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公开(公告)号：US5955423A
公开(公告)日：1999-09-21
申请号：US481762
申请日：1995-06-07
申请人： Richard E. Moore , Charles D. Smith , Gregory M. L. Patterson , Susan L. Mooberry , Thomas H. Corbett , Frederick A. Valeriote , Trimurtulu Golakoti
发明人： Richard E. Moore , Charles D. Smith , Gregory M. L. Patterson , Susan L. Mooberry , Thomas H. Corbett , Frederick A. Valeriote , Trimurtulu Golakoti
IPC分类号： C07D273/00 , C07D307/20 , C07D413/06 , A61K38/12 , C07K7/52
CPC分类号： C07D273/00 , C07D307/20 , C07D413/06 , Y10S930/27
摘要： A cryptophycin compound is provided having the structure: ##STR1## Further provided are methods for producing novel cryptophycins from the Nostoc sp. of blue-green algae (cyanobacteria). Pharmaceutical compositions comprising novel cryptophycins are also provided, as are methods for using cryptophycins to inhibit the proliferation of hyperproliferative cells. Further provided are methods for using cryptophycins to inhibit the proliferation of hyperproliferative cells with drug resistant phenotypes, and to treat pathological conditions, such as neoplasia.
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公开(公告)号：US5952298A
公开(公告)日：1999-09-14
申请号：US482141
申请日：1995-06-07
申请人： Richard E. Moore , Charles D. Smith , Gregory M.L. Patterson , Susan L. Mooberry , Thomas H. Corbett , Frederick A. Valeriote , Trimurtulu Golakoti
发明人： Richard E. Moore , Charles D. Smith , Gregory M.L. Patterson , Susan L. Mooberry , Thomas H. Corbett , Frederick A. Valeriote , Trimurtulu Golakoti
IPC分类号： A61K31/395 , C07D273/00 , C07D307/20 , C07D413/06 , A61K38/12 , C07K7/52
CPC分类号： C07D273/00 , A61K31/395 , C07D307/20 , C07D413/06 , Y10S930/27
摘要： A cryptophycin compound is provided having the structure: ##STR1## Further provided are methods for producing novel cryptophycins from the Nostoc sp. of blue-green algae (cyanobacteria). Pharmaceutical compositions comprising novel cryptophycins are also provided, as are methods for using cryptophycins to inhibit the proliferation of hyperproliferative cells. Further provided are methods for using cryptophycins to inhibit the proliferation of hyperproliferative cells with drug resistant phenotypes, and to treat pathological conditions, such as neoplasia.
摘要翻译： 提供了具有以下结构的cryptophycin化合物：还提供了用于从Nostoc sp。生产新型隐球菌素的方法。 的蓝绿色藻类（蓝细菌）。 还提供了包含新型隐球菌素的药物组合物，以及使用隐球菌抑制过度增殖细胞增殖的方法。 还提供了使用隐球菌抑制具有耐药性表型的过度增殖细胞增殖的方法，并且用于治疗诸如瘤形成的病理状况。
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公开(公告)号：US09944597B2
公开(公告)日：2018-04-17
申请号：US15021972
申请日：2014-09-16
申请人： Glen E. Kellogg , Chenxiao Da , Ashutosh Tripathi , John T. Gupton , Nakul Telang , James A. Sikorski , Susan L. Mooberry , Cristina Rohena
发明人： Glen E. Kellogg , Chenxiao Da , Ashutosh Tripathi , John T. Gupton , Nakul Telang , James A. Sikorski , Susan L. Mooberry , Cristina Rohena
IPC分类号： C07D207/34 , C07D207/36 , C07D207/46 , C07D403/04 , C07D403/06 , C07D403/12
CPC分类号： C07D207/34 , C07D207/36 , C07D207/46 , C07D403/04 , C07D403/06 , C07D403/12
摘要： The present invention provides polysubstituted pyrrole compounds, pharmaceutically effective salts, prodrugs, solvates and hydrates thereof, having antimitotic, antiproliferative and cytotoxic activity, activity against cells expressing the drug efflux protein, P-glycoprotein, or cells expressing the β-III isotype of tubulin and antitumor activity. Also provided are methods of utilizing these compounds for inhibiting the proliferation of cancer cells as well as their medical use, in particular for treating cancer, including drug resistant cancer.
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公开(公告)号：US06878699B1
公开(公告)日：2005-04-12
申请号：US09979447
申请日：2000-05-18
IPC分类号： A61K31/56 , A61K31/58 , A61K31/585 , C07J71/00
CPC分类号： C07J71/001 , A61K31/56 , A61K31/58 , A61K31/585 , C07J71/0005 , A61K2300/00
摘要： In accordance with the present invention, there have been identified extracts from a tropical plant that initiate paclitaxel-like microtubule bundling. Bioassay-directed purification yields the steroid taccalonolide A. Taccalonolide, like paclitaxel, initiates the formation of abnormal interphaes and mitotic microtubules. Cells treated with taccalonolide exhibit thick bundles of microtubules that appear to nucleate independent of the microtubule organizing center. Abnormal mitotic spindles consisting of multi-polar spindles are initiated by taccalonolide and resemble abnormal mitotic spindles found in the presence of paclitaxel. Like paclitaxel, taccalonolide causes the breakdown of the nucleus into micronuclei. Taccalonolide causes G2/M arrest, Bc1-2 phosphorylation and initiates an apoptotic cascade that includes the activation of caspase 3. Taccalonolide is an effective inhibitor of proliferation against both SK-OV-3 and MDA-MB-435 cell with IC50 values of 2.3 μM and 2.1 μM respectively. In contrast to paclitaxel, taccalonolide is effective against the multidrug resistant SKVLB-1 cellline and thus appears to be a poor substrate for P-glycoprotein-mediated transport. Although taccalonolide is almost equipotent with paclitaxel in its effects on cellular microtubules, it is much less potent than paclitaxel in its ability to initiate the polymerization of purified tubulin and microtubule protein. Taccalonolide A is the first microtubule stabilizing agent to be discovered from a plant since identification of the mechanism of action of paclitaxel and it is the first natural product steroid identified to have these cellular effects.
