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1.发明授权NOVEL ADENYL DINUCLEOTIDES WITH ANTITUMOUR ACTIVITY AND A METHOD FOR PREPARING THEREOF 有权新ADENYLDINUKLEOTIDE具有抗肿瘤作用及其制造方法
公开(公告)号：EP1879907B1
公开(公告)日：2009-05-20
申请号：EP06728073.5
申请日：2006-04-28
发明人： BASILE, Giovanna , BENATTI, Umberto , BRUZZONE, Santina , DAMONTE, Gianluca , DE FLORA, Antonio , FATTORUSSO, Ernesto , FRANCO, Luisa , GUIDA, Lucrezia , TAGLIALATELA-SCAFATI, Orazio , ZOCCHI, Elena
IPC分类号： C07H21/04
CPC分类号： C07H21/04
摘要： The invention relates to novel adenyl dinucleotides which are isomers of the dinucleotide Ap2A, having formulae (I) and (II) . The dinucleotides of the invention have antitumour activity, particularly against tumours of haematological origin, such as for example leukaemias and lymphomas. The invention further relates to the use of such dinucleotides as antitumour medicaments. Finally, the invention relates to an enzymatic method for preparing the dinucleotides of formulae (I) and (II) and to an enzymatic assay method for the dinucleotide of formula (I) which is based on its complete conversion to NAD + .
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公开(公告)号：EP0773951B1
公开(公告)日：1999-03-10
申请号：EP95943516.5
申请日：1995-07-10
CPC分类号： C07H21/00
摘要： 5',5'-Pyrophosphates of non-naturally occurring nucleosides selected from thymine-3'-azido-2',3'-dideoxy-D-riboside, 5-fluorouracil-2'-deoxy-D-riboside, uracil-3'-azido-2',3'-dideoxy-D-riboside, guanine-2',3'-dideoxy-D-riboside, hypoxanthine-2',3'-dideoxy-D-riboside, cytosine-2',3'-dideoxy-D-riboside, and adenine-2',3'-dideoxy-D-riboside, are described as well as their manufacture and use as therapeutical agents against tumors and retroviral infections including HIV infections. The compounds may be administered as the active ingredients of pharmaceutical compositions or as pro-drugs encapsulated into biological carriers, e.g., transformed erythrocytes, for targeting to specific cell population responsible of the development of the pathological disorders.
摘要翻译： 选自胸腺嘧啶-3'-叠氮基-2'，3'-二脱氧-D-核糖核苷，5-氟尿嘧啶-2'-脱氧-D-核糖苷，尿嘧啶-3的非天然存在的核苷的5'，5'-焦磷酸酯 ' - 叠氮基-2'，3'-双脱氧-D-核糖苷，鸟嘌呤-2'，3'-双脱氧-D-核糖苷，次黄嘌呤-2'，3'-双脱氧-D-核糖苷，胞嘧啶-2'，3 ' - 双脱氧-D-核糖苷和腺嘌呤-2'，3'-双脱氧-D-核糖苷以及它们的制造和用作抗肿瘤和包括HIV感染在内的逆转录病毒感染的治疗剂。 所述化合物可作为药物组合物的活性成分或作为封装到生物载体（例如转化的红细胞）中的前药施用以靶向导致病理性疾病发展的特定细胞群。
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公开(公告)号：EP1948174B1
公开(公告)日：2012-08-01
申请号：EP06821174.7
申请日：2006-10-06
发明人： ZOCCHI, Elena , GUIDA, Lucrezia , BRUZZONE, Santina , SCARFI', Sonia , MAGNONE, Mirko , BASILE, Giovanna , BENATTI, Umberto , DE FLORA, Antonio , MORESCHI, Iliana , FRANCO, Luisa , SALIS, Annalisa
IPC分类号： A61K31/4412 , A61P29/00 , A61K31/19
CPC分类号： A61K31/19 , A61K31/4412 , C07D213/68 , Y10S514/886
摘要： The invention relates to a novel use of fluridone - compound known per se and used as an aquatic erbicide - in the medical field, in particular as an active compound for preparing a medicament having anti-inflammatory activity. Pharmaceutical compositions comprising fluridone as an active compound and pharmaceutically acceptable carriers and/or diluents are also disclosed. Finally, there is disclosed the pro-inflammatory activity of abscisic acid (ABA), a plant hormone which is also found in mammal serum and against which fluridone acts an an inhibitor.
