Seco-mevinic acid derivatives useful as antihypercholesterolemic

Details Seco-mevinic acid derivatives useful as antihypercholesterolemic Seco-mevinic acid derivatives useful as antihypercholesterolemic

1989-09-28

1991-06-18

Shippen, Michael L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514336, 514357, 514438, 514444, 514460, 514461, 514471, 514529, 514530, 514532, 514544, 514550, 514552, 514562, 514563, 260404, 260410, 546268, 546336, 546342, 549 60, 549 76, 549 79, 549292, 549500, 558413, 558414, 558415, 558416, 560 1, 560 9, 560 11, 560 12, 560 17, 560 20, 560 21, 560 42, 560 52, 560 5, 560 65, 560 72, 560 75, 560102, 560105, 560106, 560107, 560122, 560123, 560124, 560125, 560126, 560127, 560150, 560152, 560185, 560187, 560188, 560193, 560194, 560228, 560231, 560255, 562451, 562500,

Patent

active

050250175

ABSTRACT:
Seco-mevinic acid derivatives are provided which has the structure ##STR1## including all stereoisomers thereof, wherein Z is ##STR2## R is H, alkali metal or lower alkyl, R.sup.1 is H, lower alkyl, aryl, lower alkoxy, cycloalkyl, heteroaryl, aralkyl, heteroaralkyl or heterocyclic; R.sup.2 is lower alkyl, cycloalkyl or aralkyl, and X is O or NR.sup.5 wherein R.sup.5 is H or lower alkyl, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis. New intermediates for preparing the above seco-mevinic acid derivatives are also provided.

REFERENCES:
patent: 3983140 (1976-09-01), Endo et al.
patent: 4049495 (1977-09-01), Endo et al.
patent: 4137322 (1979-01-01), Endo et al.
patent: 4375475 (1983-03-01), Willard et al.
patent: 4873345 (1989-10-01), Duggan
Tetrahedron Letters, vol. 29, No. 8, 929-930, 1988.
C. H. Heathcock et al., "Synthesis and Biological Evaluation of a Monocyclic, Fully Functional Analogue of Compactin," J. Med. Chem. 1989, 32, 197.

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