公开(公告)号：US06545026B1

公开(公告)日：2003-04-08

申请号：US10049905

申请日：2002-02-20

申请人： Shizuyoshi Fujimori ,  Koji Murakami ,  Masaki Tsunoda

发明人： Shizuyoshi Fujimori ,  Koji Murakami ,  Masaki Tsunoda

IPC分类号： C07D27734

CPC分类号： C07D277/34

摘要： The invention provides novel substituted benzylthiazolidine-2,4-dione derivatives which increase the transactivation of receptor as a ligand of human peroxisome proliferator-activated receptor (PPAR) and exhibit the blood glucose-decreasing action and lipid-decreasing action, and a process for preparing them. The invention relates to substituted benzylthiazolidine-2,4-dione derivatives represented by the general formula (1) [wherein A denotes a pyridyl group or cyclohexyl group], their medicinally acceptable salts, their hydrates and a process for preparing them.

摘要翻译： 本发明提供新的取代的苄基噻唑烷-2,4-二酮衍生物，其增加受体作为人类过氧化物酶体增殖物激活受体（PPAR）的配体的反式激活，并显示出血糖降低作用和降脂作用，以及 本发明涉及由通式（1）表示的取代的苄基噻唑烷-2,4-二酮衍生物[其中A表示吡啶基或环己基]，其药学上可接受的盐，它们的水合物及其制备方法。

公开(公告)号：US5234928A

公开(公告)日：1993-08-10

申请号：US721610

申请日：1991-07-17

申请人： Shizuyoshi Fujimori ,  Michiro Ohnota ,  Yoshihiro Hirata ,  Koji Murakami

发明人： Shizuyoshi Fujimori ,  Michiro Ohnota ,  Yoshihiro Hirata ,  Koji Murakami

IPC分类号： A61K31/505 ,  A61K31/517 ,  A61P3/08 ,  A61P3/10 ,  A61P7/02 ,  A61P43/00 ,  C07D239/80 ,  C07D239/95 ,  C07D239/96 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/04 ,  C07D417/06 ,  C07D491/056 ,  C07D521/00 ,  C12N9/99

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D239/80 ,  C07D239/95 ,  C07D239/96 ,  C07D249/08 ,  C07D401/06 ,  C07D403/04 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  Y02P20/55

摘要： The present invention relates to quinazoline-3-alkanoic acid derivatives having both an inhibitory effect on platelet aggregation and a hindering effect on aldose reductase together, represented by a general formula [I] ##STR1## [wherein R is hydrogen or a protecting group for carboxyl group, R.sup.1 is a lower alkyl group, alkenyl group, alkinyl group, lower alkoxy group, lower alkylthio group, halogen, phenyl group (this phenyl group may be substituted by one to three of lower alkyls, lower alkoxys, halogens, trifluoromethyls, carboxyethylenes or ethoxycarbonylethylenes, naphthyl group, heterocycle (this heterocycle may be substituted by one to three of lower alkyls), cycloalkyl group or benzoyl group (this benzoyl group may be substituted by lower alkyl or halogen), R.sup.2 and R.sup.3 are identically or differently hydrogens, halogens, lower alkyl groups, lower alkoxy groups, aralkyl groups which may be substituted, nitro groups, imidazolyl groups, imidazolylmethyl groups or ##STR2## (R.sup.4 and R.sup.5 indicate identically or differently hydrogens or lower alkyl groups, or connected with each other to make five- or six-membered heterocycles which may contain other hetero atom, X is carbonyl, thiocarbonyl or methylene group (this methylene group may be substituted by lower alkyl group), A is lower alkylene or lower alkenylene, and n indicates an integer of 1 to 3],their salts, their preparation processes and medicinal drugs containing them.