摘要翻译： 根据本发明，已经鉴定了引发紫杉醇样微管束的热带植物的提取物。 生物测定导向的纯化产生类固醇塔卡膦酸钠A.塔卡尔诺内酯，如紫杉醇，引发异常干细胞和有丝分裂微管的形成。 用卡可龙内酯处理的细胞表现出浓密的微管束，其似乎独立于微管组织中心成核。 由多极心主轴组成的异常有丝分裂主轴由塔卡膦酸钠引发，并且类似于在紫杉醇存在下发现的异常有丝分裂轴。 像紫杉醇一样，他卡多伦可导致细胞核破裂成微核。 Taccalonolide导致G2 / M阻滞，Bc1-2磷酸化并引发凋亡级联，其包括胱天蛋白酶3的激活。塔卡尔诺内酯是对SK-OV-3和MDA-MB-435细胞增殖的有效抑制剂，IC50值为2.3 亩和2.1亩。 与紫杉醇相反，塔卡洛尔内酯对多药耐药性SKVLB-1细胞有效，因此似乎是P-糖蛋白介导的转运的不良底物。 虽然他卡因内酯与紫杉醇在细胞微管上的作用几乎是等效的，但是它的紫杉醇在启动纯化的微管蛋白和微管蛋白的聚合能力方面的效力要低得多。 塔卡品内酯A是鉴定紫杉醇作用机制后从植物中发现的第一种微管稳定剂，它是被鉴定为具有这些细胞效应的第一种天然产物类固醇。
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5.发明授权2-alkoxyestradiol analogs with antiproliferative and antimitotic activity 失效具有抗增殖和抗有丝分裂活性的2-烷氧基雌二醇类似物公开(公告)号：US06852710B2
公开(公告)日：2005-02-08
申请号：US10412007
申请日：2003-04-11
摘要： The application discloses novel 2-alkoxyestradiol analogs which exhibit anti-proliferative properties, and methods of making and using such compounds to inhibit undesired cell proliferation and tumor growth. Additionally, methods are disclosed of treating diseases associated with undesired angiogenesis and undesired proliferation, and methods of treating infectious disease wherein the infectious agent is particularly susceptible to inhibition by agents that disrupt microtubule organization and function.
摘要翻译： 该申请公开了具有抗增殖性质的新型2-烷氧基雌二醇类似物，以及制备和使用这些化合物以抑制不期望的细胞增殖和肿瘤生长的方法。 此外，公开了治疗与不想要的血管生成和不想要的增殖相关的疾病的方法，以及治疗感染性疾病的方法，其中感染剂特别易于破坏微管组织和功能的药物的抑制。
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公开(公告)号：US07435754B2
公开(公告)日：2008-10-14
申请号：US10126674
申请日：2002-04-19
IPC分类号： A61K31/335 , A61K31/35 , A01N43/02 , A01N43/16
CPC分类号： A61K31/365
摘要： A method of inhibiting the proliferation of a hyperproliferative mammalian cell having a multiple drug resistant phenotype utilizing an amount of a laulimalide compound effective to disrupt the dynamic state of microtubule polymerization and depolymerization to arrest cell mitosis is disclosed, together with laulimalide compounds which find use in such method.
摘要翻译： 公开了一种抑制具有多重耐药性表型的过度增殖性哺乳动物细胞增殖的方法，该方法利用一定量的有效破坏微管聚合和解聚动力学状态以抑制细胞有丝分裂的一半乳酸盐化合物，以及可以用于 这种方法。
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公开(公告)号：US06414015B1
公开(公告)日：2002-07-02
申请号：US09493897
申请日：2000-01-28
IPC分类号： A61P3500
CPC分类号： A61K31/365
摘要： A method of inhibiting the proliferation of a hyperproliferative mammalian cell having a multiple drug resistant phenotype utilizing an amount of a laulimalide compound effective to disrupt the dynamic state of microtubule polymerization and depolymerization to arrest cell mitosis is disclosed, together with laulimalide compounds which find use in such method.
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8.发明授权2-alkoxyestradiol analogs with antiproliferative and antimitotic activity 有权具有抗增殖和抗有丝分裂活性的2-烷氧基雌二醇类似物公开(公告)号：US06593321B2
公开(公告)日：2003-07-15
申请号：US10167208
申请日：2002-06-11
IPC分类号： A61K3156
摘要： The application discloses novel 2-alkoxyestradiol analogs which exhibit anti-proliferative properties, and methods of making and using such compounds to inhibit undesired cell proliferation and tumor growth. Additionally, methods are disclosed of treating diseases associated with undesired angiogenesis and undesired proliferation, and methods of treating infectious disease wherein the infectious agent is particularly susceptible to inhibition by agents that disrupt microtubule organization and function.
摘要翻译： 该申请公开了具有抗增殖性质的新型2-烷氧基雌二醇类似物，以及制备和使用这些化合物以抑制不期望的细胞增殖和肿瘤生长的方法。 此外，公开了治疗与不想要的血管生成和不想要的增殖相关的疾病的方法，以及治疗感染性疾病的方法，其中感染剂特别易于破坏微管组织和功能的药物的抑制。
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