Hydroxyphosphinyl phosphonate squalene synthetase inhibitors and method
US5254544A · kind A · utility
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18Claims
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Key dates
| Filing date | Sep 25, 1992 |
| Grant date | Oct 19, 1993 |
| Priority date | — |
| Expiry date | Sep 25, 2012 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07F9/4816
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.