2-substituted coumaran derivatives

Details 2-substituted coumaran derivatives 2-substituted coumaran derivatives

1989-06-09

1990-10-30

Ford, John M.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

540596, 544298, 546137, 546153, 546191, 546196, 546256, 549462, 549458, 549467, 549470, 548182, 548336, 548454, 548525, C07D30779

Patent

active

049669737

ABSTRACT:
The present invention relates to a compound of the formula ##STR1## wherein R.sup.1 stands for hydrogen or a lower alkyl; n denotes an integer of 1 to 6; X stands for an optionally oxidized sulphur atom, oxygen atom or an optionally substituted imino; R.sup.2 stands for methyl or an organic residual group bonded through methylene, methine a quaternary carbon; R.sup.3 stands for a lower alkyl; R.sup.4 stands for hydrogen or acyl; R.sup.5 and R.sup.6 each stand for a lower alkoxy or a lower alkyl, or R.sup.5 and R.sup.6 combinedly stand for butadienylene, and salts thereof.
The compound (I) of the present invention has a strong 5-lipoxygenase inhibiting action, is of high safety and is useful as, among others, an agent for ameliorating dysfunction of circulatory system, an anti-allergic agent and a pharmaceutical agent for central nervous system.

REFERENCES:
patent: 4857516 (1989-08-01), Terao et al.
CPI Abstract 4854619 WPI Acc. No. 88-145145/21, Abstract of JP-A-88173/1988.
Burton, Graham W., et al., "Antioxidant Activity of Phenols Related to Vitamin E. Are There Chain-Breaking Antioxidants Better than .alpha.-Tocopherol?", J. Am. Chem. Soc., vol. 105, pp. 5950-5951 (1983).
Burton, Graham W. et al., "Autoxidation of Biological Molecules. 4. Maximizing the Antioxidant Activity of Phenols", J. Am. Chem. Soc., vol. 107, pp. 7053-7065 (1985).
Okamoto, Kayoko et al., "Synthesis of Quinones having Carboxy- and Hydroxy-Alkyl Side Chains, and their Effects on Rat-Liver Lysosomal Membrane", Chem. Pharm. Bull., vol. 30, No. 8, pp. 2797-2819 (1982).
Yutaka Maruyama et al., "5-Lipoxygenase Inhibitors for the Treatment of Inflammation and Allergy", Chemical Abstracts, vol. 108, Mar. 7, 1988, p. 445, Abstract No. 82107a.
Katsuji Ejiri et al., "Dihydrobenzofuran Derivatives as Antioxidants and Drug Intermediates", Chemical Abstracts, vol. 100, No. 9, Feb. 27, 1989, p. 630, Abstract No. 75294x.

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