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公开(公告)号：US4438105A
公开(公告)日：1984-03-20
申请号：US368415
申请日：1982-04-14
IPC分类号： C07H15/24 , A61K31/35 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , A61K31/71
CPC分类号： C07H15/252 , Y10S514/908
摘要： Starting from the known 4'-deoxy-4'-iodo-N-trifluoroacetyldaunorubicin, two new anthracycline glycosidic antibiotics, the 4'-deoxy-4'-iodo-daunorubicin and 4'-deoxy-4'-iodo-doxorubicin, have been prepared by known procedures. Both the new glycosides have been found to be endowed with outstanding antitumoral activity.
摘要翻译： 从已知的4'-脱氧-4'-碘-N-三氟乙酰基柔红霉素开始，两种新的蒽环类抗生素，4'-脱氧-4'-碘柔红霉素和4'-脱氧-4'-碘 - 多柔比星，具有 通过已知程序制备。 这些新的糖苷都被发现具有突出的抗肿瘤活性。
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22.发明授权Antitumor anthracycline glycosides, their preparation, intermediates therefor, and compositions and use thereof 失效抗癌蒽环类苷，其制备方法，其中间体及其组合物和用途
公开(公告)号：US4393052A
公开(公告)日：1983-07-12
申请号：US316058
申请日：1981-10-29
IPC分类号： A61K31/70 , A61K31/7024 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , A61P35/02 , C07D309/30 , C07H13/04 , C07H13/06 , C07H15/04 , C07H15/252 , A61K31/71 , C07H15/22
CPC分类号： C07H15/04 , C07D309/30 , C07H13/04 , C07H15/252 , Y10S514/908
摘要： Novel antitumor anthracycline glycosides are prepared by condensing daunomycinone with 2,3,4,6-tetradeoxy-4-C-methylene-3-trifluoroacetamido-L-threo-hexopyranosyl chloride; 2,3,4,6-tetradeoxy-4-C-methylene-3-trifluoroacetamido-L-arabino-hexopyranosyl chloride or 2,3,6-trideoxy-4-C-trifluoroacetamidomethyl-3-trifluoroacetamido-3-O-trifluoroacetyl-L-lyxo-hexopyranosyl chloride.
摘要翻译： 通过将道诺霉素与2,3,4,6-四脱氧-4-C-亚甲基-3-三氟乙酰氨基-L-苏 - 己酰氯氯化物缩合制备新型抗肿瘤蒽环类苷; 2,3,4,6-四脱氧-4-C-亚甲基-3-三氟乙酰氨基-L-阿拉伯 - 己酸乳酸酰氯或2,3,6-三脱氧-4-C-三氟乙酰氨基甲基-3-三氟乙酰胺基-3-羟基乙酰氨基 -L-胞嘧啶 - 六吡喃葡糖酰氯。
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23.发明授权
公开(公告)号：US4325946A
公开(公告)日：1982-04-20
申请号：US182119
申请日：1980-08-28
IPC分类号： C07H5/06 , A61K31/70 , A61K31/7008 , A61K31/7024 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , A61P35/02 , C07H13/08 , C07H15/252 , A61K31/71 , C07H15/22 , C07H15/24
CPC分类号： C07H13/08 , C07H15/252 , Y02P20/55
摘要： Anthracycline glycosides of the formula I ##STR1## wherein R is hydrogen or hydroxy, one of R.sub.1 and R.sub.2 is methyl and the other of R.sub.1 and R.sub.2 is hydroxy, and pharmaceutically acceptable acid addition salts thereof, which are useful in treating certain mammalian tumors, are prepared by condensing daunomycinone with certain novel sugars in an inert organic solvent and in the presence of a soluble silver salt and a dehydrating agent to form the corresponding protected glycosides from which the protecting groups are removed. This gives the compounds wherein R is hydrogen. The former are converted to the corresponding hydroxyl compounds by treatment with bromine and sodium formate.
