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。

公开(公告)号：US20100048603A1

公开(公告)日：2010-02-25

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： A61K31/4375 ,  A61P35/00

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。

公开(公告)号：US20100330200A1

公开(公告)日：2010-12-30

申请号：US12517926

申请日：2007-12-11

申请人： Paolo Carminati ,  Claudio Pisano ,  Loredana Vesci ,  Franco Zunino

发明人： Paolo Carminati ,  Claudio Pisano ,  Loredana Vesci ,  Franco Zunino

IPC分类号： A61K33/24 ,  A61P35/00 ,  A61P35/04

CPC分类号： A61K33/24 ,  A61K31/192 ,  A61K31/282 ,  A61K45/06 ,  A61K2300/00

摘要： A combination comprising an atypical retinoid compound, preferably E-4-(3-(1-adamantyl)-4-hydroxyphenyl)cinnamic acid and an anticancer drug of the platinum family, preferably cisuplatin, together with a pharmaceutical composition comprising it and a kit for its administration in unitary or in coordinated sequential form. The kit preferably comprises a first formulation of E-4-(3-(1-adamantyl)-4-hydroxyphenyl)cinnamic acid dissolved in a mixture of ethanol and cremophor, and susupended in a saline solution, and a second formulation of cisuplatin in saline solution. The combination is used for the preparation of a medicament to inhibit tumor growth and tumor migration, in particular for the treatment of ovarian tumor and/or carcinoma.

摘要翻译： 包含非典型类视色素化合物，优选E-4-（3-（1-金刚烷基）-4-羟基苯基）肉桂酸和铂族的抗癌药物，优选顺铂，以及包含它的药物组合物和试剂盒 以统一或协调的顺序形式进行管理。 试剂盒优选包含溶解在乙醇和Cremophor的混合物中并在盐溶液中混悬的E-4-（3-（1-金刚烷基）-4-羟基苯基）肉桂酸的第一配方，并且将顺铂的第二制剂 生理盐水。 该组合用于制备抑制肿瘤生长和肿瘤迁移的药物，特别是用于治疗卵巢肿瘤和/或癌。

公开(公告)号：US09302998B2

公开(公告)日：2016-04-05

申请号：US13996359

申请日：2011-12-13

申请人： Giuseppe Giannini ,  Walter Cabri ,  Loredana Vesci ,  Maria Luisa Cervoni ,  Claudio Pisano ,  Maurizio Taddei ,  Serena Ferrini

发明人： Giuseppe Giannini ,  Walter Cabri ,  Loredana Vesci ,  Maria Luisa Cervoni ,  Claudio Pisano ,  Maurizio Taddei ,  Serena Ferrini

IPC分类号： C07D413/12 ,  C07D401/10 ,  C07D403/10 ,  C07D249/06

CPC分类号： C07D249/06 ,  C07D401/10 ,  C07D403/10 ,  C07D413/12

摘要： The present invention relates to aryl triazole derivatives of Formula I having antitumoural activity 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 composition containing such compounds.

摘要翻译： 本发明涉及具有抗肿瘤活性的式I的芳基三唑衍生物，作为一种可能的生物靶标，分子伴侣热休克蛋白90（Hsp90）抑制。 本发明包括这些化合物在药物中的用途，涉及癌症疾病以及其中抑制Hsp90的反应性的其它疾病，以及含有这些化合物的药物组合物。

公开(公告)号：US20140329812A1

公开(公告)日：2014-11-06

申请号：US13996359

申请日：2011-12-13

申请人： Giuseppe Giannini ,  Walter Cabri ,  Loredana Vesci ,  Maria Luisa Cervoni ,  Claudio Pisano ,  Maurizio Taddei ,  Serena Ferrini

发明人： Giuseppe Giannini ,  Walter Cabri ,  Loredana Vesci ,  Maria Luisa Cervoni ,  Claudio Pisano ,  Maurizio Taddei ,  Serena Ferrini

IPC分类号： C07D249/06 ,  C07D403/10 ,  C07D401/10

CPC分类号： C07D249/06 ,  C07D401/10 ,  C07D403/10 ,  C07D413/12

摘要： The present invention relates to aryl triazole derivatives of Formula I having antitumoural activity 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 composition containing such compounds.

摘要翻译： 本发明涉及具有抗肿瘤活性的式I的芳基三唑衍生物，作为一种可能的生物靶标，分子伴侣热休克蛋白90（Hsp90）抑制。 本发明包括这些化合物在药物中的用途，涉及癌症疾病以及其中抑制Hsp90的反应性的其它疾病，以及含有这些化合物的药物组合物。

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。

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：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：US20080312265A1

公开(公告)日：2008-12-18

申请号：US12096884

申请日：2006-12-13

申请人： Claudio Pisano ,  Loredana Vesci

发明人： Claudio Pisano ,  Loredana Vesci

IPC分类号： A61K31/4375 ,  A61P35/00

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 drug-resistant tumors and/or for the administration to patients who show polymorphisms in the gene coding for DNA topoisomerase I.

摘要翻译： 喜树碱衍生物的亚类被公开用于制备用于治疗药物抗性肿瘤的药物和/或用于在编码DNA拓扑异构酶I的基因中显示多态性的患者的给药。

公开(公告)号：US20080194683A1

公开(公告)日：2008-08-14

申请号：US12078991

申请日：2008-04-09

申请人： Claudio Cavazza ,  Claudio Pisano ,  Loredana Vesci ,  Franco Mandelli

发明人： Claudio Cavazza ,  Claudio Pisano ,  Loredana Vesci ,  Franco Mandelli

IPC分类号： A61K31/205 ,  A61P25/02

CPC分类号： A61K45/06 ,  A61K31/205 ,  A61K31/221 ,  A61K31/28 ,  A61K31/335 ,  A61K31/475 ,  A61K31/555 ,  A61K33/24 ,  A61K38/14 ,  A61K2300/00

摘要： This invention disclosed the use of acetyl L-carnitine or of a pharmaceutically acceptable salt thereof for the preparation of a medicament for preventing and/or treating peripheral neuropathies induced by the administration of a peripheral neuropathy—inducing anticancer agent. In particular said anticancer agent is selected from the group consisting of the family of platin compounds, taxanes, epothilone class and vinca alkaloids, farnesyl transferase inhibitors, thalidomide, 5-fluorouracil, cryptophycin analogues, proteasome inhibitors. Said medicament can be administered in a co-ordinated manner to a subject suffering from said peripheral neuropathies, or expected to suffer from said peripheral neuropathies. Beneficial effects on the patient's quality of life are achieved and an improvement of therapeutic index of the anticancer agent is obtained.

摘要翻译： 本发明公开了乙酰基左旋肉碱或其药学上可接受的盐在制备用于预防和/或治疗通过施用周围神经病诱导抗癌剂诱发的周围神经病变的药物中的应用。 特别地，所述抗癌剂选自铂族化合物，紫杉烷类，埃坡霉素类和长春花生物碱家族，法呢基转移酶抑制剂，沙利度胺，5-氟尿嘧啶，隐球菌素类似物，蛋白酶体抑制剂。 所述药物可以以协调的方式施用于患有所述周围神经病的受试者，或预期患有所述周围神经病。 实现对患者生活质量的有益影响，获得抗癌剂治疗指数的改善。