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1. 发明申请

US20090042977A1 Anticancer Compound, Intermediate Therefor, and Processes for Producing These 有权
标题翻译：抗癌化合物，其中间体及其生产方法
公开(公告)号：US20090042977A1
公开(公告)日：2009-02-12
申请号：US11885216
申请日：2006-03-15
申请人： Harukuni Tokuda , Katsumi Nishimura
发明人： Harukuni Tokuda , Katsumi Nishimura
IPC分类号： A61K31/343 , C07D307/92 , C07D307/93
CPC分类号： C07D307/92
摘要： The present invention provides a method for easily and inexpensively preparing a racemate or an optically-active 2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]furan-4,9-dione in high yields, 2-acetyl-2,3-dihydro-5-hydroxynaphtho[2,3-b]furan-4,9-dione which is useful as an intermediate for preparing NFD, and an anticancer agent comprising 2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]furan-4,9-dione as an active ingredient.Said 2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]furan-4,9-dione is obtained in 4 or 5 steps by using comparatively inexpensive 5-hydroxynaphthalene-1,4-dione (also referred to as juglone) as a starting material.
摘要翻译：本发明提供了一种以高产率容易且廉价地制备外消旋物或光学活性的2-（1-羟基乙基）-5-羟基萘并[2,3-b]呋喃-4,9-二酮的方法，2-乙酰基 -2,3-二氢-5-羟基萘并[2,3-b]呋喃-4,9-二酮，其可用作制备NFD的中间体，以及抗癌剂，其包含2-（1-羟乙基）-5-羟基萘 [2,3-b]呋喃-4,9-二酮作为活性成分。所述2-（1-羟基乙基）-5-羟基萘并[2,3-b]呋喃-4,9-二酮通过使用相对便宜的5-羟基萘-1,4-二酮（也称为作为胡桃醇）作为原料。

2. 发明授权

US5663197A 2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]furan-4,9-dione and antitumor agents comprising this compound 失效
标题翻译： 2-（1-羟乙基）-5-羟基萘并[2,3-b]呋喃-4,9-二酮和包含该化合物的抗肿瘤剂
公开(公告)号：US5663197A
公开(公告)日：1997-09-02
申请号：US397182
申请日：1995-03-09
申请人： Shinichi Ueda , Harukuni Tokuda , Keiichi Hirai , Heihachi Hatanaka
发明人： Shinichi Ueda , Harukuni Tokuda , Keiichi Hirai , Heihachi Hatanaka
IPC分类号： A61K31/34 , A61K31/343 , A61K36/18 , A61P35/00 , C07D307/92 , C12P17/04 , A61R31/34
CPC分类号： C07D307/92 , C12P17/04
摘要： A novel antitumor compound, 2-(1-hydroxyethyl)-5-hydroxynaphto [2,3-b]furan-4,9-dione, having the following formula is provided. ##STR1##
摘要翻译： PCT No.PCT / JP93 / 01292 Sec。 371日期1995年3月9日 102（e）1995年3月9日PCT PCT 1993年9月10日PCT公布。公开号WO94 / 06786 日期1994年3月31日提供了具有下式的新型抗肿瘤化合物2-（1-羟乙基）-5-羟基萘并[2,3-b]呋喃-4,9-二酮。

3. 发明授权

US07910752B2 Anticancer compound, intermediate therefor, and processes for producing these 有权
标题翻译：抗癌化合物，其中间体及其制备方法
公开(公告)号：US07910752B2
公开(公告)日：2011-03-22
申请号：US11885216
申请日：2006-03-15
申请人： Harukuni Tokuda , Katsumi Nishimura
发明人： Harukuni Tokuda , Katsumi Nishimura
IPC分类号： C07D307/92
CPC分类号： C07D307/92
摘要： The present invention provides a method for easily and inexpensively preparing a racemate or an optically-active 2-(1 -hydroxyethyl)-5-hydroxynaphtho[2,3-b]furan-4,9-dione in high yields, 2-acetyl-2,3-dihydro-5-hydroxynaphtho[2,3-b]furan-4,9-dione which is useful as an intermediate for preparing NFD, and an anticancer agent comprising 2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]furan-4,9-dione as an active ingredient.Said 2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]furan-4,9-dione is obtained in 4 or 5 steps by using comparatively inexpensive 5 -hydroxynaphthalene-1,4-dione (also referred to as juglone) as a starting material.
摘要翻译：本发明提供了一种以高产率容易且廉价地制备外消旋物或光学活性的2-（1-羟基乙基）-5-羟基萘并[2,3-b]呋喃-4,9-二酮的方法，2-乙酰基 -2,3-二氢-5-羟基萘并[2,3-b]呋喃-4,9-二酮，其可用作制备NFD的中间体，以及抗癌剂，其包含2-（1-羟乙基）-5-羟基萘 [2,3-b]呋喃-4,9-二酮作为活性成分。所述2-（1-羟基乙基）-5-羟基萘并[2,3-b]呋喃-4,9-二酮通过使用相对便宜的5-羟基萘-1,4-二酮（也称为作为胡桃醇）作为原料。

