公开(公告)号：US5359076A

公开(公告)日：1994-10-25

申请号：US956012

申请日：1992-12-09

申请人： Yasushi Kohno ,  Katsuya Awano ,  Takayoshi Ishizaki ,  Eisuke Kojima ,  Shinji Kudoh ,  Yasuhiko Sakoe ,  Koji Saito

发明人： Yasushi Kohno ,  Katsuya Awano ,  Takayoshi Ishizaki ,  Eisuke Kojima ,  Shinji Kudoh ,  Yasuhiko Sakoe ,  Koji Saito

IPC分类号： A61K31/47 ,  A61P29/00 ,  A61P37/00 ,  A61P37/02 ,  C07C311/21 ,  C07C317/48 ,  C07C323/63 ,  C07C331/14 ,  C07D215/12 ,  C07D215/14 ,  C07D215/18 ,  C07D215/22 ,  C07D215/26 ,  C07D215/36 ,  C07D215/40 ,  C07D215/48 ,  C07D498/04 ,  C07D498/06 ,  C07F7/08 ,  C07D215/24 ,  C07D215/06 ,  C07D215/16

CPC分类号： C07D215/14 ,  C07C311/21 ,  C07C317/48 ,  C07C323/63 ,  C07C331/14 ,  C07D215/12 ,  C07D215/18 ,  C07D215/36 ,  C07D215/40 ,  C07D215/48 ,  C07F7/0812

摘要： The present invention provides novel cyclic aminophenylacetic acid derivatives having modulating action on immune response, their optical isomers, their salts and their preparative processes, and therapeutic agents for autoimmune diseases containing them as effective ingredients, the cyclic aminophenylacetic acid derivatives being represented by a general formula (1) ##STR1## wherein R and R.sup.1 each independently denotes hydrogen atom or lower alkyl group having 1 to 3 carbon atoms, R.sup.2 denotes a phenyl group (which may be substituted with 1 to 3 groups of halogen atom, methoxy group or their combinations) or trifluoromethyl group, and X denotes a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms, lower alkoxy group having 1 to 3 carbon atoms, cyano group, thiocyano group, trimethylsilylethinyl group, phenyl group (which may be substituted with halogen atom, methoxy group, methyl group or their combinations), carbamoyl group, carboxyl group, lower alkoxycarbonyl group having 1 to 3 carbon atoms, acetyl group, benzoyl group, nitro group, amino group, lower alkanoylamino group having 1 to 3 carbon atoms, benzoylamino group which may be substituted, phenylsulfonylamino group which may be substituted, lower alkylthio group having 1 to 3 carbon atoms, lower alkylsulfinyl group having 1 to 3 carbon atoms, lower alkylsulfonyl group having 1 to 3 carbon atoms or halogen atom.

摘要翻译： PCT No.PCT / JP92 / 00476 Sec。 371日期：1992年12月9日 102（e）日期1992年12月9日PCT提交1992年4月15日PCT公布。 公开号WO92 / 18482 本发明提供了具有对免疫应答的调节作用的新型环状氨基苯乙酸衍生物，其旋光异构体，其盐及其制备方法，以及含有它们作为有效成分的自身免疫性疾病的治疗剂，环状氨基苯乙酸 衍生物由通式（1）表示，其中R和R 1各自独立地表示氢原子或具有1至3个碳原子的低级烷基，R 2表示苯基（可被1至3个取代基取代） 卤素原子，甲氧基或它们的组合基团）或三氟甲基，X表示氢原子，碳原子数1〜3的低级烷基，碳原子数1〜3的低级烷氧基，氰基，硫氰基，三甲基甲硅烷基乙炔基 ，苯基（其可以被卤素原子，甲氧基，甲基或它们的组合取代），氨基甲酰基，羧基，低级烷氧基 具有1至3个碳原子的酰基，乙酰基，苯甲酰基，硝基，氨基，具有1至3个碳原子的低级烷酰基氨基，可被取代的苯甲酰基氨基，可被取代的苯基磺酰基氨基，具有1个 3个碳原子，具有1至3个碳原子的低级烷基亚磺酰基，具有1至3个碳原子的低级烷基磺酰基或卤素原子。

公开(公告)号：US5147874A

公开(公告)日：1992-09-15

申请号：US560775

申请日：1990-07-31

申请人： Eisuke Kojima ,  Shizuyoshi Fujimori ,  Katsuya Awano

发明人： Eisuke Kojima ,  Shizuyoshi Fujimori ,  Katsuya Awano

IPC分类号： C07D215/48 ,  A61K31/47 ,  A61K31/535 ,  A61K31/538 ,  A61K31/54 ,  A61P29/00 ,  A61P37/00 ,  C07D265/36 ,  C07D279/16 ,  C07D471/06 ,  C07D498/06 ,  C07D513/06

CPC分类号： C07D215/48 ,  C07D265/36 ,  C07D279/16

摘要： 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.

