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公开(公告)号：US20100286123A1
公开(公告)日：2010-11-11
申请号：US12768209
申请日：2010-04-27
申请人： Alexander Pasternak , Aurash Shahripour , Haifeng Tang , Nardos H. Teumelsan , Lihu Yang , Yuping Zhu , Shawn P. Walsh
发明人： Alexander Pasternak , Aurash Shahripour , Haifeng Tang , Nardos H. Teumelsan , Lihu Yang , Yuping Zhu , Shawn P. Walsh
IPC分类号： A61K31/55 , C07D493/04 , A61K31/496 , A61P7/10 , A61P9/12 , A61P9/04 , A61P1/16 , A61P13/12 , A61P3/10 , A61P7/02 , A61P9/10 , C07D405/12 , A61K31/551 , C07D487/08 , A61K31/4375 , C07D471/08 , A61K31/407 , C07D295/092 , A61K31/445 , C07D413/14
CPC分类号： C07D307/88 , C07D295/135 , C07D295/155 , C07D405/08 , C07D407/08 , C07D413/08 , C07D487/08 , C07D493/04
摘要： This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
摘要翻译： 本发明涉及具有结构式I的化合物及其药学上可接受的盐，它们是肾外
膜（ROMK）通道（Kir1.1）的抑制剂。 式I的化合物可用作利尿剂和利尿钠，因此可用于治疗和预防由过度的盐和水保持引起的疾病，包括心血管疾病如高血压和慢性和急性心力衰竭。-
公开(公告)号：US08673920B2
公开(公告)日：2014-03-18
申请号：US12768209
申请日：2010-04-27
申请人： Alexander Pasternak , Aurash Shahripour , Haifeng Tang , Nardos H. Teumelsan , Lihu Yang , Yuping Zhu , Shawn P. Walsh
发明人： Alexander Pasternak , Aurash Shahripour , Haifeng Tang , Nardos H. Teumelsan , Lihu Yang , Yuping Zhu , Shawn P. Walsh
IPC分类号： A61K31/496 , C07D401/12 , C07D405/12 , C07D413/12 , A61K31/407 , A61K31/495 , A61K31/551 , C07D295/092 , C07D487/08
CPC分类号： C07D307/88 , C07D295/135 , C07D295/155 , C07D405/08 , C07D407/08 , C07D413/08 , C07D487/08 , C07D493/04
摘要： This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
摘要翻译： 本发明涉及具有结构式I的化合物及其药学上可接受的盐，它们是肾外
膜（ROMK）通道（Kir1.1）的抑制剂。 式I的化合物可用作利尿剂和利尿钠，因此可用于治疗和预防由过度的盐和水保持引起的疾病，包括心血管疾病如高血压和慢性和急性心力衰竭。-
公开(公告)号：US20130225561A1
公开(公告)日：2013-08-29
申请号：US13881008
申请日：2011-10-21
申请人： Haifeng Tang , Alexander Pasternak , Lihu Yang , Shawn P. Walsh , Barbara Pio , Aurash Shahripour , Nardos Teumelsan
发明人： Haifeng Tang , Alexander Pasternak , Lihu Yang , Shawn P. Walsh , Barbara Pio , Aurash Shahripour , Nardos Teumelsan
IPC分类号： C07D295/135 , C07D295/155 , C07D471/08 , C07D487/08 , C07D271/12 , C07D213/76 , C07D295/15
CPC分类号： C07D295/135 , C07D213/61 , C07D213/76 , C07D241/04 , C07D271/04 , C07D271/12 , C07D295/073 , C07D295/15 , C07D295/155 , C07D307/88 , C07D309/30 , C07D405/12 , C07D405/14 , C07D413/12 , C07D471/08 , C07D487/08
摘要： This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
摘要翻译： 本发明涉及具有结构式I的化合物及其药学上可接受的盐，它们是肾外
膜（ROMK）通道（Kir1.1）的抑制剂。 式I的化合物可用作利尿剂和利尿钠，因此可用于治疗和预防由过度的盐和水保持引起的疾病，包括心血管疾病如高血压和慢性和急性心力衰竭。-
公开(公告)号：US09073882B2
公开(公告)日：2015-07-07
申请号：US13881008
申请日：2011-10-21
申请人： Haifeng Tang , Alexander Pasternak , Lihu Yang , Shawn P. Walsh , Barbara Pio , Aurash Shahripour , Nardos Teumelsan
发明人： Haifeng Tang , Alexander Pasternak , Lihu Yang , Shawn P. Walsh , Barbara Pio , Aurash Shahripour , Nardos Teumelsan
IPC分类号： A61K31/496 , C07D295/15 , C07D295/135 , C07D295/155 , C07D213/76 , C07D405/14 , C07D407/12 , C07D213/61 , C07D241/04 , C07D271/04 , C07D295/073 , C07D307/88 , C07D309/30 , C07D405/12 , C07D413/12 , A61K31/551 , A61K31/4745 , C07D271/12 , C07D471/08 , C07D487/08
