发明名称 COMPOUNDS CONTAINING CARBABORANE RESIDUES AND THE USE THEREOF IN MEDICINE, ESPECIALLY FOR USE IN TUMOUR THERAPY
摘要 The invention relates to compounds of the general formula (I) where A is oxygen, sulphur or selenium, (CB)n and (CB)m are each a carbaborane or a chain of carbaboranes. R1 is selected from hydroxy, alkoxy, alkenoxy, O-glycoside, thioglycoside and glycosylamine, PO4 2- or P2O7 3- and A-M+. R2 and R4 are selected from O-glycoside residue, thioglycoside residue, glycosylamine residue, PO4 2- or P2O7 3- and A-M+. R3 is selected from alkoxy, alkenoxy, O-glycoside, thioglycoside, glycosylamine or a phosphonate residue. Through their content of sugar residues, the compounds of the invention bind specifically to receptors on the surface of carcinogenic cells. In addition, the compounds act through the phosphonate groups as phosphate mimetics, resulting in binding specifically to calcium-rich tumour tissue. It is advantageous that the compounds are not themselves toxic, show a low nonspecific protein binding and are readily soluble in water. The invention further relates to the use of these compounds as medicaments, especially in radio-oncology, and processes for the preparation thereof and intermediates which are obtained during the preparation process.
申请公布号 WO2009021978(A3) 申请公布日期 2009.04.09
申请号 WO2008EP60649 申请日期 2008.08.13
申请人 UNIVERSITAET LEIPZIG;STADLBAUER, SVEN;HEY-HAWKINS, EVAMARIE 发明人 STADLBAUER, SVEN;HEY-HAWKINS, EVAMARIE
分类号 C07F5/02;C07F9/02;C07F9/48;C07F9/547;C07F9/6596;C07H11/04 主分类号 C07F5/02
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