摘要翻译： 其中R为氢或羟基的式I的蒽环酸苷，R 1和R 2之一为甲基，R 1和R 2中的另一个为羟基，以及其药学上可接受的酸加成盐，其可用于治疗某些哺乳动物肿瘤 通过在惰性有机溶剂中和在可溶性银盐和脱水剂的存在下将道诺霉素酮与某些新型糖缩合形成保护基被除去的相应的保护的糖苷来制备。 这得到其中R是氢的化合物。 前者通过用溴和甲酸钠处理而转化为相应的羟基化合物。
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公开(公告)号：US4107423A
公开(公告)日：1978-08-15
申请号：US695434
申请日：1976-08-14
IPC分类号： C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： Racemic anthracyclinones of the general formula II ##STR1## when condensed with 2,3,6-trideoxy-3-trifluoroacetamido-4-0-trifluoroacetyl-.alpha.-L-lyxo-pyranosyl chloride in the presence of silver trifluoromethane sulphonate yield an easily separable mixture of equimolar amounts of exclusively the .alpha.-glycoside of the 7S : 9S diastereomer and the .beta.-glycoside of the 7R : 9R diastereomer. In this way the biologically important .alpha.-glycosides of the 7S : 9S diastereomer of the general formula I (below) are easily prepared from a racemic anthracyclinone.
摘要翻译： 在三氟甲磺酸银存在下与2,3,6-三脱氧-3-三氟乙酰胺基-4-0-三氟乙酰-α-L-吡唑并吡喃二氯甲烷缩合时，通式II II的外消旋蒽环类产生容易 7S：9S非对映异构体的α-糖苷和7R：9R非对映异构体的β-糖苷的等摩尔量的可分离混合物。 以这种方式，通式I（下文）的7S：9S非对映异构体的生物学上重要的α-糖苷类可以容易地由外消旋蒽环类抗生素制备。
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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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26.发明授权Daunorubicin and doxorubicin labelled with .sup.14 C at the 14-position and processes for their preparation 失效柔红霉素和多柔比星在14位标记14C并进行制备
公开(公告)号：US4211864A
公开(公告)日：1980-07-08
申请号：US877755
申请日：1978-02-14
申请人： Gian P. Vicario , Sergio Penco , Federico Arcamone
发明人： Gian P. Vicario , Sergio Penco , Federico Arcamone
IPC分类号： A61K51/00 , C07B59/00 , C07H15/252 , C07H15/24
CPC分类号： C07H15/252 , Y02P20/55
摘要： [14-.sup.14 C]-daunorubicin and doxorubicin are prepared by reacting 9-desacetyl-9-formyl-N-trifluoroacetyl daunorubicin with [.sup.14 C]-diazomethane to form [14-.sup.14 C]-N-trifluoroacetyl daunorubicin from which the protecting group is removed by mild alkaline hydrolysis to afford [14-.sup.14 C]-daunorubicin which is then, in the form of the hydrochloride, reacted with bromine to form the corresponding labelled 14-bromo derivative, which, upon treatment with sodium formate leads to [14-.sup.14 C]-doxorubicin.
摘要翻译： [14-14C] - 柔红霉素和多柔比星通过9-去乙酰基-9-甲酰基-N-三氟乙酰柔红霉素与[14C] - 重氮甲烷反应制备[14-14C] -N-三氟乙酰柔红霉素，从其中除去保护基 通过轻度碱性水解得到[14-14C] - 柔红霉素，然后以盐酸盐的形式与溴反应形成相应的标记的14-溴衍生物，其在用甲酸钠处理时，得到[14-14C ] - 二柔比星。
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公开(公告)号：US4039663A
公开(公告)日：1977-08-02
申请号：US560105
申请日：1975-03-19
IPC分类号： C07H13/04 , C07H15/252 , A61K31/71 , C07H11/00
CPC分类号： C07H13/04 , C07H15/252 , Y10S514/908
摘要： The known antibiotic daunomycin, and the novel compounds daunomycin-.beta.-anomer and 4'-epidaunomycin (both .alpha.- and .beta.-anomers) are prepared by condensing daunomycinone with reactive novel intermediates which are 1-chloro-2,3,6-trideoxy-3-trifluoroacetamido-4-trifluoroacetoxy-.alpha.-L-lyxo (or arabino) hexopyranoses.
