Patent Number: 6,251,898

Title: Medical use of fluorenone derivatives for treating and preventing brain and spinal injury

Abstract: Newly-created fluorenone drugs can be used to prevent, treat, or otherwise reduce damage to a brain or spinal cord following a medical crisis. These new drugs are markedly improved analogs of previously-known fluorenone compounds that were never commercialized or developed into medically useful treatments. The new analogs have the following structure: ##STR1## where X is a lower alkyl, substituted alkyl, or cycloalkyl group, R is selected from certain types of ether, ester, or amide groups, and Y.sup.1 and Y.sup.2 are halogen, hydrogen, or methyl. These new compounds can penetrate a blood-brain barrier and potently inhibit the unwanted release of excitotoxic neurotransmitters by astrocyte cells following an injury or insult to the brain or spinal cord. As an illustration, some of these new analogs were more than 30 times more potent than the previously known best compound in reducing aspartate release by stressed astrocytes. The new analogs also reduce swelling in astrocytes, thereby promoting proper blood flow through the brain and spinal cord following an injury or other crisis. These new analogs have been shown to work with very good efficacy in in vivo animal models of focal or global brain ischemia.

Inventors: Cragoe, Jr.; Edward J. (Nacogdoches, TX), Marangos; Paul J. (La Costa, CA), Weimann; Torsten R. (Cardiff by the Sea, CA)

Assignee: Questcor Pharmaceuticals, Inc.

International Classification: C07D 213/00 (20060101); C07D 213/30 (20060101); C07D 277/00 (20060101); C07D 265/00 (20060101); C07C 65/40 (20060101); C07D 277/04 (20060101); C07D 265/06 (20060101); C07D 263/06 (20060101); C07D 263/00 (20060101); C07C 65/00 (20060101); A61K 031/535 (); A61K 031/42 (); A61K 031/425 (); A61K 031/435 (); A61K 031/415 ()

Expiration Date: 06/26/2018