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    METHODS OF CHEMOTHERAPY USING CHEMOTHERAPEUTIC AGENTS BASED ON BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS
    4.
    发明申请
    METHODS OF CHEMOTHERAPY USING CHEMOTHERAPEUTIC AGENTS BASED ON BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS 审中-公开
    使用基于β-取代的氨基酸和类似物的化学治疗剂的化疗方法

    公开(公告)号：US20160346240A1

    公开(公告)日：2016-12-01

    申请号：US15233566

    申请日：2016-08-10

    申请人： Quadriga Biosciences, Inc.

    发明人： Bernd Jandeleit ,  Wolf-Nicolas Fischer ,  Kerry J. Koller ,  Gordon Ringold

    IPC分类号： A61K31/197 ,  A61K31/27 ,  A61K31/255 ,  A61K45/06 ,  A61K31/662

    CPC分类号： A61K31/197 ,  A61K31/255 ,  A61K31/27 ,  A61K31/365 ,  A61K31/42 ,  A61K31/519 ,  A61K31/662 ,  A61K45/06 ,  C07C229/22 ,  C07C229/34 ,  C07C237/04 ,  C07C237/30 ,  C07C239/20 ,  C07C271/46 ,  C07C309/66 ,  C07C309/69 ,  C07F9/3264 ,  C07F9/4816 ,  A61K2300/00

    摘要： Compositions and methods for protecting normal, healthy cells during chemotherapy are disclosed. The methods include administering one or more compounds that inhibit the cell cycle of rapidly regenerating normal cells and a chemotherapeutic agent. The cell cycle inhibitors can be administered prior to administration of a chemotherapeutic agent. The chemotherapeutic agents can be β-substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs. Pharmaceutical compositions comprising the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and uses thereof are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs can be administered in conjunction with one or more compounds that inhibit the cell cycle of rapidly proliferating normal healthy cells. The cell cycle inhibitors can ameliorate the adverse effects of the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs.

    摘要翻译： 公开了在化疗期间保护正常健康细胞的组合物和方法。 所述方法包括施用一种或多种抑制快速再生正常细胞的细胞周期的化合物和化学治疗剂。 细胞周期抑制剂可以在施用化学治疗剂之前施用。 化学治疗剂可以是β-取代的β-氨基酸，β-取代的β-氨基酸衍生物和β-取代的β-氨基酸类似物。 还公开了包含β-取代的β-氨基酸衍生物和β-取代的β-氨基酸类似物的药物组合物及其用途。 β-取代的β-氨基酸衍生物和β-取代的β-氨基酸类似物可以与抑制快速增殖的正常健康细胞的细胞周期的一种或多种化合物联合施用。 细胞周期抑制剂可以改善β-取代的β-氨基酸衍生物和β-取代的β-氨基酸类似物的不利影响。

    BETA-SUBSTITUTED GAMMA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS
    8.
    发明申请
    BETA-SUBSTITUTED GAMMA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS 有权
    经取代的氨基酸氨基酸和类似物作为化学治疗剂

    公开(公告)号：US20160289168A1

    公开(公告)日：2016-10-06

    申请号：US15181020

    申请日：2016-06-13

    申请人： QUADRIGA BIOSCIENCES, INC.

    发明人： Bernd Jandeleit ,  Wolf-Nicolas Fischer ,  Kerry J. Koller

    IPC分类号： C07C229/08 ,  C07C271/46 ,  C07F9/48 ,  C07D257/04 ,  C07C237/30 ,  C07C309/69

    CPC分类号： A61K31/197 ,  A61K31/41 ,  A61K31/662 ,  A61K47/542 ,  C07C229/08 ,  C07C229/42 ,  C07C237/30 ,  C07C239/18 ,  C07C239/20 ,  C07C271/46 ,  C07C309/69 ,  C07D257/04 ,  C07F9/3264 ,  C07F9/48 ,  C07F9/4816

    摘要： β-Substituted γ-amino acids, β-substituted γ-amino acid derivatives, and β-substituted γ-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates, capable of passing through the blood-brain barrier, and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres and methods of using the compounds for treating tumors are also disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an improved selectivity toward tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an increased efficacy on a variety of tumor types.

    摘要翻译： β-取代的γ-氨基酸，β-取代的γ-氨基酸衍生物和β-取代的γ-氨基酸类似物和（生物）等电点及其作为化学治疗剂的用途。 β-取代的γ-氨基酸衍生物和β-取代的γ-氨基酸类似物和（生物）等分子体是能够通过血脑屏障的选择性LAT1 / 4F2hc底物，并且在表达 LAT1 / 4F2hc转运蛋白。 还公开了合成β-取代的γ-氨基酸衍生物和β-取代的γ-氨基酸类似物的方法和（生物）等离子体和使用该化合物治疗肿瘤的方法。 β-取代的γ-氨基酸衍生物和β-取代的γ-氨基酸类似物和（生物）等分子体对于表达LAT1 / 4F2hc转运蛋白的肿瘤细胞显示出改善的选择性，并且当在体内施用于受试者时积累在癌细胞中。 β-取代的γ-氨基酸衍生物和β-取代的γ-氨基酸类似物和（生物）等分子体对各种肿瘤类型表现出增加的功效。