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公开(公告)号：US08975248B2
公开(公告)日：2015-03-10
申请号：US11720776
申请日：2005-12-13
IPC分类号： A61K31/47 , A61K31/282 , A61K33/24 , A61K39/395 , A61K31/427 , A61K31/53 , A61K31/555 , A61K31/4745 , A61K31/337 , A61K45/06
CPC分类号： A61K45/06 , A61K31/282 , A61K31/337 , A61K31/427 , A61K31/4745 , A61K31/53 , A61K31/555 , A61K33/24 , A61K39/395 , A61K2300/00
摘要： A combination therapy for treating patients suffering from proliferative diseases or diseases associated with persistent angiogenesis is disclosed. The patient is treated with a camptothecin derivative and one or more chemotherapeutic agents selected from a microtubule active agent; an alkylating agent; an anti-neoplastic anti-metabolite; a platin compound; a topoisomerase II inhibitor; a VEGF inhibitor; a tyrosine kinase inhibitor; an EGFR kinase inhibitor; an mTOR kinase inhibitor; an insulin-like growth factor I inhibitor; a Raf kinase inhibitor; a monoclonal antibody; a proteasome inhibitor; a HDAC inhibitor; and ionizing radiation.
摘要翻译： 公开了用于治疗患有与持续血管发生相关的增殖性疾病或疾病的患者的联合疗法。 用喜树碱衍生物和一种或多种选自微管活性剂的化学治疗剂治疗患者; 烷基化剂; 抗肿瘤抗代谢物; 铂化合物; 拓扑异构酶II抑制剂; VEGF抑制剂; 酪氨酸激酶抑制剂; EGFR激酶抑制剂; mTOR激酶抑制剂; 胰岛素样生长因子I抑制剂; Raf激酶抑制剂; 单克隆抗体; 蛋白酶体抑制剂; HDAC抑制剂; 和电离辐射。
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公开(公告)号：US20100028338A1
公开(公告)日：2010-02-04
申请号：US11720776
申请日：2005-12-13
IPC分类号： A61K39/395 , A61K31/437 , A61K31/505 , A61K31/7068 , A61K33/24 , A61K31/704 , A61K31/496 , A61P35/00 , A61K31/69
CPC分类号： A61K45/06 , A61K31/282 , A61K31/337 , A61K31/427 , A61K31/4745 , A61K31/53 , A61K31/555 , A61K33/24 , A61K39/395 , A61K2300/00
摘要： A combination therapy for treating patients suffering from proliferative diseases or diseases associated with persistent angiogenesis is disclosed. The patient is treated with a camptothecin derivative and one or more chemotherapeutic agents selected from a microtubule active agent; an alkylating agent; an anti-neoplastic anti-metabolite; a platin compound; a topoisomerase II inhibitor; a VEGF inhibitor; a tyrosine kinase inhibitor; an EGFR kinase inhibitor; an mTOR kinase inhibitor; an insulin-like growth factor I inhibitor; a Raf kinase inhibitor; a monoclonal antibody; a proteasome inhibitor; a HDAC inhibitor; and ionizing radiation.
摘要翻译： 公开了用于治疗患有与持续血管发生相关的增殖性疾病或疾病的患者的联合疗法。 用喜树碱衍生物和一种或多种选自微管活性剂的化学治疗剂治疗患者; 烷基化剂; 抗肿瘤抗代谢物; 铂化合物; 拓扑异构酶II抑制剂; VEGF抑制剂; 酪氨酸激酶抑制剂; EGFR激酶抑制剂; mTOR激酶抑制剂; 胰岛素样生长因子I抑制剂; Raf激酶抑制剂; 单克隆抗体; 蛋白酶体抑制剂; HDAC抑制剂; 和电离辐射。
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3.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：US20080207729A1
公开(公告)日：2008-08-28
申请号：US11917065
申请日：2006-05-31
申请人： Claudio Pisano , Gianfranco Battistuzzi , Maria Di Marzo , Giuseppe Giannini , Mauro Marzi , Loredana Vesci , Franco Zunino
发明人： Claudio Pisano , Gianfranco Battistuzzi , Maria Di Marzo , Giuseppe Giannini , Mauro Marzi , Loredana Vesci , Franco Zunino
IPC分类号： A61K31/404 , A61P35/00 , C07D209/04
CPC分类号： C07D209/18
摘要： Indole derivatives of Formula (I+A) having antitumour and chemosensitizing activity are described. Also described are pharmaceutical compositions containing the above-mentioned compounds, for the treatment of tumours.
