Kyorin Pharmaceutical Co., Ltd.

Kyorin Pahrmaceutical Co., Ltd.

Kouji Murakami

Hiroyuki Miyachi

Masahiro Suzuki

Masahiro Nomura

Takahiro Tanase

Yukie Takahashi

Novel substituted carboxylic acid derivatives which bind as ligands to human peroxisome proliferator activated receptor (PPAR) to activate the receptor and thereby exhibit potent effects of decreasing neutral fat, cholesterol, and blood sugar; and a processes for preparing the derivatives. Specifically, substituted carboxylic acid derivatives represented by general formula (1), and pharmaceutically acceptable salts and hydrates of the derivatives, and a processes for preparing the derivatives, the salts, or the hydrates 

Substituted carboxylic acid derivatives

The invention provides novel substituted phenylpropionic acid derivatives that bind to the receptor as ligands of human peroxisome proliferator-activated receptor &#x3b1; (PPAR&#x3b1;) to activate and exhibit potent lipid-decreasing action, and processes for preparing them. It relates to substituted phenylpropionic acid derivatives represented by a general formula (1) [wherein Rdenotes a lower alkyl group with carbon atoms of 1 to 4, lower alkoxy group with carbon atoms of 1 to 3, trifluoromethyl group, trifluoromethoxy group, phenyl group which is unsubstituted or may have substituents, phenoxy group which is unsubstituted or may have substituents or benzyloxy group which is unsubstituted or may have substituents, Rdenotes a hydrogen atom, lower alkyl group with carbon atoms of 1 to 4 or lower alkoxy group with carbon atoms of 1 to 3, Rdenotes a lower alkoxy group with carbon atoms of 1 to 3, and the binding mode of A portion denotes &#x2014;CHCONH&#x2014;, &#x2014;NHCOCH&#x2014;, &#x2014;CHCHCO&#x2014;, &#x2014;CHCHCH&#x2014;, &#x2014;CHCHO&#x2014;, &#x2014;CONHCH&#x2014;, &#x2014;CHNHCH&#x2014;, &#x2014;COCHO&#x2014;, &#x2014;OCHCO&#x2014;, &#x2014;COCHNH&#x2014; or &#x2014;CHCHCO&#x2014;], their pharmaceutically acceptable salts and their hydrates, and processes for preparing them.

Substituted phenylpropionic acid derivatives

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Oyama, Japan

Kouji Murakami