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1. 发明授权

US5691373A Nonpeptide endothelin antagonists I 失效
标题翻译：非肽内皮素拮抗剂
公开(公告)号：US5691373A
公开(公告)日：1997-11-25
申请号：US384083
申请日：1995-02-06
申请人： Kent Alan Berryman , Annette Marian Doherty , Jeremy John Edmunds , William Chester Patt , Mark Stephen Plummer , Joseph Thomas Repine
发明人： Kent Alan Berryman , Annette Marian Doherty , Jeremy John Edmunds , William Chester Patt , Mark Stephen Plummer , Joseph Thomas Repine
IPC分类号： C07D317/60 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/54 , A61P3/08 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P37/00 , A61P43/00 , C07C45/41 , C07C45/71 , C07C45/74 , C07C47/11 , C07C47/235 , C07C47/575 , C07C49/813 , C07C49/84 , C07C59/90 , C07D307/60 , C07D333/32 , C07D405/04 , C07D405/06 , C07D405/14 , C07D407/04 , C07D407/06 , C07D407/14 , C07D409/04 , C07D409/14 , A61K31/36 , A61K31/535
CPC分类号： C07D405/04 , C07C45/41 , C07C45/71 , C07C45/74 , C07C47/11 , C07C47/235 , C07C47/575 , C07C49/813 , C07C49/84 , C07C59/90 , C07D307/60 , C07D405/06 , C07D405/14 , C07D407/04 , C07D407/06 , C07D407/14 , C07D409/04 , C07D409/14
摘要： Novel nonpeptide antagonists of endothelin I are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cerebral ischemia, cerebral infarction, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, stroke, benign prosthatic hyperplasia (BPH), and diabetes.
摘要翻译：描述了内皮素I的新型非肽拮抗剂，以及其制备方法及其药物组合物，其可用于治疗高水平的内皮素，急性和慢性肾衰竭，高血压，心肌梗死，心肌缺血，脑血管痉挛，脑缺血，脑梗死，肝硬化，败血性休克，充血性心力衰竭，内毒素性休克，蛛网膜下腔出血，心律失常，哮喘，先兆子痫，动脉粥样硬化疾病包括雷诺氏病和再狭窄，心绞痛，癌症，肺动脉高压，缺血性疾病，胃粘膜损伤，出血休克，缺血性肠病，中风，良性前列腺增生（BPH）和糖尿病。

2. 发明授权

US6017916A Nonpeptide endothelin antagonists I 失效
标题翻译：非肽内皮素拮抗剂
公开(公告)号：US6017916A
公开(公告)日：2000-01-25
申请号：US787423
申请日：1997-01-22
申请人： Kent Alan Berryman , Annette Marian Doherty , Jeremy John Edmunds , William Chester Patt , Mark Stephen Plummer , Joseph Thomas Repine
发明人： Kent Alan Berryman , Annette Marian Doherty , Jeremy John Edmunds , William Chester Patt , Mark Stephen Plummer , Joseph Thomas Repine
IPC分类号： C07D317/60 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/54 , A61P3/08 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P37/00 , A61P43/00 , C07C45/41 , C07C45/71 , C07C45/74 , C07C47/11 , C07C47/235 , C07C47/575 , C07C49/813 , C07C49/84 , C07C59/90 , C07D307/60 , C07D333/32 , C07D405/04 , C07D405/06 , C07D405/14 , C07D407/04 , C07D407/06 , C07D407/14 , C07D409/04 , C07D409/14 , A61K31/535 , A61K31/335
CPC分类号： C07D405/04 , C07C45/41 , C07C45/71 , C07C45/74 , C07C47/11 , C07C47/235 , C07C47/575 , C07C49/813 , C07C49/84 , C07C59/90 , C07D307/60 , C07D405/06 , C07D405/14 , C07D407/04 , C07D407/06 , C07D407/14 , C07D409/04 , C07D409/14
摘要： Novel nonpeptide antagonists of endothelin I are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cerebral ischemia, cerebral infarction, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, stroke, benign prosthatic hyperplasia (BPH), and diabetes.
摘要翻译：描述了内皮素I的新型非肽拮抗剂，以及其制备方法及其药物组合物，其可用于治疗高水平的内皮素，急性和慢性肾衰竭，高血压，心肌梗死，心肌缺血，脑血管痉挛，脑缺血，脑梗死，肝硬化，败血性休克，充血性心力衰竭，内毒素性休克，蛛网膜下腔出血，心律失常，哮喘，先兆子痫，动脉粥样硬化疾病包括雷诺氏病和再狭窄，心绞痛，癌症，肺动脉高压，缺血性疾病，胃粘膜损伤，出血休克，缺血性肠病，中风，良性前列腺增生（BPH）和糖尿病。

