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81. 发明授权

US5103029A Process for preparing 4-demethoxydaunomycinone 失效
标题翻译：制备4-去甲基联苯胺的方法
公开(公告)号：US5103029A
公开(公告)日：1992-04-07
申请号：US333951
申请日：1989-04-06
申请人： Walter Cabri , Silvia de Bernardinis , Franco Francalanci , Sergio Penco
发明人： Walter Cabri , Silvia de Bernardinis , Franco Francalanci , Sergio Penco
IPC分类号： C07D317/26 , B01J31/02 , B01J31/24 , C07B61/00 , C07C45/00 , C07C46/00 , C07C50/38 , C07C67/00 , C07H15/252
CPC分类号： C07C46/00 , Y02P20/55
摘要： 4-Demethoxy-daunomycinone I: ##STR1## the known aglycone of 4-demethoxy-daunorubicin, is prepared by protecting the 13-keto group of 4-demethyldaunomycinone, sulfonylating the 4-hydroxy group, reacting the sulfonylated compound, in an appropriate reducing environment, with a catalytic amount of a transition metal complex, preferably palladium or nickel with 1,3 diphenylphosphinopropane or 1,1'-bis (diphenylphosphino) ferrocene, and eliminating the 13-dioxolanyl group by treatment with trifluoroacetic acid.

82. 发明授权

US4684629A 3'-deamino-3'-hydroxy-4'-deoxy-4'-amino doxorubicin and related daunorubicin 失效
标题翻译： 3'-脱氨基-3'-羟基-4'-脱氧-4'-氨基多柔比星及相关的柔红霉素
公开(公告)号：US4684629A
公开(公告)日：1987-08-04
申请号：US843264
申请日：1986-03-24
申请人： Alberto Bargiotti , Michele Caruso , Antonino Suarato , Sergio Penco , Fernando Giuliani
发明人： Alberto Bargiotti , Michele Caruso , Antonino Suarato , Sergio Penco , Fernando Giuliani
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P31/04 , A61P35/00 , C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： Anthracycline glycosides of general formula (I) ##STR1## wherein R is hydrogen or hydroxy, and pharmaceutically acceptable salts thereof, are anti-tumor agents.
摘要翻译：通式（I）的蒽环酸苷是抗肿瘤剂，其中R是氢或羟基，及其药学上可接受的盐。

83. 发明授权

US4672057A Morpholino derivatives of daunorubicin and doxorubicin 失效
标题翻译：柔红霉素和多柔比星的吗啉衍生物
公开(公告)号：US4672057A
公开(公告)日：1987-06-09
申请号：US839936
申请日：1986-03-17
申请人： Alberto Bargiotti , Pierangelo Zini , Sergio Penco , Fernando Giuliani
发明人： Alberto Bargiotti , Pierangelo Zini , Sergio Penco , Fernando Giuliani
IPC分类号： C07H19/24 , A61K31/535 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K31/7042 , A61K31/7052 , A61P35/00 , A61P35/02 , C07D413/04 , C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： Anthracycline glycosides of the general formula (A): ##STR1## wherein X is hydrogen or hydroxy and R is hydrogen or a methyl or a hydroxymethyl group; and their pharmaceutically acceptable salts; are useful as antitumor agents.
摘要翻译：通式（A）的蒽环酸苷：其中X是氢或羟基，R是氢或甲基或羟甲基; 及其药学上可接受的盐; 作为抗肿瘤剂有用。

