Use of amino acyl amino propargyl diol compounds for treatment of glaucoma

A therapeutic method for treating glaucoma in a subject, said method comprising administering to said subject a therapeutically-effective amount of a compound of Formula I:

• ##STR41## wherein A is selected from methylene, CO, SO and SO.sub.2 ;
• wherein X is selected from oxygen atom, methylene and ##STR42## with R.sub.10 selected from hydrido, alkyl and benzyl;
• wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, alkyl, cycloalkyl, alkoxyacyl, haloalkyl, alkoxycarbonyl, benzyloxycarbonyl, loweralkanoyl, haloalkylacyl, phenyl, benzyl, naphthyl, and naphthylmethyl, any one of which groups having a substitutable position may be optionally substituted with one or more radicals selected from alkyl, alkoxy, alkenyl, alkynyl, halo, haloalkyl, cyano and phenyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide;
• wherein R.sub.2 is selected from hydrido, alkyl, dialkylaminoalkyl, alkylacylaminoalkyl, benzyl and cycloalkyl;
• wherein R.sub.3 is selected from alkyl, cycloalkylalkyl, acylaminoalkyl, phenylalkyl, naphthylmethyl, aryl, heterocyclicalkyl, heterocycliccycloalkyl, heteroaryl and heteroarylalkyl, wherein the cyclic portion of any of said phenylalkyl, naphthylmethyl, aryl, heterocyclicalkyl, heterocycliccycloalkyl, heteroaryl and heteroarylalkyl groups may be substituted by one or more radicals selected from halo, hydroxy, alkoxy and alkyl;
• wherein each of R.sub.4 and R.sub.6 is independently selected from hydrido, alkyl, benzyl and cycloalkyl;
• wherein R.sub.5 is selected from hydrido, alkyl, benzyl, cycloalkyl, cycloalkylalkyl, alkoxyalkyl, alkylthioalkyl, heteroarylalkyl and heteroarylcycloalkyl;
• wherein R.sub.7 is selected from substituted or unsubstituted alkyl, cycloalkyl, phenyl, cycloalkylalkyl and phenylalkyl, any one of which may be substituted with one or more groups selected from alkyl, hydroxy, alkoxy, halo, haloalkyl, alkenyl, alkynyl and cyano;
• wherein R.sub.8 is selected from ##STR43## wherein V is selected from hydrido, alkyl, cycloalkyl, haloalkyl, benzyl and phenyl;
• wherein each of R.sub.13 and R.sub.14 is a radical independently selected from hydrido, alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, heterocyclic and heterocyclicalkyl;
• wherein each of R.sub.11 and R.sub.12 is independently selected from hydrido, alkyl, haloalkyl, dialkylamino and phenyl;
• and wherein m is zero or one;
• wherein n is a number selected from zero through five;
• wherein p is a number selected from zero through five;
• and wherein q is a number selected from zero through five;
• or a pharmaceutically-acceptable salt thereof;
• with the proviso that for any of the foregoing R.sup.1 through R.sup.14 substituents containing a radical selected from alkyl, cycloalkyl, alkenyl, alkynyl, aryl and heterocyclic, the following shall apply:
• alkyl is a linear or branched radical having one to about twenty carbon atoms:
• cycloalkyl is a cyclic radical having three to about ten carbon-ring atoms:
• alkenyl is a linear or branched radical having two to about twenty carbon atoms and containing at least one carbon carbon double bond;
• alkynyl is a linear or branched radical having two to about twenty carbon atoms and containing at least one carbon carbon triple bond;
• aryl is selected from phenyl, naphthyl and biphenyl;
• heterocyclic is a saturated or partially unsaturated radical consisting of a carbocyclic ring system having one ring or two fused rings, which ring system contains one, two or three hetero atoms as ring members selected from nitrogen, oxygen and sulfur atoms, and which ring system has four to about twelve ring members;
• and
• heteroaryl is a fully unsaturated radical having a carbocyclic ring system consisting of one ring or two fused rings, said ring selected from five-membered rings containing one, two or three hetero atoms as ring members selected from nitrogen, oxygen, and sulfur atoms.