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11. 发明授权

US4046878A Daunomycin analogues, their preparation and use 失效
标题翻译：道诺霉素类似物，其制备和用途
公开(公告)号：US4046878A
公开(公告)日：1977-09-06
申请号：US579901
申请日：1975-05-22
申请人： Bianca Patelli , Luigi Bernardi , Federico Arcamone , Aurelio Di Marco
发明人： Bianca Patelli , Luigi Bernardi , Federico Arcamone , Aurelio Di Marco
IPC分类号： A61K31/704 , C07H15/252 , A61K31/71 , C07H11/00
CPC分类号： C07H15/252 , Y10S514/908
摘要： Daunomycin analogues of the formula: ##STR1## wherein when each R.sub.1 is hydrogen, each R is hydrogen, chlorine, bromine, methyl or methoxy and when each R.sub.1 is chlorine, bromine or methyl, each R is hydrogen, are useful in treating various mammalian tumors and are prepared by reacting a daunomycinone derivative of the formula: ##STR2## wherein R and R.sub.1 are as defined above with 1-chloro-2,3,6-trideoxy-3-trifluoroacetamido-4-trifluoroacetoxy-.alpha.-L-lyxopyranose in an inert anhydrous organic solvent in the presence of a catalyst and a hydrogen chloride acceptor.
摘要翻译：道诺霉素类似物，具有下式：其中当每个R 1是氢时，每个R是氢，氯，溴，甲基或甲氧基，并且当每个R 1是氯，溴或甲基时，每个R是氢，可用于治疗各种哺乳动物肿瘤，并且通过使下式的道诺霉素酮衍生物：其中R和R 1如上所定义的道诺霉素酮衍生物与1-氯-2,3,6-三脱氧-3-三氟乙酰氨基-4-三氟乙酰氧基 α-L-吡喃葡萄糖在惰性无水有机溶剂中，在催化剂和氯化氢受体存在下。

12. 发明授权

US4183919A Antitumor glycosides, process for their preparation including intermediates therefor and their use 失效
标题翻译：抗肿瘤糖苷，其制备方法，包括其中间体及其用途
公开(公告)号：US4183919A
公开(公告)日：1980-01-15
申请号：US860447
申请日：1977-12-14
申请人： Giuseppe Cassinelli , Federico Arcamone , Aurelio Di Marco
发明人： Giuseppe Cassinelli , Federico Arcamone , Aurelio Di Marco
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/04 , C07H15/12 , C07H15/252
CPC分类号： C07H15/04 , C07H15/12 , C07H15/252 , Y10S514/908
摘要： Disclosed is a new class of antitumor glycoside antibiotics of the formula (IA): ##STR1## wherein R is hydrogen or hydroxy; and X is ##STR2## These compounds are prepared, using novel intermediates, by condensing the appropriate aglycone and amino-deoxy sugar to form the .alpha.-glycosidic linkage.
摘要翻译：公开了一类新的式（IA）抗肿瘤糖苷抗生素：其中R是氢或羟基; 并且X是这些化合物，通过使用新的中间体，通过将适当的糖苷配基和氨基脱氧糖缩合形成α-糖苷键来制备。

13. 发明授权

US4031211A Adriamycin esters, their preparation and use 失效
标题翻译：阿霉素酯，其制备和用途
公开(公告)号：US4031211A
公开(公告)日：1977-06-21
申请号：US694656
申请日：1976-06-10
申请人： Bianca Patelli , Luigi Bernardi , Federico Arcamone , Aurelio DI Marco
发明人： Bianca Patelli , Luigi Bernardi , Federico Arcamone , Aurelio DI Marco
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。