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公开(公告)号：US5310752A
公开(公告)日：1994-05-10
申请号：US925408
申请日：1992-08-10
IPC分类号： C07D207/34 , C07D409/12 , A61K31/40 , C07D403/14
CPC分类号： C07D409/12 , C07D207/34
摘要： The invention relates to distamycin A analogs of the following formula ##STR1## wherein n is 2, 3 or 4; A is an optionally substituted divalent radical chosen from ##STR2## and --Het-- wherein Het is a pentatomic or hexatomic heteromonocyclic ring, except pyrrole; and wherein either one of R.sub.1 and R.sub.2 is hydrogen and the other is an acylating moiety or R.sub.1 and R.sub.2 are both hydrogen or both alkyl groups optionally substituted, including the pharmaceutically acceptable salts of the said compounds.The compounds of the invention can be useful antitumor and antiviral agents.
摘要翻译： 本发明涉及下列式的分心霉素A类似物：其中n为2,3或4; A是选自以下的任选取代的二价基团：其中Het是五原子或六原子异单环，除了吡咯; 并且其中R 1和R 2中的任一个是氢，而另一个是酰化部分或R 1和R 2都是氢或任选被取代的两个烷基，包括所述化合物的药学上可接受的盐。 本发明的化合物可以是有用的抗肿瘤剂和抗病毒剂。
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公开(公告)号：US5049579A
公开(公告)日：1991-09-17
申请号：US607339
申请日：1990-10-31
IPC分类号： C07D207/34 , C07D409/12
CPC分类号： C07D409/12 , C07D207/34
摘要： The invention relates to distamycin A analogs of the following formula ##STR1## wherein n is 2, 3 or 4; A is an optionally substituted divalent radical chosen from ##STR2## and -Het- wherein Het is a pentatomic or hexatomic heteromonocyclic ring, except pyrrole; and wherein either one of R.sub.1 and R.sub.2 is hydrogen and the other is an acylating moiety or R.sub.1 and R.sub.2 are both hydrogen or both alkyl groups optionally substituted, including the pharmaceutically acceptable salts of the said compounds.The compounds of the invention can be useful antitumor and antiviral agents.
摘要翻译： 本发明涉及下列式的分心霉素A类似物：其中n为2,3或4; A是选自以下的任选取代的二价基团：其中Het是五原子或六原子异单环，除了吡咯; 并且其中R 1和R 2中的任一个是氢，而另一个是酰化部分或R 1和R 2都是氢或任选被取代的两个烷基，包括所述化合物的药学上可接受的盐。 本发明的化合物可以是有用的抗肿瘤剂和抗病毒剂。
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公开(公告)号：US4477444A
公开(公告)日：1984-10-16
申请号：US434509
申请日：1982-10-15
IPC分类号： C07H15/252 , A61K31/70 , C07H15/24
CPC分类号： C07H15/252 , Y02P20/55
摘要： Disclosed is a process for preparing the new antitumor glycosides: 4'-deoxy-3'-epi-daunorubicin and 4'-deoxy-3'-epi-doxorubicin starting from the known 3'-epi-4'-keto-N-trifluoroacetyl-daunorubicin.Reduction of the 4'-keto group with sodium borohydride to the corresponding 4'-hydroxy group, reacting the so obtained intermediate with trifluoromethanesulphonic anhydride followed by treatment with n-tetrabutylammonium iodide, dehalogenated reductively, by treatment with tributyl tin hydride to 4'-deoxy-3'-epi-N-trifluoroacetyl-daunorubicin.A mild alkaline hydrolysis removes the N-protecting group to give 4'-deoxy-3'-epi-daunorubicin which is successively transformed, via its 14-bromo derivative, in its doxorubicin analogue.
摘要翻译： 公开了一种制备新型抗肿瘤糖苷的方法：从已知的3'-表面-4'-酮-n-三磷酸开始制备4'-脱氧-3'-表柔比星和4'-脱氧-3'-表阿霉素， 三氟乙酰柔红霉素。 将4'-酮基用硼氢化钠还原成相应的4'-羟基，使所得中间体与三氟甲磺酸酐反应，然后用正丁基碘化铵处理，还原脱卤，通过用三丁基锡氢化物处理至4'- 脱氧-3'-表N-N-三氟乙酰柔红霉素。 轻度碱性水解除去N-保护基，得到4'-脱氧-3'-表柔比星，其通过其14-溴衍生物在其多柔比星类似物中相继转化。
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