公开(公告)号：US06545150B2

公开(公告)日：2003-04-08

申请号：US10006589

申请日：2001-12-05

申请人： Amy Mae Bunker ,  Xue-Min Cheng ,  Annette Marian Doherty ,  Jeremy John Edmunds ,  Gerald David Kanter ,  Chitase Lee ,  Joseph Thomas Repine ,  Richard William Skeean

发明人： Amy Mae Bunker ,  Xue-Min Cheng ,  Annette Marian Doherty ,  Jeremy John Edmunds ,  Gerald David Kanter ,  Chitase Lee ,  Joseph Thomas Repine ,  Richard William Skeean

IPC分类号： C07D27916

CPC分类号： C07D417/04 ,  C07C303/40 ,  C07D279/02 ,  C07D417/10 ,  C07C311/21

摘要： The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula 1 The compounds are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.

摘要翻译： 本发明是一系列苯并噻嗪二氧化物或其药学上可接受的盐，其是具有深度体外活性的有效的内皮素A拮抗剂，以及式1的改进的合成。该化合物可用于治疗升高的内皮素水平，必需的血管性恶性和 肺动脉高压，脑梗塞，脑缺血，充血性心力衰竭和蛛网膜下腔出血。

公开(公告)号：US06265399B1

公开(公告)日：2001-07-24

申请号：US09445504

申请日：1999-12-08

申请人： Amy Mae Bunker ,  Xue-Min Cheng ,  Annette Marian Doherty ,  Jeremy John Edmunds ,  Gerald David Kanter ,  Chitase Lee ,  Joseph Thomas Repine ,  Richard William Skeean

发明人： Amy Mae Bunker ,  Xue-Min Cheng ,  Annette Marian Doherty ,  Jeremy John Edmunds ,  Gerald David Kanter ,  Chitase Lee ,  Joseph Thomas Repine ,  Richard William Skeean

IPC分类号： C07D27902

CPC分类号： C07D417/04 ,  C07C303/40 ,  C07D279/02 ,  C07D417/10 ,  C07C311/21

摘要： The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula 1 The compounds are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.

公开(公告)号：US06440962B2

公开(公告)日：2002-08-27

申请号：US09818394

申请日：2001-03-27

申请人： Amy Mae Bunker ,  Xue-Min Cheng ,  Annette Marian Doherty ,  Jeremy John Edmunds ,  Gerald David Kanter ,  Chitase Lee ,  Joseph Thomas Repine ,  Richard William Skeean

发明人： Amy Mae Bunker ,  Xue-Min Cheng ,  Annette Marian Doherty ,  Jeremy John Edmunds ,  Gerald David Kanter ,  Chitase Lee ,  Joseph Thomas Repine ,  Richard William Skeean

IPC分类号： C07D27902

CPC分类号： C07D417/04 ,  C07C303/40 ,  C07D279/02 ,  C07D417/10 ,  C07C311/21

摘要： The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula I The compounds are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.

摘要翻译： 本发明是一系列苯并噻嗪二氧化物或其药学上可接受的盐，其是具有深度体外活性的有效的内皮素A拮抗剂，并且对于式It化合物的改进的合成可用于治疗升高的内皮素水平，必需的血管性恶性和 肺动脉高压，脑梗塞，脑缺血，充血性心力衰竭和蛛网膜下腔出血。

公开(公告)号：US06252070B1

公开(公告)日：2001-06-26

申请号：US09633720

申请日：2000-08-07

申请人： Amy Mae Bunker ,  Xue-Min Cheng ,  Annette Marian Doherty ,  Jeremy John Edmunds ,  Gerald David Kanter ,  Chitase Lee ,  Joseph Thomas Repine ,  Richard William Skeean

发明人： Amy Mae Bunker ,  Xue-Min Cheng ,  Annette Marian Doherty ,  Jeremy John Edmunds ,  Gerald David Kanter ,  Chitase Lee ,  Joseph Thomas Repine ,  Richard William Skeean

IPC分类号： C07D27916

CPC分类号： C07D417/04 ,  C07C303/40 ,  C07D279/02 ,  C07D417/10 ,  C07C311/21

摘要： The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula 1 The compounds are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.

摘要翻译： 本发明是一系列苯并噻嗪二氧化物或其药学上可接受的盐，其是具有深度体外活性的有效的内皮素A拮抗剂，以及式1的改进的合成。该化合物可用于治疗升高的内皮素水平，必需的血管性恶性和 肺动脉高压，脑梗塞，脑缺血，充血性心力衰竭和蛛网膜下腔出血。