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1. 发明授权

US4218440A Antitumordeoxy-anthracyclines and use thereof 失效
标题翻译：抗过氧 - 蒽环类抗生素及其用途
公开(公告)号：US4218440A
公开(公告)日：1980-08-19
申请号：US941920
申请日：1978-09-13
申请人： Sergio Penco , Giuliano Franchi , Federico Arcamone
发明人： Sergio Penco , Giuliano Franchi , Federico Arcamone
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , A61K31/71 , C07H15/24
CPC分类号： C07H15/252
摘要： Compounds having the formula: ##STR1## wherein R is H or OH, and which are useful in treating certain mammalian tumors, are prepared from 9,10-anhydro-N-trifluoroacetyldaunorubicin, a known compound.
摘要翻译：具有下式的化合物：其中R是H或OH，可用于治疗某些哺乳动物肿瘤的化合物由已知化合物9,10-脱氢-N-三氟乙酰基柔红霉素制备。

2. 发明授权

US4325947A 4-Demethoxy-4'-deoxydoxorubicin 失效
标题翻译： 4-脱甲氧基-4'-脱氧阿霉素
公开(公告)号：US4325947A
公开(公告)日：1982-04-20
申请号：US263002
申请日：1981-05-12
申请人： Sergio Penco , Giuliano Franchi , Federico Arcamone , Annamaria Casazza
发明人： Sergio Penco , Giuliano Franchi , Federico Arcamone , Annamaria Casazza
IPC分类号： C07H15/252 , A61K31/70 , C07H15/24
CPC分类号： C07H15/252 , Y02P20/55
摘要： A new anthracycline glycoside, which is 4-demethoxy-4'-deoxydoxorubicin, provided with outstanding antitumoral activity also by oral route, has been prepared by condensation of 4-demethoxydaunomycinone with 2,3,4,6-tetradeoxy-3-trifluoroacetamido-L-threo-hexopyranosyl chloride.By elimination of the protecting group from the so obtained glycoside through a mild alkaline hydrolysis, 4-demethoxy-4'-deoxydaunorubicin was obtained which was successively brominated to give the corresponding 14-bromo derivative. By a subsequent hydrolysis with sodium formate the brominated intermediate was transformed into 4-demethoxy-4'-deoxydoxorubicin eventually isolated as its hydrochloride.
摘要翻译：通过口服途径提供了具有优异抗肿瘤活性的4-脱甲氧基-4'-脱氧阿霉素的新型蒽环苷类糖苷，已经通过4-脱甲氧基多霉素酮与2,3,4,6-四脱氧-3-三氟乙酰氨基 - L-苏 - 六吡喃葡萄糖。通过轻度碱性水解从所得糖苷中除去保护基，得到4-脱甲氧基-4'-脱氧阿诺醌，依次溴化得到相应的14-溴衍生物。随后用甲酸钠水解，将溴化中间体转化为最终以其盐酸盐分离的4-脱甲氧基-4'-脱氧阿霉素。

3. 发明授权

US4169142A Disaccharide analogs of antitumor anthracyclines, process for their preparation and use thereof 失效
标题翻译：抗癌蒽环类药物的二糖类似物，其制备方法和用途
公开(公告)号：US4169142A
公开(公告)日：1979-09-25
申请号：US851165
申请日：1977-11-14
申请人： Sergio Penco , Giuliano Franchi , Federico Arcamone
发明人： Sergio Penco , Giuliano Franchi , Federico Arcamone
IPC分类号： A61K31/65 , A61P35/00 , C07H15/252 , A61K31/70 , C07G11/00
CPC分类号： C07H15/252
摘要： Anthracycline disaccharides having antitumor activity are prepared by condensing N-trifluoroacetyldaunomycin with a 1-halosugar in the presence of a silver salt such as AgSO.sub.3 CF.sub.3 as catalyst to form a protected di-glycoside which upon mild alkaline hydrolysis yields the novel disaccharides.
摘要翻译：具有抗肿瘤活性的蒽环类二糖通过在银盐如AgSO 3 CF 3作为催化剂的存在下将N-三氟乙酰基青霉素与1-卤代糖缩合形成受保护的二糖苷，通过温和的碱水解产生新的二糖来制备。

4. 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。

5. 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。

6. 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。

7. 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。

8. 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.

9. 发明授权

US4563444A Anthracycline glycosides, use and compositions containing same 失效
标题翻译：蒽环类苷，用途和含有它们的组合物
公开(公告)号：US4563444A
公开(公告)日：1986-01-07
申请号：US621681
申请日：1984-06-18
申请人： Francesco Angelucci , Sergio Penco , Federico Arcamone
发明人： Francesco Angelucci , Sergio Penco , Federico Arcamone
IPC分类号： C07H15/252 , A61K31/71 , C07H15/24
CPC分类号： C07H15/252 , Y02P20/55
摘要： Anthracycline glycosides of the formula (I) ##STR1## wherein one of R.sub.1 and R.sub.2 is hydrogen and the other of R.sub.1 and R.sub.2 is hydroxy, each of R.sub.3, R.sub.4 and R.sub.5 is independently selected from the group consisting of hydrogen and hydroxy and X is hydrogen or trifluoroacetyl, with the provisos that R.sub.4 and R.sub.5 are not simultaneously hydroxy and that if R.sub.3 is hydroxy, then X is hydrogen, which are useful in treating certain mammalian tumors are prepared by condensing an aglycone of the formula (II) ##STR2## wherein R.sub.1 and R.sub.2 are defined as above, with a suitable protected halosugar, after which the protecting groups are removed.
摘要翻译：式（I）的蒽环酸糖苷其中R 1和R 2之一是氢，R 1和R 2中的另一个是羟基，R 3，R 4和R 5各自独立地选自氢和羟基，X 是氢或三氟乙酰基，条件是R 4和R 5不同时为羟基，如果R 3为羟基，则X为氢，其可用于治疗某些哺乳动物肿瘤通过将式（II）的糖苷配基缩合制备其中R 1和R 2如上所定义，具有合适的受保护的卤糖，之后除去保护基。

10. 发明授权

US4345068A Process for the preparation of 4'-epidaunorubicin, 3',4'-diepidaunorubicin, their doxorubicin analogs, and intermediates used in said process 失效
标题翻译：制备4'-表柔皮霉素，3'，4'-二头孢菌素，其多柔比星类似物和用于所述方法的中间体的方法
公开(公告)号：US4345068A
公开(公告)日：1982-08-17
申请号：US164088
申请日：1980-06-30
申请人： Antonio Suarato , Sergio Penco , Federico Arcamone
发明人： Antonio Suarato , Sergio Penco , Federico Arcamone
IPC分类号： C07H15/24 , C07H15/252 , A61K31/71
CPC分类号： C07H15/252
摘要： Disclosed is a process for preparing the known antitumor glycosides: 4'-epidaunorubicin, 3',4'-diepidaunorubicin, and their doxorubicin analogs by oxidizing the C-4' hydroxyl group of N-protected daunorubicin to form certain novel intermediates having a 4'-keto configuration, followed by reduction of the keto group with NaBH.sub.4 and mild alkaline hydrolysis to remove the N-protecting acyl groups.
摘要翻译：公开了通过氧化N-保护的柔红霉素的C-4'羟基来形成已知的抗肿瘤糖苷4'-表柔比星，3'，4'-二头孢菌素及其多柔比星类似物的方法，以形成具有4个 '配置，随后用NaBH 4还原酮基并进行轻度碱性水解以除去N-保护的酰基。

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