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1.发明公开NEMORUBICIN AS RADIOSENSITIZER IN COMBINATION WITH RADIATION THERAPY AGAINST TUMORS 审中-公开放射治疗对癌症奈莫ALS放射增敏剂
公开(公告)号：EP1603575A2
公开(公告)日：2005-12-14
申请号：EP04716607.9
申请日：2004-03-03
IPC分类号： A61K31/704 , A61P35/00 , A61K31/282
CPC分类号： A61K45/06 , A61K31/282 , A61K31/704 , A61K33/24 , A61K41/00 , A61K2300/00
摘要： The present invention relates to a morpholinyl anthracycline derivative for use as radiosensitizer, to be administered in combination with radiation therapy, so that a synergistic effect can be revealed.
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2.发明公开COMBINED THERAPY AGAINST TUMORS COMPRISING SUBSTITUTED ACRYLOYL DISTAMYCIN DERIVATIVES AND RADIOTHERAPY 有权基于对衍生品中的丙烯偏端霉素RADIOTHERAPIE联合肿瘤的治疗
公开(公告)号：EP1490053A1
公开(公告)日：2004-12-29
申请号：EP03714888.9
申请日：2003-03-17
CPC分类号： A61K41/0038 , A61K31/4025 , A61K33/24 , A61K2300/00
摘要： The present invention provides the use of acryloyl distamycin derivatives, in particular α-bromo- or α-chloro-acryloyl distamycin derivatives, in combination with radiotherapy, for the treatment of tumors.
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3.发明公开
公开(公告)号：EP1345604A1
公开(公告)日：2003-09-24
申请号：EP01986259.8
申请日：2001-09-21
IPC分类号： A61K31/40 , C07D403/14
CPC分类号： A61K31/40
摘要： The present invention relates to an administration schedule comprising the intravenous administration of a α-halogen-acryloyl distamycin derivative, or a pharmaceutically acceptable salt thereof. The above administration allows the treatment of a variety of tumors in mammals.
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4.发明公开COMBINED THERAPY AGAINST TUMORS COMPRISING SUBSTITUTED ACRYLOYL DISTAMYCIN DERIVATIVES AND ALKYLATING AGENTS 有权基于偏端霉素ACRYLOYLDERIVATEN和烷化剂联合肿瘤的治疗
公开(公告)号：EP1303307A2
公开(公告)日：2003-04-23
申请号：EP01960355.4
申请日：2001-06-20
IPC分类号： A61K45/06
CPC分类号： A61K45/06
摘要： Compounds which are alpha-halogenoacryloyl distamycin derivatives of formula (I) wherein R1 is a bromine or chlorine atom; R2 is a distamycin or distamycin-like framework as set forth in the specification; or a pharmaceutically acceptable salt thereof; are cytotoxic agents particularly effective in the treatment of tumors over expressing GSH/GSTs system and which are poorly responsive or even resistant to conventional antitumor therapies.
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公开(公告)号：EP1430306A2
公开(公告)日：2004-06-23
申请号：EP02779404.9
申请日：2002-09-19
发明人： FOWST, Camilla , GERONI, Maria, Cristina, Rosa , TURSI, Jennifer, Margaret , VREELAND, Franzanne
IPC分类号： G01N33/574
CPC分类号： G01N33/574 , G01N33/57488 , G01N2333/91171 , G01N2800/52
摘要： Herewith described is a novel method for predicting the sensitivity towards chemotherapy, of a patient in need thereof, which comprises obtaining a blood sample from the patient and detecting the levels of blood glutathione (GSH) as a surrogate marker for glutathione-S-transferase (GST) activity in tumor tissues.
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6.发明公开USE OF SUBSTITUTED ACRYLOYL DISTAMYCIN DERIVATIVES IN THE TREATMENT OF TUMORS ASSOCIATED WITH HIGH LEVELS OF GLUTATHIONE 有权取代偏端霉素ACRYLOYLDERIVATEN肿瘤与治疗用量增加谷胱甘肽水平有关
公开(公告)号：EP1280527A2
公开(公告)日：2003-02-05
申请号：EP01933856.5
申请日：2001-04-19
IPC分类号： A61K31/4025 , A61K31/4155 , A61K31/4178 , A61P35/00 , A61K45/06
CPC分类号： A61K31/4178 , A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/4155 , A61K31/195 , A61K2300/00
摘要： Compounds which are α-halogenoacryloyl distamycin derivatives of formula (I) wherein R1 is a bromine or chlorine atom; R2 is a distamycin or distamycin-like framework as set forth in the specification; or a pharmaceutically acceptable salt thereof; are cytotoxic agents particularly effective in the treatment of tumors over expressing GSH/GSTs system and which are poorly responsive or even resistant to conventional antitumor therapies.
