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1.发明公开7-T-BUTOXYIMINOMETHYLCAMPTOTHECIN CONJUGATED IN POSITION 20 WITH INTEGRIN ANTAGONISTS 审中-公开在适当的位置20与整共轭7T丁氧
公开(公告)号：EP1747020A2
公开(公告)日：2007-01-31
申请号：EP05743414.4
申请日：2005-04-28
申请人： SIGMA-TAU Industrie Farmaceutiche Riunite S.p.A. , ISTITUTO NAZIONALE PER LO STUDIO E LA CURA DEI TUMORI
发明人： DAL POZZO, Alma , PENCO, Sergio , MERLINI, Lucio , GIANNINI, G., Simgma-Tau Ind. Farm. Riunite S.p.A. , TINTI, M., Sigma-Tau Ind. Farm. Riunite S.p.A. , PISANO, C., Sigma-Tau Ind. Farm. Riunite S.p.A. , ZUNINO, F., Ist. Naz. per Studio e CuradeiTumori , ALLOATTI, D., Simgma-Tau Ind. Farm. Riunite S.p.A. , VESCI, L., Sigma-Tau Ind. Farm. Riunite S.p.A. , DALLAVALLE, Sabrina , NI MING, Hong Ist. di Ricerche Chimiche e Biochim.
CPC分类号： A61K47/64
摘要： Compounds of Formula (I) are described; in which the R1 group is as defined in the specification and includes the condensation of 7-t-butoxyiminomethylcamptothecin in position 20 with a cyclopeptide containing the RGD sequence. Said compounds are endowed both with high affinity for integrin receptors αvβ3 and αvβ5 and with selective cytotoxic activity on human tumour cell lines at micromolar concentrations.
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2.发明公开CAMPTOTHECIN DERIVATIVES CONJUGATED IN POSITION 20 WITH INTEGRIN ANTAGONISTS 审中-公开在适当的位置20具有共轭整合喜树碱衍生物
公开(公告)号：EP1747019A2
公开(公告)日：2007-01-31
申请号：EP05743015.9
申请日：2005-05-04
申请人： SIGMA-TAU Industrie Farmaceutiche Riunite S.p.A. , ISTITUTO NAZIONALE PER LO STUDIO E LA CURA DEI TUMORI
发明人： DAL POZZO, Alma , PENCO, Sergio , MERLINI, Lucio , GIANNINI, Giuseppe , TINTI, Maria Ornella , PISANO, Claudio , ZUNINO, Franco , ALLOATTI, Domenico , VESCI, Loredana , DALLAVALLE, Sabrina , NI MING, Hong
CPC分类号： A61K47/64
摘要： Compounds or formula (I) are described, in which R and R1 groups are as defined here below and include the condensation of the camptothecin molecule in position 20 with a cyclopeptide containing the RGD sequence. Said compounds are endowed both with high affinity for integrin receptors αvβ3 and αvβ5 and with selective cytotoxic activity on human tumor cell lines at micromolar concentrations.
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公开(公告)号：EP1751176B1
公开(公告)日：2010-03-10
申请号：EP05742999.5
申请日：2005-05-04
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公开(公告)号：EP2285396A1
公开(公告)日：2011-02-23
申请号：EP09749730.9
申请日：2009-05-11
发明人： DAL POZZO, Alma , ESPOSITO, Emiliano , NI, Minghong , PENCO, Sergio , PISANO, Claudio , CASTORINA, Massimo , VESCI, Loredana
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/06026 , C07K7/64
摘要： The present invention relates to dual-targeting cytotoxic compounds of formula (I) and to their preparation. The described compounds are endowed with tumour specific action, incorporating three functional units: a tumour recognition moiety and a tumour selective enzymatic substrate sequence connected together by means of a spacer. These conjugates are designed to guarantee serum stability and, at the same time, the desired action inside the tumour cells as a result of enzymatic cleavability. [(L-D)
n E]
m -F-D-PI-SI-CT Formula (I).-
公开(公告)号：EP1751176A1
公开(公告)日：2007-02-14
申请号：EP05742999.5
申请日：2005-05-04
发明人： DAL POZZO, Alma , PENCO, Sergio , GIANNINI, Giusepp , TINTI, Maria, Ornella , PISANO, Claudio , VESCI, Loredana , NI MING HONG
摘要： Formula (I) compounds are described c(R1-Arg- Gly-Asp-R2) where the meanings of the various groups are as described here below, which are integrin inhibitors, and particularly inhibitors of integrins of the αvβ3 and αvβ5 family, and therefore are useful as medicaments, particularly for the treatment of the diseases underlying abnormal angiogenesis, such as retinopathy, acute renal failure, osteoporosis and metastases. The compounds described herein, when suitably labelled, are also useful as diagnostic agents, especially for the detection of small tumor masses and arterial occlusion events, and as targeted drug vectors.
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