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Details for Patent: 5,972,991

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Details for Patent: 5,972,991

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; hatched segments indicate .alpha. configuration, solid triangles are used to indicate .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 =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 (Waco, TX)
Filing Date:Nov 03, 1998
Application Number:09/185,403
Claims:1. A method of treating ocular hypertension which comprises administering to a mammal having ocular hypertension a therapeutically effective amount of a compound represented by formula I: ##STR36## wherein the hatched segments represent .alpha. 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 =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, R.sup.3 and R.sup.4 are selected from the group consisting of hydrogen, halogen, lower alkyl having from 1 to 6 carbon atoms, or, together with ##STR38## R.sup.3 and R.sup.4 forms a condensed aryl ring.

4. The compound represented by Formula III: ##STR39## wherein the hatched segments represent .alpha. bonds, the solid triangle represents a .beta. bond, R.sup.1 is hydrogen or a lower alkyl radical having up to six carbon atoms, R.sup.2 is selected from the group consisting of hydrogen, halogen and lower alkyl having from up to six carbon atoms, R.sup.3 and R.sup.4 are selected from the group consisting of hydrogen, halogen, lower alkyl having up to six carbon atoms, or together with ##STR40## R.sup.3 and R.sup.4 forms a R.sup.3 and R.sup.4 forms a condensed aryl ring, A is selected from the group consisting of --CH and C, Z is selected from the group consisting of O and S, Y is O and X is --OH or --NH.sub.2.

5. A compound according to claim 4 wherein Z is S.

6. The compound of claim 4 wherein Y is =O, X is --OH or --NH.sub.2 and Z is S.

7. The compound of claim 4 wherein said compound is 7-[3.alpha.,5.alpha.-Dihydroxy-2-(3.alpha.-hydroxy-5-(3-thienyl)-1E-penten yl)cyclopentyl]-5Z-heptenoic acid.

8. A method of treating ocular hypertension which comprises administering to a mammal having ocular hyprtension a therapeutically effect amount of the compound of claim 7.

9. The compound of claim 4 wherein said compound is 7-[3.alpha.,5.alpha.-Dihydroxy-2-(3.alpha.-hydroxy-5-(3-furanyl)-1-E-pente nyl)cyclopentyl]-5Z-heptenoic acid.

10. method of treating ocular hypertension which comprises administering to a mammal having ocular hypertension a therapeutically effect amount of the compound of claim 9.
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