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1.发明申请公开(公告)号：US20110112176A1
公开(公告)日：2011-05-12
申请号：US12940083
申请日：2010-11-05
申请人： John Frederick Boylan , Birgit Bramlage , Wei He , Markus Hossbach , Ingo Roehl
发明人： John Frederick Boylan , Birgit Bramlage , Wei He , Markus Hossbach , Ingo Roehl
IPC分类号： A61K31/713 , C07H21/02 , C12N15/63 , C12N5/10 , A61P35/00
CPC分类号： C12N15/113 , C12N2310/14 , C12N2310/315 , C12N2310/3515
摘要： The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of a KIF10 gene. The invention also relates to a pharmaceutical composition comprising the dsRNA or nucleic acid molecules or vectors encoding the same together with a pharmaceutically acceptable carrier; methods for treating diseases caused by the expression of a KIF10 gene using said pharmaceutical composition; and methods for inhibiting the expression of KIF10 in a cell.
摘要翻译： 本发明涉及用于抑制KIF10基因表达的双链核糖核酸（dsRNA）。 本发明还涉及包含dsRNA或核酸分子的药物组合物或其编码与其药学上可接受的载体的载体; 用于使用所述药物组合物治疗由KIF10基因表达引起的疾病的方法; 以及抑制细胞中KIF10表达的方法。
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公开(公告)号：US08946176B2
公开(公告)日：2015-02-03
申请号：US13275377
申请日：2011-10-18
IPC分类号： C12N15/113 , C12N9/02
CPC分类号： C12N15/1137 , A01K67/00 , A61K48/00 , C12N9/0093 , C12N15/1135 , C12N2310/14 , C12N2310/315 , C12N2310/321 , C12N2310/33 , C12N2310/335 , C12N2310/346 , C12N2310/351 , C12N2310/50 , C12N2310/53 , C12Y117/04001
摘要： The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of a RRM2 gene. The invention also relates to a pharmaceutical composition comprising the dsRNA or nucleic acid molecules or vectors encoding the same together with a pharmaceutically acceptable carrier; methods for treating diseases caused by the expression of a RRM2 gene using said pharmaceutical composition; and methods for inhibiting the expression of RRM2 in a cell.
摘要翻译： 本发明涉及用于抑制RRM2基因表达的双链核糖核酸（dsRNA）。 本发明还涉及包含dsRNA或核酸分子的药物组合物或其编码与其药学上可接受的载体的载体; 使用所述药物组合物治疗由RRM2基因表达引起的疾病的方法; 以及抑制细胞中RRM2表达的方法。
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公开(公告)号：US20120159657A1
公开(公告)日：2012-06-21
申请号：US13275377
申请日：2011-10-18
IPC分类号： A01K67/00 , C12N5/00 , A61P35/00 , C12N15/63 , C12N15/113 , A61K31/713
CPC分类号： C12N15/1137 , A01K67/00 , A61K48/00 , C12N9/0093 , C12N15/1135 , C12N2310/14 , C12N2310/315 , C12N2310/321 , C12N2310/33 , C12N2310/335 , C12N2310/346 , C12N2310/351 , C12N2310/50 , C12N2310/53 , C12Y117/04001
摘要： The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of a RRM2 gene. The invention also relates to a pharmaceutical composition comprising the dsRNA or nucleic acid molecules or vectors encoding the same together with a pharmaceutically acceptable carrier; methods for treating diseases caused by the expression of a RRM2 gene using said pharmaceutical composition; and methods for inhibiting the expression of RRM2 in a cell.
摘要翻译： 本发明涉及用于抑制RRM2基因表达的双链核糖核酸（dsRNA）。 本发明还涉及包含dsRNA或核酸分子的药物组合物或其编码与其药学上可接受的载体的载体; 使用所述药物组合物治疗由RRM2基因表达引起的疾病的方法; 以及抑制细胞中RRM2表达的方法。
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4.发明申请公开(公告)号：US20130072543A1
公开(公告)日：2013-03-21
申请号：US13541891
申请日：2012-07-05
申请人： John Frederick Boylan , Wei He
IPC分类号： A61K47/22
CPC分类号： A61K47/22 , A61K9/1271 , A61K9/5123 , A61K31/7105 , C12N15/88 , Y10S977/773
摘要： The invention relates to compositions containing compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R, R1, R2, R3, and n are defined in the detailed description and claims. In addition, the present invention relates to novel formulations containing compounds of formula I for improved delivery of nucleic acids such as siRNA to the cytoplasm of target cells. In particular embodiments these formulations comprise compounds of formula I, phospholipids, cholesterol, and pegylated lipids. The present invention also relates to methods of manufacturing and using such compounds and compositions.
摘要翻译： 本发明涉及包含式I化合物及其药学上可接受的盐的组合物，其中R，R 1，R 2，R 3和n在详细描述和权利要求书中定义。 此外，本发明涉及含有式I化合物的新型制剂，用于将核酸如siRNA转移至靶细胞的细胞质。 在具体实施方案中，这些制剂包含式I化合物，磷脂，胆固醇和聚乙二醇化脂质。 本发明还涉及制备和使用这些化合物和组合物的方法。
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公开(公告)号：US08309299B2
公开(公告)日：2012-11-13
申请号：US13098527
申请日：2011-05-02
申请人： John Frederick Boylan , Wei He
发明人： John Frederick Boylan , Wei He
CPC分类号： G01N33/57407 , G01N2333/5412 , G01N2333/5421 , G01N2800/52
摘要： The present invention relates to a method for determining a subject's resistance to treatment with 2,2-dimethyl-N-((S)-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)-N′-(2,2,3,3,3-pentafluoro-propyl)-malonamide by measuring the levels a biomarker or biomarkers present in a biological sample obtained from the subject, the biomarker being IL6 and/or IL8. The present invention also relates to a combination therapy for a patient suffering from a proliferative disorder comprising administering to the patient 2,2-Dimethyl-N-((S)-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)-N′-(2,2,3,3,3-pentafluoro-propyl)-malonamide and an anti-IL6 and/or an anti-IL8 agent.