公开(公告)号：US4956372A

公开(公告)日：1990-09-11

申请号：US249996

申请日：1988-09-27

申请人： Eisuke Kojima ,  Shizuyoshi Fujimori ,  Katsuya Awano

发明人： Eisuke Kojima ,  Shizuyoshi Fujimori ,  Katsuya Awano

IPC分类号： C07D215/48 ,  A61K31/47 ,  A61K31/535 ,  A61K31/538 ,  A61K31/54 ,  A61P29/00 ,  A61P37/00 ,  C07D265/36 ,  C07D279/16 ,  C07D471/06 ,  C07D498/06 ,  C07D513/06

CPC分类号： C07D215/48 ,  C07D265/36 ,  C07D279/16

摘要： 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.

摘要翻译： 含有下式的环状邻氨基苯甲酸衍生物的抗类风湿性药物组合物，其中R1，R2和R3各自独立地表示氢原子，碳原子数1〜3的低级烷基，碳原子数1〜3的低级烷氧基 氨基，硝基，羟基，磺酰胺基，三氟甲基，氰基，羧基，氨基甲酰基，乙酰基，可被取代的苯甲酰甲基，甲硫基，可被取代的苯基乙炔基，可以被取代的乙炔基 取代的碳原子数1〜3的烷酰基氨基，可以被取代的苯甲酰基氨基，碳原子数1〜3的烷基磺酰基氨基或可被取代的苯基磺酰基氨基; R4和R5各自独立地表示氢原子，具有1至3个碳原子的低级烷基，氰基，羧基，羟甲基，可被取代的苯基或苄基; R6表示氢原子，碳原子数1〜3的低级烷基或苄基; X表示亚甲基; 它们的酸或碱盐和惰性的药学上可接受的载体。

公开(公告)号：US5281600A

公开(公告)日：1994-01-25

申请号：US929526

申请日：1992-08-14

申请人： Eisuke Kojima ,  Shizuyoshi Fujimori ,  Katsuya Awano

发明人： Eisuke Kojima ,  Shizuyoshi Fujimori ,  Katsuya Awano

IPC分类号： C07D215/48 ,  A61K31/47 ,  A61K31/535 ,  A61K31/538 ,  A61K31/54 ,  A61P29/00 ,  A61P37/00 ,  C07D265/36 ,  C07D279/16 ,  C07D471/06 ,  C07D498/06 ,  C07D513/06 ,  C07D215/12 ,  C07D215/14

CPC分类号： C07D215/48 ,  C07D265/36 ,  C07D279/16

摘要： 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.

摘要翻译： 含有下式的环状邻氨基苯甲酸衍生物的抗风湿病药物组合物（*化学结构*）（I）其中R1，R2和R3各自独立地表示氢原子，卤素原子，碳原子数1〜3的低级烷基 ，具有1至3个碳原子的低级烷氧基，氨基，硝基，羟基，磺酰胺基，三氟甲基，氰基，羧基，氨基甲酰基，乙酰基，可被取代的苯甲酰甲基，甲硫基，苯基乙炔基 可以被取代的，可以被取代的乙炔基，具有1-3个碳原子的烷酰基氨基，可被取代的苯甲酰氨基，可以被取代的苯磺酰氨基; R4和R5各自独立地表示氢原子，具有1至3个碳原子的低级烷基，氰基，羧基，羟甲基，可被取代的苯基或苄基; R6表示氢原子，碳原子数1〜3的低级烷基或苄基; X是亚甲基; 其酸或碱盐和插入物，药物上可接受的载体。

公开(公告)号：US6147101A

公开(公告)日：2000-11-14

申请号：US482268

申请日：2000-01-13

申请人： Toshio Maeda ,  Masahiro Nomura ,  Katsuya Awano ,  Susumu Kinoshita ,  Hiroya Satoh ,  Koji Murakami ,  Masaki Tsunoda

发明人： Toshio Maeda ,  Masahiro Nomura ,  Katsuya Awano ,  Susumu Kinoshita ,  Hiroya Satoh ,  Koji Murakami ,  Masaki Tsunoda

IPC分类号： C07D277/34 ,  C07D417/12 ,  A61K31/426

CPC分类号： C07D417/12 ,  C07D277/34

摘要： 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.

