发明名称 TROPINOL ESTERS AND RELATED COMPOUNDS TO PROMOTE NORMAL PROCESSING OF APP
摘要 In various embodiments, compositions and methods are provided for treatment and/or prevention of amyloidogenic diseases. In certain embodiments, the methods entail administering an effective amount of a tropinol ester to a subject in need thereof for prophylactic or therapeutic effect. The methods are particularly useful for prophylactic and therapeutic treatment of Alzheimer's disease. In certain embodiments, methods of reducing the risk, lessening the severity, or delaying the progression or onset of a disease characterized by beta-amyloid deposits in the brain of a mammal are also provided. In certain embodiments, methods of directly or indirectly inhibiting the C-terminal cleavage of APP resulting in the formation of APP-C31 peptide and APPneo (AP-P664) in a mammal are provided.
申请公布号 US2014364451(A1) 申请公布日期 2014.12.11
申请号 US201214235405 申请日期 2012.08.01
申请人 John Varghese;Bredesen Dale E. 发明人 John Varghese;Bredesen Dale E.
分类号 C07D453/02;C07D451/12 主分类号 C07D453/02
代理机构 代理人
主权项 1. A method of mitigating in a mammal one or more symptoms associated with a disease characterized by amyloid deposits in the brain, or delaying or preventing the onset of said symptoms, said method comprising: administering, or causing to be administered, to said mammal one or more compounds according to a formula selected from the group consisting of: or an enantiomer, a mixture of enantiomers, or a mixture of two or more diastereomers thereof; or a pharmaceutically acceptable salt, ester, amide, solvate, hydrate, or prodrug thereof; wherein R is selected from the group consisting of H, substituted alkyl, unsubstituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heteroaryl, benzofuran, isobenzofuran, indole, isoindole, indazole benzothiophene, benzo[c]thiophene, benzimidazole purine, benzoxazole, benzisoxazole, benzothiazole, naphathalene, quinolone, qinoxaline, isoquinoline, quinazoline, cinnoline, and acridine; R1 is selected from the group consisting of substituted alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, alkylether, phenyl, and substituted phenyl; R is notandwherein said administering is in an amount sufficient to mitigate said one or more symptoms.
地址 San Francisco CA US