发明名称 Fluorenone compounds with modified 7-position substituents for treating and preventing brain and spinal injury
摘要 Neuroprotective drugs are disclosed which are analogs of certain previously known fluorenone compounds. The new analogs have structure (I), 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<1> and Y<2> are halogen, hydrogen, or methyl. These new compounds potently inhibit the unwanted release of excitotoxins by astrocyte cells following an injury or insult to the brain or spinal cord. As an illustration, a number of new analogs were more than 30 times more potent than the previously known lead compound in reducing aspartate release by stressed astrocyte cells. The new analogs can also help reduce swelling in astrocyte cells, and can thereby help promote proper blood flow thrugh the brain following a head injury or other crisis. These new analogs have been shown to work with very good efficacy in <i>in vitro</i> animal models of focal or global brain ischemia. Accordingly, these compounds can reduce brain or spinal cord damage caused by a hypoxic, ischemic, infective, inflammatory, or other injury, crisis, or insult to the brain or spinal cord.
申请公布号 AU6924000(A) 申请公布日期 2001.03.19
申请号 AU20000069240 申请日期 2000.08.22
申请人 QUESTCOR PHARMACEUTICALS, INC. 发明人 EDWARD J. CRAGOE;PAUL J. MARANGOS;TORSTEN R. WEIMANN
分类号 C07C65/40;C07D213/30;C07D263/06;C07D265/06;C07D277/04 主分类号 C07C65/40
代理机构 代理人
主权项
地址