APP SPECIFIC BACE INHIBITORS (ASBIs) AND USES THEREOF,申请号US201314384641-传众专利搜索

APP SPECIFIC BACE INHIBITORS (ASBIs) AND USES THEREOF

申请公布号：US2015306122(A1)

申请号：US201314384641

申请日期：2013.03.15

申请公布日期：2015.10.29

申请人：

BUCK INSTITUTE FOR RESEARCH ON AGING

发明人：John Varghese;Bredesen Dale E.

分类号：A61K31/7048;A61K31/352

主分类号：A61K31/7048

地址：NOVATO CA US

摘要：In certain embodiments APP-specific BACE inhibitors (ASBIs) are provided as well as uses thereof. In certain embodiments methods of preventing or delaying the onset of a pre-Alzheimer's condition and/or cognitive dysfunction, and/or ameliorating one or more symptoms of a pre-Alzheimer's condition and/or cognitive dysfunction, or preventing or delaying the progression of a pre-Alzheimer's condition or cognitive dysfunction to Alzheimer's disease are provided where the method involves administering to a subject in need thereof an APP specific BACE inhibitor (ASBI) in an amount sufficient to prevent or delay the onset of a pre-Alzheimer's cognitive dysfunction, and/or to ameliorate one or more symptoms of a pre-Alzheimer's cognitive dysfunction, and/or to prevent or delay the progression of a pre-Alzheimer's cognitive dysfunction to Alzheimer's disease. In certain embodiments the ASBI is a flavonoid (e.g. galangin) or flavonoid progrug (e.g., galangin prodrug).

主权项：1. A method of preventing or delaying the onset of a pre-Alzheimer's condition and/or cognitive dysfunction, and/or ameliorating one or more symptoms of a pre-Alzheimer's condition and/or cognitive dysfunction, or preventing or delaying the progression of a pre-Alzheimer's condition or cognitive dysfunction to Alzheimer's disease, said method comprising: administering to a subject in need thereof an APP specific BACE inhibitor (ASBI) in an amount sufficient to prevent or delay the onset of a pre-Alzheimer's cognitive dysfunction, and/or to ameliorate one or more symptoms of a pre-Alzheimer's cognitive dysfunction, and/or to prevent or delay the progression of a pre-Alzheimer's cognitive dysfunction to Alzheimer's disease, wherein said APP specific BACE inhibitor is a flavonoid characterized by the formula:wherein: R1 is selected from the group consisting of OH, O-saccaharide, O-alkyl, O-trifluoromethyl, O-aryl, O-heteroaryl, and carbamate; R4 and R5 are independently selected from the group consisting of H, OH, NH2, O-alkyl, O-trifluoromethyl, S-alkyl, S-aryl, carboxylate, halogen, NH-alkyl, N,N-dialkyl, NHCO-alkyl, and heteroaryl, alkyl urea, and carbamate; and R2 and R3 are independently selected from the group consisting of H, OH, NH2, O-alkyl, O-trifluoromethyl, S-alkyl, S-aryl, carboxylate, halogen, NH-alkyl, N,N-dialkyl, NHCO-alkyl, heteroaryl, alkyl urea, and carbamate.