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1. 发明申请

WO2009036059A2 NOVEL STAT3 PATHWAY INHIBITORS AND CANCER STEM CELL INHIBITORS 审中-公开
标题翻译：新型STAT3途径抑制剂和癌症干细胞抑制剂
公开(公告)号：WO2009036059A2
公开(公告)日：2009-03-19
申请号：PCT/US2008075848
申请日：2008-09-10
申请人： BOSTON BIOMEDICAL INC , JIANG ZHIWEI , LI CHIANG JIA , LI WEI , LEGGETT DAVID
发明人： JIANG ZHIWEI , LI CHIANG JIA , LI WEI , LEGGETT DAVID
IPC分类号： A61K31/505 , A61K31/55 , A61K38/17
CPC分类号： C07D307/92 , A61K31/38 , C07D333/74
摘要： The present invention relates to a novel naphtho class of compounds as Stat3 pathway inhibitors and as cancer stem cell inhibitors; to methods of using such compounds to treat cancer; to methods of using such compounds to treat disorders in a mammal related to aberrent Stat3 pathway activity; to pharmaceutical compositions containing such compounds.
摘要翻译：本发明涉及新的萘酚类化合物作为Stat3途径抑制剂和癌症干细胞抑制剂; 使用这些化合物治疗癌症的方法; 涉及使用这些化合物治疗哺乳动物与异常Stat3途径活性有关的疾病的方法; 含有这些化合物的药物组合物。

2. 发明申请

WO2006020722A3 POLYMER CONJUGATES OF BETA-LAPACHONE AND BETA-LAPACHONE ANALOGS FOR TUMOR TARGETING 审中-公开
标题翻译： BETA-LAPACHONE和BETA-LAPACHONE用于肿瘤靶向的模拟物的聚合物
公开(公告)号：WO2006020722A3
公开(公告)日：2007-02-08
申请号：PCT/US2005028445
申请日：2005-08-11
申请人： ARQULE INC , ASHWELL MARK , LI CHIANG J , TANDON MANISH , LIU YANBIN , LAPIERRE JEAN-MARC , JIANG ZHIWEI
发明人： ASHWELL MARK , LI CHIANG J , TANDON MANISH , LIU YANBIN , LAPIERRE JEAN-MARC , JIANG ZHIWEI
IPC分类号： A61K47/48
CPC分类号： B82Y5/00 , A61K31/785 , A61K47/54 , A61K47/542 , A61K47/64 , A61K47/665
摘要： The present invention relates to polymer-modified quinone-containing and carbonyl-containing therapeutic agents, including polymer-modified ß-lapachone compounds, and methods of treating cancer by administering the polymer-modified therapeutic agents to a subject. Polymer-modification of therapeutic agents, such as ß-lapachone compounds, provides effective transport of polymer-modified therapeutic agents to tumor cells or tumor tissues by exploiting the EPR effect in tumor tissues.
摘要翻译：本发明涉及含有聚合物改性的含醌和含羰基的治疗剂，包括聚合物改性的β-皂草酮化合物，以及通过向受试者施用聚合物改性的治疗剂来治疗癌症的方法。治疗药物如β-皂苷化合物的聚合物修饰通过利用肿瘤组织中的EPR效应来提供聚合物修饰的治疗剂对肿瘤细胞或肿瘤组织的有效转运。

3. 发明申请

WO2004045557A3 NOVEL LAPACHONE COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：新型LAPACHONE化合物及其使用方法
公开(公告)号：WO2004045557A3
公开(公告)日：2004-08-12
申请号：PCT/US0337219
申请日：2003-11-18
申请人： ARQULE INC , JIANG ZHIWEI , REDDY DASHARATHA , ACKERMAN SAMUEL K , SALVESEN JUNE
发明人： JIANG ZHIWEI , REDDY DASHARATHA , ACKERMAN SAMUEL K , SALVESEN JUNE
IPC分类号： A61K20060101 , A61K31/38 , A61K31/382 , A61K31/385 , C07D307/92 , C07D311/92 , C07D327/06 , C07D333/74 , C07D335/08 , C07D335/10
CPC分类号： C07D335/08 , C07D307/92 , C07D311/92 , C07D327/06 , C07D333/74
摘要： The invention provides lapachone analogs and derivatives as well as methods of use thereof. These compounds can be used in pharmaceutical compositions for the treatment or prevention of cell proliferation disorders. These compounds can also be used in the treatment or prevention of psoriasis or cancer or precancerous conditions.
摘要翻译：本发明提供了拉帕酮类似物和衍生物及其使用方法。这些化合物可以用于治疗或预防细胞增殖障碍的药物组合物中。这些化合物也可用于治疗或预防牛皮癣或癌症或癌前病症。

