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1.发明授权Synthesis of novel tubulin polymerization inhibitors: benzoylphenylurea (BPU) sulfur analogs 失效新型微管蛋白聚合抑制剂的合成：苯甲酰基苯脲（BPU）硫类似物公开(公告)号：US07595326B2
公开(公告)日：2009-09-29
申请号：US11673519
申请日：2007-02-09
IPC分类号： C07D239/38 , A61K31/505 , A61P35/00
CPC分类号： A61K31/38 , A61K31/404 , A61K31/4152 , A61K31/427 , A61K31/428 , A61K31/505 , C07D239/34 , C07D239/38
摘要： A novel series of BPU analogues were synthesized and evaluated for antitumor activity. In particular, BPU sulfur analogues 6n and 7d were shown to possess up to 10-fold increased potency, when compared to compound 1, against cancer cell lines. 6n was more effective than compound 1 in causing apoptosis of MCF-7 cells. When compared to other drugs with a similar mechanism of action, 6n retained significant ability to inhibit tubulin assembly, with an IC50 of 2.1 μM.
摘要翻译： 合成了一系列新的BPU类似物，并评价其抗肿瘤活性。 特别地，与化合物1相比，BPU硫类似物6n和7d显示与癌细胞系相比具有高达10倍的效力。 6n比化合物1更有效地引起MCF-7细胞凋亡。 与具有相似作用机制的其他药物相比，6n保留显着的抑制微管蛋白装配能力，IC50为2.1μM。
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2.发明申请DESIGN AND SYNTHESIS OF NOVEL TUBULIN POLYMERIZATION INHIBITORS: BENZOYLPHENYLUREA (BPU) SULFUR ANALOGS 失效新型管霉素聚合抑制剂的设计与合成：苯甲酰基苯酚（BPU）硫化物类似物公开(公告)号：US20070232631A1
公开(公告)日：2007-10-04
申请号：US11673519
申请日：2007-02-09
IPC分类号： A61K31/505 , A61P13/12 , A61P19/10 , A61P31/06 , C07D239/38
CPC分类号： A61K31/38 , A61K31/404 , A61K31/4152 , A61K31/427 , A61K31/428 , A61K31/505 , C07D239/34 , C07D239/38
摘要： A novel series of BPU analogues were synthesized and evaluated for antitumor activity. In particular, BPU sulfur analogues 6n and 7d were shown to possess up to 10-fold increased potency, when compared to compound 1, against cancer cell lines. 6n was more effective than compound 1 in causing apoptosis of MCF-7 cells. When compared to other drugs with a similar mechanism of action, 6n retained significant ability to inhibit tubulin assembly, with an IC50 of 2.1 μM.
摘要翻译： 合成了一系列新的BPU类似物，并评价其抗肿瘤活性。 特别地，与化合物1相比，BPU硫类似物6n和7d显示与癌细胞系相比具有高达10倍的效力。 6n比化合物1更有效地引起MCF-7细胞凋亡。 当与具有相似作用机制的其他药物相比时，6n保留显着的抑制微管蛋白装配的能力，其中IC <50>为2.1μM。
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3.发明授权ON01910.Na enhances chemotherapeutic agent activity in drug-resistant tumors 有权ON01910.Na增强耐药肿瘤中的化疗药物活性公开(公告)号：US08962614B2
公开(公告)日：2015-02-24
申请号：US12988471
申请日：2008-04-17
IPC分类号： A61K31/192 , A01N43/04
CPC分类号： A61K31/7076 , A61K31/192 , A61K31/198 , A61K31/7068 , A61K31/713 , A61K2300/00
摘要： The invention includes compositions and methods of treatment of cancers susceptible to treatment with nucleotide analog chemotherapeutic agent, including cancers in which nucleotide analog resistant tumors have developed, including identifying a subject having cancer susceptible to treatment with a nucleotide analog chemotherapeutic agent and a mitotic disruptor/polo-like kinase (Plk) pathway inhibitor to a subject; and monitoring the subject for a reduction or stabilization of at least one sign or symptom of cancer.