摘要翻译： 本发明涉及一种用2,2-二甲基-N - （（S）-6-氧代-6,7-二氢-5H-二苯并[b，d]氮杂-7-基） （2,2,3,3,3-五氟 - 丙基） - 丙二酰胺，通过测量从受试者获得的生物样品中存在的生物标志物或生物标志物的水平，生物标志物是IL6和/或IL8。 本发明还涉及患有增殖性病症的患者的联合疗法，其包括向患者施用2,2-二甲基-N - （（S）-6-氧代-6,7-二氢-5H-二苯并[b ，d]氮杂-7-基）-N' - （2,2,3,3,3-五氟 - 丙基） - 丙二酰胺和抗IL6和/或抗IL8剂。
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公开(公告)号：US20110287025A1
公开(公告)日：2011-11-24
申请号：US13098527
申请日：2011-05-02
申请人： John Frederick Boylan , Wei He
发明人： John Frederick Boylan , Wei He
IPC分类号： A61K39/395 , A61K31/55 , G01N33/48 , A61K31/713 , A61P35/00 , C07K16/24 , C12Q1/68 , A61K31/7088
CPC分类号： G01N33/57407 , G01N2333/5412 , G01N2333/5421 , G01N2800/52
摘要： The present invention relates to a method for determining a subject's resistance to treatment with 2,2-dimethyl-N—((S)-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)-N′-(2,2,3,3,3-pentafluoro-propyl)-malonamide by measuring the levels a biomarker or biomarkers present in a biological sample obtained from the subject, the biomarker being IL6 and/or IL8. The present invention also relates to a combination therapy for a patient suffering from a proliferative disorder comprising administering to the patient 2,2-Dimethyl-N—((S)-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)-N′-(2,2,3,3,3-pentafluoro-propyl)-malonamide and an anti-IL6 and/or an anti-IL8 agent.
摘要翻译： 本发明涉及一种用2,2-二甲基-N - （（S）-6-氧代-6,7-二氢-5H-二苯并[b，d]氮杂-7-基） （2,2,3,3,3-五氟 - 丙基） - 丙二酰胺，通过测量从受试者获得的生物样品中存在的生物标志物或生物标志物的水平，生物标志物是IL6和/或IL8。 本发明还涉及患有增殖性病症的患者的联合疗法，其包括向患者施用2,2-二甲基-N - （（S）-6-氧代-6,7-二氢-5H-二苯并[b ，d]氮杂-7-基）-N' - （2,2,3,3,3-五氟 - 丙基） - 丙二酰胺和抗IL6和/或抗IL8剂。
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公开(公告)号：US20120225860A1
公开(公告)日：2012-09-06
申请号：US13400280
申请日：2012-02-20
CPC分类号： A61K31/55
摘要： There are provided a new dosage regimens for the gamma secretase inhibitor 2,2-Dimethyl-N-((S)-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)-N′-(2,2,3,3,3-pentafluoro-propyl)-malonamide which maximizes anti-tumor activity while maintaining acceptable toxicity levels.
摘要翻译： 为γ-分泌酶抑制剂提供新的剂量方案2,2-二甲基-N - （（S）-6-氧代-6,7-二氢-5H-二苯并[b，d]氮杂-7-基） - N' - （2,2,3,3,3-五氟 - 丙基） - 丙二酰胺，其在保持可接受的毒性水平的同时使抗肿瘤活性最大化。
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公开(公告)号：US20090181944A1
公开(公告)日：2009-07-16
申请号：US12348464
申请日：2009-01-05
CPC分类号： A61K31/55 , A61K31/7068 , A61K2300/00
摘要： The present invention provides a method for treating a patient having cancer comprising administering to the patient a therapeutically effective amount of compound (1), or a pharmaceutically acceptable salt thereof, having the formula: The present invention also provides a kit containing the above compound.
摘要翻译： 本发明提供了治疗患有癌症的患者的方法，包括向患者施用治疗有效量的具有下式的化合物（1）或其药学上可接受的盐：本发明还提供了含有上述化合物的试剂盒。
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9.发明授权Method of treating non-small cell lung cancer and colon cancer with gamma-secretase inhibitor 失效用γ-分泌酶抑制剂治疗非小细胞肺癌和结肠癌的方法公开(公告)号：US08741889B2
公开(公告)日：2014-06-03
申请号：US13450629
申请日：2012-04-19
IPC分类号： C07D313/06 , A61K31/55 , A61P35/04
CPC分类号： A61K31/55 , C07D223/22
摘要： The present invention provides a method for treating a patient having cancer comprising administering to the patient a therapeutically effective amount of compound (1), or a pharmaceutically acceptable salt thereof, having the formula: The present invention also provides a kit containing the above compound.
摘要翻译： 本发明提供了治疗患有癌症的患者的方法，包括向患者施用治疗有效量的具有下式的化合物（1）或其药学上可接受的盐：本发明还提供了含有上述化合物的试剂盒。
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公开(公告)号：US20130281437A1
公开(公告)日：2013-10-24
申请号：US13450629
申请日：2012-04-19
IPC分类号： A61K31/55 , C07D225/08 , A61P35/00
CPC分类号： A61K31/55 , C07D223/22
摘要： The present invention provides a method for treating a patient having cancer comprising administering to the patient a therapeutically effective amount of compound (1), or a pharmaceutically acceptable salt thereof, having the formula: The present invention also provides a kit containing the above compound.
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