Saitoh

A compound represented by general formula (I) wherein all the symbols are as defined in the specification has a selective S1P5 receptor agonist activity due to having a linker from a phenyl group to a cyclic substituent in a dihydronaphthalene skeleton; i.e., due to having a short linker of one atom or less as L in general formula (I), and can therefore serve as an agent for treating S1P5-mediated disease, e. g., neurodegenerative disease such as schizophrenia. 

Dihydronaphthalene derivative

An object of the present invention is to provide a DP receptor antagonist. A compound represented by general formula (I): 

DP antagonist

The compound of the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1Pantagonistic activity. The compound may therefore be used as a therapeutic agent for S1P-mediated diseases such as diseases resulting from vascular constriction, fibrosis, and respiratory diseases.

Phenyl derivative

An object of the present invention is to provide a compound having strong human S1Pantagonistic activity in order to develop a useful medicament for therapy of a S1P-mediated disease such as a disease resulting from vascular constriction, fibrosis and respiratory disease. The compound represented by the general formula (I), wherein all the symbols have the same meanings as described in the specification, has a halogen atom or a haloalkyl group and a phenoxy group at certain substitution sites, and thus has strong human S1Pantagonistic activity. Therefore, the compound can be a therapeutic agent for a S1P-mediated disease, such as a disease resulting from vascular constriction, fibrosis and respiratory disease. 

The compound represented by the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1Pantagonistic activity. The compound may therefore be used as a therapeutic agent for S1P-mediated diseases such as diseases resulting from vascular constriction, fibrosis and respiratory diseases.

A compound represented by formula (I), wherein

Phenylacetic acid compound

Carboxylic acid compounds and medicinal compositions containing the same as the active ingredient

An N-phenylarylsulfonylamide compound of formula (I) (Ris COOH etc.; Ris hydrogen, methyl, etc.; Rand Rare a combination of methyl and methyl, etc.; Ris isopropyl etc.; Ar is thiazolyl, pyridyl, 5-methyl-2-furyl each optionally substituted with methyl; n is zero or 1), a synthetic intermediate for the compound and a process for its preparation. The compound of formula (I) binds to a prostaglandin Ereceptor, especially an EPsubtype receptor, and antagonizes it. It is less affected by protein binding, so it has a satisfactory in vivo activity. Therefore, it is considered to be useful as an analgesic, an antipyretic agent, an agent for the treatment of pollakiuria (frequent urination) and/or lower urinary tract disease syndrome or an antineoplastic agent.

N-phenylarylsulfonamide compound, pharmaceutical composition comprising the compound as active ingredient, synthetic intermediate for the compound and process for its preparation

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Osaka, Japan

Atsushi Naganawa