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Generated: October 23, 2017

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Title: Cyclopentane heptan(ene)oic acid, 2-heteroarylalkenyl derivatives as therapeutic agents
Abstract:The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The PGF derivatives 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; dashed bonds represent a double bond, or a single bond, R is a substituted heteroaryl radical, 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. Certain of the compounds represented by Formula I comprise another aspect of the present invention.
Inventor(s): Burk; Robert M. (Laguna Beach, CA)
Assignee: Allergan Sales, Inc. (Irvine, CA)
Filing Date:Mar 13, 2000
Application Number:09/523,880
Claims:1. A method of treating glaucoma which comprises administering to a mammal having said disease a therapeutically effective amount of a compound represented by formula I: ##STR36##

wherein the hatched segments represent a bonds, the solid triangle represents a .beta. bond, wavy line attachments indicate either the alpha (.alpha.) or beta (.beta.) configuration; dashed bonds represent a double bond or a single bond, R is a substituted hetero aryl radical, 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.

2. The method of claim 1 wherein the substituent on the heteroaryl radical is selected from the group consisting of lower alkyl, halogen, trifluoromethyl (CF.sub.3), COR.sub.1, COCF.sub.3, SO.sub.2 NR.sub.1, SO.sub.2 NH.sub.2, NO.sub.2 and CN.

3. The method of claim 2 wherein said compound is represented by formula II: ##STR37##

wherein Z is selected from the group consisting of O and S, A is selected from the group consisting of N, --CH, and C, R.sup.2 is selected from the group consisting of hydrogen, halogen and lower alkyl having from 1 to 6 carbon atoms, together with, ##STR38##

R.sup.3 and R.sup.4 forms a condensed aryl ring.

4. The method of claim 3 wherein said compound represented by formula III: ##STR39##

wherein R.sup.5 is hydrogen or methyl.

5. The method of claim 4 wherein X is --OH or --NH.sub.2.

6. The method of claim 4 wherein Y is .dbd.O and X is --OH.

7. The method of claim 4 wherein Y is .dbd.O and X is --NH.sub.2.

8. The method of claim 4 wherein Z is S.

9. The method of claim 4 wherein Y is .dbd.O, X is --OH or --NH.sub.2 and Z is S.
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