Disulfide derivatives useful for treating allergic diseases
AssigneeAlcon Universal Ltd.
InventorsZixia Feng, Mark R. Hellberg, Steven T. Miller
Life of this patent
Estimating the term…
Abstract
Novel disulfide derivatives useful for preventing or treating allergic diseases of the eye, nose, skin, ear, gastrointestinal tract, airways or lung and preventing or treating manifestations of systemic mastocytosis are disclosed. The disulfide derivatives act as mast cell stabilizers.
Claims19
A disulfide derivative of the formula
- 7
- wherein
- X=—NHC(═O)NH—R;
- R=H;
- (un)substituted phenyl;
- (un)substituted benzyl;
- or C1-C8 alkyl or alkenyl, optionally substituted with or terminated by OH, OR2, NR3R4;
- C4-C7 cycloalkyl, (un)substituted aryl, or (un)substituted 5-7 membered heterocyclic ring;
- where optional substituents are selected from the group consisting of C1-C6 alkyl or alkoxy;
- halogen;
- OH;
- CN;
- CF3;
- NO2;
- and CO2R2;
- R2=C1-C3 alkyl;
- and
- R3 and R4 are independently H;
- benzyl;
- C1-C8 alkyl or alkenyl;
- C4-C7 cycloalkyl;
- (un)substituted aryl;
- or (un)substituted 5-7 membered heterocyclic ring;
- wherein optional substituents are selected from the group consisting of C1-C6 alkyl or alkoxy;
- halogen;
- OH;
- CN;
- CF3;
- NO2;
- and CO2R2.
A topically or locally administrable pharmaceutical composition for treating allergic diseases of the eye, nose, skin, ear or lung comprising a tonicity-adjusting agent in an amount sufficient to cause the composition to have an osmolality of 150-450 mOsm, a pharmaceutically acceptable preservative and a disulfide derivative of the formula
- 8
- wherein
- X=—NHC(═O)NH—R;
- R=H;
- (un)substituted phenyl;
- (un)substituted benzyl;
- or C1-C8 alkyl or alkenyl, optionally substituted with or terminated by OH, OR2, NR3R4;
- C4-C7 cycloalkyl, (un)substituted aryl, or (un)substituted 5-7 membered heterocyclic ring;
- where optional substituents are selected from the group consisting of C1- C6 alkyl or alkoxy;
- halogen;
- OH;
- CN;
- CF3;
- NO2;
- and CO2R2;
- R2=C1-C3 alkyl;
- and
- R3 and R4 are independently H;
- benzyl;
- C1-C8 alkyl or alkenyl;
- C4-C7 cycloalkyl;
- (un)substituted aryl;
- or (un)substituted 5-7 membered heterocyclic ring;
- wherein optional substituents are selected from the group consisting of C1-C6 alkyl or alkoxy;
- halogen;
- OH;
- CN;
- CF3;
- NO2;
- and CO2R2.
A method for preventing or treating an allergic disease of the eye, nose, skin, ear, gastrointestinal tract or lung and preventing or treating manifestations of systemic mastocytosis in a patient comprising administering to the patient a composition comprising a disulfide derivative of the formula
- 9
- wherein
- X=—NHC(═O)NH—R;
- R=H;
- (un)substituted phenyl;
- (un)substituted benzyl;
- or C1-C8 alkyl or alkenyl, optionally substituted with or terminated by OH, OR2, NR3R4;
- C4-C7 cycloalkyl, (un)substituted aryl, or (un)substituted 5-7 membered heterocyclic ring;
- where optional substituents are selected from the group consisting of C1-C6 alkyl or alkoxy;
- halogen;
- OH;
- CN;
- CF3;
- NO2;
- and CO2R2;
- R2=C1-C3 alkyl;
- and
- R3 and R4 are independently H;
- benzyl;
- C1-C8 alkyl or alkenyl;
- C4-C7 cycloalkyl;
- (un)substituted aryl;
- or (un)substituted 5-7 membered heterocyclic ring;
- wherein optional substituents are selected from the group consisting of C1-C6 alkyl or alkoxy;
- halogen;
- OH;
- CN;
- CF3;
- NO2;
- and CO2R2.
Dependencies are inferred from the claim text.