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1. 发明授权

US06506797B1 Substituted phenylpropionic acid derivatives as agonists to human peroxisome proliferator-activated receptor (PPAR) &agr; 失效
标题翻译：取代的苯丙酸衍生物作为人类过氧化物酶体增殖物激活受体（PPAR）α的激动剂
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。

2. 发明授权

US06734199B1 Substituted benzylthiazolidine-2, 4-dione derivatives 失效
标题翻译：取代的苄基噻唑烷-2,4-二酮衍生物
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。

3. 发明授权

US06730687B1 Substituted benzylthiazolidine-2, 4-dione derivatives 失效
标题翻译：取代的苄基噻唑烷-2,4-二酮衍生物
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。

4. 发明授权

US06780431B1 Substituted benzylthiazolidine-2,4-dione derivatives 失效
标题翻译：取代的苄基噻唑烷-2,4-二酮衍生物
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。

5. 发明授权

US6030990A N-benzyldioxothiazolidylbenzamide derivatives and process for producing the same 失效
标题翻译： N-苄基二氧代噻唑烷基苯甲酰胺衍生物及其制造方法
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。

6. 发明授权

US6147101A N-benzyldioxothiazolidylbenzamide derivatives and process for producing the same 有权
标题翻译： N-苄基二氧代噻唑烷基苯甲酰胺衍生物及其制造方法
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。

7. 发明授权

US5948803A N-substituted dioxothiazolidylbenzamide derivatives and process for producing the same 失效
标题翻译： N-取代的二氧代噻唑烷基苯甲酰胺衍生物及其制备方法
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。

8. 发明授权

US6001862A N-benzyldioxothiazolidylbenzamide derivatives and processes for preparing the same 有权
标题翻译： N-苄基二氧代噻唑烷基苯甲酰胺衍生物及其制备方法
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。

9. 发明申请

US20070167501A1 Bicyclo derivative 失效
标题翻译：双环衍生物
公开(公告)号：US20070167501A1
公开(公告)日：2007-07-19
申请号：US10590871
申请日：2005-02-22
申请人： Yasumichi Fukuda , Yoshikazu Asahina , Kazuya Yokota , Koji Murakami , Tomohiro Ide
发明人： Yasumichi Fukuda , Yoshikazu Asahina , Kazuya Yokota , Koji Murakami , Tomohiro Ide
IPC分类号： A61K31/426 , A61K31/421 , A61K31/401
CPC分类号： C07D207/16
摘要： A novel bicyclo derivative represented by the following general formula (1), or a pharmaceutically acceptable salt thereof, acts as an effective DPP-IV inhibitor: One example is (2S,4S)-1-[[N-(4-methylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile).
摘要翻译：由以下通式（1）表示的新型双环衍生物或其药学上可接受的盐作为有效的DPP-IV抑制剂：一个实例是（2S，4S）-1 - [[N-（4-甲基双环[ 2.2.2]辛-1-基）氨基]乙酰基] -4-氟吡咯烷-2-腈）。

10. 发明授权

US07514571B2 Bicyclo derivative 失效
标题翻译：双环衍生物
公开(公告)号：US07514571B2
公开(公告)日：2009-04-07
申请号：US10590871
申请日：2005-02-22
申请人： Yasumichi Fukuda , Yoshikazu Asahina , Kazuya Yokota , Koji Murakami , Tomohiro Ide
发明人： Yasumichi Fukuda , Yoshikazu Asahina , Kazuya Yokota , Koji Murakami , Tomohiro Ide
IPC分类号： A61K31/40 , C07D207/00
CPC分类号： C07D207/16
摘要： A novel bicyclo derivative represented by the following general formula (1), or a pharmaceutically acceptable salt thereof, acts as an effective DPP-IV inhibitor: One example is (2S,4S)-1-[[N-(4-methylbicyclo[2,2,2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile).
摘要翻译：由以下通式（1）表示的新型双环衍生物或其药学上可接受的盐作为有效的DPP-IV抑制剂：一个实例是（2S，4S）-1 - [[N-（4-甲基双环[ 2,2,2]辛-1-基）氨基]乙酰基] -4-氟吡咯烷-2-腈）。

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