摘要翻译： 本发明提供了改善胰岛素抵抗并具有强效降血糖和降脂作用的新型N-苄基二硫代噻唑烷基苯甲酰胺衍生物及其制备方法，涉及以通式（1）表示的N-苄基二硫代噻唑烷基苯甲酰胺衍生物[其中 R1和R2表示相同或不同的氢原子，碳原子数为1〜4的低级烷基，碳原子数1〜3的低级烷氧基，碳原子数1〜3的低级卤代烷基，碳原子数为1〜 1至3，卤素原子，羟基，硝基，可被具有1至3个碳原子的低级烷基取代的氨基或杂环，或R 1和R 2连接形成亚甲二氧基，R 3表示 碳原子数为1〜3的低级烷氧基，羟基或卤素原子，虚线表示双键或单键与实线组合]，工序 准备相同。

公开(公告)号：US6030990A

公开(公告)日：2000-02-29

申请号：US952672

申请日：1997-12-02

申请人： Toshio Maeda ,  Masahiro Nomura ,  Katsuya Awano ,  Susumu Kinoshita ,  Hiroya Satoh ,  Koji Murakami ,  Masaki Tsunoda

发明人： Toshio Maeda ,  Masahiro Nomura ,  Katsuya Awano ,  Susumu Kinoshita ,  Hiroya Satoh ,  Koji Murakami ,  Masaki Tsunoda

IPC分类号： C07D277/20 ,  A61K31/425 ,  A61K31/426 ,  A61P3/06 ,  A61P3/08 ,  A61P3/10 ,  C07C67/347 ,  C07C69/76 ,  C07C69/84 ,  C07C69/92 ,  C07D277/34 ,  C07D417/12

CPC分类号： C07D417/12 ,  C07D277/34

摘要： 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.

摘要翻译： PCT No.PCT / JP96 / 01459 Sec。 371日期1997年12月2日第 102（e）日期1997年12月2日PCT提交1996年5月30日PCT公布。 公开号WO96 / 38428 日期：1996年12月5日本发明提供了改善胰岛素抵抗性并具有强力降血糖和降脂效果的新型N-苄基二硫代噻唑烷基苯甲酰胺衍生物及其制备方法，涉及N-苄基二硫代噻唑烷基苯甲酰胺衍生物，其特征在于通式 （1）其中R1和R2表示相同或不同的氢原子，碳原子数为1〜4的低级烷基，碳原子数1〜3的低级烷氧基，碳原子数1〜3的低级卤代烷基，低级卤代烷氧基 具有1至3个碳原子，卤素原子，羟基，硝基，可被具有1-3个碳原子的低级烷基取代的氨基或杂环，或R 1和R 2连接形成亚甲二氧基 基团，R3表示碳原子数为1〜3的低级烷氧基，羟基或卤原子，虚线表示双键或单键与固体锂的结合 ne及其制备方法。

公开(公告)号：US06265577B1

公开(公告)日：2001-07-24

申请号：US09269734

申请日：1999-04-05

申请人： Yasushi Kouno ,  Takenobu Ogata ,  Katsuya Awano ,  Kayoko Matsuzawa ,  Taroh Tooru

发明人： Yasushi Kouno ,  Takenobu Ogata ,  Katsuya Awano ,  Kayoko Matsuzawa ,  Taroh Tooru

IPC分类号： C07D23702

CPC分类号： C07D471/04

摘要： 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 R1 is C1-C4 lower alkyl or C3-C6 cycloalkyl; and R2, R3, R4 and R5 are each independently hydrogen, C1-C4 lower alkyl or phenyl, or alternatively R3 and R5 may be united to form a double bond.

摘要翻译： 新型吡唑并吡啶酮衍生物，其特征在于由通式（1）表示，其药学上可接受的盐，其表现出磷酸二酯酶抑制活性并对呼吸道具有选择性有效的支气管扩张作用; 它们的制备过程; 和含有与活性成分相同的支气管扩张药; 其中R1是C1-C4低级烷基或C3-C6环烷基; 并且R 2，R 3，R 4和R 5各自独立地为氢，C 1 -C 4低级烷基或苯基，或者R 3和R 5可以一起形成双键。

公开(公告)号：US4985585A

公开(公告)日：1991-01-15

申请号：US313900

申请日：1989-02-23

申请人： Mitsuo Ohashi ,  Katsuya Awano ,  Toshio Tanaka ,  Tetsuya Kimura

发明人： Mitsuo Ohashi ,  Katsuya Awano ,  Toshio Tanaka ,  Tetsuya Kimura

IPC分类号： A61K31/10 ,  A61K31/19 ,  A61K31/215 ,  C07C59/215 ,  C07C69/708 ,  C07C315/02 ,  C07C317/00 ,  C07C317/14 ,  C07C317/22 ,  C07C317/24 ,  C07C317/46 ,  C07C321/00 ,  C07C323/09 ,  C07C323/20 ,  C07C323/62

CPC分类号： C07C323/00 ,  C07C317/00

摘要： 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.

