Loading patent…
AssigneeE. I. Du Pont de Nemours and Company
InventorsGhanshyam Patil, William L. Matier, Khuong H. X. Mai
Estimating the term…
In accordance with the present invention, disclosed herein are compounds of the formula ##STR1## wherein R is hydrogen, straight or branched loweralkyl, cycloalkyl, amino, loweralkoxy or acylamino, and R.sub.1 is straight or branched loweralkyl, amino, cyclohexyl phenyl or phenyl substituted with loweralkyl, loweralkoxy or halo, benzyl, morpholino, piperidino, tetrahydrofuranyl, dihydrofuranyl, furanyl, tetrahydropyranyl, dioxolanyl, 2,2-dimethyl dioxolanyl, dioxanyl, pyrrolidinyl, tetrahydrooxazolyl, and dihydrooxazolyl, R.sub.2 is hydrogen or --COR.sub.3 wherein R.sub.3 is straight or branched loweralkyl, provided, however, when R.sub.1 is loweralkyl or cyclohexyl, R.sub.2 is not hydrogen, and pharmaceutically acceptable salts thereof. The compounds are useful in the treatment of glaucoma.
A compound of the formula ##STR50## wherein R is hydrogen, straight or branched loweralkyl, cycloalkyl, amino, loweralkoxy or alkanoyl amino, and R.sub.1 is straight or branched loweralkyl, amino, cyclohexyl, phenyl or phenyl substituted with loweralkyl, loweralkoxy or halo, benzyl, tetrahydrofuranyl, dihydrofuranyl, furanyl, R.sub.2 is hydrogen or --COR.sub.3 wherein R.sub.3 is straight or branched loweralkyl, provided, however, when R.sub.1 is loweralkyl, phenyl or cyclohexyl, R.sub.2 is not hydrogen, or a pharmaceutically acceptable salt thereof.
A compound of the formula ##STR51## wherein R is hydrogen, loweralkyl, loweralkoxy or amino, R.sub.1 is loweralkyl, cycloalkyl, benzyl, phenyl, phenyl substituted with methoxy or fluoro, furanyl, or tetrahydrofuranyl, and R.sub.2 is hydrogen or --COR.sub.3, wherein R.sub.3 is straight or branched loweralkyl provided, however, when R.sub.1 is loweralkyl, cycloalkyl or phenyl, R.sub.2 is not hydrogen.
A compound of the formula ##STR52## wherein R is loweralkyl, R.sub.1 is loweralkyl or tetrahydrofuranyl, and R.sub.2 is hydrogen, loweralkyl or --COR.sub.3 wherein R.sub.3 is straight or branched loweralkyl.
A method of treating glaucoma or of lowering intraocular pressure in a patient comprising administering to the eye of a patient in need of such treatment a therapeutically effective amount of a compound of the formula ##STR53## wherein R is hydrogen, straight or branched loweralkyl, cycloalkyl, amino, loweralkoxy or alkanoyl amino, and R.sub.1 is straight or branched loweralkyl, amino, cyclohexyl, phenyl or phenyl substituted with loweralkyl, loweralkoxy or halo, benzyl, tetrahydrofuranyl, dihydrofuranyl, furanyl, R.sub.2 is hydrogen or --COR.sub.3 wherein R.sub.3 is straight or branched loweralkyl, provided, however, when R.sub.1 is loweralkyl, phenyl or cyclohexyl, R.sub.2 is not hydrogen, or a pharmaceutically acceptable salt thereof.
A pharmaceutical composition useful for the treatment of glaucoma or for lowering intraocular pressure, which composition comprises an intraocular lowering effective amount of a compound of the formula ##STR54## wherein R is hydrogen, straight or branched loweralkyl, cycloalkyl, amino, loweralkoxy or alkanoylamino, and R.sub.1 is straight or branched loweralkyl, amino, cyclohexyl, phenyl or phenyl substituted with loweralkyl, loweralkoxy or halo, benzyl, tetrahydrofuranyl, dihydrofuranyl, furanyl, R.sub.2 is hydrogen or --COR.sub.3 wherein R.sub.3 is straight or branched loweralkyl, provided, however, when R.sub.1 is loweralkyl, phenyl or cyclohexyl, R.sub.2 is not hydrogen, or a pharmaceutically acceptable salt thereof in admixture with an opthalmologically acceptable carrier or diluent.
A pharmaceutical composition useful for the treatment of glaucoma or for lowering intraocular pressure, which composition comprises an intraocular lowering effective amount of a compound of the formula ##STR55## wherein R is loweralkyl, R.sub.1 is loweralkyl or tetrahydrofuranyl, and R.sub.2 is --COR.sub.3 wherein R.sub.3 is straight or branched loweralkyl or a pharmaceutically acceptable salt thereof in admixture with an opthalmologically acceptable carrier or diluent.
A compound of the formula ##STR56## wherein R is hydrogen, straight or branched loweralkyl, cycloalkyl, amino, loweralkoxy or alkanoylamino, and R.sub.1 is straight or branched loweralkyl, amino, cyclohexyl, phenyl or phenyl substituted with loweralkyl, loweralkoxy or halo, benzyl, tetrahydrofuranyl, dihydrofuranyl, furanyl, R.sub.2 is --COR.sub.3 wherein R.sub.3 is straight or branched loweralkyl, or a pharmaceutically acceptable salt thereof.
A compound of the formula ##STR57## wherein R is loweralkyl, loweralkoxy or amino, R.sub.1 is loweralkyl, cycloalkyl, benzyl, phenyl, phenyl substituted with methoxy or fluoro, furanyl, morpholino, or tetrahydropyranyl or tetrahydrofuranyl, and R.sub.2 is --COR.sub.3 wherein R.sub.3 is straight or branched loweralkyl.
Dependencies are inferred from the claim text.