Dihydroxynaphthalene derivatives
AssigneeHoffmann-La Roche Inc.
InventorsMathew Carson, Ru-Jen L. Han, Ronald A. LeMahieu
Life of this patent
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Abstract
There are described dihydroxy naphthalene derivatives of the formula ##STR1## in which R.sub.1 is hydrogen, lower alkyl or benzyl, R.sub.2 is hydrogen, hydroxy or lower alkanoyloxy, R.sub.3 is hydrogen or lower alkyl, R.sub.4 is hydrogen or halogen, R.sub.5 is hydrogen, acyl, methyl or benzyl, m is 0 or 1, and n is an integer from 2 to 10, as well as salts thereof with pharmaceutically acceptable bases when R.sub.1 is hydrogen. These compounds are useful as agents for the treatment of inflammatory bowel diseases, for instance, colitis, as pro-drugs, or as intermediates for the preparation of such compounds.
Claims22
A compound of the formula ##STR8## in which R.sub.1 is hydrogen, lower alkyl or benzyl, R.sub.2 is hydrogen, Hydroxy or lower alkanoyloxy, R.sub.3 is hydrogen or lower alkyl, R.sub.4 is hydrogen or halogen, R.sub.5 is hydrogen, acyl, methyl or benzyl, m is 0 or 1, and n is an integer from 2 to 10, or a salt thereof with a pharmaceutically acceptable base when R.sub.1 is hydrogen.
A pharmaceutical composition comprising an effective amount of a compound of the formula ##STR9## in which R.sub.1 is hydrogen, lower alkyl or benzyl, R.sub.2 is hydrogen, hydroxy or lower alkanoyloxy, R.sub.3 is hydrogen or lower alkyl, R.sub.4 is hydrogen or halogen, R.sub.5 is hydrogen or acyl, m is 0 or 1, and n is an integer from 2 to 10, or a salt thereof with a pharmaceutically acceptable base when R.sub.1 is hydrogen,
- and an inert carrier material.
A method of inhibiting .DELTA..sup.5 -lipoxygenase in a host requiring such treatment, which comprises administering an effective amount of a compound of the formula ##STR10## in which R is hydrogen, lower alkyl or benzyl, R.sub.2 is hydrogen, hydroxy or lower alkanoyloxy, R.sub.3 is hydrogen or lower alkyl, R.sub.4 is hydrogen or halogen, R.sub.5 is hydrogen or acyl, m is 0 or 1, and n is an integer from 2 to 10, or a salt thereof with a pharmaceutically acceptable base when R.sub.1 is hydrogen.
Dependencies are inferred from the claim text.