摘要翻译： PCT No.PCT / JP90 / 01600 Sec。 371日期：1991年7月17日 102（e）日期1991年7月17日PCT 1990年12月10日PCT PCT。 出版物WO91 / 0902400 日本1991年6月27日。本发明涉及具有对血小板聚集的抑制作用和对醛糖还原酶的阻碍作用的喹唑啉-3-链烷酸衍生物，其通式[I]表示[其中R 是氢或羧基的保护基，R1是低级烷基，烯基，炔基，低级烷氧基，低级烷硫基，卤素，苯基（该苯基可被一至三个低级烷基取代， 低级烷氧基，卤素，三氟甲基，羧乙烯或乙氧基羰基乙烯，萘基，杂环（该杂环可被一至三个低级烷基取代），环烷基或苯甲酰基（该苯甲酰基可被低级烷基或卤素取代），R2 和R 3是相同或不同的氢，卤素，低级烷基，低级烷氧基，可被取代的芳烷基，硝基，咪唑基，咪唑基甲基或IM （R 4和R 5表示相同或不同的氢或低级烷基，或彼此连接以形成可含有其它杂原子的五或六元杂环，X为羰基，硫代羰基或亚甲基（该亚甲基可以 被低级烷基取代），A是低级亚烷基或低级亚烯基，n表示1〜3的整数]，它们的盐，它们的制备方法和含有它们的药用药物。

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：US06780431B1

公开(公告)日：2004-08-24

申请号：US10049937

申请日：2002-02-20

申请人： Mashiro Nomura ,  Koji Murakami ,  Masaki Tsunoda ,  Yukie Takahashi

发明人： Mashiro Nomura ,  Koji Murakami ,  Masaki Tsunoda ,  Yukie Takahashi

IPC分类号： A61K31426

CPC分类号： C07D277/34

摘要： The invention relates to substituted benzylthiazolidine-2,4-dione derivatives represented by a general formula (1) wherein R1 denotes a chlorine atom, bromine atom, nitro group, trifluoromethoxy group, ethoxy group, propoxy group or isopropoxy group, and R2 denotes a hydrogen atom or chlorine atom, their medicinally acceptable salts, their hydrates and a process for preparing them.

摘要翻译： 本发明涉及由通式（1）表示的取代的苄基噻唑烷-2,4-二酮衍生物，其中R 1表示氯原子，溴原子，硝基，三氟甲氧基，乙氧基，丙氧基或异丙氧基， R 2表示氢原子或氯原子，其药学上可接受的盐，它们的水合物及其制备方法。

公开(公告)号：US06734199B1

公开(公告)日：2004-05-11

申请号：US10049904

申请日：2002-02-20

申请人： Hiroyuki Miyachi ,  Masahiro Nomura ,  Takahiro Tanase ,  Koji Murakami ,  Masaki Tsunoda

发明人： Hiroyuki Miyachi ,  Masahiro Nomura ,  Takahiro Tanase ,  Koji Murakami ,  Masaki Tsunoda

IPC分类号： A61K31426

CPC分类号： C07D277/34

摘要： The invention provides novel substituted benzylthiazolidine-2,4-dione derivatives which increase the transactivation action of receptor as a ligand of human peroxisome proliferator-activated receptor (PPAR) and exhibit the blood glucose-decreasing action and lipid-decreasing action, and a process for preparing them. The invention relates to substituted benzylthiazolidine-2,4-dione derivatives represented by the general formula (1) [wherein A denotes a phenyl group which is unsubstituted or may have substituents, phenoxy group which is unsubstituted or may have substituents or benzyloxy group which is unsubstituted or may have substituents], their medicinally acceptable salts, their hydrates and a process for preparing them.