摘要翻译： 本发明包括治疗易受核苷酸类似物化疗剂治疗的癌症的组合物和方法，包括其中开发了核苷酸类似物抗性肿瘤的癌症，包括鉴定具有对核苷酸类似物化学治疗剂的治疗敏感的患者和有丝分裂干扰物/ polo样激酶（Plk）途径抑制剂; 以及监测受试者以减少或稳定至少一种癌症的症状或症状。
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4.发明申请Rapid prognostic assay for malignancies treated with epidermal growth factor receptor 审中-公开用表皮生长因子受体治疗的恶性肿瘤的快速预后测定公开(公告)号：US20060188895A1
公开(公告)日：2006-08-24
申请号：US11217657
申请日：2005-08-31
申请人： Piotr Kulesza , Antonio Jimeno , Manuel Hidalgo , Douglas Clark , Erik Kincaid
发明人： Piotr Kulesza , Antonio Jimeno , Manuel Hidalgo , Douglas Clark , Erik Kincaid
IPC分类号： C12Q1/68
CPC分类号： C12Q1/6886 , C12Q2600/158
摘要： A molecular assay for determining the sensitivity or resistance of malignancies to chemotherapy prior to initiation of chemotherapy and which also allows for monitoring the therapeutic effects of the chemotherapy during treatment. The molecular assay measures tumor response to therapy with EGFR modulators and utilizes tumor mRNA as a starting material and a quantitative measurement of c-fos expression as an analytical endpoint.
摘要翻译： 用于在化疗开始之前确定恶性肿瘤对化学疗法的敏感性或耐药性的分子测定法，并且还允许监测治疗期间化疗的治疗效果。 分子测定法测量肿瘤对EGFR调节剂治疗的反应，并利用肿瘤mRNA作为起始物质，并作为分析终点的c-fos表达定量测定。
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5.发明申请SYNTHESIS OF NOVEL TUBULIN POLYMERIZATION INHIBITORS: BENZOYLPHENYLUREA (BPU) SULFUR ANALOGS 审中-公开新型管状体聚合抑制剂的合成：苯甲酰基苯酚（BPU）硫化物类似物公开(公告)号：US20100113491A1
公开(公告)日：2010-05-06
申请号：US12471585
申请日：2009-05-26
IPC分类号： A61K31/505 , C12N5/00 , C07D239/38
CPC分类号： A61K31/38 , A61K31/404 , A61K31/4152 , A61K31/427 , A61K31/428 , A61K31/505 , C07D239/34 , C07D239/38
摘要： A novel series of BPU analogues were synthesized and evaluated for antitumor activity. In particular, BPU sulfur analogues 6n and 7d were shown to possess up to 10-fold increased potency, when compared to compound 1, against cancer cell lines. 6n was more effective than compound 1 in causing apoptosis of MCF-7 cells. When compared to other drugs with a similar mechanism of action, 6n retained significant ability to inhibit tubulin assembly, with an IC50 of 2.1 μM.
摘要翻译： 合成了一系列新的BPU类似物，并评价其抗肿瘤活性。 特别地，与化合物1相比，BPU硫类似物6n和7d显示与癌细胞系相比具有高达10倍的效力。 6n比化合物1更有效地引起MCF-7细胞凋亡。 与具有相似作用机制的其他药物相比，6n保留显着的抑制微管蛋白装配能力，IC50为2.1μM。
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6.发明申请RAPID PROGNOSTIC ASSAY FOR MALIGNANCIES TREATED WITH EPIDERMAL GROWTH FACTOR RECEPTOR 审中-公开用于生长因子受体治疗恶性肿瘤的快速预防性测定公开(公告)号：US20080293069A1
公开(公告)日：2008-11-27
申请号：US12125790
申请日：2008-05-22
IPC分类号： C12Q1/68 , G01N33/574
CPC分类号： C12Q1/6886 , C12Q2600/158
摘要： A molecular assay for determining the sensitivity or resistance of malignancies to chemotherapy prior to initiation of chemotherapy and which also allows for monitoring the therapeutic effects of the chemotherapy during treatment. The molecular assay measures tumor response to therapy with EGFR modulators and utilizes tumor mRNA as a starting material and a quantitative measurement of c-fos expression as an analytical endpoint.
