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公开(公告)号：US07101879B2
公开(公告)日：2006-09-05
申请号：US10051663
申请日：2002-01-18
IPC分类号： A61S31/535
CPC分类号： G01N33/5058 , A61K31/00 , A61K31/137 , A61K31/138 , A61K31/192 , A61K31/225 , A61K31/277 , A61K31/40 , A61K31/475 , A61K31/485 , A61K31/55 , G01N33/5008 , G01N33/502 , G01N33/6872 , G01N33/6896 , G01N2500/10 , G01N2800/2821
摘要： The invention involves identification of a mechanism of β-amyloid peptide cytotoxicity, which enables treatment of conditions caused by β-amyloid peptide aggregates by administration of compounds which antagonize the mechanism of cytotoxicity. The invention includes the identification and isolation of compounds which can reduce the neurotoxic effects of such aggregates. Methods for treating conditions resulting from neurotoxic β-amyloid peptide aggregates, such as Alzheimer's disease and pharmaceutical preparations are provided. Also provided are methods for selecting additional compounds which can reduce the neurotoxic effects of β-amyloid aggregates.
摘要翻译： 本发明涉及鉴定β-淀粉样蛋白肽细胞毒性的机制，其能够通过施用拮抗细胞毒性机制的化合物来治疗由β-淀粉样肽聚集体引起的病症。 本发明包括鉴定和分离可降低这种聚集体的神经毒性作用的化合物。 提供了用于治疗由神经毒性β-淀粉样肽聚集体（例如阿尔茨海默病）和药物制剂产生的病症的方法。 还提供了用于选择可以降低β-淀粉样蛋白聚集体的神经毒性作用的其它化合物的方法。
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公开(公告)号：US07067550B2
公开(公告)日：2006-06-27
申请号：US10143534
申请日：2002-05-10
IPC分类号： A61K31/4035
CPC分类号： G01N33/5008 , A61K31/00 , A61K31/137 , A61K31/138 , A61K31/192 , A61K31/225 , A61K31/277 , A61K31/40 , A61K31/4035 , A61K31/475 , A61K31/485 , A61K31/55 , G01N33/502 , G01N33/5058 , G01N33/6896 , G01N2500/10 , G01N2800/2821
摘要： The invention involves identification of a mechanism of β-amyloid peptide cytotoxicity, which enables treatment of conditions caused by β-amyloid peptide aggregates by administration of compounds which antagonize the mechanism of cytotoxicity. The invention includes the identification and isolation of compounds which can reduce the neurotoxic effects of such aggregates. Methods for treating conditions resulting from neurotoxic β-amyloid peptide aggregates, such as Alzheimer's disease and pharmaceutical preparations are provided. Also provided are methods for selecting additional compounds which can reduce the neurotoxic effects of β-amyloid aggregates.
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公开(公告)号：US08535897B2
公开(公告)日：2013-09-17
申请号：US12308593
申请日：2007-06-19
申请人： Brent R. Stockwell
发明人： Brent R. Stockwell
IPC分类号： C12Q1/00 , G01N33/574
CPC分类号： G01N33/5011 , G01N33/6872 , G01N2333/705
摘要： The invention relates to methods for identifying agents, which induce oxidative cell death in a tumor cell. The invention further relates to methods for identifying tumor cells, which are sensitive to agents that induce oxidative cell death. The invention also relates to methods for identifying subjects who are suffering from tumors, which are sensitive to agents that induce oxidative cell death.
摘要翻译： 本发明涉及用于鉴定诱导肿瘤细胞中的氧化性细胞死亡的药剂的方法。 本发明还涉及用于鉴定对诱导氧化性细胞死亡的药物敏感的肿瘤细胞的方法。 本发明还涉及用于识别患有肿瘤的受试者的方法，其对诱导氧化性细胞死亡的药物敏感。
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公开(公告)号：US20120135089A1
公开(公告)日：2012-05-31
申请号：US13256680
申请日：2010-03-17
申请人： Brent R. Stockwell , Ariel Herman
发明人： Brent R. Stockwell , Ariel Herman
IPC分类号： A61K33/24 , A61K31/515 , C12N9/99 , C07D471/04 , A61K31/573 , A61K31/5377 , A61K38/12 , A61K31/704 , A61K31/675 , A61K31/7048 , C07D403/06 , A61K31/437
CPC分类号： A61K31/535
摘要： The present invention provides, e.g., compounds having the structure of formula (I): The present invention also provides pharmaceutical compositions that include such compounds, and methods for modulating murine double minute 2 protein (Mdm2) E3 ligase activity, particularly the Mdm2-MdmX hetero-complex E3 ligase activity, using such compounds.
摘要翻译： 本发明提供了例如具有式（I）结构的化合物：本发明还提供包含这些化合物的药物组合物和调节鼠双分钟2蛋白（Mdm2）E3连接酶活性的方法，特别是Mdm2-MdmX 异构体E3连接酶活性，使用这种化合物。
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公开(公告)号：US20100081654A1
公开(公告)日：2010-04-01
申请号：US12583579
申请日：2009-08-21
IPC分类号： A61K31/5365 , C07D471/04 , A61K31/437 , C07D498/14
CPC分类号： C07D471/04
摘要： Compounds with cancer cell specific lethality are provided. In particular, RAS-selective lethal compounds and compositions are provided. Also provided are methods of screening for such compounds and methods of treating a condition in a mammal, by administering to the mammal a therapeutically effective amount of such compounds or compositions.
