Multicyclic tertiary amine polyaromatic squalene syntase inhibit

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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546133, 546137, A61K 31435, C07D45302

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active

054949181

ABSTRACT:
This invention relates to polycyclic compounds containing two mono- and/or bicyclic rings and a basic tertiary amino group capable of forming an ammonium ion at biological pH and which reduces levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.

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Poulter, C. D., et al., "Squalene Synthetase. Inhibition by an Ammonium Analogue of a Carbocationic Intermediate in the Conversion of Presqualene Pyrophosphate to Squalene," J. Am. Chem. Soc., vol. 104, No. 25, pp. 7376-7378 (1982).
Poulter, C. D., et al., "Squalene Synthetase. Inhibition by Ammonium Analogues of Carbocationic Intermediates in the Conversion of Presqualene Diphosphate to Squalene," J. Am. Chem. Soc., vol. III, No. 10, pp. 3734-3739 (1989).
Biller, S. A., et al., "Isoprenoid (Phosphenylmethyl)-phosphonates as Inhibitors of Squalene Synthetase," J. Med. Chem., vol. 31, No. 10, pp. 1869-1871 (1988).

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