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    • 1. 发明申请
    • KETOACID ENDOTHELIN ANTAGONISTS
    • KETOACID内皮素拮抗剂
    • WO1997037987A1
    • 1997-10-16
    • PCT/US1997003959
    • 1997-03-12
    • WARNER-LAMBERT COMPANYCHENG, Xue-MinDOHERTY, Annette, MarianHURLEY, Timothy, RobertLOVDAHL, Michael, JamesPATT, William, ChesterREPINE, Joseph, Thomas
    • WARNER-LAMBERT COMPANY
    • C07D317/60
    • C07C59/90C07D317/60
    • 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 acute respiratory distress syndrome (ARDS), atherosclerosis, restenosis, Raynaud's phenomenon, chronic obstructive pulmonary diseases, 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, essential or malignant hypertension, pulmonary hypertension, pulmonary hypertension after bypass, male penile erectile dysfunction, cancer, especially malignant hemangioendothelioma or prostate cancer, myocardial infarction or ischemia, acute or chronic renal failure, renal ischemia, radiocontrast-induced nephrotoxicity, endotoxic, septic, hemorrhagic shock, angina, preeclampsia, asthma, arrhythmias, benign prostatic hyperplasia, and elevated levels or endothelin.
    • 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,其可用于治疗急性呼吸窘迫综合征(ARDS),动脉粥样硬化,再狭窄,雷诺现象,慢性阻塞性肺疾病,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,青光眼,蛛网膜下腔出血,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,基本或恶性高血压,肺动脉高压,肺动脉高压 旁路后,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,心肌梗塞或局部缺血,急性或慢性肾衰竭,肾脏缺血,放射性对照诱导的肾毒性,内毒素,败血症,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 sia和升高的水平或内皮素。