公开(公告)号：US5773444A

公开(公告)日：1998-06-30

申请号：US837176

申请日：1997-04-14

申请人： Kyunghye Ahn ,  Xue-Min Cheng ,  Annette Marian Doherty ,  Edward Faith Elslager ,  Brian Kornberg ,  Chitase Lee ,  Daniele Leonard ,  Sham Nikam ,  Leslie Morton Werbel

发明人： Kyunghye Ahn ,  Xue-Min Cheng ,  Annette Marian Doherty ,  Edward Faith Elslager ,  Brian Kornberg ,  Chitase Lee ,  Daniele Leonard ,  Sham Nikam ,  Leslie Morton Werbel

IPC分类号： C07D239/74 ,  A61K31/505 ,  A61K31/517 ,  A61P43/00 ,  C07D239/90 ,  C07D239/91 ,  C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  C07D453/02 ,  A61K31/495 ,  A61K31/535

CPC分类号： C07D401/12 ,  C07D239/94 ,  C07D403/12 ,  C07D453/02

摘要： Novel quinazoline inhibitors of endothelin converting enzyme are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin and in controlling hypertension, myocardial infarction and ischemia, metabolic, endocrinological, and neurological disorders, congestive heart failure, endotoxic and hemorrhagic shock, septic shock, subarachnoid hemorrhage, arrhythmias, asthma, acute and chronic renal failure, cyclosporin-A induced nephrotoxicity, angina, gastric mucosal damage, ischemic bowel disease, cancer, pulmonary hypertension, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, cerebral ischemia and vasospasm, and diabetes.

摘要翻译： 描述了内皮素转化酶的新型喹唑啉抑制剂，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和控制高血压，心肌梗死和缺血，代谢，内分泌和神经障碍 ，充血性心力衰竭，内毒素性和出血性休克，败血性休克，蛛网膜下腔出血，心律失常，哮喘，急性和慢性肾功能衰竭，环孢菌素A诱导的肾毒性，心绞痛，胃粘膜损伤，缺血性肠病，癌症，肺动脉高压，先兆子痫，动脉粥样硬化 疾病包括雷诺氏病和再狭窄，脑缺血和血管痉挛以及糖尿病。

公开(公告)号：US5658902A

公开(公告)日：1997-08-19

申请号：US363104

申请日：1994-12-22

申请人： Kyunghye Ahn ,  Xue-Min Cheng ,  Annette Marian Doherty ,  Edward Faith Elslager ,  Brian Kornberg ,  Chitase Lee ,  Daniele Leonard ,  Sham Nikam ,  Leslie Morton Werbel

发明人： Kyunghye Ahn ,  Xue-Min Cheng ,  Annette Marian Doherty ,  Edward Faith Elslager ,  Brian Kornberg ,  Chitase Lee ,  Daniele Leonard ,  Sham Nikam ,  Leslie Morton Werbel

IPC分类号： C07D239/74 ,  A61K31/505 ,  A61K31/517 ,  A61P43/00 ,  C07D239/90 ,  C07D239/91 ,  C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  C07D453/02 ,  C07D405/12

CPC分类号： C07D401/12 ,  C07D239/94 ,  C07D403/12 ,  C07D453/02

摘要： Novel quinazoline inhibitors of endothelin converting enzyme are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin and in controlling hypertension, myocardial infarction and ischemia, metabolic, endocrinological, and neurological disorders, congestive heart failure, endotoxic and hemorrhagic shock, septic shock, subarachnoid hemorrhage, arrhythmias, asthma, acute and chronic renal failure, cyclosporin-A induced nephrotoxicity, angina, gastric mucosal damage, ischemic bowel disease, cancer, pulmonary hypertension, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, cerebral ischemia and vasospasm, and diabetes.

摘要翻译： 描述了内皮素转化酶的新型喹唑啉抑制剂，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和控制高血压，心肌梗死和缺血，代谢，内分泌和神经障碍 ，充血性心力衰竭，内毒素性和出血性休克，败血性休克，蛛网膜下腔出血，心律失常，哮喘，急性和慢性肾功能衰竭，环孢菌素A诱导的肾毒性，心绞痛，胃粘膜损伤，缺血性肠病，癌症，肺动脉高压，先兆子痫，动脉粥样硬化 疾病包括雷诺氏病和再狭窄，脑缺血和血管痉挛以及糖尿病。