14. 发明授权

US4254110A Pentofuranosyl anthracyclines, intermediates in and method for their preparation and compositions and use thereof 失效
标题翻译：戊糖醛酸蒽环类抗生素，其中间体及其制备方法及其组合物和用途
公开(公告)号：US4254110A
公开(公告)日：1981-03-03
申请号：US115725
申请日：1980-01-28
申请人： Giuseppe Cassinelli , Federico Arcamone , Aurelio di Marco
发明人： Giuseppe Cassinelli , Federico Arcamone , Aurelio di Marco
IPC分类号： C07D307/20 , A61K31/34 , A61K31/341 , A61P35/00 , C07H15/252 , A61K31/71 , C07H15/24
CPC分类号： C07H15/252
摘要： Antitumor anthracycline glycosides of the formula: ##STR1## wherein one of R.sub.1 and R.sub.2 is hydrogen and the other is formyl, hydroxymethyl or aminomethyl, and R.sub.3 is hydrogen, hydroxy or an acyloxy group; and pharmaceutically acceptable acid addition salts of said compounds in which one of R.sub.1 and R.sub. 2 is aminomethyl are prepared from daunorubicin, doxorubicin or 14-O-acyl derivatives of doxorubicin by deamination and C-3' epimerization effected with NaNO.sub.2 in a cold aqueous acidic medium, such as 1N aqueous acetic acid at 0.degree. C., to give compounds wherein one of R.sub.1 and R.sub.2 is formyl and the optional further steps of selective reduction, e.g., with NaCNBH.sub.3 in 4:1 dioxan:aqueous acetate buffer at pH 4.6 or with Na(CH.sub.3 COO).sub.3 BH in benzene under reflux, to form compounds in which one of R.sub.1 and R.sub.2 hydroxymethyl, or selective reductive amination, e.g., with NaCNBH.sub.3 in the presence of methanolic CH.sub.3 COONH.sub.4 and a dehydrating agent, to form compounds in which one of R.sub.1 and R.sub.2 is aminomethyl.
摘要翻译：下式的抗肿瘤蒽环酸苷：其中R1和R2之一是氢，另一个是甲酰基，羟甲基或氨基甲基，R3是氢，羟基或酰氧基; 和其中R 1和R 2之一是氨基甲基的所述化合物的药学上可接受的酸加成盐通过脱氨基的柔红霉素，多柔比星的多柔比星或14-O-酰基衍生物和用NaNO 2在冷酸水溶液中进行的C-3'差向异构体培养基，如1N乙酸水溶液在0℃下反应，得到其中R1和R2之一为甲酰基的化合物，以及选择性还原步骤的任选的其他步骤，例如在pH4.6的4:1二恶烷：乙酸水溶液缓冲液中的NaCNBH 3 或与Na（CH 3 COO）3·3HH）反应，生成其中R1和R2羟甲基之一或选择性还原胺化的化合物，例如与NaCNBH 3在甲醇CH 3 COONH 4和脱水剂存在下形成化合物，其中一个的R 1和R 2是氨基甲基。

15. 发明授权

US4067968A Daunosamine nucleosides 失效
标题翻译：丹诺胺类核苷
公开(公告)号：US4067968A
公开(公告)日：1978-01-10
申请号：US746851
申请日：1976-12-02
申请人： Ettore Lazzari , Federico Arcamone , Aurelio DI Marco
发明人： Ettore Lazzari , Federico Arcamone , Aurelio DI Marco
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
CPC分类号： 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。

16. 发明授权

US4024224A 14-Aminodaunomycins, their preparation and use 失效
标题翻译： 14-氨基诺乃霉素，其制备和用途
公开(公告)号：US4024224A
公开(公告)日：1977-05-17
申请号：US637170
申请日：1975-12-03
申请人： Federico Arcamone , Luigi Bernardi , Bianca Patelli , Aurelio DI Marco
发明人： Federico Arcamone , Luigi Bernardi , Bianca Patelli , Aurelio DI Marco
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。

17. 发明授权

US4265885A Anthracyclines containing branched-chain amino-deoxy sugars 失效
标题翻译：含有支链氨基脱氧糖的蒽环类
公开(公告)号：US4265885A
公开(公告)日：1981-05-05
申请号：US82293
申请日：1979-10-05
申请人： Alberto Bargiotti , Giuseppe Cassinelli , Federico Arcamone , Aurelio DiMarco
发明人： Alberto Bargiotti , Giuseppe Cassinelli , Federico Arcamone , Aurelio DiMarco
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： A new class of antitumor glycoside antibiotics of the formula (IA): ##STR1## wherein R is hydrogen or hydroxy; and X is ##STR2## These compounds are prepared, using novel intermediates, by condensing the appropriate aglycone and branched-chain aminodeoxy sugar to form the .alpha.-glycosidic linkage.
摘要翻译：一类新的式（IA）抗肿瘤糖苷抗生素：其中R是氢或羟基; 并且X是这些化合物，通过使用新的中间体，通过将适当的糖苷配基和支链氨基脱氧糖缩合形成α-糖苷键来制备。

