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1.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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2.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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3.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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4.发明公开COMBINED THERAPY AGAINST TUMORS COMPRISING SUBSTITUTED ACRYLOYL DISTAMYCIN DERIVATIVES AND PROTEIN KINASE (SERINE/THREONINE KINASE) INHIBITORS 有权基于组合肿瘤的治疗的取代的丙烯酰偏端霉素衍生物和蛋白激酶（丝氨酸/苏氨酸特异性蛋白激酶）抑制剂
公开(公告)号：EP1461083A1
公开(公告)日：2004-09-29
申请号：EP02787763.8
申请日：2002-12-18
IPC分类号： A61K45/06 , A61K31/40 , A61K31/415 , A61P35/00
CPC分类号： A61K45/06 , A61K31/40 , A61K31/415 , 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 a protein kinase (serine/threonine and tyrosine kinases) 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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5.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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公开(公告)号：EP1282602A1
公开(公告)日：2003-02-12
申请号：EP01936253.2
申请日：2001-04-19
IPC分类号： C07D213/55 , C07D233/88 , C07D233/50 , C07D239/12 , A61K31/4402 , A61K31/4168
CPC分类号： C07D401/12 , C07D213/55 , C07D233/50 , C07D233/88 , C07D239/12
摘要： Novel propanoic acid derivatives are integrin receptor antagonists or inhibitors, in particular of the avb3 integrin receptor. The compounds of the invention are for instance useful for the treatment of solid tumors by inhibition of angiogenic growth of tumor vessel network, thus promoting tumor regression, inhibition of metastatic spread, thus avoiding cancer metastases, inhibition of bone resorption, thus controlling osteoporosis, inhibition of smooth muscle cells migration into neointima, thus blocking restenosis after percutaneous coronary angioplasty and the treatment of other pathological conditions mediated by cell adhesion, cell migration or angiogenesis such e.g. diabetic retinopaty, rheumatoid arthritis and inflammation.
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7.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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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.发明授权OXIDISED SULFURATED DISTAMYCIN DERIVATIVES, PROCESS FOR PREPARING THEM, AND THEIR USE AS ANTITUMOR AGENTS 有权氧化硫化偏端霉素衍生物，制造方法及其作为抗肿瘤药
公开(公告)号：EP1100778B1
公开(公告)日：2004-12-01
申请号：EP99941465.9
申请日：1999-07-21
IPC分类号： C07D207/34 , A61K31/40
CPC分类号： C07D207/34
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10.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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