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公开(公告)号:EP0367189A2
公开(公告)日:1990-05-09
申请号:EP89120115.4
申请日:1989-10-30
CPC分类号: C07H17/04
摘要: The present invention relates to antitumor 4′-demethylepipodophyllotoxin glucosides having phosphate or sulfonate substituents on the sugar portion of the molecule.
摘要翻译: 本发明涉及在该分子的糖部分上具有磷酸酯或磺酸酯取代基的抗肿瘤剂4分钟 - 甲氧基表鬼臼毒素葡糖苷。
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公开(公告)号:EP0415453A3
公开(公告)日:1991-04-10
申请号:EP90116779.1
申请日:1990-08-31
发明人: Ohnuma, Takeshi , Hoshi, Hideaki , Kamei, Hideo , Naito, Takayuki
CPC分类号: C07H17/04
摘要: The present invention provides antitumor 4-Demethylepipodophyllotoxin glycosides characterized by the fact that the glycoside moiety is altrose.
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公开(公告)号:EP0401800A2
公开(公告)日:1990-12-12
申请号:EP90110729.2
申请日:1990-06-06
发明人: Ohnuma, Takeshi , Obata, Rika , Kamei, Hideo , Naito, Takayuki
CPC分类号: C07H17/04
摘要: The epipodophyllotoxin glucosides disclosed are acylated at herein one or both sugar hydroxyl groups. These compounds exhibit significant activity against P388 murine leukemia
wherein R² is H and R¹ is selected from the group consisting of (C₁₋₁₀)alkyl, (C₂₋₁₀)alkenyl, (C₅₋₆)cycloalkyl, 2-furyl, 2-thienyl, (C₆₋₁₀)aryl, and (C₇₋₁₄)aralkyl; or R¹ and R² are each (C₁₋₁₀)alkyl; or R¹, R² and the carbon to which they are attached together represent (C₅₋₆)cycloalkyl; one of R³ and R⁴ is H and the other is selected from the group consisting of (C₁₋₅)alkanoyl and benzoyl; or R³ and R⁴ are the same or different and are selected from the group consisting of (C₁₋₅)alkanoyl and benzoyl; R⁵ is H or a phosphate group.摘要翻译: 公开的表鬼臼毒素葡糖苷在本文中是一个或两个糖羟基进行酰化。 这些化合物对P388鼠白血病
显示出显着的活性,其中R 2是H,R 1选自(C 1-10)烷基,(C 2-10)烯基,(C 5-6) 环烷基,2-呋喃基,2-噻吩基,(C6-10)芳基和(C7-14)芳烷基; 或R 1和R 2各自为(C 1-10)烷基; 或R 1,R 2和它们所连接的碳代表(C5-6)环烷基; R 3和R 4之一是H,另一个选自(C 1-5)烷酰基和苯甲酰基; 或R 3和R 4相同或不同,并且选自(C 1-5)烷酰基和苯甲酰基; R 5是H或磷酸基。 -
公开(公告)号:EP0461556A1
公开(公告)日:1991-12-18
申请号:EP91109356.5
申请日:1991-06-07
发明人: Ohnuma, Takeshi , Hoshi, Hideaki
CPC分类号: C07H17/04
摘要: The present invention relates to novel antitumor compounds which are 4'-demethylepipodophyllotoxin derivatives. More particularly, the novel compounds are 4'-demethylepipodophyllotoxin allopyranosides, allofuranosides, and mannopyranosides.
