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公开(公告)号：US07888330B2
公开(公告)日：2011-02-15
申请号：US12092999
申请日：2006-11-09
CPC分类号： C07F9/65586 , C07D405/00
摘要： The present invention provides phosphoramidate derivatives of a furanosyluracil analog, FAU, that can effectively deliver FAU monophosphate, or a derivative thereof, intracellularly. FAU-Phosphoramidate diesters can bypass the first step of phosphorylation and be activated intracellularly so as to be converted to nucleoside monophosphates. This results in improved formation of nucleoside triphosphates, and higher incorporation into DNA. The compounds of the invention can be used to treat cancer.
摘要翻译： 本发明提供了呋喃葡萄糖尿类似物（FAU）的氨基磷酸衍生物，其能够在细胞内有效地递送FAU单磷酸酯或其衍生物。 FAU-磷酸酰胺酯二酯可以绕过磷酸化的第一步，并在细胞内活化，以转化成单核苷酸磷酸。 这导致核苷三磷酸的形成得到改善，并且更高的掺入DNA。 本发明的化合物可用于治疗癌症。
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公开(公告)号：US20080292553A1
公开(公告)日：2008-11-27
申请号：US12092999
申请日：2006-11-09
IPC分类号： A61K31/7072 , A61P35/00 , C07H19/10 , A61K49/00
CPC分类号： C07F9/65586 , C07D405/00
摘要： The present invention provides phosphoramidate derivatives of a furanosyluracil analog, FAU, that can effectively deliver FAU monophosphate, or a derivative thereof, intracellularly. FAU-Phosphoramidate diesters can bypass the first step of phosphorylation and be activated intracellularly so as to be converted to nucleoside monophosphates. This results in improved formation of nucleoside triphosphates, and higher incorporation into DNA. The compounds of the invention can be used to treat cancer.
摘要翻译： 本发明提供了呋喃葡萄糖尿类似物（FAU）的氨基磷酸衍生物，其能够在细胞内有效地递送FAU单磷酸酯或其衍生物。 FAU-磷酸酰胺酯二酯可以绕过磷酸化的第一步，并在细胞内活化，以转化成单核苷酸磷酸。 这导致核苷三磷酸的形成得到改善，并且更高的掺入DNA。 本发明的化合物可用于治疗癌症。
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公开(公告)号：US10029023B2
公开(公告)日：2018-07-24
申请号：US14008715
申请日：2012-03-30
申请人： Martin Pomper , Zaver Bhujwalla , Zhihang Chen , Cong Li , Sridhar Nimmagadda , Marie-France Penet , Sangeeta Ray
发明人： Martin Pomper , Zaver Bhujwalla , Zhihang Chen , Cong Li , Sridhar Nimmagadda , Marie-France Penet , Sangeeta Ray
IPC分类号： A61B10/00 , A61B5/00 , A61B8/00 , A61K51/08 , A61K47/48 , A61K49/00 , A61K49/12 , A61K51/06 , A61K9/00 , C12N15/113 , A61K31/513 , A61K31/713 , A61K38/50
摘要： The present invention provides targeted nanoplex molecules which carry multimodality imaging reporters together with target enzyme inhibitors such as siRNAs and target prodrug enzymes, that are useful for theranostic imaging of cells and diseases, including, for example, various cancers, and including metastatic prostate cancer. The nanoplex molecules of the present invention provide a platform technology toward many cancer subtypes and alternative therapeutic targets. Downregulation of specific pathways using targeted enzyme inhibitors further provides unique opportunities to target cancer cells selectively while sparing normal tissue. The nanoplex molecule platform described herein has the ability to deliver multiple siRNA enzyme inhibitors. Methods of diagnosis and treatment of various diseases are also included. The strategy described herein can be useful to down-regulate multi-drug resistance pathways, or repair enzymes with the goal of increasing the efficacy, safety, and efficiency of chemotherapeutic or irradiation therapies.
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公开(公告)号：US20140178300A1
公开(公告)日：2014-06-26
申请号：US14008715
申请日：2012-03-30
申请人： Martin Pomper , Zaver Bhujwalla , Zhihang Chen , Cong Li , Sridhar Nimmagadda , Marie-France Penet , Sangeeta Ray
发明人： Martin Pomper , Zaver Bhujwalla , Zhihang Chen , Cong Li , Sridhar Nimmagadda , Marie-France Penet , Sangeeta Ray
IPC分类号： A61K51/08 , A61K31/513 , A61K31/713 , A61K38/50
CPC分类号： A61K51/083 , A61K9/0019 , A61K31/513 , A61K31/713 , A61K38/50 , A61K47/556 , A61K47/59 , A61K47/60 , A61K47/64 , A61K47/645 , A61K47/65 , A61K47/6929 , A61K49/0032 , A61K49/0054 , A61K49/126 , A61K51/065 , C12N15/113 , C12N2310/14 , C12N2310/141 , C12N2320/30 , C12N2320/32
摘要： The present invention provides targeted nanoplex molecules which carry multimodality imaging reporters together with target enzyme inhibitors such as siRNAs and target prodrug enzymes, that are useful for theranostic imaging of cells and diseases, including, for example, various cancers, and including metastatic prostate cancer. The nanoplex molecules of the present invention provide a platform technology toward many cancer subtypes and alternative therapeutic targets. Downregulation of specific pathways using targeted enzyme inhibitors further provides unique opportunities to target cancer cells selectively while sparing normal tissue. The nanoplex molecule platform described herein has the ability to deliver multiple siRNA enzyme inhibitors. Methods of diagnosis and treatment of various diseases are also included. The strategy described herein can be useful to down-regulate multi-drug resistance pathways, or repair enzymes with the goal of increasing the efficacy, safety, and efficiency of chemotherapeutic or irradiation therapies.
摘要翻译： 本发明提供了靶向的纳米复合物分子，其携带多靶区成像记录物与靶酶抑制剂如siRNA和靶前体药物酶，其可用于细胞和疾病（包括例如各种癌症，包括转移性前列腺癌）的静脉成像。 本发明的纳米复合物分子为许多癌症亚型和替代治疗靶标提供了平台技术。 使用靶向酶抑制剂的特异性途径的下调进一步提供了选择性靶向癌细胞同时保留正常组织的独特机会。 本文描述的纳米复合物分子平台具有递送多种siRNA酶抑制剂的能力。 还包括各种疾病的诊断和治疗方法。 本文描述的策略可用于下调多药耐药途径或修复酶，目的是提高化学治疗或照射疗法的功效，安全性和效率。
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