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公开(公告)号：US4067969A
公开(公告)日：1978-01-10
申请号：US722689
申请日：1976-09-13
IPC分类号： A61K31/35 , A61K31/351 , A61K31/65 , A61K31/704 , A61P35/00 , A61P35/02 , C07D309/14 , C07H13/04 , C07H15/252 , A61K31/70 , C07H15/24
CPC分类号： C07H13/04 , C07D309/14 , C07H15/252 , Y02P20/55 , Y10S514/908
摘要： The novel compounds, 4'-deoxy-daunomycin and 4'-deoxy-adriamycin, as well as derivatives thereof are useful as anti-tumor antibiotics. These compounds are prepared by condensing the corresponding aglycone with a novel trifluoracetyl protected reactive halo sugar which is 2,3,4,6-tetradeoxy-3-trifluoroacetamido-L-threo-hexopyranosyl chloride.
摘要翻译： 新型化合物4'-脱氧 - 道诺霉素和4'-脱氧阿霉素及其衍生物可用作抗肿瘤抗生素。 这些化合物通过将相应的糖苷配基与2,3,4,6-四脱氧-3-三氟乙酰胺基-L-苏 - 六吡喃葡萄糖氯化物的新型三氟乙酰基保护的反应性卤代糖缩合来制备。
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公开(公告)号：US4112076A
公开(公告)日：1978-09-05
申请号：US675696
申请日：1976-04-09
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , G04B37/00 , C07H15/24
CPC分类号： C07H15/252 , C07H5/06 , G04B37/0025 , Y02P20/55 , Y10S514/908
摘要： Disclosed is a process for preparing glycoside antitumor antibiotics, including the known compounds daunomycin, adriamycin, 4'-epi-daunomycin and 4'-epi-adriamycin and the novel antibiotics, 3',4'-epi-6'-hydroxydaunomycin, 3',4'-epi-6'-hydroxyadriamycin. 3',4'-epi-daunomycin, 3',4'-epi-adriamycin, 4-demethoxy-4'-epi-daunomycin and 4-demethoxy-4'-epi-adriamycin. Process involves reacting daunomycinone or 4-demethoxy-daunomycinone with a protected 1-halo derivative of 3,4-epi-6-hydroxydaunosamine, 3,4-epi-daunosamine or 4-epi-daunosamine in an inert solvent in the presence of a soluble silver salt catalyst to form a protected derivative of the glycoside antibiotic and removing the protecting groups.
摘要翻译： 公开了一种制备糖苷抗肿瘤抗生素的方法，包括已知的化合物道诺霉素，阿霉素，4'-表柔比星霉素和4'-表阿霉素，以及新型抗生素3'，4'-表 - 6'-羟基天然霉素3 '，4'-表6-hydroxydriamycin。 3'，4'-表柔比星霉素，3'，4'-表阿霉素，4-脱甲氧基-4'-表柔比星霉素和4-脱甲氧基-4'-表阿霉素。 方法包括使道诺霉素酮或4-脱甲氧基道诺霉素酮与3,4-外延-6-羟基丹酰胺，3,4-外延诺胺或4-外 - 柔红霉素的保护的1-卤代衍生物在惰性溶剂中，在 可溶性银盐催化剂以形成糖苷抗生素的被保护的衍生物并除去保护基团。
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公开(公告)号：US4125607A
公开(公告)日：1978-11-14
申请号：US737473
申请日：1976-11-01
IPC分类号： A61K31/65 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： Disclosed is a class of novel daunosaminyl anthracyclinones which are useful in treating Sarcoma 180 ascites.
摘要翻译： 公开了一类可用于治疗肉瘤180腹水的新型氨基甲酰基蒽环类抗生素。
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公开(公告)号：US4031211A
公开(公告)日：1977-06-21
申请号：US694656
申请日：1976-06-10
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , A61P35/02 , C07H15/252 , C07H15/24
CPC分类号： C07H15/252 , Y10S514/908
摘要： Disclosed are novel C-14 adriamycin esters which are useful in the treatment of certain tumors.
摘要翻译： 公开了可用于治疗某些肿瘤的新型C-14阿霉素酯。
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公开(公告)号：US4067968A
公开(公告)日：1978-01-10
申请号：US746851
申请日：1976-12-02
IPC分类号： C07D405/04 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61P35/00 , C07D239/36 , C07H17/02 , C07H19/06 , C07H19/16
摘要： The antitumor efficacy of the known antibiotics daunomycin (daunorubicin) and adriamycin (doxorubicin) is synergized by the use of said antibiotics together with a daunosamine nucleoside. The latter compounds are prepared by condensing a reactive protected daunosamine with a reactive protected heterocyclic base.
摘要翻译： 已知的抗生素道诺霉素（柔红霉素）和阿霉素（多柔比星）的抗肿瘤功效通过使用所述抗生素与柔红霉素核苷进行协同作用。 后一种化合物通过将反应性保护的柔红霉素与反应性保护的杂环碱缩合来制备。
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公开(公告)号：US4024224A
公开(公告)日：1977-05-17
申请号：US637170
申请日：1975-12-03
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C07H15/22 , A61K31/71
CPC分类号： C07H15/252
摘要： 14-Aminodaunomycins, which are prepared by reacting 14-bromodaunomycin with an amine in a solvent at about 20.degree.-60.degree. C. are useful in treating certain tumors such as ascites Sarcoma 180 and solid Sarcoma 180.
摘要翻译： 通过使14-溴原子素霉素与胺在溶剂中在约20-60℃下反应制备的14-氨基诺乃霉素可用于治疗某些肿瘤如腹水肉瘤180和固体肉瘤180。
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