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：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：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。

公开(公告)号：US6001862A

公开(公告)日：1999-12-14

申请号：US292955

申请日：1999-04-16

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： C07D277/34 ,  C07D417/12 ,  A61K31/425

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：US06706763B1

公开(公告)日：2004-03-16

申请号：US10070425

申请日：2002-03-18

申请人： Hiroya Satoh ,  Masakatsu Komuro ,  Koji Murakami ,  Katsuya Awano

发明人： Hiroya Satoh ,  Masakatsu Komuro ,  Koji Murakami ,  Katsuya Awano

IPC分类号： A61K31195

CPC分类号： C07C317/46 ,  C07C235/60 ,  C07C323/60

摘要： O-anisamide compounds and their addition salts effective for the prevention and/or therapy of metabolic diseases such as hyperlipidemia and diabetes, in which peroxisome proliferator-activated receptor (PPAR) being intranuclear receptor, in particular, human PPAR participates, as agonistic drugs thereon, and processes for preparing them, wherein the o-anisamide compounds are represented by a general formula (1) [wherein R denotes a carboxyl group, carboxymethyl group or CH2CHXCOY (here X denotes a mercapto group or S(O)nMe (n=0, 1 or 2) and Y denotes an amino group or hydroxyl group)], their medicinally acceptable salts, and their hydrates.

摘要翻译： 作为其上的激动药物，有效用于预防和/或治疗代谢性疾病如高脂血症和糖尿病的O-茴香酰胺化合物及其加成盐，其中作为核内受体的过氧化物酶体增殖物激活受体（PPAR），特别是人PPAR参与其中 及其制备方法，其中邻甲氧基苯甲酰胺化合物由通式（1）表示[其中R表示羧基，羧甲基或CH 2 CHXCOY（这里X表示巯基或S（O）nMe（n = 0,1或2），Y表示氨基或羟基）]，其药学上可接受的盐及其水合物。

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：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。