3. 发明授权

US5658943A Phenylalanine derivatives as endothelin antagonists 失效
标题翻译：苯丙氨酸衍生物作为内皮素拮抗剂
公开(公告)号：US5658943A
公开(公告)日：1997-08-19
申请号：US369209
申请日：1995-01-05
申请人： Kent Alan Berryman , Xue-Min Cheng , Annette Marian Doherty , Jeremy John Edmunds , Sylvester Klutchko
发明人： Kent Alan Berryman , Xue-Min Cheng , Annette Marian Doherty , Jeremy John Edmunds , Sylvester Klutchko
IPC分类号： C07C229/36 , C07C233/51 , C07C275/28 , C07C323/59 , C07D317/54 , C07D317/60 , C07C229/30 , C07C317/60
CPC分类号： C07C233/51 , C07C229/36 , C07C275/28 , C07C323/59 , C07D317/54 , C07D317/60 , C07C2101/08
摘要： Novel antagonists of endothelin are described, as well as novel intermediates used in their preparation, methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, essential, renovascular, malignant and pulmonary hypertension, cerebral infarction, myocardial ischemia, cerebral ischemia, congestire heart failure and subarachnoid hemorrhage.
摘要翻译：本文描述了内皮素的新型拮抗剂，以及其制备中使用的新型中间体，其制备方法及其药物组合物，其可用于治疗内皮素水平升高，必需，肾血管性，恶性和肺动脉高压，脑梗死，心肌缺血，脑缺血，充血性心力衰竭和蛛网膜下腔出血。

4. 发明授权

US06297274B1 Nonpeptide endothelin antagonists with increased water solubility 失效
标题翻译：具有增加的水溶性的非肽内皮素拮抗剂
公开(公告)号：US06297274B1
公开(公告)日：2001-10-02
申请号：US09117667
申请日：1998-08-04
申请人： Xue-Min Cheng , Annette Marian Doherty , William Chester Patt , Joseph Thomas Repine
发明人： Xue-Min Cheng , Annette Marian Doherty , William Chester Patt , Joseph Thomas Repine
IPC分类号： A61K3134
CPC分类号： C07D407/04 , C07D307/60
摘要： Novel nonpeptide endothelin I antagonists of Formula are described wherein R1 is unsubstituted or substituted cycloalkyl, phenyl, naphthyl or heteroaryl, R2 is unsubstituted or substituted alkyl, aryl or heteroaryl, R3 is unsubstituted or substituted alkyl, cycloalkyl, aryl or heteroayl, and R1 and/or R2 and/or R3 are independently substituted by a total of from 1 to 4 substituents which enhance aqueous solubility with the proviso that when R2 is alkyl and is substituted, the substituent is not oxygen at the &agr;-position of the furanone ring. Further described are methods for the preparation and pharmaceutical compositions of compounds of Formula I, which are useful in treating atherosclerosis, restenosis, Raynaud's phenomenon, mild or severe congestive heart failure, cerebral ischemia, cerebral infarction, embolic stroke, cerebral vasospasm, glaucoma, subarachnoid hemorrhage, hemorrhagic stroke, diabetes, gastric ulceration and mucosal damage, ischemic bowel disease, Chrohn's disease, male penile erectile dysfunction, essential or malignant hypertension, pulmonary hypertension, pulmonary hypertension after bypass, cancer, especially malignant hemangioendothelioma or prostate cancer, myocardial infarction or ischemia, acute or chronic renal failure, renal ischemia, radiocontrast-induced nephrotoxcity, endotoxic, septic hemorrhagic shock, angina, preeclampsia, asthma, arrhythmias, benign prostatic hyperplasia, and elevated levels of endothelin.
摘要翻译：苯基，萘基或杂芳基，R2为未取代或取代的烷基，芳基或杂芳基，R3为未取代或取代的烷基，环烷基，芳基或杂芳基，R1和/ 或R 2和/或R 3独立地被总共1至4个增强水溶性的取代基取代，条件是当R 2是烷基且被取代时，该取代基不是在呋喃酮环的α-位上的氧。进一步描述了用于制备治疗动脉粥样硬化，再狭窄，雷诺现象，轻度或重度充血性心力衰竭，脑缺血，脑梗死，栓塞性中风，脑血管痉挛，青光眼，蛛网膜下腔出血出血性，出血性中风，糖尿病，胃溃疡和粘膜损伤，缺血性肠病，克罗恩病，男性阴茎勃起功能障碍，基本或恶性高血压，肺动脉高压，旁路后肺动脉高压，癌症，特别是恶性血管内皮瘤或前列腺癌，心肌梗塞或缺血，急性或慢性肾衰竭，肾缺血，放射性对照诱导的肾毒性，内毒素性，败血性出血性休克，心绞痛，先兆子痫，哮喘，心律失常，良性前列腺增生和内皮素水平升高。

