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1.发明申请公开(公告)号：US20060211759A1
公开(公告)日：2006-09-21
申请号：US11402989
申请日：2006-04-13
申请人： Giuseppe Giannini , Mauro Marzi , Maria Ornella Tinti , Claudio Pisano , Gian Piero Moretti , Patrizia Minetti , Enrico Garattini , Sergio Penco
发明人： Giuseppe Giannini , Mauro Marzi , Maria Ornella Tinti , Claudio Pisano , Gian Piero Moretti , Patrizia Minetti , Enrico Garattini , Sergio Penco
IPC分类号： A61K31/404 , C07D403/02
CPC分类号： C07D207/325 , C07D207/34 , C07D207/416 , C07D209/10 , C07D209/12 , C07D233/64 , C07D235/20 , C07D277/64 , C07D403/06 , C07D405/14 , C07D471/04 , C07D491/04
摘要： Bis-heterocyclic compounds of general formula (I) are described which are useful as antitumour and chemosensitising agents.
摘要翻译： 描述了可用作抗肿瘤和化学敏化剂的通式（I）的双杂环化合物。
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2.发明授权公开(公告)号：US07084166B2
公开(公告)日：2006-08-01
申请号：US10415898
申请日：2001-07-26
申请人： Giuseppe Giannini , Mauro Marzi , Maria Ornella Tinti , Claudio Pisano , Gian Piero Moretti , Patrizia Minetti , Enrico Garattini , Sergio Penco
发明人： Giuseppe Giannini , Mauro Marzi , Maria Ornella Tinti , Claudio Pisano , Gian Piero Moretti , Patrizia Minetti , Enrico Garattini , Sergio Penco
IPC分类号： A61K31/404 , C07D209/08
CPC分类号： C07D209/08 , C07D209/12 , C07D233/22 , C07D277/64 , C07D491/04
摘要： Bis-heterocyclic compounds of general formula (I) are described which are useful as antitumour and cheomsensitising agents.
摘要翻译： 描述了可用作抗肿瘤和促敏剂的通式（I）的双杂环化合物。
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3.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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4.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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5.发明授权7-Polyaminoalkyl(oxy)iminomethylcamptothecins bearing protective groups 失效带有保护基团的7-聚氨基烷基（氧基）亚氨基甲基冠心病公开(公告)号：US07612081B2
公开(公告)日：2009-11-03
申请号：US10564637
申请日：2004-07-06
申请人： Giuseppe Giannini , Claudio Pisano , Loredana Vesci , Maria Ornella Tinti , Lucio Merlini , Sergio Penco , Franco Zunino
发明人： Giuseppe Giannini , Claudio Pisano , Loredana Vesci , Maria Ornella Tinti , Lucio Merlini , Sergio Penco , Franco Zunino
IPC分类号： A61K31/4745 , C07D491/22
CPC分类号： C07D491/22 , Y02P20/55
摘要： Compounds are disclosed with the general formula in which the groups are as defined in the description here below and characterized by the presence of polyamine substituents on the imine/oxime residue, such amine groups being in turn protected by suitable protective groups. Said compounds are endowed with potent topoisomerase I inhibiting activity and therefore are useful as medicaments for the treatment of tumors and viral and parasite infections.
摘要翻译： 公开了具有通式的化合物，其中基团如下文描述中所定义，并且其特征在于亚胺/肟残基上存在多胺取代基，此类胺基又被合适的保护基保护。 所述化合物具有有效的拓扑异构酶I抑制活性，因此可用作治疗肿瘤和病毒和寄生虫感染的药物。
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公开(公告)号：US06887892B2
公开(公告)日：2005-05-03
申请号：US10415896
申请日：2001-10-16
IPC分类号： C07D491/056 , A61K31/404 , A61K31/4045 , A61K31/407 , A61K31/437 , A61K45/00 , A61P3/10 , A61P9/10 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P35/02 , A61P35/04 , A61P43/00 , C07D209/16 , C07D209/80 , C07D209/86 , C07D403/04 , C07D471/04 , C07D491/04 , C07D519/00 , A61K31/403
CPC分类号： C07D209/80 , C07D209/86 , C07D471/04 , C07D491/04
摘要： Compounds of formula useful for treating tumors, particularly mammary carcinoma and colon carcinoma.
