Phenolic thioethers as inhibitors of 5-lipoxygenase

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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514532, 514539, 514548, 514562, 514570, 514571, 548252, 560 11, 560 12, 560 17, 560138, 560141, 562429, 562430, 562431, C07C14940, A61K 3710

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active

047119039

ABSTRACT:
The compounds of the present invention comprise substituted phenolic thioethers represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different and independently represent tert-alkyl or phenyl; A represents methylene or methylene substituted by alkyl, dialkyl or hydroxy, provided that when A includes hydroxymethylene, the hydroxymethylene group is not adjacent to a heteroatom; B represents sulfur, sulfoxide, sulfone, oxygen, --NH-- or nitrogen substituted by alkyl, phenyl, benzyl, substituted phenyl or substituted benzyl; C represents methylene or methylene substituted by alkyl; R.sub.3 represents CO.sub.2 H, CO.sub.2 -alkyl or a tetrazole group; m is 0 or 1, n is 2, 3 or 4 and p is 1, 2 or 3; amd the pharmaceutically acceptable salts thereof. The compounds of the present invention are specific inhibitors of 5-lipoxygenase and, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.

REFERENCES:
patent: 4029812 (1977-06-01), Wagner et al.
patent: 4076841 (1978-02-01), Wagner et al.
patent: 4078084 (1978-03-01), Wagner et al.
patent: 4153803 (1979-05-01), Thiele et al.
"Typical Methods for Obtaining Stabilizers Containing Sulfur", Khimiya; Khimicheskaya Tekhnologiya, Medvedv et al. (1977); pp. 568-574, (Translation).

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