Pharmaceutical compositions
AssigneeSmith and Nephew Associated Companies Limited
InventorMichael Horlington
Life of this patent
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Abstract
The present invention relates to pharmaceutical compositions adapted for topical administration to the eye and to their preparation and use. More specifically this invention relates to anti-glaucoma ophthalmic compositions containing tetraazabicyclic compounds of the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, X and Y are hereinafter defined and to the preparation and use of such compositions.
Claims61
A method for reducing the intra-ocular pressure in the eye of a patient having glaucoma which comprises topically applying of the surface of the eye a sterile composition comprising an effective intra-ocular pressure reducing amount of a compound of the formula (I):
- ##STR7## wherein X.dbd.Y is CR.dbd.N or N.dbd.CR wherein at least two of R,R.sup.1,R.sup.2 and R.sup.3 are amino and the other groups of R,R.sup.1,R.sup.2 and R.sup.3 are hydrogen, lower alkyl, aryl, carboxamido or lower alkoxycarbonyl, in combination with an ocularly acceptable carrier.
A method for reducing the intra-ocular pressure in the eye of a patient having glaucoma which comprises topically applying to the surface of the eye a sterile composition comprising an effective intra-ocular pressure reducing amount of a compound of the formula (III):
- ##STR9## wherein R.sup.7 is phenyl unsubstituted or substituted by fluoro, chloro, bromo, lower alkyl, lower alkoxy, amino, nitro, hydroxyl or sulphated hydroxyl and R.sup.8 is hydrogen, lower alkyl, aryl, lower alkoxycarbonyl or carboxamido, in combination with an ocularly acceptable carrier.
A method for reducing the intra-ocular pressure in the eye of a patient having glaucoma which comprises topically applying to the surface of the eye a sterile composition comprising an effective intra-ocular pressure reducing amount of a compound of the formula (IV):
- ##STR10## wherein R.sup.9 is hydrogen, amino, lower alkyl or aryl and R.sup.10 is hydrogen, lower alkyl, carboxyamido or phenyl unsubstituted or substituted by fluoro, chloro, bromo, lower alkyl, lower alkoxy, amino, nitro, hydroxyl or sulphated hydroxyl, in combination with an ocularly acceptable carrier.
A method for reducing the intra-ocular pressure in the eye of a patient having glaucoma which comprises topically applying to the surface of the eye a sterile composition comprising an effective intra-ocular pressure reducing amount of a compound of the formula (V):
- ##STR11## or a pharmaceutically acceptable salt thereof, wherein at least two of R.sup.12, R.sup.13 and R.sup.14 are amino and the other group is hydrogen or phenyl unsubstituted or substituted by fluoro, chloro, bromo, lower alkyl, lower alkoxy, amino, nitro, hydroxyl or sulphated hydroxyl and R.sup.11 is hydrogen or phenyl unsubstituted or substituted by fluoro, chloro, bromo, lower alkyl, lower alkoxy, amino, nitro, hydroxyl or sulphated hydroxyl, in combination with an ocularly acceptable carrier.
A sterile pharmaceutical composition for reducing the intra-ocular pressure in the eye of a patient having glaucoma adapted for topical application to the eye which comprises an effective intra-ocular pressure reducing amount of a compound of formula (I):
- ##STR12## wherein X.dbd.Y is CR.dbd.N or N.dbd.CR wherein at least two of R,R.sup.1,R.sup.2 and R.sup.3 are amino and the other groups of R,R.sup.1,R.sup.2 and R.sup.3 are hydrogen, lower alkyl, aryl, carboxamido or lower alkoxycarbonyl, in combination with an ocularly acceptable carrier.
A sterile pharmaceutical composition for reducing the intra-ocular pressure in the eye of a patient having glaucoma adapted for topical application to the eye which comprises an effective intra-ocular pressure reducing amount of a compound of the formula (III):
- ##STR14## wherein R.sup.7 is phenyl unsubstituted or substituted by fluoro, chloro, bromo, lower alkyl, lower alkoxy, amino, nitro, hydroxyl or sulphated hydroxyl and R.sup.8 is hydrogen, lower alkyl, aryl, lower alkoxycarbonyl or carboxamido, in combination with an ocularly acceptable carrier.
A sterile pharmaceutical composition for reducing the intra-ocular pressure in the eye of a patient having glaucoma adapted for topical application to the eye which comprises an effective intra-ocular pressure reducing amount of a compound of the formula (IV):
- ##STR15## wherein R.sup.9 is hydrogen, amino, lower alkyl or aryl and R.sup.10 is hydrogen, lower alkyl, carboxyamido or phenyl unsubstituted or substituted by fluoro, chloro, bromo, lower alkyl, lower alkoxy, amino, nitro, hydroxyl or sulphated hydroxyl, in combination with an ocularly acceptable carrier.
A sterile pharmaceutical composition for reducing the intra-ocular pressure in the eye of a patient having glaucoma adapted for topical application to the eye which comprises an effective intra-ocular pressure reducing amount of a compound of the formula (V):
- ##STR16## or a pharmaceutically acceptable salt thereof, wherein at least two of R.sup.12, R.sup.13 and R.sup.14 are amino and the other group is hydrogen or phenyl unsubstituted or substituted by fluoro, chloro, bromo, lower alkyl, lower alkoxy, amino, nitro, hydroxyl or sulphated hydroxyl and R.sup.11 is hydrogen or phenyl unsubstituted or substituted by fluoro, chloro, bromo, lower alkyl, lower alkoxy, amino, nitro, hydroxyl or sulphated hydroxyl, in combination with an ocularly acceptable carrier.
Dependencies are inferred from the claim text.