Phenol derivatives, pharmaceutical compositions containing these

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai

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514548, 514719, 514720, 514729, 514733, 560130, 560138, 560144, 560146, 568645, 568646, 568649, 568650, 568652, 568662, 568764, 568765, 568766, C07C 5742, C07C 69108

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active

049593919

ABSTRACT:
Phenol derivatives of the formula ##STR1## wherein A and B have the same or different meanings and each represent one of the groups --C.tbd.C--, cis--CH.dbd.CH-- or trans--CH.dbd.CH--, R.sub.1 is hydrogen, an optionally substituted alkyl or phenyl group or a cycloalkyl group, R.sub.2 is hydrogen, methyl or ethyl, R.sub.3 represents hydrogen, acetyl or propionyl, R.sub.4 has the same meaning as R.sub.3 or represents an alkyl group, R.sub.5 is a carboxylic or a hydroxy group or a functional derivative of such groups or R.sub.5 is a nitrile group and R.sub.6 is hydrogen, an alkyl group or the group OR.sub.4 which specifically inhibit 5-lipoxygenase and are useful in pharmaceutical compositions for prophylaxis and treatment of diseases due to the action of leukotrienes. The compounds are prepared by reacting suitable acetylene compounds or metal derivatives thereof with alkyl or aryl halides or by means of Wittig reactions optionally followed by transforming the member R.sub.5 into another carboxylic acid derivative. By hydrogenation A and B may be varied within the scope of the definition.

REFERENCES:
patent: 4432906 (1984-02-01), Cohen et al.
patent: 4564476 (1986-01-01), Ho
patent: 4733002 (1988-03-01), Yokoyama et al.
patent: 4801735 (1989-01-01), Finch et al.
Burger; Medicinal Chemistry, 2nd Edition; pp. 564-571, (1960).
Corey et al., Journal of the American Chemical Society, vol. 104, No. 6, pp. 1750-1754 (1982).
Jakschik et al., Biochem. and Biophys. Res. Comm., vol. 102, No. 2, pp. 624-629 (1981).
Pfister et al., J. Med. Chem., vol. 26, pp. 1099-1103 (1983).

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