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Claims for Patent: 6,248,741

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Claims for Patent: 6,248,741

Title: Method of using (2-imidazolin-2-ylamino) quinoxalines in treating ocular neural injury
Abstract:The present invention provides a method of providing neuroprotection to a mammal comprising administering to said mammal suffering from or at risk of suffering a noxious action on its nerve cells an effective amount of a compound of formula I to inhibit or prevent nerve cell injury or death ##STR1## wherein the 2-imidazolin-2-ylamino group is in either the 5- or 6-position of the quinoxaline nucleus; x, y and z are in any of the remaining 5-, 6-, 7- or 8-positions and are selected from hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl; and R is an optional substituent in either the 2- or 3-position of the quinoxaline nucleus and may be hydrogen, lower alkyl or lower alkoxy, or pharmaceutically acceptable salts thereof and mixtures thereof. Such noxious action may result from ischemia, e.g. spinal ischemia.
Inventor(s): Wheeler; Larry A. (Irvine, CA), Woldemussie; Elizabeth (Laguna Niguel, CA), Lai; Ronald K. (Irvine, CA)
Assignee: Allergan Sales, Inc. (Irvine, CA)
Application Number:09/655,579
Patent Claims: 1. A method of providing neural protection to a mammal comprising administering to said mammal suffering from or at risk of suffering a noxious action on its nerve cells an effective amount of a compound of formula I to inhibit or prevent nerve cell injury or death ##STR7##

wherein the 2-imidazolin-2-ylamino group is in either the 5- or 6-position of the quinoxaline nucleus; x, y and z are in any of the remaining 5-, 6-, 7- or 8-positions and are selected from hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl; and R is an optional substituent in either the 2- or 3-position of the quinoxaline nucleus and may be hydrogen, lower alkyl or lower alkoxy, or pharmaceutically acceptable salts thereof and mixtures thereof.

2. The method of claim 1 wherein the noxious action is a result of a crushed or compressed nerve.

3. The method of claim 1 wherein the noxious action is a result of ischemia.

4. The method of claim 1 wherein the noxious action is a result of spinal ischemia.

5. The method of claim 4 wherein said compound is administered intrathecally, epidurally or systemically.

6. The method of claim 5 wherein said compound is administered orally or by injection.

7. The method of claim 1 wherein said noxious action is a result of glutamate induced excitotoxic effects on nerve cells.

8. The method of claim 1 wherein said compound is administered in combination with an NMDA antagonist.

9. The method of claim 8 wherein said NMDA antagonist is memantine.

10. The method of claim 1 wherein the compound is 6-methyl-(2-imidazolin-2-ylamino) quinoxaline.

11. The method of claim 1 wherein said compound is administered in an amount sufficient to achieve a serum concentration of from 0.01 nM to 500 nM.
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