Kissei Pharmaceutical Co., Ltd.

Satoshi Akahane

Tetsuro Tamai

Takehiro Ishikawa

Junichi Kobayashi

Hiromu Harada

Harunobu Mukaiyama

Nobuyuki Tanaka

Hideyuki Muranaka

Tetsuya Nakamura

Yuichiro Kai

Tatsuhiro Kondo

Ritsu Suzuki

Tomonaga Ozawa

Kenji Yokoyama

Hideki Takeuchi

Kiyoshi Kasai

Hidetoshi Isawa

Yoshihiro Terao

Yukihiko Hotei

Yuji Hoyano

Junichi Sonehara

Takashi Koizumi

Kouichi Kaidoh

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 relates to an agent for the prevention or treatment of a renal disease comprising as an active ingredient a 5-amidino-2- hydroxybenzenesulfonamide derivative represented by the general formula:

Agents for the prevention or treatment of renal diseases

A compound which can be used as an agent for treating interstitial cystitis. An agent for treating interstitial cystitis, which comprises a phenoxyacetic acid derivative represented by a general formula (I) wherein Rrepresents hydroxyl group or a lower alkoxy group, or a pharmacologically acceptable salt thereof. Since the phenoxyacetic acid derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof or a hydrate or solvate thereof has a selective &#x3b2;-adrenoceptor stimulating activity and a remarkable action to inhibit a capsaicin-sensitive sensory nerve, it can be used as a preventive or therapeutic agent for interstitial cystitis and hyperactive bladder which are accompanied by pain, other diseases in which the capsaicin-sensitive sensory nerve is concerned (e.g., acute or chronic and systemic or topical pain and inflammation) and irritable bowel syndrome (IBS) and the like.

Agent for treating interstitial cystitis

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. 

The present invention provides a novel crystalline form of n-butyl[4-[2-[2-hydroxy-5-(N-hydroxycarbamimidoyl) benzenesulfonylamino]ethyl]-2'-methanesulfonyl-3-yloxy] acetate hydrochloride, pharmaceutical compositions containing the same and their uses, which exhibits excellent inhibitory activities against activated blood coagulation factor X, and is useful for the treatment or prevention of a tromboembolic disease.

Crystals of 5-hydroxycarbamimidoyl-2-hydroxybenzenesulfonamide derivative

The present invention provides ethyl (&#x2212;)-2-[4-[2-[[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxy]acetate hydrochloride, crystalline forms thereof and pharmaceutical compositions containing them, which have excellent &#x3b2;-adrenoceptor stimulating effects, therapeutic effects on pollakiuria or urinary incontinence and storage stabilities and are useful as a medicament.

Crystals of hydroxynorephedrine derivative

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Nagano, Japan

Satoshi Akahane