发明名称 Proanthocyanidins for the treatment of amyloid and alpha-synuclein diseases such as alzheimer's disease and parkinson's
摘要 A method of treating amyloid, alpha-synuclein or NAC fibrillogenesis in an in vitro environment comprises administrating into the in vitro environment a proanthocyanidin selected from proanthocyanidin characterized by Formula I or Formula II and proanthocyanidin characterized by oligomeric combinations of Formula I and II wherein: n is 2 to 20 R1 and R2 are hydrogen or Hydroxy R3 is hydrogen, optionally substituted O-glycosyl, -C(O)-(optionally substituted aryl) or BC(O)-(optionally substituted heteroaryl); R4 is hydrogen, catechin, epicatechin, epifzelechin or galletes of catechin and epicatechin; The lines at the 2-, 3-, and 4- positions denote R and S configurations; The lines at the 4- and 8- positions in Formula I and the 4- and 6- positions in Formula II denote possible oligomer bonds between individual units. Pharmaceutical compositions can comprises the compounds described, for the treatment of an amyloid disease, or a disease characterized by alpha-synuclein or NAC fibrillogenesis. A method for isolating proanthocyanidin from a plant material comprise dissolving the plant material with ethanol or methanol, or then loading the ethanol/methanol-extracted plant material onto a LH20 column or silica gel column, and eluting the column with a series of increasing proportions of ethanol/methanol to elute the proanthocyanidins and then separating the proanthocyanidin in the extract by reverse phase HPLC and collecting and freeze drying the pure proanthocyanidin.
申请公布号 NZ528322(A) 申请公布日期 2005.03.24
申请号 NZ20020528322 申请日期 2002.02.15
申请人 PROTEOTECH, INC 发明人 SNOW, ALAN D;CASTILLO, GERALDO M;CHOI, PAULA Y;NGUYEN, BETH P
分类号 C07D311/62;A61K31/215;A61K31/35;A61K31/352;A61K31/353;A61K31/40;A61K36/00;A61K36/18;A61K39/385;A61P3/10;A61P25/16;A61P25/28;A61P29/00;A61P35/00;A61P35/02;C07B63/00 主分类号 C07D311/62
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