Kissei Pharmaceutical Co., Ltd.

Tetsuro Tamai

Nobuyuki Tanaka

Hideyuki Muranaka

Harunobu Mukaiyama

Takehiro Ishikawa

Satoshi Akahane

Junichi Kobayashi

Masuo Akahane

Masaaki Sato

Akihito Hirabayashi

Hiromu Harada

Ken Kikuchi

Makio Kitazawa

Tetsuya Nakamura

Kosuke Okazaki

Hiroaki Kobayashi

Masaru Saito

Yuichiro Kai

Tatsuhiro Kondo

Ritsu Suzuki

Tomonaga Ozawa

Eiji Tsuru

Kiyoshi Kasai

Junichi Sonehara

Michio Toda

The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein Rand Rare each hydrogen or lower alkyl; R, R, Rand Rare each hydrogen, halogen, lower alkyl or lower alkoxy; Rand Rare each hydrogen, halogen, lower alkyl, halo-lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, cyano, a hydroxyl group, lower acyl, carboxy or the like; Ris &#x2014;C(O)&#x2014;R, -A-C(O)&#x2014;R, &#x2014;O-A-C(O)&#x2014;Ror a tetrazol-5-yl group, which exhibit potent and selective &#x3b2;3-adrenoceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

Amino alcohol derivatives, pharmaceutical compositions containing the same, and use thereof

The present invention provides compounds represented by general formula (I): a prodrug thereof, or pharmaceutical acceptable salts thereof, wherein Ris hydrogen or lower alkyl; each of R2 and R3 is independently hydrogen or lower alkyl; each of R, Rand Ris independently hydrogen, halogen, lower alkyl or lower alkoxy; Ris hydrogen or lower alkyl; Ris hydrogen, halogen, lower alkyl, lower alkoxy, etc; Ris &#x2014;COR, -A-COR, &#x2014;O-A-COR, etc; Ar is optionally substituted phenyl or heteroaryl; and A is a bond, &#x2014;OCH&#x2014;, etc, which exhibit potent and selective &#x3b2;3-adrenoceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

Amino alcohol derivatives, medicinal composition containing the same, and use of these

The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has &#x3b2;3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression or biliary calculus. The present invention also provides a process for preparing said intermediates and a method of using said intermediates 

Intermediates in producing phenoxyacetic acid derivatives and method of using the same

Intermediates in producing phenoxyacetic acid preventives and method of using the same

The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has &#x3b2;3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression or biliary calculus. The present invention also provides a process for preparing said intermediates and a method of using said intermediates. 

2-methylpropionic acid derivatives and pharmaceutical compositions comprising the same

2-Methylpropionic acid derivatives and medicinal compositions containing the same

Phenoxyacetic acid derivatives and medicinal compositions containing the same

Aminoethylphenoxyacetic acid derivatives and drugs for pain remission and calculi removal promotion in urinary lithiasis

The present invention relates to a crystalline polymorph of 2-&lsqb;4-&lsqb;2-&lsqb;&lsqb;(1S,2R)-2-hydroxy-2-(4-hydroxy-phenyl)-1-methylethyl&rsqb;amino&rsqb;ethyl&rsqb;phenoxy&rsqb;acetic acid having strong diffraction peaks (diffraction angle: 2&thgr;&plusmn;0.1&deg;) at 10.8, 19.1, 19.3, 19.8, 20.6 and 27.0&deg; in powder X-ray diffraction pattern, which has potent &bgr; - and &bgr; -adrenoceptor stimulating effects and is useful as an agent for relieving pain and promoting the removal of calculi in urolithiasis, and the like. For example, the crystalline polymorph can be prepared by hydrolyzing ethyl 2-&lsqb;4-&lsqb;2-&lsqb;&lsqb;(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl&rsqb;-amino&rsqb;ethyl&rsqb;phenoxy&rsqb;acetate phosphate by sodium hydroxide, adding an aqueous phosphoric acid solution at 40&deg; C. and over, adding a mixed solvent of water and methanol or methanol to the resulting compound, and stirring the suspension at 40&deg; C. to reflux temperature for 30 minutes to several hours.

Crystal polymorphism of aminoethylphenoxyacetic acid derivative

Phenylaminoalkylcarboxylic acid derivatives and pharmaceutical compositions comprising the same

3,4-disubstituted phenylethanolaminotetralincarboxylic acid derivatives

3,4-disubstituted phenylethanolaminotetralincarboxamide derivatives

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Nagano, Japan

Tetsuro Tamai