Kyorin Pharmaceutical Co., Ltd.

Kyorin Pahrmaceutical Co., Ltd.

Hiroyuki Miyachi

Masahiro Nomura

Takahiro Tanase

Koji Murakami

Masaki Tsunoda

Mitsuru Segawa

Kei Okazaki

Yukie Takahashi

Kouji Murakami

Hiromi Kiyota

Masahiro Suzuki

Tomohiro Ide

Fumiyoshi Kobayashi

Hideo Okubo

Masato Hoshino

Emiko Tagami

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

Substituted benzylthiazolidine-2, 4-dione derivatives

Substituted phenylpropionic acid derivatives as agonists to human peroxisome proliferator-activated receptor (PPAR) &agr;

The invention relates to the imidazole derivatives as selective antagonistic substances against muscarinic acetylcholine and provides imidazole derivatives represented by a general formula (1) or (2) ##STR1## [wherein R.sub.1 is a phenyl group which may have substituent or thienyl group, R.sub.2 is a cyano group, a carboxyl group, CONR.sub.7 R.sub.8 group (wherein R.sub.7 and R.sub.8 each independently represent hydrogen atom or lower alkyl group, or R.sub.7 and R.sub.8 may form a ring by alkylene chain which may contain hetero atom) or COOR.sub.9 group (wherein R.sub.9 is a lower alkyl group), R.sub.3 is a hydrogen atom or lower alkyl group, R.sub.4, R.sub.5 and R.sub.6 each independently represent hydrogen atom, lower alkyl group which may have substituent or cycloalkyl groups, or may form a condensed ring at the positions of R.sub.5 and R.sub.6 with benzene ring, R.sub.10 is a lower alkyl group or an aralkyl group which may have substituent, m is an integer from 1 to 6, and z is a halogen atom].

Imidazole derivatives and process for preparing the same

N-substituted pyrrolidine derivatives and process for preparing the same

Arylglycinamide derivatives represented by a general formula (1) ##STR1## (wherein Ar denotes a phenyl group which may have 1 to 3 substituents or naphthyl group which may have 1 to 3 substituents, R.sub.1 and R.sub.4 denote identically or differently hydrogen atoms or lower alkyl groups with 1 to 3 carbon atoms, R.sub.2 denotes a lower alkyl group with 1 to 6 carbon atoms, cycloalkyl group with 3 to 6 carbon atoms, lower alkyl group with 1 to 4 carbon atoms which may have a phenyl group which may have 1 to 3 substituents, norbornyl group, adamantyl group or phenyl group which may have 1 to 3 substituents, R.sub.3 denotes a hydrogen atom or lower alkyl group with 1 to 6 carbon atoms or it may form a ring constituting alkylene together with R.sub.2, R.sub.5 denotes a lower alkyl group with 1 to 6 carbon atoms or cycloalkyl group with 5 or 6 carbon atoms, R.sub.6 denotes a hydrogen atom or lower alkyl group with 1 to 6 carbon atoms or it may form a ring constituting alkylene together with R.sub.5, and m denotes 2 or 3), and their salts, which function as effective therapeutic drugs for the dysurias such as urinary incontinence and pollakiuria, and the preparative processes therefor are presented.

Arylglycinamide derivatives and preparative processes therefor

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Kazo, Japan

Hiroyuki Miyachi