CPC分类号： C07D295/135 , C07D213/61 , C07D213/76 , C07D241/04 , C07D271/04 , C07D271/12 , C07D295/073 , C07D295/15 , C07D295/155 , C07D307/88 , C07D309/30 , C07D405/12 , C07D405/14 , C07D413/12 , C07D471/08 , C07D487/08
摘要： This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
摘要翻译： 本发明涉及具有结构式I的化合物及其药学上可接受的盐，它们是肾外
膜（ROMK）通道（Kir1.1）的抑制剂。 式I的化合物可用作利尿剂和利尿钠，因此可用于治疗和预防由过度的盐和水保持引起的疾病，包括心血管疾病如高血压和慢性和急性心力衰竭。-
公开(公告)号：US20130217680A1
公开(公告)日：2013-08-22
申请号：US13881574
申请日：2011-10-24
申请人： Alexander Pasternak , Reynalda K. deJesus , Yuping Zhu , Lihu Yang , Shawn Walsh , Haifeng Tang , Dooseop Kim , Barbara Pio , Aurash Shahripour , Kevin Belyk
发明人： Alexander Pasternak , Reynalda K. deJesus , Yuping Zhu , Lihu Yang , Shawn Walsh , Haifeng Tang , Dooseop Kim , Barbara Pio , Aurash Shahripour , Kevin Belyk
IPC分类号： C07D405/12 , C07D405/14 , C07D471/08 , C07D413/14 , C07D487/08 , C07D413/12 , C07D257/04
CPC分类号： C07D405/12 , A61K31/496 , C07D257/04 , C07D307/88 , C07D311/02 , C07D311/76 , C07D311/80 , C07D403/10 , C07D405/06 , C07D405/14 , C07D413/12 , C07D413/14 , C07D471/08 , C07D487/08 , C07D495/04
摘要： This invention relates to compounds having structural Formula (I); and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir 1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
摘要翻译： 本发明涉及具有结构式（I）的化合物; 和它们的药学上可接受的盐，它们是肾外
膜髓质（ROMK）通道（Kir1.1）的抑制剂。 式I的化合物可用作利尿剂和利尿钠，因此可用于治疗和预防由过度的盐和水保持引起的疾病，包括心血管疾病如高血压和慢性和急性心力衰竭。-
公开(公告)号：US09056859B2
公开(公告)日：2015-06-16
申请号：US13881574
申请日：2011-10-24
申请人： Alexander Pasternak , Reynalda K. deJesus , Yuping Zhu , Lihu Yang , Shawn Walsh , Haifeng Tang , Dooseop Kim , Barbara Pio , Aurash Shahripour , Kevin Belyk
发明人： Alexander Pasternak , Reynalda K. deJesus , Yuping Zhu , Lihu Yang , Shawn Walsh , Haifeng Tang , Dooseop Kim , Barbara Pio , Aurash Shahripour , Kevin Belyk
IPC分类号： C07D257/04 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D495/04 , A61K31/496 , C07D311/76 , C07D311/80 , C07D403/10 , C07D307/88 , C07D311/02 , C07D405/06 , C07D471/08 , C07D487/08
CPC分类号： C07D405/12 , A61K31/496 , C07D257/04 , C07D307/88 , C07D311/02 , C07D311/76 , C07D311/80 , C07D403/10 , C07D405/06 , C07D405/14 , C07D413/12 , C07D413/14 , C07D471/08 , C07D487/08 , C07D495/04
摘要： This invention relates to compounds having structural Formula (I); and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir 1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
摘要翻译： 本发明涉及具有结构式（I）的化合物; 和它们的药学上可接受的盐，它们是肾外
膜髓质（ROMK）通道（Kir1.1）的抑制剂。 式I的化合物可用作利尿剂和利尿钠，因此可用于治疗和预防由过度的盐和水分滞留引起的疾病，包括心血管疾病如高血压和慢性和急性心力衰竭。-
公开(公告)号：US20070265332A1
公开(公告)日：2007-11-15
申请号：US11801841
申请日：2007-05-11
申请人： Min Ge , Jiafang He , Fiona Wai Yu Lau , Gui-Bai Liang , Songnian Lin , Weiguo Liu , Shawn P. Walsh , Lihu Yang
发明人： Min Ge , Jiafang He , Fiona Wai Yu Lau , Gui-Bai Liang , Songnian Lin , Weiguo Liu , Shawn P. Walsh , Lihu Yang
IPC分类号： A61K31/381 , A61K31/343 , A61K31/192 , A61K31/195
CPC分类号： C07D213/643 , C07C62/34 , C07C62/38 , C07C229/50 , C07C2603/08 , C07D307/93 , C07D311/94 , C07D333/78 , C07D405/04 , C07D407/12 , C07D413/12 , C07D417/12
摘要： Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
