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filingDate 1997-09-12-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2005-05-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_885fd607a35da61d05960a4d47488d3f
publicationDate 2005-05-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-0946177-B1
titleOfInvention METHOD OF INHIBITING BIOSYNTHESIS OF EIf5A
abstract Inhibition of the intracellular biosynthesis of EIf-5A comprises administration of a polyamine of formula R1N1(R2)(CH2)mN2(R3)(CH2)nN3(R4)(CH2)mN4(R5)R6 (I), R1N1H(CH2)vN2H(CH2)wN3H(CH2)xN4H(CH2)yN5H(CH2)zN6HR6 (I'), (I'') or (I''') in an amount sufficient to deplete the intracellular supply of spermidine (required for EIf-5A biosynthesis) but insufficient to affect polyamine homeostasis: R, R6 = H (except for (I)) alkyl or 1-12C aralkyl; R2-R5 = H, R1 or R6; R7 = H, alkyl, aryl or 1-12C aralkyl; m, n = 3-6; v-z = 3-10; R8-R13 = H, alkyl, aryl, arylalkyl or cycloalkyl such that any alkyl chains are optionally interrupted by >= 1 etheric O; N1-N4 = nitrogen atoms capable of protonation at physiological pH; a, b = 0-4, but both may not be 0; A-C = bridging groups which effectively maintain the distance between the N atoms such that the polyamine: (i) is capable of uptake by a target cell or is capable of binding to >= 1 polyamine site of a receptor located within or on the surface of a cell upon administration; (ii) upon uptake by the target cell, competitively binds via an electrostatic interaction between the positively charged nitrogen to biological counter-ions such that the polyamine on binding to the biological counter ion, functions in a manner biologically different from the intracellular polyamines; and where >= 1 of the bridging groups may contain >= 1 CH(OH) group which is not alpha to either of the nitrogen atoms.
priorityDate 1996-09-13-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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