18. 发明授权

US4600537A Preparation of (.+-.) 4-demethoxy-6 (and-11-)-deoxydaunomycinone 失效
标题翻译：（+/-）4-脱甲氧基-6（和 - 11 - ） - 脱氧果阿霉素酮的制备
公开(公告)号：US4600537A
公开(公告)日：1986-07-15
申请号：US599015
申请日：1984-04-11
申请人： Francesco Angelucci , Sergio Penco , Federico Arcamone
发明人： Francesco Angelucci , Sergio Penco , Federico Arcamone
IPC分类号： C07C50/38 , C07H15/252 , C07C49/423 , C07D307/89
CPC分类号： C07H15/252 , C07C50/38 , Y02P20/55
摘要： (.+-.)4-demethoxy-6(and-11-)-deoxydaunomycinone which are starting materials for anthracycline antitumor antibiotics are prepared by reacting 1,2,3,6-tetrahydrophthalic anhydride with an alcohol of the formula ROH, wherein R is lower alkyl, substituted lower alkyl or aryl to form a monoester, subjecting the monoester to a Friedel-Crafts reaction with acetyl chloride, followed by mild alkaline treatment, to give the corresponding .alpha.,.beta. unsaturated ketone, catalytically reducing same to form the corresponding 4-acetyl-perhydrophthalate reacting the latter with 1,4-dimethoxynaphthalone in the presence of tritluoroacetic anhydride and trifluoroacetic acid to form a mixture of two isomeric compounds, submitting said mixture of isomers to a catalytic reduction of the benzylic carbonyl function, followed by treatment thereof with sulphuric acid at room temperature to afford a mixture of tetracyclic isomers, treating the mixture of tetracyclic isomers with sulphuric acid at 80.degree. C. for one hour to give a 1:1 mixture of the racemic anthracyclinones above mentioned.
摘要翻译：通过使1,2,3,6-四氢邻苯二甲酸酐与式ROH的醇反应，制备作为蒽环类抗肿瘤抗生素原料的（+/-）4-脱甲氧基-6（和-11-） - 脱氧余甘杆菌酮，其中R 是低级烷基，取代的低级烷基或芳基以形成单酯，使单酯与乙酰氯进行Friedel-Crafts反应，然后进行温和的碱处理，得到相应的α，β不饱和酮，催化还原形成相应的 4-乙酰基 - 过氢邻苯二甲酸酐与后者与1,4-二甲氧基萘酮在三氟乙酸酐和三氟乙酸的存在下反应形成两种异构化合物的混合物，将所述异构体混合物引入苄羰基官能团的催化还原，用硫酸在室温下反应，得到四环异构体的混合物，用硫酸在80℃处理四环异构体的混合物， 1小时，得到上述外消旋蒽环霉素的1:1混合物。

19. 发明授权

US4251513A 9-Desacetyl-9-ethylen oxide daunorubicin, process for its manufacture and use therefor 失效
标题翻译： 9-脱乙酰基-9-氧化烯柔红霉素，其制造和使用方法
公开(公告)号：US4251513A
公开(公告)日：1981-02-17
申请号：US877754
申请日：1978-02-14
申请人： Sergio Penco , Francesco Angelucci , Federico Arcamone
发明人： Sergio Penco , Francesco Angelucci , Federico Arcamone
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： 9-Desacetyl-9-ethylen oxide daunorubicin hydrochloride is an effective antitumor antibiotic.
摘要翻译： 9-脱乙酰基-9-乙烯氧化物柔红霉素盐酸盐是一种有效的抗肿瘤抗生素。

20. 发明授权

US4211864A Daunorubicin and doxorubicin labelled with .sup.14 C at the 14-position and processes for their preparation 失效
标题翻译：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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