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1.发明授权7-t-butoxyiminomethylcamptothecin conjugated in position 20 with integrin antagonists 失效在20位缀合有整联蛋白拮抗剂的7-叔丁氧基亚氨基甲基喜树碱公开(公告)号：US07589099B2
公开(公告)日：2009-09-15
申请号：US11596016
申请日：2005-04-28
申请人： Claudio Pisano , Giuseppe Giannini , Loredana Vesci , Domenico Alloatti , Sergio Penco , Alma Dal Pozzo , Ni Ming Hong , Sabrina Dallavalle , Lucio Merlini , Maria Ornella Tinti , Franco Zunino
发明人： Claudio Pisano , Giuseppe Giannini , Loredana Vesci , Domenico Alloatti , Sergio Penco , Alma Dal Pozzo , Ni Ming Hong , Sabrina Dallavalle , Lucio Merlini , Maria Ornella Tinti , Franco Zunino
IPC分类号： A61K31/4745 , C07D491/22
CPC分类号： A61K47/64
摘要： Compounds of Formula (I) are described: in which the R1 group is as defined in the specification and includes the condensation of 7-t-butoxyiminomethylcamptothecin in position 20 with a cyclopeptide containing the RGD sequence. Said compounds are endowed both with high affinity for integrin receptors αvβ3 and αvβ5 and with selective cytotoxic activity on human tumour cell lines at micromolar concentrations.
摘要翻译： 描述式（I）的化合物：其中R 1基团如本说明书中所定义，并且包括位置20上的7-叔丁氧基亚氨基甲基喜树碱与含有RGD序列的环肽的缩合。 所述化合物赋予对整联蛋白受体alphavbeta3和alphavbeta5的高亲和力，并且在微摩尔浓度下对人肿瘤细胞系具有选择性细胞毒性活性。
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公开(公告)号：US20080319082A1
公开(公告)日：2008-12-25
申请号：US11993184
申请日：2006-05-31
申请人： Claudio Pisano , Giuseppe Giannini , Loredana Vesci , Franco Zunino , Sabrina Dallavalle , Lucio Merlini , Sergio Penco
发明人： Claudio Pisano , Giuseppe Giannini , Loredana Vesci , Franco Zunino , Sabrina Dallavalle , Lucio Merlini , Sergio Penco
IPC分类号： A61K31/165 , C07C233/02 , A61P35/00
CPC分类号： C07C259/06 , C07C259/10 , C07C2603/74 , C07D319/18
摘要： Biphenyl and phenyl-naphthyl compounds bearing a hydroxamic group, which are endowed with antitumour, and anti-angiogenic activity These compounds are therefore particularly useful for the treatment of drug-resistant tumours.
摘要翻译： 具有抗肿瘤抗生素的异羟肟基的联苯和苯基萘基化合物和抗血管生成活性因此，这些化合物特别可用于治疗耐药肿瘤。
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3.发明申请Camptothecins Conjugated in Position 7 to Cyclic Peptides as Cytostatic Agents 失效第7位缀合于环状肽作为细胞抑制剂的喜树碱公开(公告)号：US20080033003A1
公开(公告)日：2008-02-07
申请号：US11596015
申请日：2005-05-04
申请人： Claudio Pisano , Giuseppe Giannini , Maria Omella Tinti , Loredana Vesci , Domenico Alloatti , Sergio Penco , Alma Dal Pozzo , Ni Minghong , Sabrina Dallavalle , Lucio Merlini , Franco Zunino
发明人： Claudio Pisano , Giuseppe Giannini , Maria Omella Tinti , Loredana Vesci , Domenico Alloatti , Sergio Penco , Alma Dal Pozzo , Ni Minghong , Sabrina Dallavalle , Lucio Merlini , Franco Zunino
IPC分类号： A61K31/436 , A61P31/12 , A61P33/00 , A61P35/00 , A61P35/04
摘要： Compounds of Formula (I) are described in which the R1 group is as defined in the specification and includes the condensation of the camptothecin molecule in position 7 with a cyclopeptide containing the RGD sequence. Said compounds are endowed both with high affinity for integrin receptors αvβ3 and αvβ5 and with selective cytotoxic activity on human tumour cell lines at micromolar concentrations.