摘要翻译： 描述了具有抗肿瘤和化学敏化活性的式（I + A）的吲哚衍生物。 还描述了含有上述化合物的药物组合物，用于治疗肿瘤。
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5.发明申请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：US20070043067A1
公开(公告)日：2007-02-22
申请号：US10564637
申请日：2004-07-06
申请人： Giuseppe Giannini , Claudio Pisano , Loredana Vesci , Maria Omella Tinti , Lucio Merlini , Sergio Penco , Franco Zunino
发明人： Giuseppe Giannini , Claudio Pisano , Loredana Vesci , Maria Omella Tinti , Lucio Merlini , Sergio Penco , Franco Zunino
IPC分类号： A61K31/4745 , C07D491/14
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 tumours 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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6.发明授权公开(公告)号：US08853233B2
公开(公告)日：2014-10-07
申请号：US12526225
申请日：2008-02-07
申请人： Claudio Pisano , Loredana Vesci , Franco Zunino
发明人： Claudio Pisano , Loredana Vesci , Franco Zunino
IPC分类号： A61K31/4745
CPC分类号： A61K31/4745
摘要： A subclass of camptothecin derivatives is disclosed to be useful for the preparation of a medicament for the treatment of a cancer or tumor pathology selected from the group consisting of head and neck carcinoma, pancreas carcinoma, melanoma, bladder carcinoma, mesothelioma and epidermoid skin carcinoma.
摘要翻译： 喜树碱衍生物的亚类被公开用于制备用于治疗选自头颈癌，胰腺癌，黑素瘤，膀胱癌，间皮瘤和表皮样皮肤癌的癌症或肿瘤病理学的药物。
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公开(公告)号：US08829021B2
公开(公告)日：2014-09-09
申请号：US12669134
申请日：2008-07-03
申请人： Claudio Pisano , Loredana Vesci , Paolo Carminati
发明人： Claudio Pisano , Loredana Vesci , Paolo Carminati
IPC分类号： A61K31/4375 , A61P35/00 , C07D457/14 , A61K31/4745
CPC分类号： A61K31/4745
摘要： A subclass of camptothecin derivatives is disclosed to be useful for the preparation of a medicament for the treatment of pediatric tumors such as for examplerhabdomyosarcoma, primitive neuroectodermal tumors (PNET) and neuroblastoma.
摘要翻译： 喜树碱衍生物的亚类被公开用于制备用于治疗儿科肿瘤的药物，例如用于示例性腹膜肉瘤，原始神经外胚层肿瘤（PNET）和神经母细胞瘤。
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8.发明授权Retinoid derivatives with antiangiogenic, antitumoral and proapoptotic activities 失效维甲酸衍生物具有抗血管生成，抗肿瘤和促凋亡活性公开(公告)号：US08101793B2
公开(公告)日：2012-01-24
申请号：US10485530
申请日：2002-07-18
申请人： Lucio Merlini , Sabrina Dallavalle , Sergio Penco , Giuseppe Giannini , Claudio Pisano , Loredana Vesci
发明人： Lucio Merlini , Sabrina Dallavalle , Sergio Penco , Giuseppe Giannini , Claudio Pisano , Loredana Vesci
IPC分类号： C07C62/32 , C07C69/618 , C07C59/72 , C07D317/50 , A61P35/00 , A61P35/02 , A61P35/04 , A61K31/195 , A61K31/192 , A61K31/222 , 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： Are described 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： 描述了式（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理学的有效试剂和抗肿瘤剂。
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公开(公告)号：US20100113504A1
公开(公告)日：2010-05-06
申请号：US12528912
申请日：2008-03-12
申请人： Stephan Hanessian , Luciana Auzzas , Giuseppe Giannini , Claudio Pisano , Loredana Vesci , Walter Cabri
发明人： Stephan Hanessian , Luciana Auzzas , Giuseppe Giannini , Claudio Pisano , Loredana Vesci , Walter Cabri
IPC分类号： A61K31/4353 , C07C233/00 , C07D273/01 , C07D273/02 , C07D498/04 , A61K31/16 , A61K31/395 , A61K31/4162 , A61K31/407 , A61P35/04
CPC分类号： C07D273/02 , C07C259/06 , C07D273/01 , C07D498/04
摘要： The present invention relates to a compound of Formula (I), its geometrical isomers, in an optically active form as enantiomers, diastereomers, as well as in the form of racemate, as well as pharmaceutically acceptable salts thereof, wherein R is selected from CONHOH, CONHCH2SH, CONHCH2SCOCH3, SH, SCOCH3, SCH3, N(OH)COH, COCONHCH3 and CF3 for the preparation of a medicament, in particular for selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells, for inducing differentiation of tumor cells in a tumor, for inhibiting the activity of histone deacetylase and for the treatment of primary cancer or secondary cancer.
摘要翻译： 本发明涉及作为对映异构体，非对映异构体，以外消旋物形式的旋光形式的式（I）化合物及其几何异构体及其药学上可接受的盐，其中R选自CONHOH ，CONHCH2SH，CONHCH2SCOCH3，SH，SCOCH3，SCH3，N（OH）COH，COCONHCH3和CF3，用于制备药物，特别是用于选择性诱导肿瘤细胞的终末分化，从而抑制这些细胞的增殖，诱导肿瘤分化 肿瘤中的细胞，用于抑制组蛋白脱乙酰酶的活性和用于治疗原发性癌症或继发性癌症。
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10.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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