摘要翻译： 用于在化疗开始之前确定恶性肿瘤对化学疗法的敏感性或耐药性的分子测定法，并且还允许监测治疗期间化疗的治疗效果。 分子测定法测量肿瘤对EGFR调节剂治疗的反应，并利用肿瘤mRNA作为起始物质，并作为分析终点的c-fos表达定量测定。
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7.发明申请ON01910.Na ENHANCES CHEMOTHERAPEUTIC AGENT ACTIVITY IN DRUG-RESISTANT TUMORS 有权ON01910.Na增强耐药肿瘤中的化学药物活性公开(公告)号：US20110201675A1
公开(公告)日：2011-08-18
申请号：US12988471
申请日：2008-04-17
IPC分类号： A61K31/7088 , A61K31/198 , A61K31/7076 , A61K31/7068 , A61K31/513 , A61K31/7072 , A61K31/551 , A61K31/52 , A61P35/00
CPC分类号： A61K31/7076 , A61K31/192 , A61K31/198 , A61K31/7068 , A61K31/713 , A61K2300/00
摘要： The invention includes compositions and methods of treatment of cancers susceptible to treatment with nucleotide analog chemotherapeutic agent, including cancers in which nucleotide analog resistant tumors have developed, including identifying a subject having cancer susceptible to treatment with a nucleotide analog chemotherapeutic agent and a mitotic disruptor/polo-like kinase (Plk) pathway inhibitor to a subject; and monitoring the subject for a reduction or stabilization of at least one sign or symptom of cancer.
摘要翻译： 本发明包括治疗易受核苷酸类似物化疗剂治疗的癌症的组合物和方法，包括其中开发了核苷酸类似物抗性肿瘤的癌症，包括鉴定具有对核苷酸类似物化学治疗剂的治疗敏感的患者和有丝分裂干扰物/ polo样激酶（Plk）途径抑制剂; 以及监测受试者以减少或稳定至少一种癌症的症状或症状。
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8.发明申请公开(公告)号：US20090221522A1
公开(公告)日：2009-09-03
申请号：US12372373
申请日：2009-02-17
申请人： Manuel Hidalgo , Antonio Jimeno , Aik Choon Tan
发明人： Manuel Hidalgo , Antonio Jimeno , Aik Choon Tan
IPC分类号： A61K31/7068 , C12Q1/68 , C40B30/00 , A61K31/337 , A61K31/4353 , A61P35/00
CPC分类号： C12Q1/6809
摘要： The present invention comprises a treatment approach based on gene set-expression signatures that systematically connects a sample to a profile from a reference database to extrapolate the most effective therapeutic agent. Further disclosed are methods to optimize combination treatments.
摘要翻译： 本发明包括一种基于基因设定表达特征的处理方法，该方法将样品系统地连接到参考数据库中的分布图，以外推最有效的治疗剂。 进一步公开的是优化组合治疗的方法。
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9.发明申请SYNTHESIS OF NOVEL TUBULIN POLYMERIZATION INHIBITORS: BENZOYLPHENYLUREA (BPU) SULFUR ANALOGS 审中-公开新型管状体聚合抑制剂的合成：苯甲酰基苯酚（BPU）硫化物类似物公开(公告)号：US20090099218A1
公开(公告)日：2009-04-16
申请号：US12211492
申请日：2008-09-16
IPC分类号： A61K31/505 , C07D239/38 , A61K31/513 , C07D239/34 , A61P35/00
CPC分类号： C07D239/34 , C07D239/38
摘要： This invention provides a series of BPU analogues; their synthesis and evaluated biological activity. BPU sulfur analogues were found to possess up to 20 fold increased potency, when compared to compound 1, in various cancerous cell lines.
摘要翻译： 本发明提供了一系列BPU类似物; 其合成和评估生物活性。 与各种癌细胞系中的化合物1相比，发现BPU硫类似物具有高达20倍的效力。
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