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Details for Patent: 6,602,900

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Details for Patent: 6,602,900

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, --N(R.sup.1).sub.2, 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, --N(R.sup.1).sub.2 and --N(R.sup.5)SO.sub.2 R.sup.6, wherein R.sup.5 represents hydrogen or CH.sub.2 OR.sup.6 and R.sup.6 represents hydrogen or a lower alkyl radical having up to six carbon atoms and halogen substituted derivatives of said lower alkyl radical, e.g. a fluoro substituted lower alkyl radical; 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, Inc. (Irvine, CA)
Filing Date:Oct 29, 2001
Application Number:10/021,485
Claims:1. A method of treating ocular hypertension which administering to a mammal having ocular hypertension a therapeutically-effective amount of a compound wherein said compound is represented by formula II: ##STR60## wherein the hatched segments represent a bonds, the solid triangle represents a b bond, wavy line attachments indicate either the alpha (a) or beta (b) configuration; 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, --N(R1)2, and --N(R.sup.5)SO.sub.2 R.sup.6, wherein R.sup.5 represents hydrogen or CH.sub.2 OR.sup.6 and R.sup.6 represents hydrogen or a lower alkyl radical having up to six carbon atoms and halogen substituted derivatives of said lower alkyl radical; Y is .dbd.O or represents 2 hydrogen radicals, 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 atoms, or, together with, ##STR61## R.sup.3 and R.sup.4 forms a condensed aryl ring; provided however when A is selected from the group consisting of CH and C, R.sup.3 and R.sup.4 together with ##STR62## forms a condensed aryl ring.

2. The method of claim 1 wherein said compound represented by formula IV: ##STR63## wherein R.sup.5 is hydrogen or methyl.

3. The method of claim 2 wherein Z is S.

4. The method of claim 3 wherein at least one of R.sup.2, R.sup.3 and R.sup.4 are selected from the group consisting of halogen and lower alkyl having from 1 to 4 carbon atoms.

5. The method of claim 3 wherein at least one of R.sup.2, R.sup.3 and R.sup.4 is selected from the group consisting of chloro, bromo and iodo.

6. The method of claim 3 wherein at least one of R.sup.2, R.sup.3 and R.sup.4 are bromo.

7. The method of claim 3 wherein R.sup.5 is selected from the group consisting of hydrogen, ##STR64##

8. The method of claim 3 wherein R.sup.6 is selected from the group consisting of methyl, ethyl and trifluoromethyl.

9. A pharmaceutical product, comprising a container adapted to dispense the contents of said container in metered form; and an ophthalmic solution in said container comprising a compound of formula II as defined in claim 1, or a pharmaceutically acceptable salt thereof, in admixture with a non-toxic, ophthalmically acceptable liquid vehicle.

10. The compound is represented by Formula III: ##STR65## wherein 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, --N(R.sup.1).sub.2, and --N(R.sup.5)SO.sub.2 R.sup.6, wherein R.sup.5 represents hydrogen or CH.sub.2 OR.sup.6 and R.sup.6 represents hydrogen or a lower alkyl radical having up to six carbon atoms and halogen substituted derivatives of said lower alkyl radical; Y is .dbd.O or represents 2 hydrogen radicals; 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 ##STR66## R.sup.3 and R.sup.4 forms a condensed aryl ring; provided however when A is selected from the group consisting of CH and C, R.sup.3 and R.sup.4 together with ##STR67## with forms a condensed aryl ring.

11. The compound of claim 10 wherein said compound is represented by formula IV: ##STR68## wherein R.sup.5 is hydrogen or methyl.

12. The compound of claim 11 wherein Z is S.

13. The compound of claim 12 wherein at least one of R.sup.2, R.sup.3 and R.sup.4 are selected from the group consisting of halogen and lower alkyl having from 1 to 4 carbon atoms.

14. The compound of claim 12 wherein at least one of R.sup.2, R.sup.3 and R.sup.4 is selected from the group consisting of chloro, bromo and iodo.

15. The compound of claim 12 wherein at least one of R.sup.2, R.sup.3 and R.sup.4 are bromo.

16. The compound of claim 12 wherein R.sup.5 is selected from the group consisting of hydrogen, ##STR69##

17. The compound of claim 12 wherein R.sup.6 is selected from the group consisting of methyl, ethyl and trifluoromethyl.
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