Cyclopentane heptenylnitro and heptanylnitro-2-aliphatic or aryl aliphatic derivatives and homologues
AssigneeAllergan, Inc.
InventorMing F. Chan
Life of this patent
Estimating the term…
Abstract
The present invention relates to cyclopentane heptenylnitro and heptanylnitro-2-aliphatic or arylaliphatic derivatives. In particular, heptenylnitrate and heptanylnitrate 2-aliphatic or arylaliphatic derivatives, substituted at the 3 and/or 5 position of the cyclopentane ring with radicals selected from the group consisting of hydroxy, alkylcarboxy and mixtures thereof, are disclosed. These compounds are useful as ocular hypotensives.
Claims24
A method of treating ocular hypertension which comprises administering an effective amount of a compound represented by the formula VI ##STR11## wherein X is an integer from one to three and R.sub.8 is selected from the group consisting of hydrogen and C.sub.1 -C.sub.3 alkyl, the dashed bonds represent a single bond or a double bond which can be in the cis or trans configuration, A is an alkylene or alkenylene radical having from two to seven carbon atoms, which radical may be substituted with one or more hydroxy, oxo, alkyloxy or alkylcarboxy groups containing 1 to 10 carbon atoms in the alkyl moieties, B is a methyl radical or a cycloalkyl radical having from three to seven carbon atoms, or an aryl radical selected from the group consisting of aryl and monoheteroaryl radicals having from 4 to 10 carbon atoms wherein the heteroatom is selected from the group consisting of nitrogen, oxygen and sulfur atoms, any of the groups defining B may be substituted by radicals from the group consisting of halo, nitro, amino, thiol, hydroxy, alkyloxy and alkylcarboxy containing 1 to 10 carbon atoms in the alkyl moieties, and R.sub.1 and R.sub.2 are independently selected from the group consisting of hydryl, hydroxy and 1-20 carbon alkyl ester derivatives thereof, or a pharmaceutically acceptable salt thereof.
A pharmaceutical composition for treating ocular hypertension which comprises an effective amount of a compound represented by the formula VI ##STR16## wherein X is an integer from one to three and R.sub.8 is selected from the group consisting of hydrogen and C.sub.1 -C.sub.3 alkyl, the dashed bonds represent a single bond or a double bond which can be in the cis or trans configuration, A is an alkylene or alkenylene radical having from two to seven carbon atoms, which radical may be substituted with one or more hydroxy, oxo, alkyloxy or alkylcarboxy groups containing 1 to 10 carbon atoms in the alkyl moieties, B is a methyl radical or a cycloalkyl radical having from three to seven carbon atoms, or an aryl radical selected from the group consisting of aryl and monoheteroaryl radicals having from 4 to 10 carbon atoms wherein the heteroatom is selected from the group consisting of nitrogen, oxygen and sulfur atoms, any of the groups defining B may be substituted by radicals from the group consisting of halo, nitro, amino, thiol, hydroxy, alkyloxy and alkylcarboxy containing 1 to 10 carbon atoms in the alkyl moieties, and R.sub.1 and R.sub.2 are independently selected from the group consisting of hydryl, hydroxy and 1-20 carbon alkyl ester derivatives thereof, or a pharmaceutically acceptable salt thereof in connection with an ophthalmically-acceptable vehicle.
A compound, useful for treating ocular hypertension which comprises a compound represented by the formula VI ##STR21## wherein X is an integer from one to three and R.sub.8 is selected from the group consisting of hydrogen and C.sub.1 -C.sub.3 alkyl, the dashed bonds represent a single bond or a double bond which can be in the cis or trans configuration, A is an alkylene or alkenylene radical having from two to seven carbon atoms, which radical may be substituted with one or more hydroxy, oxo, alkyloxy or alkylcarboxy groups containing 1 to 10 carbon atoms in the alkyl moieties, B is a methyl radical or a cycloalkyl radical having from three to seven carbon atoms, or an aryl radical selected from the group consisting of aryl and monoheteroaryl radicals having from 4 to 10 carbon atoms wherein the heteroatom is selected from the group consisting of nitrogen, oxygen and sulfur atoms, any of the groups defining B may be substituted by radicals from the group consisting of halo, nitro, amino, thiol, hydroxy, alkyloxy and alkylcarboxy containing 1 to 10 carbon atoms in the alkyl moieties, and R.sub.1 and R.sub.2 are independently selected from the group consisting of hydryl, hydroxy and 1-20 carbon alkyl ester derivatives thereof, or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.