Cyclopentane heptan(ene)oic acid, 2-heteroarylalkenyl derivatives as therapeutic agents
AssigneeAllergan Sales, Inc.
InventorRobert M. Burk
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AssigneeAllergan Sales, Inc.
InventorRobert M. Burk
Estimating the term…
The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The compounds used in accordance with the invention are represented by the following formula I: ##STR1## wherein wavy line attachments indicate either the alpha (.alpha.) or beta (.beta.) configuration; hatched segments indicate a configuration; the solid triangle is used to indicate .beta. configuration; dashed bonds represent a double bond, or a single bond; R is a substituted heteroaryl radical having at least two pendant substituents selected from the group consisting of C.sub.1 to C.sub.6 alkyl; halogen; trifluoromethyl; COR.sup.1 ; COCF.sub.3 ; SO.sub.2 NR.sup.1 ; NO.sub.2 and CN or at least one cyano group; R.sup.1 is hydrogen or a lower alkyl radical having up to six carbon atoms, X is selected from the group consisting of --OR.sup.1 and --N(R.sup.1).sub.2 ; Y is .dbd.O or represents 2 hydrogen radicals and the 9, 11 or 15 lower alkyl esters thereof; provided, however, when said heteroaryl radical is a dichlorothienyl radical, the compound is not a 1-carboxylic add or amide thereof. Certain of the compounds represented by Formula I are novel and comprise another aspect of the present invention.
A method of treating ocular hypertension which comprises administering to a mammal having ocular hypertension a therapeutically effective amount of a cyclopentane heptan(ene)oic acid, 2-heteroaryl alkenyl compound represented by formula II ##STR48## wherein the hatched segments represent .alpha. bonds, the solid triangle represents a .beta. bond, the wavy line represents either an .alpha. or .beta. bond, R.sup.1 is hydrogen or a lower alkyl radical hazing up to six carbon atoms, X is selected from the soup consisting of --OR.sup.1 and --N(R.sup.1).sub.2 ;
The cyclopentane heptan(ene)oic acid, 2-heteroarylalkenyl compound represented by Formula III:
The cyclopentane heptan(ene)oic acid, 2-heteroarylalkenyl compound represented by Formula III:
Dependencies are inferred from the claim text.