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1.发明公开GLUTATHIONE CONJUGATES WITH DISTAMYCIN DERIVATIVES HAVING ANTITUMOR ACTIVITY 审中-公开与偏端霉素衍生物，谷胱甘肽结合物和它们作为抗肿瘤剂的用途
公开(公告)号：EP1330470A1
公开(公告)日：2003-07-30
申请号：EP01972032.5
申请日：2001-09-07
CPC分类号： C07K5/0215 , A61K38/00
摘要： The present invention refers to distamycin and derivatives thereof, such as bromo-or chloro-acryloyl derivatives of distamycin, which are conjugated with glutathione, to a process for their preparation and to pharmaceutical compositions thereof. The compounds of the invention are endowed with a remarkable antitumor activity and are thus useful in therapy in the treatment of cancer.
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2.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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公开(公告)号：EP1324983A1
公开(公告)日：2003-07-09
申请号：EP01951593.1
申请日：2001-06-14
发明人： BERIA, Italo , COZZI, Paolo , MONGELLI, Nicola , ORZI, Fabrizio
IPC分类号： C07D207/34
CPC分类号： C07D403/14 , C07D207/34
摘要： A process for preparing distamycin derivatives possessing antitumor activity, by starting from distamycin A itself, is described. The process involves the preparation of the novel intermediates of formula (III).
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公开(公告)号：EP1311481A1
公开(公告)日：2003-05-21
申请号：EP01960493.3
申请日：2001-07-12
发明人： BERIA, Italo , COZZI, Paolo , MONGELLI, Nicola , NESI, Marcella
IPC分类号： C07D207/34
CPC分类号： C07D207/34
摘要： Herewith provided is a process for preparing useful intermediates in the preparation of distamycin derivatives possessing antitumor activity, said derivatives having the formula reported in the specification, by using distamycin A as the starting material.
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5.发明授权CINNAMOYL DISTAMYCIN ANALOGOUS DERIVATIVES, PROCESS FOR THEIR PREPARATION, AND THEIR USE AS ANTITUMOR AGENTS 有权偏端霉素肉桂酸衍生物，其制造方法及其作为抗肿瘤剂的类似物
公开(公告)号：EP1084120B1
公开(公告)日：2004-03-10
申请号：EP99926405.4
申请日：1999-05-22
发明人： COZZI, Paolo , BARALDI, Pier, Giovanni , BERIA, Italo , CALDARELLI, Marina , GERONI, Maria, Cristina , PENNELLA, Giulia , ROMAGNOLI, Romeo
IPC分类号： C07D403/14 , A61K31/415
CPC分类号： C07D403/14
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6.发明授权SULFURATED DISTAMYCIN DERIVATIVES, PROCESS FOR PREPARING THEM, AND THEIR USE AS ANTITUMOR AGENTS 有权含硫醚偏端霉素衍生物，用于生产及其作为抗肿瘤药
公开(公告)号：EP1100777B1
公开(公告)日：2003-05-28
申请号：EP99936609.9
申请日：1999-07-21
IPC分类号： C07D207/34 , A61K31/40
CPC分类号： C07D207/34
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7.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：EP0722446B1
公开(公告)日：2002-12-11
申请号：EP95926927.5
申请日：1995-07-18
IPC分类号： C07D403/14 , C07D417/14 , A61K31/40
CPC分类号： C07D231/38 , C07D403/14 , C07D417/14
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9.发明授权BENZOHETEROCYCLIC DISTAMYCIN DERIVATIVES, PROCESS FOR PREPARING THEM, AND THEIR USE AS ANTITUMOR AGENTS 有权苯并杂环偏端霉素衍生物，用于生产及其作为抗肿瘤药
公开(公告)号：EP1064281B1
公开(公告)日：2005-05-25
申请号：EP99915665.6
申请日：1999-03-17
发明人： COZZI, Paolo , BARALDI, Pier, Giovanni , BERIA, Italo , CALDARELLI, Marina , CAPOLONGO, Laura , ROMAGNOLI, Romeo
IPC分类号： C07D403/14 , A61K31/40 , A61K31/415 , C07D405/14 , C07D409/14
CPC分类号： C07D403/14 , C07D405/14 , C07D409/14
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10.发明授权BENZOHETEROCYCLIC DISTAMYCIN DERIVATIVES, PROCESS FOR PREPARING THEM, AND THEIR USE AS ANTITUMOR AND ANTIVIRAL AGENTS 失效苯并杂环偏端霉素衍生物，用于生产及其作为抗肿瘤和抗病毒药物
公开(公告)号：EP0937070B1
公开(公告)日：2003-12-03
申请号：EP97945879.1
申请日：1997-10-23
发明人： COZZI, Paolo , BARALDI, Pier, Giovanni , BERIA, Italo , CALDARELLI, Marina , CAPOLONGO, Laura , SPALLUTO, Giampiero , ROMAGNOLI, Romeo
IPC分类号： C07D403/14 , A61K31/40 , C07D407/14 , A61K31/415 , C07D409/14 , C07D417/14 , A61K31/425
CPC分类号： C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14
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