摘要翻译： 用于治疗肿瘤，特别是乳腺癌和结肠癌的配方化合物。
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7.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：US07498340B2
公开(公告)日：2009-03-03
申请号：US11783495
申请日：2007-04-10
申请人： Mauro Marzi , Domenico Alloatti , Claudio Pisano , Maria Ornella Tinti , Loredana Vesci , Franco Zunino
发明人： Mauro Marzi , Domenico Alloatti , Claudio Pisano , Maria Ornella Tinti , Loredana Vesci , Franco Zunino
IPC分类号： A61K31/4745 , C07D491/22
CPC分类号： C07D491/22
摘要： Formula (I) compounds are described: (I) where the groups are as defined in the description here below, the racemic mixtures, their individual enantiomers, their individual diastereoisomers, their mixtures, and their pharmaceutically acceptable salts. Said compounds are topoisomerase I inhibitors.
摘要翻译： 描述了式（I）化合物：其中基团如下文所述的定义，外消旋混合物，其各自的对映异构体，其各自的非对映异构体，它们的混合物及其药学上可接受的盐。 所述化合物是拓扑异构酶I抑制剂。
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公开(公告)号：US07273873B2
公开(公告)日：2007-09-25
申请号：US10511724
申请日：2003-05-28
申请人： Mauro Marzi , Elena Marastoni , Claudio Pisano , Maria Ornella Tinti , Cabri Walter , Alpegiani Marco , Vergani Domenico , Danelli Tamara , Gomez Patricio Martin , Vesci Loredana , Zunino Franco , Penco Sergio
发明人： Mauro Marzi , Elena Marastoni , Claudio Pisano , Maria Ornella Tinti , Cabri Walter , Alpegiani Marco , Vergani Domenico , Danelli Tamara , Gomez Patricio Martin , Vesci Loredana , Zunino Franco , Penco Sergio
IPC分类号： A61K31/4745 , C07D491/22
CPC分类号： C07D491/22
摘要： Compounds of formula (I) or (II) are described: where the groups are as defined in the description here below, the racemic mixtures, their individual enantiomers, their individual diastereoisomers, their mixtures, and their pharmaceutically acceptable salts. Said compounds are topoisomerase I inhibitors.
摘要翻译： 描述式（I）或（II）的化合物：其中基团如下文所述的定义，外消旋混合物，其各自的对映异构体，它们的各自的非对映异构体，它们的混合物及其药学上可接受的盐。 所述化合物是拓扑异构酶I抑制剂。
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公开(公告)号：US20050154003A1
公开(公告)日：2005-07-14
申请号：US10511724
申请日：2003-05-28
申请人： Mauro Marzi , Elena Marastoni , Claudio Pisano , Maria Ornella Tinti , Cabri Walter , Alpegiani Marco , Vergani Domenico , Danelli Tamara , Gomez Patricio Martin , Vesci Loredana , Zunino Franco , Penco Sergio
发明人： Mauro Marzi , Elena Marastoni , Claudio Pisano , Maria Ornella Tinti , Cabri Walter , Alpegiani Marco , Vergani Domenico , Danelli Tamara , Gomez Patricio Martin , Vesci Loredana , Zunino Franco , Penco Sergio
IPC分类号： A61K31/4745 , A61P31/12 , A61P33/00 , A61P35/00 , A61P43/00 , C07D491/22 , C07D471/14
CPC分类号： C07D491/22
摘要： Compounds of formula (I) or (II) are described: where the groups are as defined in the description here below, the racemic mixtures, their individual enantiomers, their individual diastereoisomers, their mixtures, and their pharmaceutically acceptable salts. Said compounds are topoisomerase I inhibitors.
摘要翻译： 描述式（I）或（II）的化合物：其中基团如下文所述的定义，外消旋混合物，其各自的对映体，它们的各自的非对映异构体，它们的混合物及其药学上可接受的盐。 所述化合物是拓扑异构酶I抑制剂。
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