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    Nonpeptide endothelin antagonists with increased water solubility
    1.
    发明授权
    Nonpeptide endothelin antagonists with increased water solubility 失效
    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。

    Endothelin antagonists with ether-linked groups
    3.
    发明授权
    Endothelin antagonists with ether-linked groups 失效
    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。

    Furanone endothelin antagonists
    4.
    发明授权
    Furanone endothelin antagonists 失效
    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。