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公开(公告)号：US20090176705A1
公开(公告)日：2009-07-09
申请号：US12255947
申请日：2008-10-22
IPC分类号： A61K38/17 , A61K31/439 , C07D221/22 , A61K31/711 , C12N5/00 , A61P35/00
CPC分类号： C07D221/22 , A61K47/54
摘要： Pharmaceutical compounds, pharmaceutical compositions and methods of treatment are disclosed, wherein a compound comprises a targeting moiety which, in free form, binds a cell receptor with a dissociation constant Kd of less than about 10−7 M, and a pharmaceutically active moiety, wherein the targeting moiety is other than an oligopeptide, a polypeptide, a peptidomimetic, a protein or a protein domain, and wherein the targeting moiety and the pharmaceutically active moiety are covalently attached. In some aspects, the targeting moiety binds a sigma-2 receptor with high affinity and high specificity, and the pharmaceutically active moiety is a pro-apoptotic peptide moiety. Methods of cancer treatment are disclosed comprising administering a disclosed pharmaceutical compound to a subject in need of thereof. The treatments selectively induce apoptosis in cancer cells. These methods can further comprise co-administration of radiation therapy and/or an additional chemotherapeutic agent.
摘要翻译： 公开了药物化合物，药物组合物和治疗方法，其中化合物包含以游离形式结合小于约10-7M的解离常数Kd的细胞受体的靶向部分和药学活性部分，其中 靶向部分不同于寡肽，多肽，肽模拟物，蛋白质或蛋白质结构域，并且其中靶向部分和药学活性部分共价连接。 在一些方面，靶向部分以高亲和力和高特异性结合σ-2受体，并且药物活性部分是促凋亡肽部分。 公开了癌症治疗方法，其包括将所公开的药物化合物施用于需要其的受试者。 治疗选择性诱导癌细胞凋亡。 这些方法还可以包括放射治疗和/或另外的化学治疗剂的共同给药。
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公开(公告)号：US08143222B2
公开(公告)日：2012-03-27
申请号：US12255947
申请日：2008-10-22
CPC分类号： C07D221/22 , A61K47/54
摘要： Pharmaceutical compounds, pharmaceutical compositions and methods of treatment are disclosed, wherein a compound comprises a targeting moiety which, in free form, binds a cell receptor with a dissociation constant Kd of less than about 10−7 M, and a pharmaceutically active moiety, wherein the targeting moiety is other than an oligopeptide, a polypeptide, a peptidomimetic, a protein or a protein domain, and wherein the targeting moiety and the pharmaceutically active moiety are covalently attached. In some aspects, the targeting moiety binds a sigma-2 receptor with high affinity and high specificity, and the pharmaceutically active moiety is a pro-apoptotic peptide moiety. Methods of cancer treatment are disclosed comprising administering a disclosed pharmaceutical compound to a subject in need of thereof. The treatments selectively induce apoptosis in cancer cells. These methods can further comprise co-administration of radiation therapy and/or an additional chemotherapeutic agent.
摘要翻译： 公开了药物化合物，药物组合物和治疗方法，其中化合物包含以游离形式结合小于约10-7M的解离常数Kd的细胞受体的靶向部分和药学活性部分，其中 靶向部分不同于寡肽，多肽，肽模拟物，蛋白质或蛋白质结构域，并且其中靶向部分和药学活性部分共价连接。 在一些方面，靶向部分以高亲和力和高特异性结合σ-2受体，并且药物活性部分是促凋亡肽部分。 公开了癌症治疗方法，其包括将所公开的药物化合物施用于需要其的受试者。 治疗选择性诱导癌细胞凋亡。 这些方法还可以包括放射治疗和/或另外的化学治疗剂的共同给药。
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公开(公告)号：US20130217647A1
公开(公告)日：2013-08-22
申请号：US13812183
申请日：2011-07-27
IPC分类号： G01N33/574 , A61K31/7072 , A61K31/685
CPC分类号： G01N33/57434 , A61K31/685 , A61K31/7072 , G01N2800/52 , G01N2800/56
摘要： Biomarkers (and suites of biomarkers) relating to prostate cancer are provided, as well as methods for using such biomarkers (ans suites thereof), including early prediction of prostate cancer, disease grading, target identification/validation, and monitoring of drug efficacy.
摘要翻译： 提供了与前列腺癌相关的生物标志物（以及生物标志物的套件），以及使用这些生物标志物（及其适用于其）的方法，包括对前列腺癌的早期预测，疾病分级，靶标鉴定/验证和药物功效的监测。
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