Cyclopentane heptenylsulfinylalkyl and heptanylsulfinylalkyl-2-aliphatic or aryl aliphatic derivatives
AssigneeAllergan, Inc.
InventorMing Fai Chan
Life of this patent
Estimating the term…
Abstract
The present invention relates to cyclopentane heptenylsulfinylalkyl and heptanylsulfinylalkyl-2-aliphatic or arylaliphatic derivatives. In particular, heptenylsulfinylmethyl and heptanylsulfinylmethyl 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.
Claims19
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 alkyl radical having from one to seven carbon atoms, 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 wherein the alkyl moiety has from 1 to 10 atoms, 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 having from 1 to 10 atoms in the alkyl moiety 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 alkyl radical having from one to seven carbon atoms, 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 wherein the alkyl moiety has from 1 to 10 atoms, 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 having from 1 to 10 atoms in the alkyl moiety 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. of the formula (IV)
A compound for treating ocular hypertension of the formula (IV) ##STR21## wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of hydryl, hydroxy and 1-20 carbon atom alkyl ester derivatives thereof, R.sub.3 is =O, --OH or --O(CO)R.sub.6 wherein R6 is a saturated or unsaturated acyclic hydrocarbon group having from 1 to 20 carbon atoms or --(CH.sub.2).sub.m R.sub.7 wherein m is 0-20 and R.sub.7 is an aliphatic ring having from 3 to 7 carbon atoms, or an aryl radical selected from the group consisting of 4 to 10 carbon aryl and monoheteroaryl wherein the heteroatom is selected from the group consisting of nitrogen, oxygen and sulfur atoms.
Dependencies are inferred from the claim text.