摘要翻译： 描述了式（I）的化合物，其中R 1 H 1基团如说明书中所定义，并且包括位置7上的喜树碱分子与含有RGD序列的环肽的缩合。 所述化合物赋予对整联蛋白受体α和β5β5的高亲和力，并与 在微摩尔浓度下对人肿瘤细胞系的选择性细胞毒活性。
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公开(公告)号：US07728039B2
公开(公告)日：2010-06-01
申请号：US11993184
申请日：2006-05-31
申请人： Claudio Pisano , Giuseppe Giannini , Loredana Vesci , Franco Zunino , Sabrina Dallavalle , Lucio Merlini , Sergio Penco
发明人： Claudio Pisano , Giuseppe Giannini , Loredana Vesci , Franco Zunino , Sabrina Dallavalle , Lucio Merlini , Sergio Penco
IPC分类号： A61K31/185 , C07C259/06
CPC分类号： C07C259/06 , C07C259/10 , C07C2603/74 , C07D319/18
摘要： Biphenyl and phenyl-naphthyl compounds bearing a hydroxamic group, which are endowed with antitumor, and anti-angiogenic activity These compounds are therefore particularly useful for the treatment of drug-resistant tumors.
摘要翻译： 具有抗肿瘤活性的异羟肟基的联苯和苯基萘基化合物和抗血管生成活性因此，这些化合物特别可用于治疗耐药性肿瘤。
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公开(公告)号：US07105492B2
公开(公告)日：2006-09-12
申请号：US10388587
申请日：2003-03-17
IPC分类号： A61K31/44 , A61K31/70 , C07H15/24 , C07D498/22
CPC分类号： C07D491/22
摘要： Camptothecin derivatives of camptothecin of formula (I) exhibit antitumor activity and show a good therapeutic index and are used in the treatment of tumors, viral infections and antiplasmodium falciparum.
摘要翻译： 式（I）喜树碱喜树碱衍生物具有抗肿瘤活性，显示出良好的治疗指标，用于治疗肿瘤，病毒感染和恶性疟原虫。
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6.发明授权Camptothecins conjugated in position 7 to cyclic peptides as cytostatic agents 失效缀合在位置7的喜树碱与环肽作为细胞抑制剂公开(公告)号：US07705012B2
公开(公告)日：2010-04-27
申请号：US11596015
申请日：2005-05-04
申请人： Claudio Pisano , Giuseppe Giannini , Maria Ornella Tinti , Loredana Vesci , Domenico Alloatti , Sergio Penco , Alma Dal Pozzo , Ni Minghong , Sabrina Dallavalle , Lucio Merlini , Franco Zunino
发明人： Claudio Pisano , Giuseppe Giannini , Maria Ornella Tinti , Loredana Vesci , Domenico Alloatti , Sergio Penco , Alma Dal Pozzo , Ni Minghong , Sabrina Dallavalle , Lucio Merlini , Franco Zunino
IPC分类号： A61K31/4745 , C07D491/22
摘要： Compounds of Formula (I) are described in which the R1 group is as defined in the specification and includes the condensation of the camptothecin molecule in position 7 with a cyclopeptide containing the RGD sequence. Said compounds are endowed both with high affinity for integrin receptors αvβ3 and αvβ5 and with selective cytotoxic activity on human tumour cell lines at micromolar concentrations.
摘要翻译： 描述了式（I）的化合物，其中R 1基团如说明书中所定义，并且包括7位的喜树碱分子与含有RGD序列的环肽的缩合。 所述化合物对整联蛋白受体αv＆bgr 3和αv＆bgr 5具有高亲和力，并且在微摩尔浓度下对人肿瘤细胞系具有选择性细胞毒性活性。
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7.发明申请Camptothecin Derivatives Conjugated in Position 20 with Integrin Antagonists 审中-公开喜树碱衍生物与20位整合素拮抗剂共轭公开(公告)号：US20070232639A1
公开(公告)日：2007-10-04
申请号：US11596189
申请日：2005-05-04
申请人： Claudio Pisano , Giuseppe Giannini , Maria Ornella Tinti , Loredana Vesci , Domenico Alloatti , Sergio Penco , Alma Dal Pozzo , Ni Minghong , Sabrina Dallavalle , Lucio Merlini , Franco Zunino
发明人： Claudio Pisano , Giuseppe Giannini , Maria Ornella Tinti , Loredana Vesci , Domenico Alloatti , Sergio Penco , Alma Dal Pozzo , Ni Minghong , Sabrina Dallavalle , Lucio Merlini , Franco Zunino
IPC分类号： A61K31/437 , A61K31/4375 , C07D405/14
CPC分类号： A61K47/64
摘要： Compounds or formula (I) are described, in which the R and R1 groups are as defined here below and include the condensation of the camptothecin molecule in position 20 with a cyclopeptide containing the RGD sequence. Said compounds are endowed both with high affinity for integrin receptors αvβ3 and αvβ5 and with selective cytotoxic activity on human tumour cell lines at micromolar concentrations.
