Endothelin receptor antagonists isolated from microbispora

C - Chemistry – Metallurgy – 12 – P

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C12P 21/00 (2006.01) A61K 38/15 (2006.01) C07K 7/06 (2006.01) C07K 11/02 (2006.01) C12N 1/20 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2059380

0499H 18285 TITLE OF THE INVENTION NOVEL ENDOTHELIN RECEPTOR ANTAGONISTS ISOLATED FROM MICROBISPORA ABSTRACT OF THE DISCLOSURE Novel cyclic depsipeptides derived from a culture of Microbispora are receptor antagonists of endothelin, a potent vasoconstrictor, and are thus useful in treating cardiovascular disorders. Endothenlin has also other physiological effects, and the endothenlin receptor antagonists of the present invention thus have also other therapeutic uses. The compounds are cyclic depsipeptides of N-(pyrrol-2-carboxy) - L-Phe, D-allo-Thr, D-Phe, D-Ala, D- or L-dihydroxyphenyl-Gly, and D-dihydroxyphenyl-Gly.

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