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A Letter from The Office of the Vice Chancellor for Research

A Letter from The Office of the Vice Chancellor for Research

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OVCR Annual ReportFiscal Year 2011Technology Management & Intellectual PropertyRadiation and adjuvant <strong>the</strong>rapy are not effective in differentiated chondrosarcoma. Moreeffective antitumor reagents <strong>for</strong> chondrosarcoma are needed. <strong>The</strong> present invention utilizes ananti-integrin reagent which has chondrosarcoma tumor cell killing activity in vitro. Promisinganimal data indicates that this is also true in vivo.Primary Investigator: Linda Sandell,Orthopaedic SurgeryAnticonvulsant and Anxiolytic Lactam and Thiolactam DerivativesThis invention relates to lactam and thiolactam derivatives having useful anticonvulsant andanxiolytic activity, pharmaceutical compositions containing <strong>the</strong>se compounds and <strong>the</strong>rapeuticapplications using such compositions. Convulsant seizures occur in various chronic centralnervous system (CNS) disorders, particularly epilepsies. <strong>The</strong>se seizures are generally correlatedwith abnormal and excessive EEG (electroencephalogram) discharges. A variety <strong>of</strong> drugs havebeen used <strong>for</strong> treatment <strong>of</strong> <strong>the</strong>se seizures. <strong>The</strong> compounds covered under this patentsignificantly enhance GABA neuronal inhibition and are more active anticonvulsant andanxiolytic agents than prior art lactones and thiolactones. Fur<strong>the</strong>r, <strong>the</strong>se lactams and thiolactamshave been found to have relatively low toxicity and low sedative activity. Primary Investigator:Doug Covey, Developmental BiologyMethods <strong>of</strong> Prevention and Treatment <strong>of</strong> Ischemic Damage<strong>The</strong> present invention in various embodiments provides methods <strong>of</strong> treating stroke andconferring protection on a population <strong>of</strong> cells associated with ischemia in a subject following anischemic event, comprising: (a) providing an estrogen compound; and (b) administering <strong>the</strong>effective amount <strong>of</strong> <strong>the</strong> compound over a course that includes at least one dose within a timethat is effectively proximate to <strong>the</strong> ischemic event, so as to confer protection on <strong>the</strong> population<strong>of</strong> cells. Novel methods are provided <strong>for</strong> <strong>the</strong> delivery <strong>of</strong> an estrogen compound. Examples <strong>of</strong>ischemic events treatable according to <strong>the</strong> invention are cerebrovascular disease or stroke,subarachnoid subhemorrhage, myocardial infarct, surgery and trauma. A method <strong>of</strong> treatingischemic damage utilizing hormones that are non-sex hormones is also provided. A method <strong>of</strong>treating stroke with ent-17.beta.-estradiol, and a method <strong>of</strong> syn<strong>the</strong>sis, and compounds produced<strong>from</strong> <strong>the</strong> syn<strong>the</strong>sis are provided. Primary Investigator: Doug Covey, Developmental BiologyNeuroactive 13, 24-Cyclo-18, 21-Dinorcholanes and Structurally RelatedPentacyclic Steroids<strong>The</strong> present invention is directed to novel pentacyclic steroids and novel pentacyclic D-homosteroids that have utility as anes<strong>the</strong>tics and in <strong>the</strong> treatment <strong>of</strong> disorders relating to GABAfunction and activity. In addition to anes<strong>the</strong>tic properties, neuroactive steroids may be used totreat disorders related to GABA function. For example, neuroactive steroids may be used assedative-hypnotics e.g. insomnia, mood disorders, convulsive disorders, anxiety, or symptoms <strong>of</strong>ethanol withdrawal. <strong>The</strong>se agents act by enhancing GABA.sub.A receptor desensitization anddisplay different degrees <strong>of</strong> enantioselectivity. <strong>The</strong>se compounds may be useful as memoryenhancers and in reversing <strong>the</strong> anes<strong>the</strong>tic effects <strong>of</strong> compounds that potentiate GABA atGABA.sub.A receptors. Primary Investigator: Doug Covey, Developmental Biology48

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