Hydroxyphosphinyl phosphonate squalene synthetase inhibitors and

Details Hydroxyphosphinyl phosphonate squalene synthetase inhibitors and Hydroxyphosphinyl phosphonate squalene synthetase inhibitors and

1992-09-25

1993-10-19

Lee, Mary C.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Phosphorus containing other than solely as part of an...

514 39, 514 54, 514108, 558155, 558161, 562 21, A61K 3166, C07F 948

Patent

active

052545440

ABSTRACT:
Hydroxyphosphinyl phosphonate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.2, R.sup.3 and R.sup.4 are independently H, alkyl, metal ion or a prodrug ester; and R.sup.1 is a lipophilic group which contains at least 6 carbons and is alkyl, alkenyl, alkynyl, mixed alkenylalkynyl, a hetero-containing moiety as defined herein, or a phenylalkyl or phenylalkenyl group including those containing a biphenyl group.

REFERENCES:
patent: 4871721 (1989-10-01), Biller
Prischenko et al, Zh. Obsch. Khim, 1977, 47, 2689-2698.

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