4. 发明授权

US06312697B1 Inhibitory effect of synthetic and natural colorants on carcinogenesis 失效
标题翻译：合成和天然着色剂对致癌作用的抑制作用
公开(公告)号：US06312697B1
公开(公告)日：2001-11-06
申请号：US09256206
申请日：1999-02-24
申请人： Govind J. Kapadia , Harukuni Tokuda , Takao Konoshima , Midori Takasaki , Hoyoku Nishino
发明人： Govind J. Kapadia , Harukuni Tokuda , Takao Konoshima , Midori Takasaki , Hoyoku Nishino
IPC分类号： A61K3578
CPC分类号： G01N33/5017
摘要： A method of reducing the percentage of Epstein-Barr virus genome-carrying cells which exhibit Epstein-Barr virus early antigen induction, where the Epstein-Barr virus genone-carrying cells have been cultivated in the presence of at least one tumor-promoting chemical. The method is carried out by cultivating Epstein-Barr virus genome-carrying cells in the presence of a tumor-promoting chemical; and treating the Epstein-Barr virus genome-carrying cells with betanins. The betanins are effectively reduce the incidence of Epstein-Barr virus early antigen induction in the cultivated Epstein-Barr virus genome-carrying cells.
摘要翻译：一种降低表现出爱泼斯坦 - 巴尔病毒早期抗原诱导的爱泼斯坦 - 巴尔病毒基因组携带细胞的百分比的方法，其中在至少一种促肿瘤化学物质存在下培养含有爱泼斯坦 - 巴尔病毒基因的细胞。该方法通过在促进肿瘤的化学物质的存在下培养含有Epstein-Barr病毒基因组的细胞进行; 并用β-甜菜碱治疗带有EB病毒基因组的细胞。甜菜碱有效地降低了Epstein-Barr病毒基因组载体细胞中Epstein-Barr病毒早期抗原诱导的发生率。

5. 发明授权

US5414015A Anti-skin tumor promoting composition 失效
标题翻译：抗皮肤肿瘤促进作用
公开(公告)号：US5414015A
公开(公告)日：1995-05-09
申请号：US2091
申请日：1993-01-08
申请人： Takao Konoshima , Harukuni Tokuda , Munekazu Iinuma , Mizuo Mizuno
发明人： Takao Konoshima , Harukuni Tokuda , Munekazu Iinuma , Mizuo Mizuno
IPC分类号： A61K31/35 , A61K31/352 , A61P35/00 , C07D311/30
CPC分类号： A61K31/35
摘要： An anti-skin tumor promotor comprising a compound of the general formula ##STR1## wherein R means a hydrogen atom or a hydroxyl group. The promotor may be an extract of the crude drug Scutellaria or a synthetic compound.
摘要翻译：一种抗皮肤肿瘤促进剂，其包含通式“IMAGE”的化合物，其中R表示氢原子或羟基。促进剂可以是黄芩生物药物或合成化合物的提取物。

