Mevalonolactone derivatives

Details Mevalonolactone derivatives Mevalonolactone derivatives

1978-05-08

1980-04-15

Milestone, Norma S.

Drug, bio-affecting and body treating compositions

Nonspecific immunoeffector, per se ; or nonspecific...

Synthetic or structurally-modified peptidoglycan or...

542413, 542441, 2603435, A61K 31365, C07D30930

Patent

active

041984250

ABSTRACT:
This invention concerns novel mevalonolactone derivatives having the formula ##STR1## wherein A represents a direct linkage, methylene, ethylene, trimethylene or vinylene group; R.sup.1 represents hydrogen atom, or an aliphatic acyl group, benzoyl group, or a benzoyl group substituted with hydroxy, lower alkoxy, aliphatic acyloxy or halogen; R.sup.2 represents hydrogen atom, a halogen atom or methyl group; and R.sup.3, R.sup.4 and R.sup.5 are same or different and each represents hydrogen atom, a halogen atom, a lower alkyl group with or without halogen as the substituent, phenyl group, or a phenyl group substituted with halogen, lower alkoxy, aliphatic acyloxy or lower alkyl with or without halogen, or a group represented by the formula R.sup.6 O-- (in the formula, R.sup.6 means hydrogen atom, an aliphatic acyl group, benzoyl group, phenyl group, a phenylalkyl group, cinnamyl group, or a group of benzoyl, phenyl, phenylalkyl or cinnamyl in all of which the aromatic ring is substituted with hydroxy, halogen, lower alkoxy, aliphatic acyloxy or lower alkyl with or without halogen as the substituent, or a lower alkyl group with or without halogen as the substituent).
The compounds are useful for the treatment of hyperlipidemia.
They may be prepared by halo-lactonizing the corresponding .gamma.,.delta.-unsaturated carboxylic acid derivatives and optionally dehalogenating the resulting product, or lactonizing the corresponding .delta.-hydroxy-carboxylic acid derivatives.

REFERENCES:
patent: 3075997 (1963-01-01), Tschesche et al.
patent: 3119842 (1964-01-01), Hulcher et al.
patent: 3522245 (1970-07-01), Brinkhoff
patent: 3600403 (1971-08-01), Brinkhoff
patent: 3983140 (1976-09-01), Endo et al.,
M. F. Ansell et al., J. Chem. Soc. (1961) (1), 206-212.
F. H. Hulcher, Archives of Biochemistry and Biophysics, vol. 146 (1971) _pp. 422-427.
F. M. Singer et al., Proc. Soc. Exp. Biol. and Med., vol. 102, Nov. 1959, pp. 370-373.

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