公开(公告)号：USRE38921E1

公开(公告)日：2005-12-13

申请号：US10622589

申请日：2003-07-21

申请人： Mitsuo Ohashi ,  Katsuya Awano ,  Toshio Tanaka ,  Tetsuya Kimura

发明人： Mitsuo Ohashi ,  Katsuya Awano ,  Toshio Tanaka ,  Tetsuya Kimura

IPC分类号： A61K31/10 ,  A61K31/19 ,  A61K31/215 ,  C07C59/215 ,  C07C69/708 ,  C07C315/02 ,  C07C317/00 ,  C07C317/14 ,  C07C317/22 ,  C07C317/24 ,  C07C317/46 ,  C07C321/00 ,  C07C323/09 ,  C07C323/20 ,  C07C323/62 ,  C07C32/00

CPC分类号： C07C323/00 ,  C07C317/00

摘要： Phenoxyalkylcarboxylic acid derivative represented by the following formula, wherein R1 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, X1 and X2 each independently represent sulfur atom, oxygen atom, sulfinyl group or sulfonyl group, proviso X1 and X2 are not simultaneously oxygen atom; their alkali salts and hydrates thereof are useful as antiallergic agents.

摘要翻译： 下式表示的苯氧基烷基羧酸衍生物，其中R 1表示氢原子，甲基或乙基，m为2〜5的整数，n为3〜8的整数，X < SUP 1和X 2各自独立地表示硫原子，氧原子，亚磺酰基或磺酰基，条件是X 1和X 2， SUP>不是同时氧原子; 其碱金属盐和水合物可用作抗过敏剂。

公开(公告)号：US5948803A

公开(公告)日：1999-09-07

申请号：US77899

申请日：1998-06-16

申请人： Toshio Maeda ,  Masahiro Nomura ,  Katsuya Awano ,  Susumu Kinoshita ,  Hiroya Satoh ,  Koji Murakami ,  Masaki Tsunoda

发明人： Toshio Maeda ,  Masahiro Nomura ,  Katsuya Awano ,  Susumu Kinoshita ,  Hiroya Satoh ,  Koji Murakami ,  Masaki Tsunoda

IPC分类号： C07D277/20 ,  A61K31/425 ,  A61K31/426 ,  A61K31/44 ,  A61P3/06 ,  A61P3/08 ,  A61P43/00 ,  C07D277/34 ,  C07D417/12

CPC分类号： C07D417/12 ,  C07D277/34

摘要： The invention provides novel N-substituted dioxothiazolidylbenzamide derivatives that improve the insulin resistance and have potent hypoglycemic effect and lipid-lowering effect, and the process for preparing them, and relates to N-substituted dioxothiazolidylbenzamide 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 or hydroxyl groups, or R.sup.1 and R.sup.2 combine to form a methylenedioxy group, R.sup.3 denotes a hydrogen atom, lower alkoxys group with carbon atoms of 1 to 3, hydroxyl group or halogen atom, R.sup.4 denotes a hydrogen or lower alkyl group with carbon atoms of 1 to 3, n denotes an integer of 0 to 2, and X denotes N or CH!, and process for preparing the same.

摘要翻译： PCT No.PCT / JP96 / 03664 Sec。 371日期：1998年6月16日 102（e）日期1998年6月16日PCT 1996年12月16日PCT公布。 公开号WO97 / 22600 PCT 日期：1997年6月26日本发明提供了改善胰岛素抵抗并具有强效降血糖作用和降脂作用的新型N-取代二氧代噻唑烷基苯甲酰胺衍生物及其制备方法，涉及N-取代二氧代噻唑烷基苯甲酰胺衍生物，其特征在于以 通式（1）[其中R 1和R 2表示相同或不同的氢原子，碳原子数1〜4的低级烷基，碳原子数1〜3的低级烷氧基，碳原子数1〜3的低级卤代烷基 碳原子数为1〜3的低级卤代烷氧基，卤素原子或羟基或R1和R2结合形成亚甲二氧基，R3表示氢原子，碳原子数1〜3的低级烷氧基，羟基或卤素 原子，R4表示碳原子数为1〜3的氢原子或低级烷基，n表示0〜2的整数，X表示N或CH]表示的化合物及其制备方法。