Kyorin Pharmaceutical Co., Ltd.

Kyorin Pharameuticals Co., Ltd.

Katsuya Awano

Koji Murakami

Hiroya Satoh

Masahiro Nomura

Masaki Tsunoda

Susumu Kinoshita

Eisuke Kojima

Mitsuo Ohashi

Toshio Maeda

Shizuyoshi Fujimori

Toshio Tanaka

Tetsuya Kimura

Yasushi Kohno

Takayoshi Ishizaki

Kuniyoshi Masuzawa

Kyuya Okamura

Koji Saito

Keigo Nishino

Takenobu Ogata

Yasushi Kouno

Taroh Tooru

Shinji Kudoh

Yasuhiko Sakoe

Masakatsu Komuro

Kayoko Matsuzawa

Phenoxyalkylcarboxylic acid derivative represented by the following formula,wherein Rindicates hydrogen atom, methyl group or ethyl group, m is an integer from 2 to 5, and n is an integer from 3 to 8, Xand Xeach independently represent sulfur atom, oxygen atom, sulfinyl group or sulfonyl group, proviso Xand Xare not simultaneously oxygen atom; their alkali salts and hydrates thereof are useful as antiallergic agents.

Phenoxyalkylcarboxylic acid derivatives and process for their preparations

O-anisamide derivatives

Novel pyrazolopyridylpyridazinone derivatives characterized by being represented by general formula (1) and pharnacologically acceptable salts thereof, which exhibit a phosphodiesterase inhibiting activity and have a selective potent bronchodilating effect on the respiratory tract; a process for the preparation of them; and bronchodilators containing the same as the active ingredient; wherein R,is C,-C,lower alkyl or C,-C,cycloalkyl; and R,, R,, R,and R,are each independently hydrogen, C,-C,lower alkyl or phenyl, or alternatively R,and R,may be united to form a double bond.

Pyrazolopyridylpyridazinone derivatives and process for the preparation thereof

The present invention provides novel N-benzyldioxothiazolidylbenzamide derivatives that improve the insulin resistance and have potent hypoglycemic and lipid-lowering effects and processes for preparing the same, and relates to N-benzyldioxothiazolidylbenzamide derivatives characterized by being represented by a general formula (1) ##STR1## [wherein R.sup.1 and R.sup.2 denote identically or differently hydrogen atoms, lower alkyl groups with carbon atoms of 1 to 4, lower alkoxy groups with carbon atoms of 1 to 3, lower haloalkyl groups with carbon atoms of 1 to 3, lower haloalkoxy groups with carbon atoms of 1 to 3, halogen atoms, hydroxyl groups, nitro groups, amino groups which may be substituted with lower alkyl group(s) with carbon atoms of 1 to 3 or hetero rings, or R.sup.1 and R.sup.2 link to form a methylenedioxy group, R.sup.3 denotes a lower alkoxy group with carbon atoms of 1 to 3, hydroxyl group or halogen atom, and dotted line indicates double bond or single bond in combination with solid line], and processes for preparing the same.

N-benzyldioxothiazolidylbenzamide derivatives and process for producing

N-benzyldioxothiazolidylbenzamide derivatives and processes for

N-substituted dioxothiazolidylbenzamide derivatives and process for

Cyclic aminophenylacetic acid derivatives, process for preparing the

An antirheumatoid pharmaceutical composition containing a cyclic anthranilic acid derivative of the following formula, ##STR1## wherein R.sup.1, and R.sup.2 and R.sup.3 each independently indicate a hydrogen atom, halogen atom, lower alkyl group having 1 to 3 carbon atoms, lower alkoxy group having 1 to 3 carbon atoms, amino group, nitro group, hydroxy group, sulfonamide group, trifluoromethyl group, cyano group, carboxyl group, carbamoyl group, acetyl group, benzoylmethyl group which may be substituted, methylthio group, phenylethynyl group which may be substituted, ethynyl group which may be substituted, alkanoylamino group having 1 to 3 carbon atoms, benzoylamino group which may be substituted, alkylsulfonylamino group having 1 to 3 carbon atoms or phenylsulfonylamino group which may be substituted; R.sup.4 and R.sup.5 each independently indicate a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms, cyano group, carboxyl group, hydroxymethyl group, phenyl group which may be substituted or benzyl group; R.sup.6 indicates a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms or benzyl group; X is a methylene; the acid or alkali salts thereof and an insert, pharamaceutically acceptable carrier.

