Use of 2,5-dihydroxybenzene compounds and derivatives for the treatment of rosacea
AssigneeAmDerma Pharmaceuticals, LLC
InventorPedro Cuevas Sànchez
Life of this patent
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Abstract
The present invention relates to the use of a 2,5-dihydroxybenzene derivative of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the treatment and/or prophylaxis of, inter alia, rosacea.
Claims18
A method for the treatment of rosacea, comprising administering topically to a subject in need thereof, an effective amount of a 2,5-dihydroxybenzene derivative represented by Formula (I) or a pharmaceutically acceptable salt, solvate, or isomer thereof, wherein the compound of Formula (I) is:
- wherein:
- R1 is —(CH2)aY or —CH═CH—(CH2)pY;
- Y is —SO3H, —SO3−.X+, —SO3R3, —PO3H, —PO3−.X+, or —PO3R3, wherein when Y is —SO3H, —SO3−.X+ or —SO3R3, then R9 and R9′ are independently selected from —OH and —OR2, wherein at least one of R9 and R9′ is a substituted or unsubstituted alkylsulfonyloxy group, a substituted or unsubstituted arylsulfonyloxy group, a substituted or unsubstituted alkylcarbonyloxy group or a substituted or unsubstituted arylcarbonyloxy group;
- X+ is an organic cation or an inorganic cation, such that the general charge of the compound is neutral;
- R9 and R9′ are independently selected from —OH and —OR2, wherein when R9 and R9′ are both —OR2, then said R9 and R9′ can be the same or different;
- R2 is a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted alkylsulfonyl group, a substituted or unsubstituted arylsulfonyl group, a substituted or unsubstituted alkylcarbonyl group or a substituted or unsubstituted arylcarbonyl group;
- R3 is selected from methyl and ethyl;
- a is a number selected from 0, 1, 2, 3, 4, 5 and 6, provided that a is not 0 when Y is —SO3H;
- and
- p is an integer selected from 0, 1, 2, 3, 4, 5 and 6.
A method for the treatment of rosacea, comprising administering topically to a subject in need thereof, an effective amount of a 2,5-dihydroxybenzene derivative represented by Formula (I) or a pharmaceutically acceptable salt, solvate, or isomer thereof, wherein the compound of Formula (I) is:
- wherein:
- R1 is —(CH2)aY or —CH═CH—(CH2)pZ;
- Y is —SO3H, —SO3−.X+, —SO3R3, —PO3H, —PO3−.X+, or —PO3R3, wherein when Y is —SO3H, —SO3−.X+ or —SO3R3, then R9 and R9′ are independently selected from —OH and —OR2, wherein at least one of R9 and R9′ is a substituted or unsubstituted alkylsulfonyloxy group, a substituted or unsubstituted arylsulfonyloxy group, a substituted or unsubstituted alkylcarbonyloxy group or a substituted or unsubstituted arylcarbonyloxy group;
- Z is —SO3H, —SO3−.X+, —SO3R3, —PO3H, —PO3−.X+, —PO3R3, —CO2H, —CO2−.X+ or —CO2R3;
- X+ is an organic cation or an inorganic cation, such that the general charge of the compound is neutral;
- R9 and R9′ are, independently, a substituted or unsubstituted alkylsulfonyloxy group, a substituted or unsubstituted arylsulfonyloxy group, a substituted or unsubstituted alkylcarbonyloxy group or a substituted or unsubstituted arylcarbonyloxy group;
- R2 is a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted alkylsulfonyl group, a substituted or unsubstituted arylsulfonyl group, a substituted or unsubstituted alkylcarbonyl group or a substituted or unsubstituted arylcarbonyl group;
- R3 is a substituted or unsubstituted alkyl group or a substituted or unsubstituted aryl group;
- a is a number selected from 0, 1, 2, 3, 4, 5 and 6, provided that a is not 0 when Y is —SO3H;
- and
- p is an integer selected from 0, 1, 2, 3, 4, 5 and 6.
A method for the treatment of rosacea, comprising administering topically to a subject in need thereof, an effective amount of a 2,5-dihydroxybenzene derivative represented by Formula (I) or a pharmaceutically acceptable salt, solvate, or isomer thereof, wherein the compound of Formula (I) is:
- wherein:
- R1 is —(CH2)aY or —CH═CH—(CH2)pZ;
- Y is —SO3H, —SO3−.X+, —SO3R3, —PO3H, —PO3−.X+, or —PO3R3, wherein when Y is —SO3H, —SO3−.X+ or —SO3R3 then R9 and R9′ are independently selected from —OH and —OR2, wherein at least one of R9 and R9′ is a substituted or unsubstituted alkylsulfonyloxy group, a substituted or unsubstituted arylsulfonyloxy group, a substituted or unsubstituted alkylcarbonyloxy group or a substituted or unsubstituted arylcarbonyloxy group;
- Z is —SO3H, —SO3−.X+, —SO3R3, —PO3H, —PO3−.X+, —PO3R3, —CO2H, —CO2−.X+ or —CO2R3;
- X+ is an organic cation or an inorganic cation, such that the general charge of the compound is neutral;
- R9 and R9′ are independently selected from —OH and —OR2, wherein when R9 and R9′ are both —OR2, then said R9 and R9′ can be the same or different;
- R2 is selected from methylcarbonyl, phenylsulfonyl, 4-methylphenylsulfonyl, benzylsulfonyl, benzyl and phenyl;
- R3 is a substituted or unsubstituted alkyl group or a substituted or unsubstituted aryl group;
- a is a number selected from 0, 1, 2, 3, 4, 5 and 6, provided that a is not 0 when Y is —SO3H;
- and
- p is an integer selected from 0, 1, 2, 3, 4, 5 and 6.
Dependencies are inferred from the claim text.