POLYPEPTIDE HAVING TERMINAL SUBSTITUTED BY AN ALPHA-SUBSTITUTED ACETIC ACID, THE SUBSTITUENT BEING A XANTHENE, THIOXANTHENE OR DIBENZOCYCLOHEPTENE DERIVATIVE

摘要

Novel antagonists of endothelin 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, metabolic, endocrinological, neurological disorders, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease, restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, and diabetes. In the claimed new compounds, the N-terminal 16-His is replaced by a building-block of formula ( alpha ).