Endothelin antagonists

Organic compounds -- part of the class 532-570 series – Organic compounds – Four or more ring nitrogens in the bicyclo ring system

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5462791, 548125, 548132, 548253, 5482662, 5482666, 548412, 548413, 548517, 548518, 548525, 548526, 548531, 548541, 548543, 548544, 548556, 548557, 548566, 548567, 548570, 548571, 548572, 548577, C07D40514

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active

057314349

ABSTRACT:
A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.

REFERENCES:
patent: 3342833 (1967-09-01), Fremery
patent: 4340715 (1982-07-01), Gounder et al.
Tsuge, et al., Chemistry Letters, 801-804 (1984).
Tsuge, et al., Bull Chem. Soc. Jpn., 59:2537 (1986).
Bhagwat, S., "Synthesis of Enantiomerically Pure Pyrrolidinones as Endothelin Receptor Antagonists", Tetrahedron Letters, 37(27):4627-4630, 1986.
Winn, et al., "2,4-Diarylpyrrolidine-3-carboxylic Acids-Potent ET.sub.A Selective Endothelin Receptor Antagonists." 1. Discovery of A-127722, 1984.
CA 119: 258811 Preparation of . . . A2 antagonists, Lavielle et al, 1993.
CA74:41752t Conformation of . . . Piperidinols. Settimj et al., 1974.

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