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4.发明公开NOVEL ADENYL DINUCLEOTIDES WITH ANTITUMOUR ACTIVITY AND A METHOD FOR PREPARING THEREOF 有权新ADENYLDINUKLEOTIDE具有抗肿瘤作用及其制造方法
公开(公告)号：EP1879907A1
公开(公告)日：2008-01-23
申请号：EP06728073.5
申请日：2006-04-28
发明人： BASILE, Giovanna , BENATTI, Umberto , BRUZZONE, Santina , DAMONTE, Gianluca , DE FLORA, Antonio , FATTORUSSO, Ernesto , FRANCO, Luisa , GUIDA, Lucrezia , TAGLIALATELA-SCAFATI, Orazio , ZOCCHI, Elena
IPC分类号： C07H21/04
CPC分类号： C07H21/04
摘要： The invention relates to novel adenyl dinucleotides which are isomers of the dinucleotide Ap2A, having formulae (I) and (II) . The dinucleotides of the invention have antitumour activity, particularly against tumours of haematological origin, such as for example leukaemias and lymphomas. The invention further relates to the use of such dinucleotides as antitumour medicaments. Finally, the invention relates to an enzymatic method for preparing the dinucleotides of formulae (I) and (II) and to an enzymatic assay method for the dinucleotide of formula (I) which is based on its complete conversion to NAD+ .
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公开(公告)号：EP1948174A2
公开(公告)日：2008-07-30
申请号：EP06821174.7
申请日：2006-10-06
发明人： ZOCCHI, Elena , GUIDA, Lucrezia , BRUZZONE, Santina , SCARFI', Sonia , MAGNONE, Mirko , BASILE, Giovanna , BENATTI, Umberto , DE FLORA, Antonio , MORESCHI, Iliana , FRANCO, Luisa , SALIS, Annalisa
IPC分类号： A61K31/4412 , A61P29/00 , A61K31/19
CPC分类号： A61K31/19 , A61K31/4412 , C07D213/68 , Y10S514/886
摘要： The invention relates to a novel use of fluridone - compound known per se and used as an aquatic erbicide - in the medical field, in particular as an active compound for preparing a medicament having anti-inflammatory activity. Pharmaceutical compositions comprising fluridone as an active compound and pharmaceutically acceptable carriers and/or diluents are also disclosed. Finally, there is disclosed the pro-inflammatory activity of abscisic acid (ABA), a plant hormone which is also found in mammal serum and against which fluridone acts an an inhibitor.
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公开(公告)号：EP0773951A1
公开(公告)日：1997-05-21
申请号：EP95943516.0
申请日：1995-07-10
CPC分类号： C07H21/00
摘要： 5',5'-Pyrophosphates of non-naturally occurring nucleosides selected from thymine-3'-azido-2',3'-dideoxy-D-riboside, 5-fluorouracil-2'-deoxy-D-riboside, uracil-3'-azido-2',3'-dideoxy-D-riboside, guanine-2',3'-dideoxy-D-riboside, hypoxanthine-2',3'-dideoxy-D-riboside, cytosine-2',3'-dideoxy-D-riboside, and adenine-2',3'-dideoxy-D-riboside, are described as well as their manufacture and use as therapeutical agents against tumors and retroviral infections including HIV infections. The compounds may be administered as the active ingredients of pharmaceutical compositions or as pro-drugs encapsulated into biological carriers, e.g., transformed erythrocytes, for targeting to specific cell population responsible of the development of the pathological disorders.
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