Prostaglandin conjugates and derivatives for treating glaucoma and ocular hypertension
AssigneeNovartis AG
InventorsDavid Ellis, Lukas Scheibler, Najam A. Sharif
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Abstract
Prostaglandin conjugates and derivatives and methods for their use to treat glaucoma and/or lower intraocular pressure are disclosed. Additionally, ophthalmic pharmaceutical compositions useful in the treatment of eye diseases such as glaucoma and elevated intraocular pressure are disclosed. Such compositions comprise an effective amount of prostaglandin conjugates or derivatives of the present invention.
Claims15
An ophthalmic pharmaceutical composition useful in the treatment of glaucoma and control of intraocular pressure, comprising an effective amount of a compound (I) of the following formula:
- in which A is selected from the following:
- where:
- n is 1-6;
- R1, R2, R3 independently=OH or O—NO2;
- R4, R5 independently=H, alkyl, or heteroalkyl;
- or R4 and R5 can combine to form cyclic alkyl or cyclic heteroalkyl;
- and
- R6 independently=H, NO2, organic nitrate, organic nitrite, metal —NO complex, sodium nitroprusside (SNP), dinitrosyl iron thiol complex (DNICs), N-nitrosamine, N-hydroxy-N-nitrosamine, N-nitrosimine, nitrosimine, C-nitroso, diazetine dioxide, furoxan, benzofuroxan, oxatriazole-5-imine, sydnonimine, oxime, hydroxylamine, N-hydroxyguanidine, or hydroxyurea;
- and
- a pharmaceutically acceptable vehicle therefor.
A method for lowering intraocular pressure comprising:
- applying a therapeutically effective amount of an ophthalmic pharmaceutical composition to the affected eye of a human or other mammal, the composition comprising an effective amount of a compound of the following formula:
- in which A is selected from the following:
- where:
- n is 1-6;
- R1, R2, R3 independently=OH or O—NO2;
- R4, R5 independently=H, alkyl, or heteroalkyl;
- or R4 and R5 can combine to form cyclic alkyl or cyclic heteroalkyl;
- and
- R6 independently=H, NO2, organic nitrate, organic nitrite, metal —NO complex, sodium nitroprusside (SNP), dinitrosyl iron thiol complex (DNICs), N-nitrosamine, N-hydroxy-N-nitrosamine, N-nitrosimine, nitrosimine, C-nitroso, diazetine dioxide, furoxan, benzofuroxan, oxatriazole-5-imine, sydnonimine, oxime, hydroxylamine, N-hydroxyguanidine, or hydroxyurea;
- and
- a pharmaceutically acceptable vehicle therefor.
A compound represented by Formula (I):
- in which A is selected from the following:
- where:
- n is 1-6;
- R1, R2, R3 independently=OH or O—NO2;
- R4, R5 independently=H, alkyl, or heteroalkyl;
- or R4 and R5 can combine to form cyclic alkyl or cyclic heteroalkyl;
- and
- R6 independently=H, NO2, organic nitrate, organic nitrite, metal —NO complex, sodium nitroprusside (SNP), dinitrosyl iron thiol complex (DNICs), N-nitrosamine, N-hydroxy-N-nitrosamine, N-nitrosimine, nitrosimine, C-nitroso, diazetine dioxide, furoxan, benzofuroxan, oxatriazole-5-imine, sydnonimine, oxime, hydroxylamine, N-hydroxyguanidine, or hydroxyurea.
Dependencies are inferred from the claim text.