发明名称 |
BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS AND USES THEREOF |
摘要 |
β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types. |
申请公布号 |
WO2017024009(A1) |
申请公布日期 |
2017.02.09 |
申请号 |
WO2016US45302 |
申请日期 |
2016.08.03 |
申请人 |
QUADRIGA BIOSCIENCES, INC. |
发明人 |
JANDELEIT, Bernd;FISCHER, Wolf-Nicolas;KOLLER, Kerry J.;RINGOLD, Gordon |
分类号 |
C07C229/34;A61K31/197;A61K31/27;A61K31/336;A61K31/662;A61P35/00;C07C215/68;C07C229/22;C07C229/42;C07C229/60;C07C233/54;C07C237/04;C07C237/30;C07C239/20;C07C271/14;C07C271/22;C07C271/46;C07C309/66;C07D303/46;C07F9/48 |
主分类号 |
C07C229/34 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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