摘要翻译: 本发明涉及新的抗肿瘤化合物,它们是4'-去甲基表鬼臼脂素衍生物。 更具体地说,这些新化合物是4'-去甲基表鬼臼毒素异吡喃糖苷,allofuranoside和甘露吡喃糖苷。
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公开(公告)号:EP0455159A1
公开(公告)日:1991-11-06
申请号:EP91106788.2
申请日:1991-04-26
发明人: Ohnuma, Takeshi , Obata, Rika
CPC分类号: C07H17/04
摘要: The present invention relates to antitumor 4'-demethylepipodophyllotoxin glycosides having the formula
wherein R is a pentose selected from the group consisting of
β-D-ribopyranosyl, peracyl β-D-ribopyranosyl,
β-D-xylopyranosyl, peracyl β-D-xylopyranosyl,
α-D-xylopyranosyl, peracyl α-D-xylopyranosyl,
α-D-arabinopyranosyl,
3,4-O-(C₁₋₄)alkylidene-D-ribopyranosyl,
2-O-acyl-3,4-O-(C₁₋₄)alkylidene-D-ribopyranosyl, and β-D-ribofuranosyl; P is hydrogen, or -PO₃H₂ or a pharmaceutically acceptable salt thereof.摘要翻译: 本发明涉及具有下式的抗肿瘤4'-去甲基表鬼臼脂素糖苷:其中R是选自β-D-吡喃核糖基,戊酰基β-D-吡喃核糖基,β-D-吡喃木糖基,过酰基β-D-吡喃木糖基 ,α-D-吡喃木糖基,过酰基α-D-吡喃木糖基,α-D-阿拉伯吡喃糖基,3,4-O-(C 1-4)亚烷基-D-吡喃核糖基,2-O-酰基-3,4-0- C 1-4)亚烷基-D-吡喃核糖基和β-D-呋喃核糖基; P是氢或-PO 3 H 2或其药学上可接受的盐。
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公开(公告)号:EP0433678A1
公开(公告)日:1991-06-26
申请号:EP90122095.4
申请日:1990-11-19
发明人: Ohnuma, Takeshi , Naito, Takayuki , Kamei, Hideo
CPC分类号: C07H17/04
摘要: Novel cyclic orthoesters and orthocarbonates of 4′-demethylepipodophyllotoxin glucoside of formula I are disclosed in the present invention. These compounds are active against experimental murine P388 leukemia.
wherein one of R¹ and R² is C₁₋₅ alkoxy and the other is selected from the group consisting of hydrogen, C₁₋₅ alkyl, and C₁₋₅ alkoxy; R³ is hydrogen or -P(O)(OM)₂ wherein M is hydrogen or an alkali metal cation.摘要翻译: 在本发明中公开了式I的4分钟的新型环状原酸酯和原碳酸酯 - 式I的甲氧基表鬼臼毒素葡糖苷。 这些化合物对实验鼠P388白血病具有活性。 其中R 1和R 2之一是C 1-5烷氧基,另一个选自氢,C 1-5烷基和C 1-5烷氧基; R 3是氢或-P(O)(OM)2,其中M是氢或碱金属阳离子。
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公开(公告)号:EP0358197A3
公开(公告)日:1991-04-03
申请号:EP89116448.5
申请日:1989-09-06
摘要: The present invention provides antitumor fluoro-substituted 4'-demethylepipodophyllotoxin glucosides.
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公开(公告)号:EP0415453A2
公开(公告)日:1991-03-06
申请号:EP90116779.1
申请日:1990-08-31
发明人: Ohnuma, Takeshi , Hoshi, Hideaki , Kamei, Hideo , Naito, Takayuki
CPC分类号: C07H17/04
摘要: The present invention provides antitumor 4-Demethylepipodophyllotoxin glycosides characterized by the fact that the glycoside moiety is altrose.
摘要翻译: 本发明提供了抗肿瘤4-脱甲基表鬼臼脂素糖苷,其特征在于糖苷部分是阿卓糖。
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公开(公告)号:EP0401800A3
公开(公告)日:1991-04-10
申请号:EP90110729.2
申请日:1990-06-06
发明人: Ohnuma, Takeshi , Obata, Rika , Kamei, Hideo , Naito, Takayuki
CPC分类号: C07H17/04
摘要: The epipodophyllotoxin glucosides disclosed are acylated at herein one or both sugar hydroxyl groups. These compounds exhibit significant activity against P388 murine leukemia
wherein R² is H and R¹ is selected from the group consisting of (C₁₋₁₀)alkyl, (C₂₋₁₀)alkenyl, (C₅₋₆)cycloalkyl, 2-furyl, 2-thienyl, (C₆₋₁₀)aryl, and (C₇₋₁₄)aralkyl; or R¹ and R² are each (C₁₋₁₀)alkyl; or R¹, R² and the carbon to which they are attached together represent (C₅₋₆)cycloalkyl; one of R³ and R⁴ is H and the other is selected from the group consisting of (C₁₋₅)alkanoyl and benzoyl; or R³ and R⁴ are the same or different and are selected from the group consisting of (C₁₋₅)alkanoyl and benzoyl; R⁵ is H or a phosphate group.-
公开(公告)号:EP0367189A3
公开(公告)日:1991-04-10
申请号:EP89120115.4
申请日:1989-10-30
CPC分类号: C07H17/04
摘要: The present invention relates to antitumor 4′-demethylepipodophyllotoxin glucosides having phosphate or sulfonate substituents on the sugar portion of the molecule.
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