发明名称 Imaging beta-amyloid peptides and inhibition of beta-amyloid peptide aggregation
摘要 The present invention is in the field of pharmaceuticals and chemical industries. In particular, the present invention relates to methods for labeling, imaging and detecting the beta-amyloid (Aβ) peptides, oligomers, and fibrils in vitro by using carbazole-based fluorophores. A further aspect of the present invention relates to a method of reducing and preventing aggregation of beta-amyloid peptides for Alzheimer's disease (AD) as well as of treating and/or preventing Alzheimer's disease by using carbazole-based fluorophores.
申请公布号 US9403794(B2) 申请公布日期 2016.08.02
申请号 US201414231724 申请日期 2014.03.31
申请人 HONG KONG BAPTIST UNIVERSITY 发明人 Guo Lei;Xu Di;Ho See-Lok;Poon Chung-Yan;Ng Olivia T. W.;Li Hung Wing;Yung Ken K. L.;Kwong Daniel W. J.;Wong Ricky M. S.
分类号 A61K49/10;A61K49/00;C07D401/06;A61K49/08;A61K31/4709;A61K45/06 主分类号 A61K49/10
代理机构 Ella Cheong Hong Kong 代理人 Ella Cheong Hong Kong ;Yip Sam T.
主权项 1. A method for treating beta amyloid (Aβ) peptides aggregation-associated diseases and preventing development and progression of said diseases due to increased beta-amyloid aggregates-induced neurotoxicity by administering carbazole-based fluorophores comprising a formula S series: said method comprising: binding said carbazole-based fluorophores to Aβ peptides, oligomers and/or fibrils thereof; inhibiting the growth and/or aggregation of said Aβ peptides, oligomers and/or fibrils upon said binding; and protecting neuronal cells against neurotoxic activities of the Aβ oligomers and/or fibrils; wherein Ar is a heteraromatic ring selected from the group consisting of pyridinyl, substituted pyridinyl, quinolinyl, substituted quinolinyl, acridinyl, substituted acridinyl, benzothiazolyl, substituted benzothiazolyl, benzoxazolyl, and substituted benzoxazolyl; R1 is a radical selected from the group consisting of polyethylene glycol chain, alkyl, substituted alkyl, peptide chain, glycosidyl, and C(O)NHCH((CH2CH2O)2CH3)2; R2 is selected from the group consisting of ethenyl, ethynyl, azo and azomethinyl, R3 is a radical selected from the group consisting of HO-alkyl, alkyl-COOalkyl, alkyl-CONH2, alkyl-CONHalkyl, polyethylene glycol chain; X is an anion selected from the group consisting of F, Cl, Br, I, HSO4, H2PO4, HCO3, tosylate, and mesylate; Y is selected from the group consisting of H, F, Cl, OH, and OCH3, and wherein when Y is H, R3 cannot be HO-alkyl.
地址 Kowloon Tong, Kowloon HK