6. 发明申请

US20080300415A1 Preparation of optically active 2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]furan-4, 9-diones having anticancer activities 有权
标题翻译：制备具有抗癌活性的光学活性的2-（1-羟乙基）-5-羟基萘并[2,3-b]呋喃-4,9-二酮
公开(公告)号：US20080300415A1
公开(公告)日：2008-12-04
申请号：US12011759
申请日：2008-01-29
申请人： Akira Iida , Harukuni Tokuda , Mitsuaki Yamashita
发明人： Akira Iida , Harukuni Tokuda , Mitsuaki Yamashita
IPC分类号： C07D307/77
CPC分类号： C07D307/92 , C07D307/79
摘要： An object of the present invention is to provide a method for efficiently preparing (S)-2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]-furan-4,9-dione useful as a medicine at a low cost and in large amounts. According to the present invention, the desired (S)-2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]furan-4,9-dione can be prepared with high efficiency at a low cost and in large amounts by asymmetrically reducing 2-acetyl-5-hydroxynaphtho[2,3-b]furan-4,9-dione in the presence of an asymmetric ruthenium complex and a hydrogen donor.
摘要翻译：本发明的目的是提供一种有效制备（S）-2-（1-羟基乙基）-5-羟基萘并[2,3-b] - 呋喃-4,9-二酮在低成本和大量。根据本发明，可以低成本和大量地制备所需的（S）-2-（1-羟基乙基）-5-羟基萘并[2,3-b]呋喃-4,9-二酮通过在不对称钌络合物和氢供体的存在下不对称还原2-乙酰基-5-羟基萘并[2,3-b]呋喃-4,9-二酮的量。

7. 发明授权

US06291215B1 Inhibitory effects on synthetic and natural colorants on carcinogenes 失效
标题翻译：合成和天然着色剂对致癌物质的抑制作用
公开(公告)号：US06291215B1
公开(公告)日：2001-09-18
申请号：US09256205
申请日：1999-02-24
申请人： Govind J. Kapadia , Harukuni Tokuda , Takao Konoshima , Midori Takasaki , Hoyoku Nishino
发明人： Govind J. Kapadia , Harukuni Tokuda , Takao Konoshima , Midori Takasaki , Hoyoku Nishino
IPC分类号： A61K3135
CPC分类号： G01N33/5017
摘要： A method of reducing the percentage of Epstein-Barr virus genome-carrying cells which exhibit Epstein-Barr virus early antigen induction, where the Epstein-Barr virus genome-carrying cells have been cultivated in the presence of at least one tumor-promoting or tumor-inducing chemical. The method is carried out by cultivating Epstein-Barr virus genome-carrying cells in the presence of a tumor-promoting or tumor-inducing chemical; and treating the Epstein-Barr virus genome-carrying cells with a synthetic fluorescein dye. The dyes effectively reduce the incidence of Epstein-Barr virus early antigen induction in the cultivated Epstein-Barr virus genome-carrying cells.
摘要翻译：一种降低Epstein-Barr病毒基因组携带细胞百分比的方法，其表现出Epstein-Barr病毒早期抗原诱导，其中已经在至少一种肿瘤促进或肿瘤存在下培养了Epstein-Barr病毒基因组携带细胞诱导化学品。该方法通过在肿瘤促进或肿瘤诱导化学品的存在下培养含有Epstein-Barr病毒基因组的细胞进行; 并用合成荧光素染料处理含有Epstein-Barr病毒基因组的细胞。这些染料有效地降低了Epstein-Barr病毒基因组载体细胞中Epstein-Barr病毒早期抗原诱导的发生率。

8. 发明授权

US5935581A Inhibitory effects of synthetic and natural colorants on carcinogenesis 失效
标题翻译：合成和天然着色剂对致癌作用的抑制作用
公开(公告)号：US5935581A
公开(公告)日：1999-08-10
申请号：US845166
申请日：1997-04-21
申请人： Govind J. Kapadia , Harukuni Tokuda , Takao Konoshima , Midori Takasaki , Hoyoku Nishino
发明人： Govind J. Kapadia , Harukuni Tokuda , Takao Konoshima , Midori Takasaki , Hoyoku Nishino
IPC分类号： A61K36/81 , A61K41/00 , G01N33/50 , A61K35/78
CPC分类号： G01N33/5017
摘要： The invention relates to a method of determining the effect of betanins on tumor formation in epidermal tissue in mammals which have been exposed to a substance which initiates or promotes tumor formation by sequentially exposing a first group of mammals to a topically applied chemical substance selected from the group consisting of tumor promoters and tumor initiators; providing the first group of mammals with drinking water containing betanins, said betanin having been extracted from beetroot; measuring a percentage of mammals in the first group which exhibit epidermal tumors; and comparing the percentage of mammals in the first group which exhibit epidermal tumors to a percentage of mammals in a second group which exhibit epidermal tumors, said mammals in the second group having been (a) exposed to a chemical substance selected from the group consisting of tumor promoters and tumor initiators and (b) providing with drinking water containing no betanins.
摘要翻译：本发明涉及一种确定β-葡聚糖对哺乳动物表皮组织中肿瘤形成的影响的方法，所述方法已暴露于通过将第一组哺乳动物依次暴露于选自下列物质的局部施用的化学物质中来引发或促进肿瘤形成的物质由肿瘤启动子和肿瘤引发剂组成的组; 向第一组哺乳动物提供含有甜菜碱的饮用水，所述甜菜碱已从甜菜根中提取出来; 测量显示表皮肿瘤的第一组哺乳动物的百分比; 并且将表现出表皮肿瘤的第一组中的哺乳动物的百分比与表现为表皮肿瘤的第二组中的哺乳动物的百分比进行比较，所述第二组中的哺乳动物已经（a）暴露于选自以下的化学物质：肿瘤启动子和肿瘤引发剂，（b）提供不含甜菜碱的饮用水。