84. 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。

85. 发明授权

US4522815A Anthracycline glycosides 失效
标题翻译：蒽环类苷
公开(公告)号：US4522815A
公开(公告)日：1985-06-11
申请号：US499308
申请日：1983-05-31
申请人： Alberto Bargiotti , Sergio Penco , Anna M. Casazza
发明人： Alberto Bargiotti , Sergio Penco , Anna M. Casazza
IPC分类号： A61K31/704 , C07H15/252 , A61K31/71 , C07H15/24
CPC分类号： C07H15/252 , Y02P20/55
摘要： Disclosed is a process for preparing the glycoside antitumor anthracyclines 7-0-(2,6-dideoxy-.alpha.-L-arabino-hexopyranosyl)-daunomycinone (Ia); 4-demethoxy-7-0-(2,6-dideoxy-.alpha.-L-arabino-hexopyranosyl)-daunomycinone (Ib); 7-0-(2,6-dideoxy-.alpha.-L-arabino-hexopyranosyl)-adriamycinone (Ic); 4-demethoxy-7-0-(2,6-dideoxy-.alpha.-L-arabino-hexopyranosyl)-adriamycinone (Id); 7-0-(2,3,6-trideoxy-.alpha.-L-erythro-hex-2-enopyranosyl)-daunomycinone (IIa); 4-demethoxy-7-0-(2,3,6-trideoxy-.alpha.-L-erythro-hex-2-enopyranosyl)-daunomycinone (IIb); 7-0-(2,3,6-trideoxy-.alpha.-L-erythro-hex-2-enopyranosyl)-adriamycinone (IIc); and 4-demethoxy-7-0-(2,3,6-trideoxy-.alpha.-L-erythro-hex-2-enopyranosyl)-adriamycinone (IId). Compounds Ia, Ib, IIa, IIb are prepared by condensing daunomycinone and 4-demethoxydaunomycinone with 3,4-di-0-acetyl-2,6-dideoxy-.alpha.-L-arabino-hexopyranosyl chloride in an inert solvent in the presence of silver triflate (silver trifluoromethansulfonate), as catalyst, and by removing the protecting groups. Analogously the derivatives Ic, Id, IIc and IId are prepared by condensing a novel reactive protected derivative of adriamycinone and 4-demethoxyadriamycinone in the presence of mercuric bromide/mercuric oxide with the above mentioned sugar halide. The new compounds of the invention are useful in treating certain tumors in mammals.
摘要翻译：公开了制备糖苷抗肿瘤蒽环类抗生素7-0-（2,6-二脱氧-α-α-阿拉伯 - 六吡喃糖基） - 日诺霉素酮（Ia）的方法; 4-脱甲氧基-7-0-（2,6-二脱氧-α-α-阿拉伯 - 六吡喃糖基） - 日诺霉素酮（Ib）; 7-0-（2,6-二脱氧-α-L-阿拉伯 - 六吡喃糖基） - 阿德米霉素（Ic）; 4-脱甲氧基-7-0-（2,6-二脱氧-α-L-阿拉伯 - 六吡喃糖基） - 阿德米霉素（Id）; 7-0-（2,3,6-三脱氧-α-L-赤 - 己-2- -2-吡喃糖基） - 日诺霉素酮（IIa）; 4-脱甲氧基-7-0-（2,3,6-三脱氧-α-L-赤 - 己-2- -2-吡喃糖基） - 日诺霉素酮（IIb）; 7-0-（2,3,6-三脱氧-α-L-赤 - 己-2- -2-吡喃糖基） - 阿德米霉素（IIc）; 和4-脱甲氧基-7-0-（2,3,6-三脱氧-α-L-赤 - 二-2-吡喃葡萄糖基） - 阿德米霉素（IId）。化合物Ia，Ib，IIa，IIb是通过在惰性溶剂中存在下，将道诺霉素酮和4-脱甲氧基多余霉素酮与3,4-二-O-乙酰基-2,6-二脱氧-α-L-阿拉伯 - 六吡喃葡萄酰氯缩合制备的三氟甲磺酸银（三氟甲磺酸银），作为催化剂，除去保护基。类似地，衍生物Ic，Id，IIc和IId是通过在溴化汞/氧化汞存在下与上述卤化糖缩合一种新型的反应性保护的阿霉素和4-脱甲氧基对映体霉素衍生物来制备的。本发明的新化合物可用于治疗哺乳动物中的某些肿瘤。

86. 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。

87. 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。

88. 发明授权

US4131649A Daunorubicin derivatives, their preparation and their use 失效
标题翻译：柔红霉素衍生物，其制备及其用途
公开(公告)号：US4131649A
公开(公告)日：1978-12-26
申请号：US810077
申请日：1977-06-27
申请人： Sergio Penco , Francesco Angelucci , Federico Arcamone
发明人： Sergio Penco , Francesco Angelucci , Federico Arcamone
IPC分类号： A61K31/65 , A61K31/704 , A61P35/00 , C07H15/252 , A61K31/70 , C07H15/24
CPC分类号： C07H15/252 , Y10S514/908
摘要： Daunorubicin (also known as daunomycin) derivatives of the formula ##STR1## wherein X is ##STR2## and R is --COCF.sub.3 or H which are prepared by hydrogenating 9-desacetyl-9-keto-N-trifluoroacetyldaunorubicin, an unexpectedly stable key-intermediate which is itself a new compound, are useful in treating certain mammalian tumors.
摘要翻译：通过氢化9-去乙酰基-9-酮-N-三氟乙酰基柔红霉素制备的式（I）所示的柔红霉素（也称为道诺霉素）衍生物，其中X为“IMA”，R为-COCF 3或H，本身是新化合物的中间体可用于治疗某些哺乳动物肿瘤。

89. 发明授权

US4039663A Daunomycins, process for their uses and intermediates 失效
标题翻译：大赦国际，其使用和中间程序
公开(公告)号：US4039663A
公开(公告)日：1977-08-02
申请号：US560105
申请日：1975-03-19
申请人： Federico Arcamone , Aurelio Di Marco , Sergio Penco
发明人： Federico Arcamone , Aurelio Di Marco , Sergio Penco
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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