5. 发明授权

US6043241A Ketoacid endothelin antagonists 失效
标题翻译：酮酸内皮素拮抗剂
公开(公告)号：US6043241A
公开(公告)日：2000-03-28
申请号：US117575
申请日：1998-07-31
申请人： Xue-Min Cheng , Annette Marian Doherty , Timothy Robert Hurley , Michael James Lovdahl , William Chester Patt , Joseph Thomas Repine
发明人： Xue-Min Cheng , Annette Marian Doherty , Timothy Robert Hurley , Michael James Lovdahl , William Chester Patt , Joseph Thomas Repine
IPC分类号： C07C59/90 , C07D317/60 , A61K31/36 , C07D317/54
CPC分类号： C07C59/90 , C07D317/60
摘要： Compounds of the Formula I ##STR1## are nonpeptide antagonists of endothelin which are useful in treating a variety of diseasses such as elevated levels of endothelin, acute respiratory distress syndrome (ARDS), atherosclerosis, restenosis, Raynaud's phenomenon etc. The compounds are prepared by reacting an alpha-hydroxy butenolide with one or more equivalents of a suitable base, and exposing the solution to UV light.
摘要翻译： PCT No.PCT / US97 / 03959 Sec。 371日期：1998年7月31日 102（e）日期1998年7月31日PCT 1997年3月12日PCT PCT。出版物WO97 / 37987 日期1997年10月16日式I化合物是内皮素的非肽拮抗剂，其可用于治疗各种疾病，例如内皮素水平升高，急性呼吸窘迫综合征（ARDS），动脉粥样硬化，再狭窄，雷诺现象等。通过使α-羟基丁烯内酯与一种或多种当量的合适的碱反应制备，并将溶液暴露于UV光下。

