Kissei Pharmaceutical Co., Ltd.

Takehiro Ishikawa

Tetsuro Tamai

Satoshi Akahane

Junichi Kobayashi

Nobuyuki Tanaka

Hiromu Harada

Harunobu Mukaiyama

Hideyuki Muranaka

Tetsuya Nakamura

Masako Yoshida

Ritsu Suzuki

Yasunori Ueno

Yuichiro Kai

Tatsuhiro Kondo

Hitoshi Inoue

Tomonaga Ozawa

Satoko Kobayashi

Hideki Takeuchi

Kiyoshi Kasai

Hiroaki Shiohara

Atsushi Kondo

Tetsuji Ozawa

Koji Kamata

Akihiro Moriyama

Isao Wanajo

Naohide Morita

The present invention aims to provide a novel compound which has CGRP receptor antagonist activity and which is useful for the treatment of various diseases mediated by CGRP receptors. That is, the present invention relates to the pyrrolidine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof. In the formulae, W is ring, X is a carbon atom or the like, Yto Yare carbon atoms or the like, and Rto Ris alkyl or the like. The compounds of the present invention or a pharmaceutically acceptable salt thereof have an excellent CGRP receptor antagonist activity, and thus are useful as agents for the treatment of various diseases mediated by CGRP receptors. 

Pyrrolidine derivative

The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein Rand Rare each hydrogen, lower acyl, lower alkoxycarbonyl or the like; Ris lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or the like; Ris cyano, lower alkoxycarbonyl, carboxy or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

Catechol derivative, pharmaceutical composition containing the same, use of the catechol derivative, and use of the pharmaceutical composition

The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein Rand Rare each hydrogen, lower acyl, lower alkoxycarbonyl or the like; Ris halo-lower alkyl, lower acyl, halo-lower alkylcarbonyl, cycloalkylcarbonyl, optionally substituted arylcarbonyl, lower alkoxycarbonyl or the like; Ris lower alkyl, halo-lower alkyl, cycloalkyl, lower alkoxy-lower alkyl or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

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

Crystals of a salt of 4'-{2-[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethylamino]ethoxy}-3-isopropyl-3&#x2032;,5&#x2032;-dimethylbiphenyl-4-carboxylic acid. The &#x3b1; type, &#x3b2; type and &#x3b3; type crystals produced by treating hydrochloride of 4&#x2032;-{2-[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethylamino]ethoxy}-3-isopropyl-3&#x2032;,5&#x2032;-dimethylbiphenyl-4-carboxylic acid with specified solvents, which can be discriminated by the characteristic diffraction peaks of powder X-ray diffractometry and the like.

Polymorphic crystal of 4'-{2-[ (1S, 2R)&#x2014;2-  hydroxy-2- (4-hydroxyphenyl)-1-methylethylamino]ethoxy} - 3 - isopropyl-3&#x2032;, 5&#x2032; -dimethylbiphenyl- 4 - carboxylic acid hydrochloride

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. 

Growing community of inventors

Toyoshina-machi, Japan

Takehiro Ishikawa