9. 发明申请

US20100215625A1 EFFICIENT PREPARATION OF NAPHTHOQUINONE ANTICANCER ACTIVE INGREDIENTS 审中-公开
标题翻译：有效制备萘普生抗体活性成分
公开(公告)号：US20100215625A1
公开(公告)日：2010-08-26
申请号：US12605684
申请日：2009-10-26
申请人： Akira Iida , Ryuji Takeda , Masafumi Kaneko , Harukuni Tokuda
发明人： Akira Iida , Ryuji Takeda , Masafumi Kaneko , Harukuni Tokuda
IPC分类号： A61K36/185 , C12N5/04 , C07D307/92
CPC分类号： C07D307/92 , A23L33/105 , A23V2002/00 , A61K36/185 , A23V2250/21 , A23V2200/308
摘要： One of the problems to be resolved by the present invention is to stably and sustainably produce active ingredients contained in Bignoniaceous plants of which a mass production is difficult in a conventional manner. The present invention relates to a method for efficiently preparing an anticancer active ingredient NQ801 by a cell cultivation of Bignoniaceous plants under specific culture conditions. An ingredient-production system in the present invention has an anticancer activity.
摘要翻译：通过本发明要解决的问题之一是稳定且可持续地生产常规方式难以大量生产的Bignoniaceous植物中含有的活性成分。本发明涉及通过在特定培养条件下培育Bignoniaceous植物来有效制备抗癌活性成分NQ801的方法。本发明的成分制造系统具有抗癌活性。

10. 发明授权

US07538234B2 Preparation of Optically active 2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]furan-4, 9-diones having anticancer activities 有权
标题翻译：制备具有抗癌活性的光学活性的2-（1-羟乙基）-5-羟基萘并[2,3-b]呋喃-4,9-二酮
公开(公告)号：US07538234B2
公开(公告)日：2009-05-26
申请号：US12011759
申请日：2008-01-29
申请人： Akira Iida , Harukuni Tokuda , Mitsuaki Yamashita
发明人： Akira Iida , Harukuni Tokuda , Mitsuaki Yamashita
IPC分类号： C07D307/92
CPC分类号： C07D307/92 , C07D307/79
摘要： An object of the present invention is to provide a method for efficiently preparing (S)-2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]-furan-4,9-dione useful as a medicine at a low cost and in large amounts. According to the present invention, the desired (S)-2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]furan-4,9-dione can be prepared with high efficiency at a low cost and in large amounts by asymmetrically reducing 2-acetyl-5-hydroxynaphtho[2,3-b]furan-4,9-dione in the presence of an asymmetric ruthenium complex and a hydrogen donor.
摘要翻译：本发明的目的是提供一种有效制备（S）-2-（1-羟基乙基）-5-羟基萘并[2,3-b] - 呋喃-4,9-二酮在低成本和大量。根据本发明，可以低成本和大量地制备所需的（S）-2-（1-羟基乙基）-5-羟基萘并[2,3-b]呋喃-4,9-二酮通过在不对称钌络合物和氢供体的存在下不对称还原2-乙酰基-5-羟基萘并[2,3-b]呋喃-4,9-二酮的量。

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