Cyclic anthranilic acid derivatives

An antirheumatoid pharmaceutical composition containing a cyclic anthranilic acid derivative of the following formula, ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each independently indicate a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms, lower alkoxy group having 1 to 3 carbon atoms, amino group, nitro group, hydroxy group, sulfonamide group, trifluoromethyl group, cyano group, carboxyl group, carbamoyl group, acetyl group, benzoylmethyl group which may be substituted, methylthio group, phenylethynyl group which may be substituted, ethynyl group which may be substituted, alkanoylamino group having 1 to 3 carbon atoms, benzoylamino group which may be substituted, alkylsulfonylamino group having 1 to 3 carbon atoms or phenylsulfonylamino group which may be substituted; R.sup.4 and R.sup.5 each independently indicate a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms, cyano group, carboxyl group, hydroxymethyl group, phenyl group which may be substituted or benzyl group; R.sup.6 indicates a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms or benzyl group; X is oxygen, sulfur, SO or SO.sub.2 ; the acid or alkali salts thereof and an inert, pharmaceutically acceptable carrier.

Cyclic anthranilic acid derivatives and process for their preparation

Phenoxyalkylcarboxylic acid derivatives of the following formula, ##STR1## wherein R.sup.1 indicates a hydrogen atom, a methyl group or an ethyl group, m is equal to 2, 3 or 4, and n is equal to 3 or 4, their alkali salts and hydrates thereof are useful as antiallergic agents.

Phenoxyalkylcarboxylic acid derivatives and process for their preparation

Phenoxyalkylcarboxylic acid derivatives of the following formula, ##STR1## wherein R.sup.1 indicates hydrogen atom, methyl group or ethyl group, m is an integer from 2 to 5, and n is an integer from 3 to 8, X.sup.1 and X.sup.2 each independently represent sulfur atom, oxygen atom, sulfinyl group or sulfonyl group, proviso X.sup.1 and X.sup.2 are not simultaneously oxygen atom; their alkali salts and hydrates thereof are useful as antiallergic agents.

Phenoxyalkylcarboxylic acid derivatives and process for their

An antirheumatoid pharmaceutical composition containing a cyclic anthranilic acid derivative of the following formula, ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each independently indicate a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms, lower alkoxy group having 1 to 3 carbon atoms, amino group, nitro group, hydroxy group, sulfonamide group, trifluoromethyl group, cyano group, carboxyl group, carbamoyl group, acetyl group, benzoylmethyl group which may be substituted, methylthio group, phenylethynyl group which may be substituted, ethynyl group which may be substituted, alkanoylamino group having 1 to 3 carbon atoms, benzoylamino group which may be substituted, alkylsulfonylamino group having 1 to 3 carbon atoms or phenylsulfonylamino group which may be substituted; R.sup.4 and R.sup.5 each independently indicate a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms, cyano group, carboxyl group, hydroxymethyl group, phenyl group which may be substituted or benzyl group; R.sup.6 indicates a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms or benzyl group; X indicates a methylene group; their acid or alkali salts and an inert, pharmaceutically acceptable carrier.

Benzimidazole derivatives of the following formula, ##STR1## wherein R.sup.1 indicates hydrogen atom, lower alkyl group having carbon atoms of 1 to 6 or dimethylaminopropyl group, R.sup.2 indicates hydrogen atom or lower alkanoyl group having carbon atoms of 1 to 3, R.sup.3 indicates hydrogen atom, lower alkyl group having carbon atoms of 1 to 3 or lower alkanoyl group having carbon atoms of 1 to 3, X indicates sulfur atom, sulfinyl group, sulfonyl group, amino group or methylene group, A indicates alkylene group having carbon atoms of 1 to 12, which alkylene group may optionally be substituted by hydroxy group or lower alkyl group having carbon atoms of 1 to 3, --(CHR')N--CR'.dbd.CR'--(CHR')M--, ##STR2## (in which R' and R' are each independently hydrogen atom, lower alkyl group having carbon atoms of 1 to 3 or hydroxy group, and n and m are equal to 0, 1, 2 or 3) and Y indicates oxygen atom or sulfur atom; their acid or alkali salts and hydrate thereof are useful as antiallergic agents.

Benzimidazole Derivatives

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Oyama, Japan

Katsuya Awano