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1. 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。

2. 发明授权

US4839346A Antitumor anthracycline glycosides, intermediates thereof, and composition and use thereof 失效
标题翻译：抗癌蒽环类苷，其中间体及其组成和用途
公开(公告)号：US4839346A
公开(公告)日：1989-06-13
申请号：US101382
申请日：1987-09-28
申请人： Alberto Bargiotti , Teresa Bordoni , Pierangelo Zini , Sergio Penco
发明人： Alberto Bargiotti , Teresa Bordoni , Pierangelo Zini , Sergio Penco
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , A61P35/02 , C07H13/04 , C07H15/04 , C07H15/252
CPC分类号： C07H13/04 , C07H15/04 , C07H15/252
摘要： New anthracycline glycosides having formula: ##STR1## wherein R.sup.1 is hydrogen or hydroxy and either R.sup.2 or R.sup.3 is hydrogen with the other amino-methyl are described. The new compounds and their pharmaceutically acceptable addition salts are useful as antitumour agents.
摘要翻译：描述了具有下式的新的蒽环类苷：其中R1是氢或羟基，R2或R3与另一个氨基甲基是氢。新化合物及其药学上可接受的加成盐可用作抗肿瘤剂。

3. 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。

4. 发明授权

US4366149A Antitumor anthracycline glycosides, their preparation, intermediates therefor, and compositions and use thereof 失效
标题翻译：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：US4366149A
公开(公告)日：1982-12-28
申请号：US316057
申请日：1981-10-29
申请人： Alberto Bargiotti , Giuseppe Cassinelli , Sergio Penco , Federico Arcamone , Annamaria Casazza
发明人： Alberto Bargiotti , Giuseppe Cassinelli , Sergio Penco , Federico Arcamone , Annamaria Casazza
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H13/04 , C07H15/04 , C07H15/252 , C07H5/06 , C07H15/24
CPC分类号： C07H13/04 , C07H15/04 , C07H15/252 , Y10S514/908
摘要： Novel antitumor anthracycline glycosides are prepared by condensing daunomycinone with 2,3,4,6-tetradeoxy-3,4-ditrifluoroacetamido-L-lyxo-[or L-arabino-]hexopyranosyl chloride.
摘要翻译：通过将道诺霉素酮与2,3,4,6-四脱氧-3,4-二三氟乙酰氨基-L-赖氨酸 - 或[L-阿拉伯糖]六吡喃葡萄糖氯化物缩合来制备新型抗肿瘤蒽环苷。

5. 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。

6. 发明授权

US4112076A Epi-daunomycin and epi-adriamycin compounds and method of use 失效
标题翻译：依托霉素和表阿霉素化合物及其使用方法
公开(公告)号：US4112076A
公开(公告)日：1978-09-05
申请号：US675696
申请日：1976-04-09
申请人： Federico Arcamone , Alberto Bargiotti , Aurelio DI Marco , Sergio Penco
发明人： Federico Arcamone , Alberto Bargiotti , Aurelio DI Marco , Sergio Penco
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。

7. 发明授权

US4393052A Antitumor anthracycline glycosides, their preparation, intermediates therefor, and compositions and use thereof 失效
标题翻译：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
申请人： Alberto Bargiotti , Giuseppe Cassinelli , Sergio Penco , Federico Arcamone , Annamaria Casazza
发明人： Alberto Bargiotti , Giuseppe Cassinelli , Sergio Penco , Federico Arcamone , Annamaria Casazza
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。

8. 发明授权

US4325946A Anthracycline glycosides, their preparation, use and compositions thereof 失效
标题翻译：蒽环类苷，其制备方法，用途及其组合物
公开(公告)号：US4325946A
公开(公告)日：1982-04-20
申请号：US182119
申请日：1980-08-28
申请人： Alberto Bargiotti , Giueseppe Cassinelli , Sergio Penco , Federico Arcamone , Aurelio di Marco
发明人： Alberto Bargiotti , Giueseppe Cassinelli , Sergio Penco , Federico Arcamone , Aurelio di Marco
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。

9. 发明授权

US4749693A Nitro anthracyclines, process for their preparation and use thereof 失效
标题翻译：硝基蒽环类药物，其制备及使用方法
公开(公告)号：US4749693A
公开(公告)日：1988-06-07
申请号：US912070
申请日：1986-09-26
申请人： Francesco Angelucci , Mauro Gigli , Sergio Penco , Fernando Giuliani
发明人： Francesco Angelucci , Mauro Gigli , Sergio Penco , Fernando Giuliani
IPC分类号： C07H15/24 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252
CPC分类号： C07H15/252
摘要： Anthracycline glycosides of the general formula (A'): ##STR1## wherein R.sub.1 represents a hydrogen atom, a hydroxy group or a methoxy group; one of R.sub.2 and R.sub.3 represents a hydroxy group and the other of R.sub.2 and R.sub.3 represents a nitro group; and R.sub.4 represents a hydrogen atom or a hydroxy group; and their pharmaceutically acceptable salts; have anti-tumor activity.
摘要翻译：通式（A'）的蒽环酸苷：其中R 1表示氢原子，羟基或甲氧基; R2和R3中的一个表示羟基，R2和R3中的另一个表示硝基; R4代表氢原子或羟基; 及其药学上可接受的盐; 具有抗肿瘤活性。

10. 发明授权

US08067555B2 Derivatives of partially desulphated glycosaminoglycans as heparanase inhibitors, endowed with antiangiogenic activity and devoid of anticoagulating effect 有权
标题翻译：部分脱硫的糖胺聚糖衍生物作为乙酰肝素酶抑制剂，具有抗血管生成活性，无抗凝作用
公开(公告)号：US08067555B2
公开(公告)日：2011-11-29
申请号：US11882978
申请日：2007-08-08
申请人： Benito Casu , Giangiacomo Torri , Anna Maria Naggi , Giuseppe Giannini , Claudio Pisano , Sergio Penco
发明人： Benito Casu , Giangiacomo Torri , Anna Maria Naggi , Giuseppe Giannini , Claudio Pisano , Sergio Penco
IPC分类号： C08B37/10 , C07H5/04
CPC分类号： A61K31/727 , A61K31/737 , C07H5/04 , C08B37/0063
摘要： Partially desulphated glycosaminoglycan derivatives are described, particularly heparin, and more particularly a compound of formula (I) where the U, R and R1 groups have the meanings indicated in the description. These glycosaminoglycan derivatives have antiangiogenic and heparanase-inhibiting activity and are devoid of anticoagulant activity.
摘要翻译：描述了部分脱硫的糖胺聚糖衍生物，特别是肝素，更具体地，其中U，R和R 1基团具有说明书中所示含义的式（I）化合物。这些糖胺聚糖衍生物具有抗血管生成和乙酰肝素酶抑制活性，并且没有抗凝血活性。

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