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7.发明公开
公开(公告)号：EP1299110A2
公开(公告)日：2003-04-09
申请号：EP01945297.8
申请日：2001-06-20
IPC分类号： A61K31/70
CPC分类号： A61K31/409 , A61K31/40 , A61K31/475 , A61K31/505 , A61K31/565 , A61K31/7064 , A61K31/7068 , A61K45/06 , A61K2300/00
摘要： The present invention provides the combined use of acryloyl distamycin derivatives, in particular α-bromo- and -α-chloro-acryloyl distamycin derivatives of formula (I), as set forth in the specification, antimicrotubule agents and/or an antimetabolites. Also provided is the use of the said combination in the treatment or prevention of metastasis or in the treatment of tumors by inhibition of angiogenesis.
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8.发明授权USE OF SUBSTITUTED ACRYLOYL DISTAMYCIN DERIVATIVES IN THE TREATMENT OF TUMORS ASSOCIATED WITH HIGH LEVELS OF GLUTATHIONE 有权取代偏端霉素ACRYLOYLDERIVATEN肿瘤与治疗用量增加谷胱甘肽水平有关
公开(公告)号：EP1280527B1
公开(公告)日：2005-08-03
申请号：EP01933856.5
申请日：2001-04-19
IPC分类号： A61K31/4025 , A61K31/4155 , A61K31/4178 , A61P35/00 , A61K45/06
CPC分类号： A61K31/4178 , A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/4155 , A61K31/195 , A61K2300/00
摘要： Compounds which are α-halogenoacryloyl distamycin derivatives of formula (I) wherein R1 is a bromine or chlorine atom; R2 is a distamycin or distamycin-like framework as set forth in the specification; or a pharmaceutically acceptable salt thereof; are cytotoxic agents particularly effective in the treatment of tumors over expressing GSH/GSTs system and which are poorly responsive or even resistant to conventional antitumor therapies.
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9.发明公开PHARMACEUTICAL COMPOSITIONS COMPRISING ACRYLOYL DISTAMYCIN DERIVATIVES AND TOPOISOMERASE I AND II INHIBITORS 有权药物组合物丙烯酰偏端霉素取代衍生物和拓扑异构酶II抑制剂含
公开(公告)号：EP1292290A2
公开(公告)日：2003-03-19
申请号：EP01956495.4
申请日：2001-06-20
IPC分类号： A61K31/00
CPC分类号： A61K45/06 , A61K31/00 , A61K2300/00
摘要： The present invention provides the combined use of acryloyl distamycin derivatives, in particular α-bromo- and α-chloro-acryloyl distamycin derivatives of formula (I), as set forth in the specification, and an antineoplastic topoisomerase I or II inhibitor, in the treatment of tumors. Also provided is the use of the said combinations in the treatment or prevention of metastasis or in the treatment of tumors by inhibition of angiogenesis.
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10.发明公开ACRYLOYL PEPTIDIC DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS ANTITUMOR AGENTS 审中-公开ACRYLOYLPEPTIDISCHENDERIVATE，其制造方法及其作为抗肿瘤药
公开(公告)号：EP1242374A1
公开(公告)日：2002-09-25
申请号：EP00993255.9
申请日：2000-11-23
发明人： COZZI, Paolo , BERIA, Italo , CALDARELLI, Marina , GERONI, Maria, Cristina, Rosa , BARALDI, Pier, Giovanni , ROMAGNOLI, Romeo
IPC分类号： C07D207/34 , C07D403/14 , A61P35/02 , A61K31/40
CPC分类号： C07D403/12 , C07D207/34 , C07D403/14
摘要： Compounds which are acryloyl peptidic derivatives of formula (I), wherein n is 3 or 4; m is 0, 1 or 2; X and Y are the same or different and are selected, independently for each heterocyclic ring, from N or CH; R1 and R2, the same or different, are selected from hydrogen, halogen or C1-C4 alkyl; R3 is hydrogen or halogen, B is selected from the groups consisting of formulae (1), (2), (3), (4), (5), (6) and (7) wherein R4, R5, R7, and R8 are, independently from each other, hydrogen or C1-C4 alkyl; R6 is hydrogen, hydroxy or C1-C4 alkyl; or a pharmaceutically acceptable salt thereof; with the provisos that X and Y are not both N atoms for the same heterocyclic ring; when all of X and Y are CH groups and m is 0, then at least one of R4, R5, or R6 is other than hydrogen; when at least one of X and Y is other than CH, then at least one of R4 and R5 is other than hydrogen; are useful as antitumor agents.
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