摘要翻译： 提供具有癌细胞特异性致死性的化合物。 特别地，提供RAS选择性致死化合物和组合物。 还提供了筛选这些化合物的方法和通过向哺乳动物施用治疗有效量的这种化合物或组合物来治疗哺乳动物的病症的方法。
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公开(公告)号：US07358262B2
公开(公告)日：2008-04-15
申请号：US10767018
申请日：2004-01-29
申请人： Brent R. Stockwell
发明人： Brent R. Stockwell
IPC分类号： A61K31/02 , A61K31/185 , A61K31/445
CPC分类号： C07D295/185 , C07D239/90 , G01N33/5011
摘要： The present invention relate to methods of identifying a genotype-selective agent. In certain embodiments, the invention relates to agents that are selectively toxic to engineered human tumorigenic cells.
摘要翻译： 本发明涉及识别基因型选择性试剂的方法。 在某些实施方案中，本发明涉及对工程化的人致瘤细胞有选择性毒性的药剂。
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7.发明授权Combinations of chlorpromazine and pentamidine for the treatment of neoplastic disorders 失效组合氯丙嗪和喷他脒治疗肿瘤性疾病公开(公告)号：US06569853B1
公开(公告)日：2003-05-27
申请号：US09706929
申请日：2000-11-06
IPC分类号： A61K3154
CPC分类号： A61K45/06 , A61K31/155 , A61K31/495 , A61K31/54 , A61K31/5415 , A61K31/135 , A61K2300/00
摘要： The invention features a method for treating a patient having a cancer or other neoplasm, by administering to the patient (i) chlorpromazine or a metabolite or analog thereof; and (ii) pentamidine or a metabolite or analog thereof simultaneously or within 14 days of each other in amounts sufficient to inhibit the growth of the neoplasm.
摘要翻译： 本发明的特征在于通过给予患者（i）氯丙嗪或其代谢物或类似物来治疗患有癌症或其他肿瘤的患者的方法; 和（ii）戊脒或其代谢物或类似物同时或彼此之间的14天内以足以抑制肿瘤生长的量。
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公开(公告)号：US08546421B1
公开(公告)日：2013-10-01
申请号：US12583579
申请日：2009-08-21
IPC分类号： A61K31/437 , C07D471/04 , C07D495/04
CPC分类号： C07D471/04
摘要： Compounds with cancer cell specific lethality are provided. In particular, RAS-selective lethal compounds and compositions are provided. Also provided are methods of screening for such compounds and methods of treating a condition in a mammal, by administering to the mammal a therapeutically effective amount of such compounds or compositions.
摘要翻译： 提供具有癌细胞特异性致死性的化合物。 特别地，提供RAS选择性致死化合物和组合物。 还提供了筛选这些化合物的方法和通过向哺乳动物施用治疗有效量的这种化合物或组合物来治疗哺乳动物的病症的方法。
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9.发明申请IDENTIFICATION OF ANTI-CANCER COMPOUNDS AND COMPOUNDS FOR TREATING HUNTINGTON'S DISEASE AND METHODS OF TREATMENT THEREOF 审中-公开用于治疗亨廷顿病的抗癌化合物和化合物的鉴定及其治疗方法公开(公告)号：US20100022637A1
公开(公告)日：2010-01-28
申请号：US11992867
申请日：2006-09-29
申请人： Brent R. Stockwell , Inese Smukste
发明人： Brent R. Stockwell , Inese Smukste
CPC分类号： C07D407/12 , C07D307/68 , C07D309/04 , C07D405/06 , C07D405/14 , C07D493/10 , C07D495/04
摘要： Small molecule screening via high-throughput screening (HTS) methods was employed to identify compounds useful for treating or preventing cancer (such as compounds that enable cells to overcome E6-oncoprotein-mediated drug resistance) or neurodegenerative disorders (such as Huntington's disease, HD). Compounds were identified that potentiate the lethality of anti-tumor agents as well as rescue a disease-state lethality. These compounds are acylated secondary amines referred to herein as indoxins and revertins.
摘要翻译： 使用通过高通量筛选（HTS）方法的小分子筛选来鉴定可用于治疗或预防癌症的化合物（例如使细胞克服E6-癌蛋白介导的药物抗性的化合物）或神经变性疾病（例如亨廷顿氏病，HD ）。 鉴定出化合物能增强抗肿瘤药物的致死性，并拯救疾病致死率。 这些化合物是本文称为茚满素和revertins的酰化仲胺。
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公开(公告)号：US07109377B2
公开(公告)日：2006-09-19
申请号：US10185364
申请日：2002-06-27
IPC分类号： C07C233/00
CPC分类号： C07D307/33 , B01J19/0046 , B01J2219/00317 , B01J2219/00364 , B01J2219/00367 , B01J2219/005 , B01J2219/00511 , B01J2219/00531 , B01J2219/00585 , B01J2219/00596 , B01J2219/00605 , B01J2219/0061 , B01J2219/00612 , B01J2219/0065 , B01J2219/00659 , B01J2219/00702 , C07C227/10 , C07C231/12 , C07C235/40 , C07C237/20 , C07C237/24 , C07C247/14 , C07C2601/14 , C07C2601/16 , C07D261/20 , C07D493/04 , C40B40/00 , C40B60/14 , C40B80/00 , G01N33/50 , Y10S435/975 , C07C229/34
摘要： The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
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