Ube Industries, Inc.

Sankyo Company, Limited

Sanwa Kagaku Kenkyusho Co., Ltd.

Santen Pharmaceutical Co., Ltd.

Yasunori Tsuzaki

Masahiko Hagihara

Tomio Kimura

Hiroyuki Koike

Shigeyoshi Nishino

Teruhiko Inoue

Yukinori Wada

Yasuhito Yamamoto

Fumitoshi Asai

Ken-ichi Komori

Atsuhiro Sugidachi

Kazutaka Kido

Hiroshi Nishida

Takeshi Matsugi

Akira Takama

Ryo Iwamura

Hiroyuki Setoguchi

Tomokazu Fujimoto

Hiroto Akaza

Motohisa Shimizu

Hidetoshi Sunamoto

Yasuhiro Aga

Atsushi Shimazaki

Masayoshi Oue

Kaori Taniko

Kimihiko Yoshimura

Naoto Suzuki

Morio Okabe

Toru Izuchi

Satoko Harada

Daisuke Kurumazuka

Toshiyuki Miyazawa

Yuka Kuno

Gen Mizuno

Yuuki Imura

Kenichi Arai

Nobuyoshi Fujii

Masao Maruyama

Tatsuroh Kaneko

Kurumazuka Daisuke

Kaneko Tatsuroh

Miyazawa Toshiyuki

Taniko Kaori

Harada Satoko

Izuchi Toru

Okabe Morio

Ken-Ichi Komori

The present invention provides: a method for producing a mixed sulfonic acid anhydride of the general formula (1) by reacting a sulfonic acid compound of the general formula (2) with a perfluoroalkyl sulfonic acid anhydride or a perfluoroalkyl sulfonic acid halide; and a method for producing a sulfonamide compound of the general formula (4) obtained by reacting an amine compound of the general formula (3) with a mixed sulfonic acid anhydride of the general formula (1).

Method for producing heteroaromatic sulfonamide compound

Disclosed herein are a crystal comprising a compound, which has &#x3bc;-opioid receptor antagonistic action, few side effects, and high safety, and having high purity and excellent physical properties (stability, solubility, etc.), and a method for producing the crystal. The crystal is a crystal of a salt comprising: a compound represented by a formula (I) [wherein Ris a hydrogen atom or a halogen atom, and Ris a group selected from the group consisting of and an acid selected from the group consisting of hydrochloric acid, hydrobromic acid, and oxalic acid, or a hydrate thereof.

Crystal of salt of novel 3-azabicyclo[3.1.0]hexane derivative and pharmaceutical use thereof

The object of the present invention is to provide a compound having an antagonistic action against &#x3bc;-opioid receptors, which causes less side effects and thus is highly safe. A compound represented by the general formula (I), or a pharmacologically acceptable salt thereof:   

3-azabicyclo[3.1.0]hexane derivative and use thereof for medical purpose

A compound represented by formula (1) or salt thereof and a production intermediate thereof are created. The compound exhibited an excellent antioxidation action in a microsome lipid peroxidation measuring system using a rat liver microsome. Therefore, the compound or salt thereof is useful as an antioxidant. The present invention also provides use of a compound represented by the formula (1) or a pharmaceutically acceptable salt thereof for production of an antioxidant. 

Indazole derivative or salt thereof and production intermediate thereof, and antioxidant using same, and use of indazole derivative or salt thereof

The present invention relates to a benzazepinone compound represented by the following formula (I): wherein Rrepresents a C-Calkyl group or halogeno C-Calkyl group, Rrepresents a carboxyl group which may be protected, and Y represents a group represented by the formula (II): wherein Z represents CH or a nitrogen atom,or a pharmaceutically acceptable salt thereof.

Benzazepinone compound

An object of the present invention is to create a novel indazole derivative having a spiro ring structure in a side chain, which is useful as a pharmaceutical, and to find a new pharmacological activity of the derivative. The present invention compound is represented by the general formula [I] and has an excellent Rho kinase inhibitory activity. In the formula, the ring X represents a benzene ring or a pyridine ring; Rand Rrepresent halogen, H, OH, alkoxy, cycloalkyloxy, aryloxy, alkyl, cycloalkyl or the like; Rrepresents halogen, H or the like; Rand Rrepresent halogen, H or the like; Rand Rrepresent H, alkyl or the like; and m, n, p and q represent an integer of 0 to 3. In this connection, each group may have a substituent.

Indazole derivative having spiro ring structure in side chain

Compounds of formula (I): ##STR1## wherein R.sup.1 is hydrogen, alkyl, halogen, haloalkyl, hydroxy, alkoxy, haloalkoxy, alkylthio, haloalkylthio, amino, alkanoyl, haloalkanoyl, carboxy, alkoxycarbonyl, carbamoyl, cyano, nitro, alkanesulfonyl, haloalkanesulfonyl or sulfamoyl; R.sup.2 is 5,6-dihydro-1,4,2-dioxazin-3-yl; R.sup.3 is hydrogen, hydroxy, optionally substituted alkoxy, aralkyloxy, alkanoyloxy, alkenoyloxy, cycloalkylcarbonyloxy, arylcarbonyloxy, alkoxycarbonyloxy, aralkyloxycarbonylxy, phthalidyloxy, (5-methyl-2-oxo-1,3-dioxolen-4-yl)methoxy, (5-phenyl-2-oxo-1,3-dioxolen-4-yl)methoxy, optionally substituted amino or nitro; Y is --NH-- or oxygen or sulfur; n is 1 to 5; and tautomers and salts of said compounds of formula (I), have the ability to inhibit blood platelet aggregation, and can thus be used for treatment and prophylaxis of thrombosis and embolisms.

Tetrahydrothienopyridine derivatives, furo and pyrrolo analogs thereof

Compounds of formula (I): ##STR1## wherein: R.sup.1 is hydrogen, alkyl, halogen, haloalkyl, hydroxy, alkoxy, haloalkoxy, alkylthio, haloalkylthio, amino, alkanoyl, haloalkanoyl, carboxy, alkoxycarbonyl, carbamoyl, cyano, nitro, alkanesulfonyl, haloalkanesulfonyl or sulfamoyl; R.sup.2 is optionally substituted alkanoyl, optionally substituted alkenoyl, optionally substituted cycloalkylcarbonyl, substituted benzoyl, or 5,6-dihydro-1,4,2-dioxazin-3-yl; R.sup.3 is hydrogen, hydroxy, optionally substituted alkoxy, aralkyloxy, alkanoyloxy, alkenoyloxy, cycloalkylcarbonyloxy, arylcarbonyloxy, alkoxycarbonyloxy, aralkyloxycarbonylxy, phthalidyloxy, (5-methyl-2-oxo-1,3-dioxolen-4-yl)methoxy, (5-phenyl-2-oxo-1,3-dioxolen-4-yl)methoxy, optionally substituted amino or nitro; Y is --NH-- or oxygen or sulfur; n is 1 to 5; and tautomers and salts of said compounds of formula (I), have the ability to inhibit blood platelet aggregation, and can thus be used for treatment and prophylaxis of thrombosis and embolisms.

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Ube, Japan

Yasunori Tsuzaki