Compounds of formulas I-X and other mevinolin derivatives are known to inhibit the biosynthesis of cholesterol and thus are useful for their antihypercholesterolemic activity. (see U.S. Pat. No. 4,444,784 issued to Hoffman et al on Apr. 24, 1984 and U.S. Pat. No. 4,450,171 issued to Hoffman et al on May 22, 1984). The compounds of formula I-X may be isolated from the microfungus of the genus Aspergillus as described in U.S. Pat. Nos. 4,231,938 issued to Monaghan et al on Nov. 4, 1980 and U.S. Pat. No. 4,294,926 issued to Monaghan et al on Oct. 13, 1981.
The most active member of this group of natural compounds in inhibiting cholesterol biosynthesis has a mevinolin structure. (see U.S. Pat. No. 4,450,171, col. 1., lines 43-51; also see U.S. Pat. Nos. 4,444,784; 4,293,496; 4,450,171; 4,582,915; 4,231,938; 4,294,926; and 4,668,699 hereby incorporated by reference). As antihypercholesterolemic agents, these known compounds may be administered orally or parenterally, although the oral route is generally desirable. Moreover, the known compounds have been found to be useful as anti-fungal agents which may be sprayed or dusted on plants to be protected. (see U.S. Pat. No. 4,450,171, col. 12, lines 45-66).
USPTO Backgrounds
USPTO Backgrounds