摘要翻译： 描述了化合物或式（I），其中R和R 1个基团如下文所定义，并且包括20位的喜树碱分子与含有RGD序列的环肽的缩合。 所述化合物赋予对整联蛋白受体α和β5β5的高亲和力，并与 在微摩尔浓度下对人肿瘤细胞系的选择性细胞毒活性。
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公开(公告)号：US07351714B2
公开(公告)日：2008-04-01
申请号：US10546211
申请日：2004-03-10
IPC分类号： A61K31/4745 , C07D491/22
CPC分类号： C07D491/22
摘要： Camptothecin derivatives of camptothecin of formula (I) wherein the groups R1, R2 and R3 are as defined in the description are disclosed. The compounds of formula (I) are endowed with antitumor activity and show a good therapeutic index.Processes for the preparation of the compounds of formula (I) and their use in the preparation of medicaments useful in the treatment of tumors, viral infections and antiplasmodium falciparum are also disclosed.
摘要翻译： 公开了式（I）的喜树碱喜树碱衍生物，其中基团R 1，R 2和R 3 3如说明书中所定义。 式（I）化合物具有抗肿瘤活性，显示出良好的治疗指标。 还公开了制备式（I）化合物及其在制备用于治疗肿瘤，病毒感染和恶性疟原虫药物中的用途的方法。
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公开(公告)号：US20060167033A1
公开(公告)日：2006-07-27
申请号：US10546211
申请日：2004-03-10
IPC分类号： A61K31/4745 , C07D519/04
CPC分类号： C07D491/22
摘要： Camptothecin derivatives of camptothecin of formula (I) wherein the groups R1, R2 and R3 are as defined in the description are disclosed. The compounds of formula (I) are endowed with antitumor activity and show a good therapeutic index. Processes for the preparation of the compounds of formula (I) and their use in the preparation of medicaments useful in the treatment of tumors, viral infections and antiplasmodium falciparum are also disclosed.
摘要翻译： 公开了式（I）的喜树碱喜树碱衍生物，其中基团R 1，R 2和R 3 3如说明书中所定义。 式（I）化合物具有抗肿瘤活性，显示出良好的治疗指标。 还公开了制备式（I）化合物及其在制备用于治疗肿瘤，病毒感染和恶性疟原虫药物中的用途的方法。
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10.发明申请Retinoid Derivatives With Antiangiogenic, Antitumoral And Proapoptotic Activities 失效维生素A衍生物与抗血管生成，抗肿瘤和前体细胞凋亡活动公开(公告)号：US20080021088A1
公开(公告)日：2008-01-24
申请号：US11765737
申请日：2007-06-20
申请人： Sabrina Dallavalle , Lucio Merlini , Claudio Pisano , Loredana Vesci , Giuseppe Giannini , Sergio Penco
发明人： Sabrina Dallavalle , Lucio Merlini , Claudio Pisano , Loredana Vesci , Giuseppe Giannini , Sergio Penco
IPC分类号： A61K31/40 , A61K31/19 , A61P35/04 , C07D205/00 , C07D307/00 , C07C63/00 , A61K31/36
CPC分类号： C07D209/48 , C07C59/54 , C07C59/72 , C07C62/32 , C07C69/732 , C07C69/734 , C07C229/34 , C07C2601/14 , C07C2603/74 , C07D317/50 , C07F7/1804
摘要： Described and claimed are compounds of Formula (I) in which R, R′, R″, A, and D have the meanings described in the text, as useful agents in the cure of pathologies characterized by altered angiogenesis and as antitumorals.
摘要翻译： 描述和要求保护的是式（I）的化合物，其中R，R'，R“，A和D具有本文中所述的含义，作为治疗以血管生成改变为特征的病态的有用试剂和抗肿瘤剂。
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