4. 发明申请

WO03011224A3 PHARMACEUTICAL COMPOSITIONS CONTAINING BETA-LAPACHONE, OR DERIVATIVES OR ANALOGS THEREOF, AND METHODS OF USING SAME 审中-公开
标题翻译：含有BETA-LAPACHONE或衍生物或其类似物的药物组合物及其使用方法
公开(公告)号：WO03011224A3
公开(公告)日：2003-05-08
申请号：PCT/US0224262
申请日：2002-07-31
申请人： CYCLIS PHARMACEUTICALS INC , JIANG ZHIWEI , REDDY DASHARATHA G
发明人： JIANG ZHIWEI , REDDY DASHARATHA G
IPC分类号： C07D311/78 , A61K9/08 , A61K9/19 , A61K31/337 , A61K31/352 , A61K47/10 , A61K47/24 , A61K47/30 , A61K47/32 , A61K47/34 , A61K47/40 , A61K47/44 , A61P17/06 , A61P35/00 , A61K31/35 , A61K31/335
CPC分类号： A61K9/0019 , A61K31/337 , A61K31/352 , A61K47/10 , A61K47/24 , A61K47/32 , Y10S514/937 , Y10S514/941 , Y10S514/97 , A61K2300/00
摘要： Beta-lapachone, which is poorly soluble in most pharmaceutically acceptable solvents, has demonstrated significant antineoplastic activity against human cancer lines. The present invention overcomes this significant limitation by teaching novel pharmaceutical compositions comprising a therapeutically effective amount of Beta-lapachone, or a derivative or analog thereof, and a pharmaceutically acceptable solubilizing carrier molecule, which may be at water-solubilizing carrier molecule such as hydroxypropyl- beta -cyclodextrin, or an oil-based solubilizing carrier molecule, for enhancing the solubility of Beta-lapachone in aqueous solution. The therapeutically effective amount of Beta-lapachone, or a derivative or analog thereof, may be complexed with the pharmaceutically acceptable solubilizing carrier molecule in aqueous solution. The novel pharmaceutical compositions may be administered with a second anticancer agent or in combination with radiation therapy. A formulation of Beta-lapachone or a derivative or analog thereof, complexed with a pharmaceutically acceptable solubilizing carrier molecule, wherein the complex can be freeze-dried and when subsequently reconstituted in aqueous solution is substantially soluble is also disclosed. Emulsions of Beta-Lapachone in a pharmaceutically acceptable fat emulsion vehicle are also provided. Also disclosed are methods for treating cancer by administering to a patient the novel pharmaceutical compositions and formulations. Pharmaceutical kits are also provided.
摘要翻译：在大多数药学上可接受的溶剂中溶解性差的β-吡拉酮已经证明对人类癌细胞系具有显着的抗肿瘤活性。本发明通过教导新颖的药物组合物来克服这个显着的限制，该药物组合物包含治疗有效量的β-吡拉酮或其衍生物或类似物，以及药学上可接受的增溶载体分子，其可以在水溶性载体分子例如羟丙基 - β-环糊精或油基增溶载体分子，用于提高β-萘酮在水溶液中的溶解度。 β-吡拉酮或其衍生物或类似物的治疗有效量可与药学上可接受的增溶载体分子在水溶液中络合。新型药物组合物可以与第二抗癌剂一起施用或与放射治疗组合施用。与药学上可接受的增溶载体分子络合的β-拉帕酮或其衍生物或类似物的制剂，其中所述复合物可以冷冻干燥，并且当随后在水溶液中重构时基本上可溶。还提供了在药学上可接受的脂肪乳剂中的β-拉帕酮的乳液。还公开了通过向患者施用新的药物组合物和制剂来治疗癌症的方法。还提供药物包。

5. 发明申请

WO02059103A9 SYNTHESIS OF BETA-LAPACHONE AND ITS INTERMEDIATES 审中-公开
标题翻译： BETA-LAPACHONE及其中间体的合成
公开(公告)号：WO02059103A9
公开(公告)日：2003-01-03
申请号：PCT/US0202359
申请日：2002-01-23
申请人： CYCLIS PHARMACEUTICALS INC , JIANG ZHIWEI , HOGELAND JANE
发明人： JIANG ZHIWEI , HOGELAND JANE
IPC分类号： C07D311/92 , C07B61/00 , C07D311/78 , C07D311/72
CPC分类号： C07D311/78
摘要： A novel process for synthesizing beta -lapachone (beta-lapachone), an agent that has demonstrated significant antineoplastic activity against human cancer lines. The process comprises the conversion of starting material, 2-hydroxy-1,4-naphothoquinone into beta -lapachone intermediate, lapachol. The lapachol is then converted to beta -lapachone by treatment with sulfuric acid and purified by recrystallization from ethanol. This novel process is extremely simple and provides beta -lapachone in excellent quality and high yield.
摘要翻译： β-拉帕酮（β-lapachone）的合成新方法，该试验已显示出对人类癌细胞系具有显着的抗肿瘤活性。该方法包括将起始物质2-羟基-1,4-辛氧基醌转化为β-Lapapone中间体，Lapanhol。然后通过用硫酸处理将皮肤胆固醇转化成β-papone，并通过乙醇重结晶纯化。这种新颖的方法非常简单，提供了优质和高产量的β-lapachone。

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