Benzopyranyl and benzothiopyranyl compounds and uses
AssigneeHoffman-La Roche Inc.
InventorsMichael Klaus, Peter Loeliger
Life of this patent
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Abstract
Novel p-[2(4,4-dimethyl-6-heterophenyl)substituted phenyl derivatives and salts thereof which are useful for combatting neoplasms and dermatoses including oral and topical compositions containing said derivatives which are suitable for such uses.
Claims40
A compound of the formula:
- ##STR11## wherein X is --O--, ##STR12## or --SO.sub.2 ;
- R.sup.1 is methyl, ##STR13## R.sup.3 is hydrogen or methyl;
- R.sup.4 is hydrogen, lower alkyl or alkanoyl;
- R.sup.5 is hydrogen, lower alkyl, amino, lower alkylamino, di(lower alkyl)-amino or OR.sup.6 ;
- and R.sup.6 is hydrogen or lower alkyl;
- or pharmaceutically acceptable salts thereof.
A method for combatting acne or psoriasis comprising administering to a patient an effective amount of a compound of the formula:
- ##STR19## wherein X is --O--, ##STR20## --SO, or --SO.sub.2 ;
- R.sup.1 is methyl, ##STR21## R.sup.3 is hydrogen or methyl;
- R.sup.4 is hydrogen, lower alkyl or alkanoyl;
- R.sup.5 is hydrogen, lower alkyl, amino, lower alkylamino, di(lower-alkyl)amino or OR.sup.6 ;
- and R.sup.6 is hydrogen or lower alkyl;
- or pharmaceutically acceptable salts thereof.
A method for combatting neoplasms comprising administering to a patient in an effective amount of a compound of the formula:
- ##STR22## wherein X is --O--, ##STR23## --SO, or --SO.sub.2 ;
- R.sup.1 is methyl, ##STR24## R.sup.3 is hydrogen or methyl;
- R.sup.4 is hydrogen, lower alkyl or alkanoyl;
- R.sup.5 is hydrogen, lower alkyl, amino, lower alkylamino, di(lower-alkyl)amino or OR.sup.6 ;
- and R.sup.6 is hydrogen or lower alkyl;
- or pharmaceutically acceptable salts thereof.
A composition in oral unit dosage form comprising from about 0.5 to about 100 mg of a compound of the formula:
- ##STR25## wherein X is --O--, ##STR26## --SO, or --SO.sub.2 ;
- R.sup.1 is methyl, ##STR27## R.sup.3 is hydrogen or methyl;
- R.sup.4 is hydrogen, lower alkyl or alkanoyl;
- R.sup.5 is hydrogen, lower alkyl, amino, lower alkylamino, di(lower-alkyl)amino or OR.sup.6 ;
- and R.sup.6 is hydrogen or lower alkyl;
- and an inert pharmaceutically acceptable carrier.
A composition for topical administration comprising a therapeutically inert pharmaceutically acceptable carrier and from about 0.1 to 5% by weight based upon the weight of the composition of a compound of the formula:
- ##STR28## wherein X is --O--, ##STR29## --SO, or --SO.sub.2 ;
- R.sup.1 is methyl, ##STR30## R.sup.3 is hydrogen or methyl;
- R.sup.4 is hydrogen, lower alkyl or alkanoyl;
- R.sup.5 is hydrogen, lower alkyl, amino, lower alkylamino, di(lower-alkyl)amino or OR.sup.6 ;
- and R.sup.6 is hydrogen or lower alkyl;
- or pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.