6. 发明授权

US6133263A Endothelin antagonists with ether-linked groups 失效
标题翻译：具有醚连接基团的内皮素拮抗剂
公开(公告)号：US6133263A
公开(公告)日：2000-10-17
申请号：US117649
申请日：1998-08-03
申请人： Xue-Min Cheng , Annette Marian Doherty , William Chester Patt , Joseph Thomas Repine
发明人： Xue-Min Cheng , Annette Marian Doherty , William Chester Patt , Joseph Thomas Repine
IPC分类号： C07D307/60 , C07D407/04 , A61K31/365 , A61K31/535 , C07D407/02 , C07D413/14
CPC分类号： C07D407/04 , C07D307/60
摘要： Novel nonpeptide endothelin antagonists with ether-linked groups are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating atherosclerosis, restenosis, Raynaud's phenomenon, mild or severe congestive heart failure, cerebral ischemia, cerebral infarction, embolic stroke, cerebral vasospasm, subarachnoid hemorrhage, hemorrhagic stroke, diabetes, gastric ulceration and mucosal damage, ischemnic bowel disease, Chrohn's disease, essential or malignant hypertension, pulmonary hypertension, pulmonary hypertension after bypass, acute respiratory distress syndrome, chronic obstructive pulmonary diseases, male penile erectile dysfunction, cancer, especially malignant hemangicendothelioma or prostate cancer, myocardial infarction or ischemia, acute or chronic renal failure, renal ischemia, radiocontrast-induced nepbrotoxicity, endotoxic, septic, hemorrhagic shock, angina, preeclampsia, asthma, arhythmias, benign prostatic hyperplasia, and elevated levels of endothelin.
摘要翻译： PCT No.PCT / US97 / 03930 Sec。 371日期1998年8月3日 102（e）日期1998年8月3日PCT 1997年3月12日PCT公布。公开号WO97 / 37986 日期1997年10月16日描述了具有醚连接基团的新型非肽内皮素拮抗剂以及其制备方法及其药物组合物，其可用于治疗动脉粥样硬化，再狭窄，雷诺现象，轻度或严重充血性心力衰竭，脑缺血，脑梗死，栓塞性中风，脑血管痉挛，蛛网膜下腔出血，出血性卒中，糖尿病，胃溃疡和粘膜损伤，缺血性肠病，克罗恩病，基本或恶性高血压，肺动脉高压，旁路后肺动脉高压，急性呼吸窘迫综合征慢性阻塞性肺疾病，男性阴茎勃起功能障碍，癌症，特别是恶性血管内皮瘤或前列腺癌，心肌梗死或局部缺血，急性或慢性肾功能衰竭，肾缺血，放射性对照诱导的中毒，内毒素，败血症，出血性休克，心绞痛，先兆子痫，哮喘，心律失常，beni 前列腺增生，内皮素水平升高。

7. 发明授权

US5998468A Furanone endothelin antagonists 失效
标题翻译：呋喃酮内皮素拮抗剂
公开(公告)号：US5998468A
公开(公告)日：1999-12-07
申请号：US983554
申请日：1997-12-15
申请人： Xue-Min Cheng , Annette Marian Doherty , William Chester Patt , Joseph Thomas Repine
发明人： Xue-Min Cheng , Annette Marian Doherty , William Chester Patt , Joseph Thomas Repine
IPC分类号： C07D307/58 , C07D407/04 , A61K31/335 , C07D305/12
CPC分类号： C07D407/04 , C07D307/58
摘要： Novel nonpeptide antagonists of endothelin (I) are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cerebral ischemia, cerebral infarction, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, stroke, benign prostatic hyperplasia (BPH), and diabetes.
摘要翻译： PCT No.PCT / US96 / 12431 Sec。 371 1997年12月15日第 102（e）日期1997年12月15日PCT提交1996年7月29日PCT公布。公开号WO97 / 08169 日期1997年3月6日描述了内皮素（I）的新型非肽拮抗剂，以及其制备方法及其药物组合物，其可用于治疗高水平的内皮素，急性和慢性肾衰竭，高血压，心肌梗死，心肌缺血，脑血管痉挛，脑缺血，脑梗死，肝硬化，脓毒性休克，充血性心力衰竭，内毒素性休克，蛛网膜下腔出血，心律失常，哮喘，先兆子痫，动脉粥样硬化疾病包括雷诺氏病和再狭窄，心绞痛，癌症，肺动脉高压，缺血疾病，胃粘膜损伤，出血性休克，缺血性肠病，中风，良性前列腺增生（BPH）和糖尿病。

8. 发明授权

US06545150B2 Certain benzothiazine dioxide endothelin antagonists and processes for their preparation 失效
标题翻译：某些苯并噻嗪二氧化物内皮素拮抗剂及其制备方法
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。

9. 发明授权

US06265399B1 Certain benzothiazine dioxide endothelin antagonists and processes for their preparation 失效
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.

10. 发明授权

US06440962B2 Certain benzothiazine dioxide endothelin antagonists and processes for their preparation 失效
标题翻译：某些苯并噻嗪二氧化物内皮素拮抗剂及其制备方法
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。

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