Benzoxazepine-2-one compounds and their use

Details Benzoxazepine-2-one compounds and their use Benzoxazepine-2-one compounds and their use

1996-08-13

1997-10-14

Berch, Mark L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

540490, 549549, A61K 3155, C07D26714, C07D30348, A01N 4372

Patent

active

056772980

ABSTRACT:
Disclosed is a squalene synthetase inhibitor which comprises the compound represented by the formula (I) ##STR1## wherein R.sub.1 stands for H or an optionally substituted hydrocarbon group; R.sub.2 and R.sub.3 independently stand for H, an optionally substituted alkyl group, an optionally substituted phenyl group or an optionally substituted aromatic heterocyclic group; Z stands for a carbon chain containing a double bond or --Z'--C(OH)-- (Z' stands for a bond or a straight-chain or branched alkylene chain); the symbol ......... stands for a double bond or a single bond; Y stands for an optionally esterified carboxyl group, an optionally substituted carbamoyl group, an optionally substituted hydroxyl group, an optionally substituted amino group or an optionally substituted heterocyclic radical having a protonizable hydrogen; X stands for O or S; G stands for O or S; and the ring A is optionally substituted, or a pharmaceutically acceptable salt thereof, and which is useful for the prophylaxis or therapy of hypercholesteremia or coronary sclerosis of mammals.

REFERENCES:
Biller J. Medicinal Chemistry 31, 1869-1871 (1988), "Isoprenoid (Phosphinylmethyl)phosphonates as Inhibitors of Squalene Synthetase".
Masuoka Chem. Pharm. Bull. 34, 140-149(1986), "Synthesis of Medium-Sized Heterocycles Using an Interamolecular Michael Reaction".
Baxter, J. Biol. Chem 268, 24832 (1993).
Hoeg, T.A.M.A. 258 3532 (1987).

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