摘要翻译： 与环双环稠合的环状羧酸或羧酸衍生物（如酰胺）的三环化合物（包括其药学上可接受的盐和前体药物）是G-蛋白偶联受体40（GPR40）的激动剂，可用作治疗性化合物，特别是在 2型糖尿病的治疗，以及经常与该疾病相关的病症，包括肥胖症和脂质疾病，例如混合或糖尿病性血脂异常，高脂血症，高胆固醇血症和高甘油三酯血症。
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公开(公告)号：US08039484B2
公开(公告)日：2011-10-18
申请号：US12441733
申请日：2007-10-26
申请人： Min Ge , Songnian Lin , Shawn P. Walsh , Lihu Yang , Changyou Zhou
发明人： Min Ge , Songnian Lin , Shawn P. Walsh , Lihu Yang , Changyou Zhou
IPC分类号： A61K31/47 , A61K31/192 , A61K31/277 , C07D487/02 , C07D217/24 , C07D213/36 , C07D209/34 , C07D311/34 , C07D333/56
CPC分类号： C07D333/60 , C07C59/72 , C07C59/90 , C07C235/46 , C07C255/54 , C07C2602/08 , C07C2602/10 , C07D207/34 , C07D209/34 , C07D209/46 , C07D213/61 , C07D215/233 , C07D217/24 , C07D307/80 , C07D311/58 , C07D333/48 , C07D405/12 , C07D487/04
摘要： Diaryl ethers in which one of the aryl groups is a phenyl fused to a cycloalkyl or heterocyclic ring, to which is attached an acetic acid group, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that often accompany this disease, including insulin resistance, obesity and lipid disorders.
摘要翻译： 其中一个芳基是与环烷基或杂环稠合的苯基，其中连接有乙酸基的二芳基醚是G-蛋白偶联受体40（GPR40）的激动剂，并且可用作治疗化合物，特别是在 治疗2型糖尿病以及经常伴随该疾病的病症，包括胰岛素抵抗，肥胖和脂质疾病。
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公开(公告)号：US20100105725A1
公开(公告)日：2010-04-29
申请号：US12441733
申请日：2007-10-26
申请人： Min Ge , Songnian Lin , Shawn P. Walsh , Lihu Yang , Changyou Zhou
发明人： Min Ge , Songnian Lin , Shawn P. Walsh , Lihu Yang , Changyou Zhou
IPC分类号： A61K31/47 , A61K31/192 , A61K31/277 , C07D487/02 , C07C255/52 , C07C59/84 , C07D217/24 , C07D213/36 , C07D209/34 , C07D311/34 , C07D333/56
CPC分类号： C07D333/60 , C07C59/72 , C07C59/90 , C07C235/46 , C07C255/54 , C07C2602/08 , C07C2602/10 , C07D207/34 , C07D209/34 , C07D209/46 , C07D213/61 , C07D215/233 , C07D217/24 , C07D307/80 , C07D311/58 , C07D333/48 , C07D405/12 , C07D487/04
摘要： Diaryl ethers in which one of the aryl groups is a phenyl fused to a cycloalkyl or heterocyclic ring, to which is attached an acetic acid group, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that often accompany this disease, including insulin resistance, obesity and lipid disorders.
摘要翻译： 其中一个芳基是与环烷基或杂环稠合的苯基，其中连接有乙酸基的二芳基醚是G-蛋白偶联受体40（GPR40）的激动剂，并且可用作治疗化合物，特别是在 治疗2型糖尿病以及经常伴随该疾病的病症，包括胰岛素抵抗，肥胖和脂质疾病。
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公开(公告)号：US07442808B2
公开(公告)日：2008-10-28
申请号：US11801841
申请日：2007-05-11
申请人： Min Ge , Jiafang He , Fiona Wai Yu Lau , Gui-Bai Liang , Songnian Lin , Weiguo Liu , Shawn P. Walsh , Lihu Yang
发明人： Min Ge , Jiafang He , Fiona Wai Yu Lau , Gui-Bai Liang , Songnian Lin , Weiguo Liu , Shawn P. Walsh , Lihu Yang
IPC分类号： C07D495/00 , C07D307/92 , C07D209/94 , C07D209/00 , C07C229/00 , C07C62/00 , A61K31/38 , A61K31/34 , A61K31/19 , A61K31/195 , A61K31/40
CPC分类号： C07D213/643 , C07C62/34 , C07C62/38 , C07C229/50 , C07C2603/08 , C07D307/93 , C07D311/94 , C07D333/78 , C07D405/04 , C07D407/12 , C07D413/12 , C07D417/12
摘要： Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
摘要翻译： 与环双环稠合的环状羧酸或羧酸衍生物（如酰胺）的三环化合物（包括其药学上可接受的盐和前体药物）是G-蛋白偶联受体40（GPR40）的激动剂，可用作治疗性化合物，特别是在 2型糖尿病的治疗，以及经常与该疾病相关的病症，包括肥胖症和脂质疾病，例如混合或糖尿病性血脂异常，高脂血症，高胆固醇血症和高甘油三酯血症。
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