公开(公告)号：US08975248B2

公开(公告)日：2015-03-10

申请号：US11720776

申请日：2005-12-13

申请人： Sara Zaknoen ,  Margaret Ma Woo ,  Richard William Versace ,  Claudio Pisano ,  Loredana Vesci

发明人： Sara Zaknoen ,  Margaret Ma Woo ,  Richard William Versace ,  Claudio Pisano ,  Loredana Vesci

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。

公开(公告)号：US20120093809A1

公开(公告)日：2012-04-19

申请号：US13256531

申请日：2009-12-01

申请人： Claudio Cavazza ,  Giulia Tagliafico ,  Paolo Carminati ,  Gabriella Singrossi ,  Silvia Carminati ,  Giuseppe Paolo Carminati ,  Claudio Pisano

发明人： Claudio Cavazza ,  Giulia Tagliafico ,  Paolo Carminati ,  Gabriella Singrossi ,  Silvia Carminati ,  Giuseppe Paolo Carminati ,  Claudio Pisano

IPC分类号： A61K31/205 ,  A61K31/282 ,  A61P35/02 ,  A61K31/704 ,  A61P35/00 ,  A61K39/395 ,  A61K33/24

CPC分类号： A61K45/06 ,  A61K31/205 ,  A61K31/282 ,  A61K31/337 ,  A61K31/427 ,  A61K31/4745 ,  A61K31/475 ,  A61K31/513 ,  A61K31/555 ,  A61K38/14 ,  A61K2300/00

摘要： The present invention relates to the use of an alkanoyl L-carnitine selected from the group consisting of acetyl, propionyl, valeryl, isovaleryl and butirryl L-carnitine; in combination with one or more chemotherapeutic agent selected from the group consisting of: a camptothecin derivative; an alkylating agent; an anti-neoplastic anti-metabolite; a platin compound; a topoisomerase 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; toxins; and imides; for the treatment of neoplasms.

摘要翻译： 本发明涉及选自乙酰基，丙酰基，戊酰基，异戊酰基和丁基L-肉毒碱的烷酰基L-肉毒碱的用途; 与一种或多种选自以下的化学治疗剂组合：喜树碱衍生物; 烷基化剂; 抗肿瘤抗代谢物; 铂化合物; 拓扑异构酶抑制剂; 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; 毒素 和imides; 用于治疗肿瘤。

公开(公告)号：US20110245221A1

公开(公告)日：2011-10-06

申请号：US13001652

申请日：2009-06-30

申请人： Giuseppe Giannini ,  Walter Cabri ,  Daniele Simoni ,  Riccardo Baruchello ,  Paolo Carminati ,  Gabriella Singrossi ,  Silvia Carminati ,  Giuseppe Paolo Carminati ,  Claudio Pisano

发明人： Giuseppe Giannini ,  Walter Cabri ,  Daniele Simoni ,  Riccardo Baruchello ,  Paolo Carminati ,  Gabriella Singrossi ,  Silvia Carminati ,  Giuseppe Paolo Carminati ,  Claudio Pisano

IPC分类号： A61K31/5377 ,  C07D261/18 ,  C07D413/12 ,  A61K31/42 ,  A61K31/422 ,  A61K31/496 ,  A61K31/454 ,  A61P35/00 ,  A61P25/00 ,  A61P29/00 ,  A61P9/10 ,  A61P33/06 ,  A61P25/16 ,  A61P25/28 ,  A61P35/04

CPC分类号： C07D261/18 ,  C07D413/06 ,  C07D413/12 ,  C07D498/04

摘要： The present invention relates to formula I compounds having antitumoural activities through, as one possible biological target, the molecular chaperone heat shock protein 90 (Hsp90) inhibition. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of Hsp90 is responsive, and the pharmaceutical compositions containing such compounds.

摘要翻译： 本发明涉及具有抗肿瘤活性的式I化合物，作为一种可能的生物靶标，分子伴侣热休克蛋白90（Hsp90）抑制。 本发明包括这样的化合物在药物中与癌症疾病以及其中抑制Hsp90有反应性的其它疾病的用途，以及含有这些化合物的药物组合物的用途。

公开(公告)号：US20100028338A1

公开(公告)日：2010-02-04

申请号：US11720776

申请日：2005-12-13

申请人： Sara Zaknoen ,  Margaret Ma Woo ,  Richard William Versace ,  Claudio Pisano ,  Loredana Vesci

发明人： Sara Zaknoen ,  Margaret Ma Woo ,  Richard William Versace ,  Claudio Pisano ,  Loredana Vesci

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。

公开(公告)号：US07629003B2

公开(公告)日：2009-12-08

申请号：US10624645

申请日：2003-07-23

申请人： Claudio Pisano ,  Maria Ornella Tinti ,  Mosé Santaniello ,  Luciana Critelli ,  Giovanni Salvatori

发明人： Claudio Pisano ,  Maria Ornella Tinti ,  Mosé Santaniello ,  Luciana Critelli ,  Giovanni Salvatori

IPC分类号： A61K9/127

CPC分类号： C07C229/22 ,  A61K8/14 ,  A61K8/44 ,  A61K9/0019 ,  A61K9/127 ,  A61K9/1272 ,  A61K9/1277 ,  A61K9/19 ,  A61K31/225 ,  A61K48/00 ,  A61Q19/00

摘要： Esters of L-carnitine and alkanoyl L-carnitines are described which can be used as cationic lipids for the intracellular delivery of pharmacologically active compounds. New esters of L-carnitine and alkanoyl L-carnitines of formula (I) are also disclosed wherein the R groups are as defined in the description.

摘要翻译： 描述了左旋肉碱和烷酰基L-肉碱的酯，其可用作阳离子脂质用于药理学活性化合物的细胞内递送。 还公开了式（I）的L-肉碱和烷酰基L-肉毒碱的新酯，其中R基团如说明书中所定义。

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。

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。

公开(公告)号：US07351714B2

公开(公告)日：2008-04-01

申请号：US10546211

申请日：2004-03-10

申请人： Sabrina Dallavalle ,  Sergio Penco ,  Claudio Pisano ,  Franco Zunino

发明人： Sabrina Dallavalle ,  Sergio Penco ,  Claudio Pisano ,  Franco Zunino

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。

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。

公开(公告)号：US20060172968A1

公开(公告)日：2006-08-03

申请号：US11314736

申请日：2005-12-22

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： A61K31/727 ,  A61K31/737

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个基团具有说明书中指出的含义的式（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。