摘要翻译： 本发明提供新的取代的苄基噻唑烷-2,4-二酮衍生物，其增加受体作为人过氧化物酶体增殖物激活受体（PPAR）的配体的反式激活作用，并显示出降血糖作用和降脂作用， 本发明涉及由通式（1）表示的取代的苄基噻唑烷-2,4-二酮衍生物[其中A表示未取代或可具有取代基的苯基，未取代或可具有取代基的苯氧基或 未取代或可具有取代基的苄氧基，其药学上可接受的盐，它们的水合物及其制备方法。

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：US06730687B1

公开(公告)日：2004-05-04

申请号：US10049645

申请日：2002-02-25

申请人： Hiroyuki Miyachi ,  Masahiro Nomura ,  Takahiro Tanase ,  Koji Murakami ,  Masaki Tsunoda

发明人： Hiroyuki Miyachi ,  Masahiro Nomura ,  Takahiro Tanase ,  Koji Murakami ,  Masaki Tsunoda

IPC分类号： A61K31426

CPC分类号： C07D277/34

摘要： The invention provides novel substituted benzylthiazolidine-2,4-dione derivatives that bind to receptor to activate as ligands of human peroxisome proliferator-activated receptor (PPAR) and exhibit blood glucose-decreasing action and lipid-decreasing action, and processes for preparing them. It relates to substituted benzylthiazolidine-2,4-dione derivatives represented by the general formula (1) [wherein the bond mode of A denotes —CH2CONH—, —NHCONH—, —CH2CH2CO— or —NHCOCH2—, and B denotes a lower alkyl group with carbon atoms of 1 to 4, lower alkoxy group with carbon atoms of 1 to 3, halogen atom, trifluoromethyl group, trifluoromethoxy group, phenyl group which is unsubstituted or may have substituents, phenoxy group which is unsubstituted or may have substituents or benzyloxy group which is unsubstituted or may have substituents], their medicinally acceptable salts, their hydrates and processes for preparing them.

摘要翻译： 本发明提供了新的取代的苄基噻唑烷-2,4-二酮衍生物，其结合受体以作为人类过氧化物酶体增殖物激活受体（PPAR）的配体活化并显示出血糖降低作用和降脂作用，以及制备它们的方法。 它涉及由通式（1）表示的取代的苄基噻唑烷-2,4-二酮衍生物[其中A的键合模式表示-CH 2 CONH-，-NHCONH-，-CH 2 CH 2 CO-或-NHCOCH 2 - ，B表示低级烷基 具有1至4个碳原子的烷基，具有1至3个碳原子的低级烷氧基，卤素原子，三氟甲基，三氟甲氧基，未取代或可具有取代基的苯基，未被取代或可具有取代基的苯氧基或可具有取代基的苯氧基 未取代或可具有取代基的基团]，它们的药学上可接受的盐，它们的水合物及其制备方法。

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：US06506797B1

公开(公告)日：2003-01-14

申请号：US10009175

申请日：2001-12-10

申请人： Masahiro Nomura ,  Yukie Takahashi ,  Takahiro Tanase ,  Hiroyuki Miyachi ,  Masaki Tsunoda ,  Tomohiro Ide ,  Koji Murakami

发明人： Masahiro Nomura ,  Yukie Takahashi ,  Takahiro Tanase ,  Hiroyuki Miyachi ,  Masaki Tsunoda ,  Tomohiro Ide ,  Koji Murakami

IPC分类号： A01N3712

CPC分类号： C07D263/26 ,  A61K31/195 ,  C07C235/60 ,  C07C323/60

摘要： The invention provides novel substituted phenylpropanoic acid derivatives that activate by binding to receptor as ligands of human peroxisome preliferant-activated receptor &agr; (PPAR&agr;), and exhibit potent decreasing action on lipids in blood (cholesterol and triglyceride). It relates to a substituted phenylpropanoic acid derivatives represented by a general formula (1), their pharmaceutically acceptable salts and their hydrates, and processes for preparing them.

摘要翻译： 本发明提供新的取代苯丙酸衍生物，其通过与作为人过氧化物酶体增生物激活受体α（PPARα）的配体的受体结合而活化，并且对血液中的脂质（胆固醇和甘油三酸酯）表现出有效的降低作用。涉及取代的苯丙酸 由通式（1）表示的衍生物，其药学上可接受的盐及其水合物及其制备方法。

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。