Kyorin Pharmaceutical Co., Ltd.

Shigeki Isogai

Masahiro Nomura

Koji Murakami

Yasuo Takano

Kazuhiro Yumoto

Wataru Hori

Jun Asano

Takehiro Shinozaki

The present invention relates to cyclic amino benzoic acid derivatives which are effective in therapy of lipid metabolism abnormality, diabetes and the like as a human peroxisome proliferators-activated receptor (PPAR) agonist, in particular, as an agonist against human PPAR&#x3b1; isoform, and addition salts thereof, and pharmaceutical compositions containing these compounds. A cyclic amino benzoic acid derivative represented by the general formula (1) [wherein a ring Ar represents an aryl group which may have substituent, or the like; Y represents a C-Calkylene, C-Calkenylene, C-Calkynylene, or the like; Z represents an oxygen atom, sulfur atom or &#x2014;(CH)&#x2014; (n represents 0, 1 or 2); X represents a hydrogen atom, halogen atom, lower alkyl group which may be substituted with a halogen atom, or the like; R represents a hydrogen atom or lower alkyl group, and &#x2014;COOR substitutes for an ortho position or metha position of binding position of ring W] or a pharmaceutically acceptable salt thereof.

Cyclic amino benzoic acid derivative

The invention provides novel (2S)-2-ethylphenylpropanoic acid derivatives that bind to the receptor as ligands of human peroxisome proliferator-activated receptor (PPAR) &#x3b1; to activate and exhibit lipid-lowering effect, inhibitory effect on the arteriosclerosis, antiobesity effect, blood glucose-lowering effect, etc., their addition salts, and their medicinal compositions. (2S)-2-Ethylphenylpropanoic acid derivatives represented by a general formula (1) [wherein R1 denotes a halogen atom or trifluoromethyl group, R2 denotes a hydrogen atom, halogen atom or trifluoromethyl group, and, when R2 denotes a hydrogen atom, R3 denotes a halogen atom or trifluoromethyl group and, when R2 denotes a halogen atom or trifluoromethyl group, R3 denotes a hydrogen atom, halogen atom or trifluoromethyl group], and their addition salts.

(2S)-2-ethylphenylpropionic acid derivative

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Tokyo, Japan

Shigeki Isogai