Endothelin antagonists ii

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 14/575 (2006.01) A61K 38/08 (2006.01) A61K 38/22 (2006.01) C07K 7/06 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2190756

Novel antagonists of endotholin containing an N-terminal fragment (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, metabolic, endocrinological, neurological disorders especially cerebral vasospasm, stroke, and head injury, 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.

La présente invention concerne des antagonistes de l'endothéline contenant un fragment d'extrémité N représenté par la formule (I). L'invention concerne également des procédés de préparation et des compositions pharmaceutiques à base de ladite substance, utilisées pour le traitement des taux élevés d'endothéline, de l'insuffisance rénale aiguë ou chronique, de l'hypertension, de l'infarctus du myocarde, des troubles métaboliques, endocriniens, neurologiques, et particulièrement les vasospasmes cérébraux et l'ictus cérébral, des traumatismes crâniens, de l'insuffisance cardiaque oedémateuse, du choc endotoxinique, de l'hémorragie sous-arachnoïdienne, des arythmies, de la prééclampsie, des troubles athéroscléreux (y compris la maladie de Raynaud), de la resténose, de l'angine de poitrine, du cancer, de l'hypertension artérielle pulmonaire, des affections à étiologie ischémique, des lésions de la muqueuse gastrique, du choc hémorragique, des affections intestinales à étiologie ischémique, et du diabète.

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